US10385026B2ActiveUtilityA1
Phthalazinones and isoquinolinones as rock inhibitors
Est. expiryJan 18, 2033(~6.5 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 37/02A61P 9/12A61P 9/10A61P 9/08A61P 9/04A61P 9/02A61P 9/00A61P 35/00A61P 29/00A61P 27/06A61P 27/02A61P 25/28A61P 25/00A61P 21/02A61P 21/00A61P 19/04A61P 19/02A61P 15/10A61P 11/06A61P 11/00A61P 1/04C07D 237/32C07D 405/12A61K 31/496C07D 401/12A61K 31/428C07D 513/04C07D 403/12C07D 405/10C07D 403/10C07D 487/04C07D 217/24C07D 417/12A61K 31/422C07D 417/14C07D 471/04A61K 31/497A61K 31/4985A61K 31/519C07D 491/048C07D 413/12C07D 413/10A61K 31/5377C07D 405/14C07D 409/14C07D 401/10C07D 417/10A61K 31/502A61K 31/4545C07D 403/14A61K 31/437C07D 401/14C07D 413/14
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Claims
Abstract
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1. A compound of Formula (I):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof, wherein:
M is N;
L is selected from —CR 4 R 4 C(O)—, —OC(O)—, —NR 6 C(O)—, and —NR 6 —;
R 1 is selected from NR 5 R 5 , C 3-10 carbocycle and 4- to 15-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p ; wherein said carbocycle and heterocycle are substituted with 1-4 R 7 ;
R 2 , at each occurrence, is independently selected from halogen, C 1-6 alkyl, C 1-4 alkoxy, C 1-4 alkylthio, C 1-4 haloalkyl, —OH, —CH 2 OH, —OCH 2 F, —OCHF 2 , —OCF 3 , CN, —NH 2 , —NH(C 1-4 alkyl), —N(C 1-4 alkyl) 2 , —CO 2 H, —CH 2 CO 2 H, —CO 2 (C 1-4 alkyl), —CO(C 1-4 alkyl), —CH 2 NH 2 , —CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , —OCH 2 CO 2 H, —NHCO(C 1-4 alkyl), —NHCO 2 (C 1-4 alkyl), —NHSO 2 (C 1-4 alkyl), —SO 2 NH 2 , —C(═NH)NH 2 , carbocycle, and heterocycle, wherein said alkyl, alkoxy, alkylthio, haloalkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 3 , at each occurrence, is independently selected from halogen, C 1-6 alkyl, C 1-4 alkoxy, C 1-4 alkylthio, C 1-4 haloalkyl, —CH 2 OH, —OCH 2 F, —OCHF 2 , —OCF 3 , CN, —NH 2 , —NH(C 1-4 alkyl), —N(C 1-4 alkyl), 2 , —CO 2 H, —CH 2 CO 2 H, —CO 2 (C 1-4 alkyl), —CO(C 1-4 alkyl), —CH 2 NH 2 , —CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , —OCH 2 CO 2 H, —NHCO(C 1-4 alkyl), —NHCO 2 (C 1-4 alkyl), —NHSO 2 (C 1-4 alkyl), —SO 2 NH 2 , —C(═NH)NH 2 , carbocycle, and heterocycle, wherein said alkyl, alkoxy, alkylthio, haloalkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 4 , at each occurrence, is independently selected from H, OH, NH 2 , CH 2 NH 2 , C 1-4 haloalkyl, OCH 2 F, OCHF 2 , OCF 3 , —NH(C 1-4 alkyl), —N(C 1-4 alkyl) 2 , C 1-4 alkoxy, CH 2 OH, CH 2 O(C 1-4 alkyl), CH 2 CO 2 H, CH 2 CO 2 (C 1-4 alkyl), C 1-4 alkyl, carbocycle, and heterocycle, wherein said alkyl, alkoxy, haloalkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 5 , at each occurrence, is independently selected from H, C 1-4 alkyl, —(CR 6 R 6 ) n —C 3-10 carbocycle and —(CR 6 R 6 ) n -4-10 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, carbocycle and heterocycle are substituted with 1-4 R 7 ;
alternatively, R 5 and R 5 are taken together with the nitrogen atom to which they are attached to form 4- to 15-membered heterocycle substituted with 1-4 R 7 ;
R 6 , at each occurrence, is independently selected from H and C 1-4 alkyl;
