US2008113991A1PendingUtilityA1
Pyridopyrazines and the use thereof as kinase inhibitors
Est. expiryMay 23, 2023(expired)· nominal 20-yr term from priority
A61P 43/00A61P 9/10A61P 35/00A61P 9/00A61P 1/16A61P 17/14A61P 17/06C07D 471/04A61K 31/50
57
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Claims
Abstract
The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general Formula I, their preparation and use as medicaments, in particular for the treatment of malignant and other disorders based on pathological cell proliferations.
Claims
exact text as granted — not AI-modified1 . A method of modulating function of a kinase, comprising:
administering to a subject in need thereof a pharmaceutical composition comprising a compound; and a pharmaceutically acceptable diluent, said compound is a pyrido[2,3-b]pyrazine of the general Formula I in which the substituents R1-R3 have the following meaning: R1 and R2 are independently of one another: (i) hydrogen (ii) hydroxyl (iii) alkyl, alkenyl or alkynyl, where the alkyl radical is saturated and having 1 to 8 C atoms, the alkenyl radical has 2 to 8 C atoms, the alkynyl radical has 2 to 8 C atoms, (iv) unsubstituted or substituted aryl, where the aryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-hetero-aryl, NH-alkyl-cycloalkyl, NH-alkyl-heterocyclyl, NH-alkyl-aryl, NH-alkyl-heteroaryl, NH-alkyl-NH 2 , NH-alkyl-OH, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl-heterocyclyl, O-alkyl-aryl, O-alkyl-heteroaryl, O-alkyl-OH, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkylcycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NH-alkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenylheterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkylcycloalkenyl, CO 2 -alkenyl-heterocyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocycyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, alkenyl, cycloalkenyl, NH-alkyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkylcycloalkynyl, CO 2 -alkynyl-heterocyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents, and the alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, alkyl-cycloalkyl, alkyl-heterocyclyl, alkyl-aryl, alkylheteroaryl, alkenyl, cycloalkenyl, alkenyl-cycloalkenyl, alkenyl-heterocyclyl, alkenyl-aryl, alkenylheteroaryl, alkynyl, cycloalkynyl, alkynyl-cycloalkynyl, alkynyl-heterocyclyl, alkynyl-aryl, alkynylheteroaryl substituents may in turn themselves be substituted, (v) unsubstituted or substituted heteroaryl, where the heteroaryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-aryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-aryl, O-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-hetero-cyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, N(alkyl) 2 , SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl, NH-cycloalkenyl, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, O-alkenyl, O-cycloalkenyl, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, N(alkenyl) 2 , SO 2 O-alkenyl, alkenyl, cycloalkenyl, NH-alkynyl, NH-cycloalkynyl, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, O-alkynyl, O-cycloalkynyl, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, N(alkynyl) 2 , SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents, and the alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, alkenyl, cycloalkenyl, alkynyl, and cycloalkynyl substituents may in turn themselves be substituted. R3 is A, B, or C, where: (A) is —C(Y)NR4R5, where Y is O, or S and R4 and R5 are independently of one another
(i) hydrogen,
(ii) unsubstituted or substituted alkyl, alkenyl or alkynyl, where the alkyl, the alkenyl or the alkynyl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO2, SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N (aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 3 H, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl, NH-cycloalkenyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, NHSO 2 -cycloalkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-hetero-cyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO 2 -alkenyl, alkenyl, cycloalkenyl, NH-alkynyl, NH-cycloalkynyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, NHSO 2 -cycloalkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-hetero-cyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO 2 -alkynyl, alkynyl, or cycloalkynyl, substituents,
(iii) unsubstituted or substituted cycloalkyl, cycloalkenyl, or cycloalkynyl, where the cycloalkyl, the cycloalkenyl or the cycloalkynyl radical may have one or more identical or different F, Cl, Br, I, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, OH, O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, CO2H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, C(O)—NH 2 , C(O)NH-aryl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , alkyl, aryl, NH-alkenyl, NH-cycloalkenyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, NHSO 2 -cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , alkenyl, NH-alkynyl, NH-cycloalkynyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, NHSO 2 -cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , or alkynyl substituents,
(iv) unsubstituted or substituted heterocyclyl, where the heterocyclyl radical may have one or more identical or different OH, O-alkyl, O-aryl, NH-alkyl, NH-aryl, alkyl, alkyl-aryl, aryl, O-alkenyl, NH-alkenyl, alkenyl, alkenyl-aryl, O-alkynyl, NH-alkynyl, alkynyl, or alkynyl-aryl substituents,