R 7 , at each occurrence, is independently selected from H, ═O, NO 2 , halogen, C 1-4 alkyl, C 1-4 alkoxy, CN, OH, CF 3 , —(CH 2 ) n —CO 2 H, —(CH 2 ) n —CO 2 (C 1-4 alkyl), —(CH 2 ) n —NR 8 R 8 , —NHCO(C 1-4 alkyl), —NHCOCF 3 , —NHCO 2 (C 1-4 alkyl), —NHCO 2 (CH 2 ) 2 O(C 1-4 alkyl), —NHCO 2 (CH 2 ) 3 O(C 1-4 alkyl), —NHCO 2 (CH 2 ) 2 OH, —NHCO 2 (CH 2 ) 2 NH 2 , —NHCO 2 (CH 2 ) 2 N(C 1-4 alkyl) 2 , —NHCO 2 CH 2 CO 2 H, —CH 2 NHCO 2 (C 1-4 alkyl), —NHC(O)NR 8 R 8 , —NHSO 2 (C 1-4 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1-4 alkyl), —SO 2 N(C 1-4 alkyl) 2 , —SO 2 NH(CH 2 ) 2 OH, —SO 2 NH(CH 2 ) 2 O(C 1-4 alkyl), —(CH 2 ) n —CONR 8 R 8 , —O(CH 2 ) n -carbocycle, —O(CH 2 ) n -heterocycle, —NHCO-carbocycle, —NHCO-heterocycle, —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 8 , at each occurrence, is independently selected from H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, —(CH 2 ) n —C(O)C 1-4 alkyl, —(CH 2 ) n —C(O)carbocycle, —(CH 2 ) n —C(O)heterocycle, —(CH 2 ) n —C(O)NR a R a , —(CH 2 ) n —C(O)O-alkyl, —(CH 2 ) n —C(O)O-carbocycle, —(CH 2 ) n —C(O)O-heterocycle, —(CH 2 ) n —SO 2 alkyl, —(CH 2 ) n SO 2 carbocycle, —(CH 2 ) n —SO 2 heterocycle, —(CH 2 ) n —SO 2 NR a R a , —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle, wherein said alkyl, alkenyl, alkynyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
alternatively, R 8 and R 8 are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle substituted with 0-4 R 9 ;
R 9 , at each occurrence, is independently selected from halogen, OH, NO 2 , CHF 2 , CF 3 , C 1-4 alkyl, C 1-4 alkoxy, CH 2 OH, CO(C 1-4 alkyl), CO 2 H, CO 2 (C 1-4 alkyl), —(CH 2 ) n NR a R a , —(CH 2 ) n CONR a R a , —O(CH 2 ) n carbocycle, —O(CH 2 ) n heterocycle, —O(CH 2 ) n NR a R a , —(CR 10 R 10 ) n -4-10 membered heterocycle, wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R b ;
R 10 is selected from H and C 1-4 alkyl;
R a , at each occurrence, is independently selected from H, C 1-4 alkyl, —(CH 2 ) n OH, CO(C 1-4 alkyl), COCF 3 , CO 2 (C 1-4 alkyl), —CONH 2 , —CONH—C 1-4 alkylene-CO 2 (C 1-4 alkyl), C 1-4 alkylene-CO 2 (C 1-4 alkyl), R c , CO 2 R c , and CONHR c ; alternatively, R a and R a are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle, wherein said alkyl, alkylene, and heterocycle are substituted with 0-4 R b ;
R b , at each occurrence, is independently selected from ═O, OH, halogen, C 1-4 alkyl, C 1-4 alkoxy, OCF 3 , NH 2 , NO 2 , N(C 1-4 alkyl) 2 , CO(C 1-4 alkyl), CO(C 1-4 haloalkyl), CO 2 (C 1-4 alkyl), CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , —CONH—C 1-4 alkylene-O(C 1-4 alkyl), —CONH—C 1-4 alkylene-N(C 1-4 alkyl) 2 , —CONH—C 1-4 alkylene-N(C 1-4 alkyl) 2 , —C 1-4 alkylene-O—P(O)(OH) 2 , —NHCO 2 (C 1-4 alkyl), —R c , COR c , CO 2 R c , and CONHR c ;
R c , at each occurrence, is independently selected from —(CH 2 ) n —C 3-6 cycloalkyl, —(CH 2 ) n -phenyl, and —(CH 2 ) n -5- to 6-membered heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4 alkyl), O, and S(O) p ; wherein each ring moiety is substituted with 0-2 R d ;
R d , at each occurrence, is independently selected from ═O, halogen, —OH, C 1-4 alkyl, NH 2 , NH(C 1-4 alkyl), N(C 1-4 alkyl) 2 , C 1-4 alkoxy, and —NHCO(C 1-4 alkyl), and heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4 alkyl), O, and S(O) p ;
n, at each occurrence, is independently selected from 0, 1, 2, 3, and 4;
p, at each occurrence, is independently selected from 0, 1, and 2;
provided
when L is NHC(O), R 1 is other than
wherein X is N or a substituted or unsubstituted carbon atom;
when L is NR 6 , R 1 is heterocycle substituted with 1-4 R 7 ; wherein “carbocycle” means a 3- to 13 membered hydrocarbon ring; “heterocycle” if the ring size is not defined means a 3- to 13 membered heterocycle comprising carbon atoms and 1, 2, 3 or 4 heteroatoms independently selected from the group consisting of N, O and S.