(v) unsubstituted or substituted aryl, where the aryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkyl-heterocyclyl, NH-alkyl-aryl, NH-alkyl-heteroaryl, NH-alkyl-NH 2 , NH-alkyl-OH, N (alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl-heterocyclyl, O-alkyl-aryl, O-alkyl-heteroaryl, O-alkyl-OH, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-hetero-cyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-hetero-cyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NH-alkenyl-NH 2 , NH-alkenyl-O H, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(vi) unsubstituted or substituted heteroaryl, where the heteroaryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-aryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO2-aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NH-alkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(vii) or R4 and R5 together are cycloalkyl cycloalkenyl, cycloalkynyl or heterocyclyl;
(B) is —C(Y)NR6R7, where Y is NH and R6 and R7 are independently of one another
(i) hydrogen,
(ii) unsubstituted or substituted alkyl, alkenyl or alkynyl, where the alkyl, the alkenyl or the alkynyl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-hetero-aryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO2-heterocyclyl, CO 2 -aryl, CO2-heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkylheterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-hetero-cyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-hetero-aryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 3 H, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NH-alkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(iii) unsubstituted or substituted cycloalkyl, cycloalkenyl or cycloalkynyl, where the cycloalkyl, the cycloalkenyl or the cycloalkynyl radical may have one or more identical or different F, Cl, Br, I, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, OH, O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , alkyl, aryl, NH-cycloalkenyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, NHSO 2 -cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , alkenyl, NH-cycloalkynyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, NHSO 2 -cycloalkynyl, NHSO 2 -aryl, O-alkynyl, O-cycloalkynyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , or alkynyl substituents,
(iv) unsubstituted or substituted heterocyclyl, where the heterocyclyl radical may have one or more identical or different OH, O-alkyl, O-aryl, NH-alkyl, NH-aryl, alkyl, aryl, O-alkynyl, NH-alkynyl, alkynyl, O-alkenyl, NH-alkenyl, or alkenyl substituents,
(v) unsubstituted or substituted aryl, where the aryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkylheterocyclyl, NH-alkyl-aryl, NH-alkyl-heteroaryl, NH-alkyl-NH 2 , NH-alkyl-OH, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkylheterocyclyl, O-alkyl-aryl, O-alkyl-heteroaryl, O-alkyl-OH, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NH-alkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(vi) unsubstituted or substituted heteroaryl, where the heteroaryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-aryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkylheterocyclyl, CO 2 -alkylaryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NHalkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(vii) or R6 and R7 together are cycloalkyl, cycloalkenyl, cycloalkynyl or heterocyclyl;
(C) is —C(NR8)R9 where R8 is H and R9 is
(i) unsubstituted or substituted alkyl, alkenyl or alkynyl, where the alkyl, the alkenyl or the alkynyl radical may have one or more identical or different F, Cl, Br, I, CF 3 , NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-hetero-aryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-hetero-cyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 3 H, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NHalkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(ii) unsubstituted or substituted cycloalkyl, cycloalkenyl or cycloalkynyl, where the cycloalkyl, the cycloalkenyl or the cycloalkynyl radical may have one or more identical or different F, Cl, Br, I, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-hetero-aryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, OH, O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , alkyl, aryl, NH-cycloalkenyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, NHSO 2 -cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , alkenyl, NH-cycloalkynyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, NHSO 2 -cycloalkynyl, NHSO 2 -aryl, O-alkynyl, O-cycloalkynyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , or alkynyl substituents,
(iii) unsubstituted or substituted heterocyclyl, where the heterocyclyl radical may have one or more identical or different OH, O-alkyl, O-aryl, NH-alkyl, NH-aryl, alkyl, aryl, O-alkynyl, NH-alkynyl, alkynyl, O-alkenyl, NH-alkenyl, or alkenyl substituents,
(iv) unsubstituted or substituted aryl, where the aryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkyl-heterocyclyl, NH-alkyl-aryl, NH-alkyl-heteroaryl, NH-alkyl-NH 2 , NH-alkyl-OH, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkylheterocyclyl, O-alkyl-aryl, O-alkyl-heteroaryl, O-alkyl-OH, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkylheterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NHalkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(v) unsubstituted or substituted heteroaryl, where the heteroaryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-aryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NHalkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents or a physiologically tolerated salt, solvate or hydrate thereof.
2 . The method of claim 1 , wherein said kinase is a serine/threonine kinase or a tyrosine kinase.
3 . The method of claim 2 , wherein said kinase has an aberrant activation and is associated with a disorder selected from the group consisting of pathological cell proliferation and tumor.
4 . The method of claim 3 , wherein said pathological cell proliferation is selected from the group consisting of restenosis, psoriasis, arteriosclerosis and liver cirrhosis.
5 . The method of claim 3 , wherein said disorder is tumor.
6 . The method of claim 3 , wherein said kinase is selected from the group consisting of c-Raf, B-Raf, Mek, PDGFRbeta, Flt-3, IGF1R, PKB/Akt1, c-Kit, c-Abl, FGFR1 and KDR.
7 . The method of claim 1 , wherein the subject is a human, a mammal or a poultry.
8 . The method of claim 7 , wherein said mammal is a domestic animal selected from the group consisting of horse, cow, dog, cat, rabbit, and sheep.
9 . The method of claim 1 , wherein said pyrido[2,3-b]pyrazine of the general Formula I is at least one compound selected from the group consisting of:
1-allyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-allyl-3-(3-naphthalen-2-ylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-allyl-3-[3-(4-methoxyphenyl)pyrido[2,3-b]pyrazin-6-yl]thiourea; 1-allyl-3-[3-(4-hydroxyphenyl)pyrido[2,3-b]pyrazin-6-yl]thiourea hydrochloride; 1-(2-methylallyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-(2-methylallyl)-3-(3-naphthalen-2-ylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-[3-(4-methoxyphenyl)pyrido[2,3-b]pyrazin-6-yl]-3-(2-methylallyl)thiourea; 1-(3-naphthalen-2-ylpyrido[2,3-b]pyrazin-6-yl)-3-(4-nitrophenyl)thiourea; 1-[3-(4-methoxyphenyl)pyrido[2,3-b]pyrazin-6-yl]-3-(4-nitrophenyl)thiourea; 1-tert-butyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-cyclopropyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-methyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-benzyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-(4-fluorophenyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-(3-phenylpyrido[2,3-b]pyrazin-6-yl)-3-p-tolylurea; 1-(4-chloro-3-trifluoromethylphenyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)urea; and 1-(2-morpholin-4-ylethyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)urea.
10 . A method of modulating function of a kinase, comprising:
administering to a subject in need thereof a pharmaceutical composition comprising a pyrido[2,3-b]pyrazine compound selected from the group consisting of: 1-allyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-allyl-3-(3-naphthalen-2-ylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-allyl-3-[3-(4-methoxyphenyl)pyrido[2,3-b]pyrazin-6-yl]thiourea; 1-allyl-3-[3-(4-hydroxyphenyl)pyrido[2,3-b]pyrazin-6-yl]thiourea hydrochloride; 1-(2-methylallyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-(2-methylallyl)-3-(3-naphthalen-2-ylpyrido[2,3-b]pyrazin-6-yl) thiourea; 1-[3-(4-methoxyphenyl)pyrido[2,3-b]pyrazin-6-yl)-3-(2-methylallyl) thiourea; 1-(3-naphthalen-2-ylpyrido[2,3-b]pyrazin-6-yl)-3-(4-nitrophenyl) thiourea; 1-[3-(4-methoxyphenyl)pyrido[2,3-b]pyrazin-6-yl]-3-(4-nitrophenyl) thiourea; 1-tert-butyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-cyclopropyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-methyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-benzyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-(4-fluorophenyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-(3-phenylpyrido[2,3-b]pyrazin-6-yl)-3-p-tolylurea; 1-(4-chloro-3-trifluoromethylphenyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)urea; and 1-(2-morpholin-4-ylethyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)urea;
and a pharmaceutically acceptable diluent thereof.
11 . The method of claim 10 , wherein said kinase is a serine/threonine kinase or a tyrosine kinase.
12 . The method of claim 11 , wherein said kinase has an aberrant activation and is associated with a disorder selected from the group consisting of pathological cell proliferation and tumor.
13 . The method of claim 12 , wherein said pathological cell proliferation is selected from the group consisting of restenosis, psoriasis, arteriosclerosis and liver cirrhosis.
14 . The method of claim 12 , wherein said disorder is tumor.
15 . The method of claim 12 , wherein said kinase is selected from the group consisting of c-Raf, B-Raf, Mek, PDGFRbeta, Flt-3, IGF1R, PKB/Akt1, c-Kit, c-Abl, FGFR1 and KDR.
16 . The method of claim 10 , wherein the subject is a human, a mammal or a poultry.
17 . The method of claim 16 , wherein said mammal is a domestic animal selected from the group consisting of horse, cow, dog, cat, rabbit, and sheep.
18 . A method of administering to a subject in need thereof a pharmaceutical composition comprising a compound; and a pharmaceutically acceptable diluent, said compound is a pyrido[2,3-b]pyrazine of the general Formula I
in which the substituents R1-R3 have the following meaning:
R1 and R2 are independently of one another:
(i) hydrogen
(ii) hydroxyl
(iii) alkyl, alkenyl or alkynyl, where the alkyl radical is saturated and having 1 to 8 C atoms, the alkenyl radical has 2 to 8 C atoms, the alkynyl radical has 2 to 8 C atoms,
(iv) unsubstituted or substituted aryl, where the aryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-hetero-aryl, NH-alkyl-cycloalkyl, NH-alkyl-heterocyclyl, NH-alkyl-aryl, NH-alkyl-heteroaryl, NH-alkyl-NH 2 , NH-alkyl-OH, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl-heterocyclyl, O-alkyl-aryl, O-alkyl-heteroaryl, O-alkyl-OH, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkylcycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NH-alkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenylheterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkylcycloalkenyl, CO 2 -alkenyl-heterocyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, alkenyl, cycloalkenyl, NH-alkyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkylcycloalkynyl, CO 2 -alkynyl-heterocyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents, and the alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, alkyl-cycloalkyl, alkyl-heterocyclyl, alkyl-aryl, alkylheteroaryl, alkenyl, cycloalkenyl, alkenyl-cycloalkenyl, alkenyl-heterocyclyl, alkenyl-aryl, alkenylheteroaryl, alkynyl, cycloalkynyl, alkynyl-cycloalkynyl, alkynyl-heterocyclyl, alkynyl-aryl, alkynylheteroaryl substituents may in turn themselves be substituted,
(v) unsubstituted or substituted heteroaryl, where the heteroaryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-aryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-aryl, O-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-hetero-cyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, N(alkyl) 2 , SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl, NH-cycloalkenyl, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, O-alkenyl, O-cycloalkenyl, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, N(alkenyl) 2 , SO 2 O-alkenyl, alkenyl, cycloalkenyl, NH-alkynyl, NH-cycloalkynyl, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, O-alkynyl, O-cycloalkynyl, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, N(alkynyl) 2 , SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents, and the alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, alkenyl, cycloalkenyl, alkynyl, and cycloalkynyl substituents may in turn themselves be substituted.
R3 is A, B, or C, where:
(A) is —C(Y)NR4R5, where Y is O, or S and R4 and R5 are independently of one another
(i) hydrogen,
(ii) unsubstituted or substituted alkyl, alkenyl or alkynyl, where the alkyl, the alkenyl or the alkynyl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO2, SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-hetero-cyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-hetero-cyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N (aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 3 H, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl, NH-cycloalkenyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, NHSO 2 -cycloalkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-hetero-cyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO 2 -alkenyl, alkenyl, cycloalkenyl, NH-alkynyl, NH-cycloalkynyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, NHSO 2 -cycloalkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-hetero-cyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO 2 -alkynyl, alkynyl, or cycloalkynyl, substituents,
(iii) unsubstituted or substituted cycloalkyl, cycloalkenyl, or cycloalkynyl, where the cycloalkyl, the cycloalkenyl or the cycloalkynyl radical may have one or more identical or different F, Cl, Br, I, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, OH, O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, CO2H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, C(O)—NH 2 , C(O)NH-aryl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , alkyl, aryl, NH-alkenyl, NH-cycloalkenyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, NHSO 2 -cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , alkenyl, NH-alkynyl, NH-cycloalkynyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, NHSO 2 -cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , or alkynyl substituents,
(iv) unsubstituted or substituted heterocyclyl, where the heterocyclyl radical may have one or more identical or different OH, O-alkyl, O-aryl, NH-alkyl, NH-aryl, alkyl, alkyl-aryl, aryl, O-alkenyl, NH-alkenyl, alkenyl, alkenyl-aryl, O-alkynyl, NH-alkynyl, alkynyl, or alkynyl-aryl substituents,
(v) unsubstituted or substituted aryl, where the aryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkyl-heterocyclyl, NH-alkyl-aryl, NH-alkyl-heteroaryl, NH-alkyl-NH 2 , NH-alkyl-OH, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl-heterocyclyl, O-alkyl-aryl, O-alkyl-heteroaryl, O-alkyl-OH, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-hetero-cyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-hetero-cyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NH-alkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(vi) unsubstituted or substituted heteroaryl, where the heteroaryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-aryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO2-aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NH-alkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(vii) or R4 and R5 together are cycloalkyl cycloalkenyl, cycloalkynyl or heterocyclyl;
(B) is —C(Y)NR6R7, where Y is NH and R6 and R7 are independently of one another
(i) hydrogen,
(ii) unsubstituted or substituted alkyl, alkenyl or alkynyl, where the alkyl, the alkenyl or the alkynyl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-hetero-aryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO2-heterocyclyl, CO 2 -aryl, CO2-heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkylheterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-hetero-cyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-hetero-aryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 3 H, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NH-alkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(iii) unsubstituted or substituted cycloalkyl, cycloalkenyl or cycloalkynyl, where the cycloalkyl, the cycloalkenyl or the cycloalkynyl radical may have one or more identical or different F, Cl, Br, I, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, OH, O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocycyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , alkyl, aryl, NH-cycloalkenyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, NHSO 2 -cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , alkenyl, NH-cycloalkynyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, NHSO 2 -cycloalkynyl, NHSO 2 -aryl, O-alkynyl, O-cycloalkynyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , or alkynyl substituents,
(iv) unsubstituted or substituted heterocyclyl, where the heterocyclyl radical may have one or more identical or different OH, O-alkyl, O-aryl, NH-alkyl, NH-aryl, alkyl, aryl, O-alkynyl, NH-alkynyl, alkynyl, O-alkenyl, NH-alkenyl, or alkenyl substituents,
(v) unsubstituted or substituted aryl, where the aryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkylheterocyclyl, NH-alkyl-aryl, NH-alkyl-heteroaryl, NH-alkyl-NH 2 , NH-alkyl-OH, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkylheterocyclyl, O-alkyl-aryl, O-alkyl-heteroaryl, O-alkyl-OH, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NH-alkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(vi) unsubstituted or substituted heteroaryl, where the heteroaryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , CN, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-aryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkylheterocyclyl, CO 2 -alkylaryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NHalkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(vii) or R6 and R7 together are cycloalkyl, cycloalkenyl, cycloalkynyl or heterocyclyl;
(C) is —C(NR8)R9 where R8 is H and R9 is
(i) unsubstituted or substituted alkyl, alkenyl or alkynyl, where the alkyl, the alkenyl or the alkynyl radical may have one or more identical or different F, Cl, Br, I, CF 3 , NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-hetero-aryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-hetero-cyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 3 H, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NHalkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(ii) unsubstituted or substituted cycloalkyl, cycloalkenyl or cycloalkynyl, where the cycloalkyl, the cycloalkenyl or the cycloalkynyl radical may have one or more identical or different F, Cl, Br, I, NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-hetero-aryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -cycloalkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, OH, O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-aryl, O-alkyl-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , alkyl, aryl, NH-cycloalkenyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, NHSO 2 -cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , alkenyl, NH-cycloalkynyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, NHSO 2 -cycloalkynyl, NHSO 2 -aryl, O-alkynyl, O-cycloalkynyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , or alkynyl substituents,
(iii) unsubstituted or substituted heterocyclyl, where the heterocyclyl radical may have one or more identical or different OH, O-alkyl, O-aryl, NH-alkyl, NH-aryl, alkyl, aryl, O-alkynyl, NH-alkynyl, alkynyl, O-alkenyl, NH-alkenyl, or alkenyl substituents,
(iv) unsubstituted or substituted aryl, where the aryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-cycloalkyl, NH-alkyl-heterocyclyl, NH-alkyl-aryl, NH-alkyl-heteroaryl, NH-alkyl-NH 2 , NH-alkyl-OH, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-cycloalkyl, S-heterocyclyl, S-aryl, S-heteroaryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, O-alkyl-cycloalkyl, O-alkylheterocyclyl, O-alkyl-aryl, O-alkyl-heteroaryl, O-alkyl-OH, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkylheterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO-alkyl, SO-aryl, SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NHalkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents,
(v) unsubstituted or substituted heteroaryl, where the heteroaryl radical may have one or more identical or different F, Cl, Br, I, CF 3 , NH 2 , NH-alkyl, NH-cycloalkyl, NH-heterocyclyl, NH-aryl, NH-heteroaryl, NH-alkyl-aryl, NH-alkyl-heteroaryl, N(alkyl) 2 , NHC(O)-alkyl, NHC(O)-cycloalkyl, NHC(O)-heterocyclyl, NHC(O)-aryl, NHC(O)-heteroaryl, NHSO 2 -alkyl, NHSO 2 -aryl, NHSO 2 -heteroaryl, NO 2 , SH, S-alkyl, S-aryl, OH, OCF 3 , O-alkyl, O-cycloalkyl, O-heterocyclyl, O-aryl, O-heteroaryl, OC(O)-alkyl, OC(O)-cycloalkyl, OC(O)-heterocyclyl, OC(O)-aryl, OC(O)-heteroaryl, OSO 2 -alkyl, OSO 2 -cycloalkyl, OSO 2 -aryl, OSO 2 -heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, CO 2 H, CO 2 -alkyl, CO 2 -cycloalkyl, CO 2 -heterocyclyl, CO 2 -aryl, CO 2 -heteroaryl, CO 2 -alkyl-cycloalkyl, CO 2 -alkyl-heterocyclyl, CO 2 -alkyl-aryl, CO 2 -alkyl-heteroaryl, C(O)—NH 2 , C(O)NH-alkyl, C(O)NH-cycloalkyl, C(O)NH-heterocyclyl, C(O)NH-aryl, C(O)NH-heteroaryl, C(O)NH-alkyl-cycloalkyl, C(O)NH-alkyl-heterocyclyl, C(O)NH-alkyl-aryl, C(O)NH-alkyl-heteroaryl, C(O)N(alkyl) 2 , C(O)N(cycloalkyl) 2 , C(O)N(aryl) 2 , C(O)N(heteroaryl) 2 , SO 2 -alkyl, SO 2 -aryl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 NH-aryl, SO 2 NH-heteroaryl, SO 3 H, SO 2 O-alkyl, SO 2 O-aryl, SO 2 O-heteroaryl, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, NH-alkenyl-cycloalkenyl, NH-alkenyl-heterocyclyl, NH-alkenyl-aryl, NH-alkenyl-heteroaryl, NHalkenyl-NH 2 , NH-alkenyl-OH, N(alkenyl) 2 , NHC(O)-alkenyl, NHC(O)-cycloalkenyl, NHSO 2 -alkenyl, S-alkenyl, S-cycloalkenyl, O-alkenyl, O-cycloalkenyl, O-alkenyl-cycloalkenyl, O-alkenyl-heterocyclyl, O-alkenyl-aryl, O-alkenyl-heteroaryl, O-alkenyl-OH, OC(O)-alkenyl, OC(O)-cycloalkenyl, OSO 2 -alkenyl, OSO 2 -cycloalkenyl, C(O)-alkenyl, CO 2 -alkenyl, CO 2 -cycloalkenyl, CO 2 -alkenyl-cycloalkenyl, CO 2 -alkenyl-hetero-cyclyl, CO 2 -alkenyl-aryl, CO 2 -alkenyl-heteroaryl, C(O)NH-alkenyl, C(O)NH-cycloalkenyl, C(O)NH-alkenyl-cycloalkenyl, C(O)NH-alkenyl-heterocyclyl, C(O)NH-alkenyl-aryl, C(O)NH-alkenyl-heteroaryl, C(O)N(alkenyl) 2 , C(O)N(cycloalkenyl) 2 , SO-alkenyl, SO 2 -alkenyl, SO 2 NH-alkenyl, SO 2 O-alkenyl, SO 2 O-aryl, alkenyl, cycloalkenyl, NH-alkynyl-cycloalkynyl, NH-alkynyl-heterocyclyl, NH-alkynyl-aryl, NH-alkynyl-heteroaryl, NH-alkynyl-NH 2 , NH-alkynyl-OH, N(alkynyl) 2 , NHC(O)-alkynyl, NHC(O)-cycloalkynyl, NHSO 2 -alkynyl, S-alkynyl, S-cycloalkynyl, O-alkynyl, O-cycloalkynyl, O-alkynyl-cycloalkynyl, O-alkynyl-heterocyclyl, O-alkynyl-aryl, O-alkynyl-heteroaryl, O-alkynyl-OH, OC(O)-alkynyl, OC(O)-cycloalkynyl, OSO 2 -alkynyl, OSO 2 -cycloalkynyl, C(O)-alkynyl, CO 2 -alkynyl, CO 2 -cycloalkynyl, CO 2 -alkynyl-cycloalkynyl, CO 2 -alkynyl-hetero-cyclyl, CO 2 -alkynyl-aryl, CO 2 -alkynyl-heteroaryl, C(O)NH-alkynyl, C(O)NH-cycloalkynyl, C(O)NH-alkynyl-cycloalkynyl, C(O)NH-alkynyl-heterocyclyl, C(O)NH-alkynyl-aryl, C(O)NH-alkynyl-heteroaryl, C(O)N(alkynyl) 2 , C(O)N(cycloalkynyl) 2 , SO-alkynyl, SO 2 -alkynyl, SO 2 NH-alkynyl, SO 2 O-alkynyl, alkynyl, or cycloalkynyl substituents or a physiologically tolerated salt, solvate or hydrate thereof,
wherein said compound, when tested in an in vitro kinase assay of a kinase selected from the group consisting of PKB/Akt1, c-Raf, B-Raf, Mek, PDGFRbeta, Flt-3, c-Kit, c-Abl, KDR, FGFR1, and IGF1R, exhibits an inhibitory effect on the kinase.
19 . The method of claim 18 , wherein said subject suffers from a disorder selected from the group consisting of pathological cell proliferation and tumor.
20 . The method of claim 19 , wherein said pathological cell proliferation is selected from the group consisting of restenosis, psoriasis, arteriosclerosis and liver cirrhosis.
21 . The method of claim 19 , wherein said disorder is tumor.
22 . The method of claim 18 , wherein the subject is a human, a mammal or a poultry.
23 . The method of claim 22 , wherein said mammal is a domestic animal selected from the group consisting of horse, cow, dog, cat, rabbit, and sheep.
24 . The method of claim 18 , wherein said pyrido[2,3-b]pyrazine of the general Formula I is at least one compound selected from the group consisting of:
1-allyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-allyl-3-(3-naphthalen-2-ylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-allyl-3-[3-(4-methoxyphenyl)pyrido[2,3-b]pyrazin-6-yl]thiourea; 1-allyl-3-[3-(4-hydroxyphenyl)pyrido[2,3-b]pyrazin-6-yl]thiourea hydrochloride; 1-(2-methylallyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-(2-methylallyl)-3-(3-naphthalen-2-ylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-[3-(4-methoxyphenyl)pyrido[2,3-b]pyrazin-6-yl]-3-(2-methylallyl)thiourea; 1-(3-naphthalen-2-ylpyrido[2,3-b]pyrazin-6-yl)-3-(4-nitrophenyl)thiourea; 1-[3-(4-methoxyphenyl)pyrido[2,3-b]pyrazin-6-yl]-3-(4-nitrophenyl)thiourea; 1-tert-butyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-cyclopropyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-methyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-benzyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-(4-fluorophenyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea; 1-(3-phenylpyrido[2,3-b]pyrazin-6-yl)-3-p-tolylurea; 1-(4-chloro-3-trifluoromethylphenyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl) urea; and 1-(2-morpholin-4-ylethyl)-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)urea.Cited by (0)
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