2. The compound of claim 1 , having Formula (II):
or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein:
M is N;
R 5 , at each occurrence, is independently selected from H, C 1-4 alkyl, —(CR 6 R 6 ) n —C 3-10 carbocycle, and —(CR 6 R 6 ) n -4-10 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, carbocycle, and heterocycle are substituted with 1-4 R 7 ;
alternatively, R 5 and R 5 are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle substituted with 1-4 R 7 ;
R 7 , at each occurrence, is independently selected from H, ═O, NO 2 , halogen, C 1-4 alkyl, C 1-4 alkoxy, CN, OH, CF 3 , —(CH 2 ) n —CO 2 H, —(CH 2 ) n —CO 2 (C 1-4 alkyl), —(CH 2 ) n —NR 8 R 8 , —NHCO(C 1-4 alkyl), —NHCOCF 3 , —NHCO 2 (C 1-4 alkyl), —NHCO 2 (CH 2 ) 2 O(C 1-4 alkyl), —NHCO 2 (CH 2 ) 3 O(C 1-4 alkyl), —NHCO 2 (CH 2 ) 2 OH, —NHCO 2 (CH 2 ) 2 NH 2 , —NHCO 2 (CH 2 ) 2 N(C 1-4 alkyl) 2 , —NHCO 2 CH 2 CO 2 H, —CH 2 NHCO 2 (C 1-4 alkyl), —NHC(O)NR 8 R 8 , —NHSO 2 (C 1-4 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1-4 alkyl), —SO 2 N(C 1-4 alkyl) 2 , —SO 2 NH(CH 2 ) 2 OH, —SO 2 NH(CH 2 ) 2 O(C 1-4 alkyl), —(CH 2 ) n —CONR 8 R 8 , —O(CH 2 ) n -carbocycle, —O(CH 2 ) n -heterocycle, —NHCO-carbocycle, —NHCO-heterocycle, —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 8 , at each occurrence, is independently selected from H, C 1-4 alkyl, C(O)C 1-4 alkyl, C(O)carbocycle, C(O)heterocycle, —(CH 2 ) n C(O)NR a R a , C(O)O-alkyl, C(O)O-carbocycle, C(O)O-heterocycle, SO 2 alkyl, SO 2 carbocycle, SO 2 heterocycle, SO 2 NR a R a , —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle, wherein said alkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 9 , at each occurrence, is independently selected from halogen, OH, NO 2 , CHF 2 , CF 3 , C 1-4 alkyl, C 1-4 alkoxy, CH 2 OH, CO 2 H, CO 2 (C 1-4 alkyl), CONH 2 , —(CH 2 ) n NR a R a , —(CH 2 ) n CONR a R a , —O(CH 2 ) n heterocycle, —O(CH 2 ) (2-4) NR a R a , —(CR 10 R 10 ) n -4-10 membered heterocycle, wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R b ;
R 10 is selected from H and C 1-4 alkyl;
R a , at each occurrence, is independently selected from H, C 1-4 alkyl, —(CH 2 ) n OH, CO(C 1-4 alkyl), COCF 3 , CO 2 (C 1-4 alkyl), —CONH 2 , —CONH—C 1-4 alkylene-CO 2 (C 1-4 alkyl), C 1-4 alkylene-CO 2 (C 1-4 alkyl), R c , CO 2 R c , and CONHR c ; alternatively, R a and R a are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle, wherein said alkyl, alkylene, and heterocycle are substituted with 0-4 R b ;
R b , at each occurrence, is independently selected from ═O, halogen, C 1-4 alkyl, C 1-4 alkoxy, OCF 3 , NH 2 , NO 2 , N(C 1-4 alkyl) 2 , CO(C 1-4 alkyl), CO(C 1-4 haloalkyl), CO 2 (C 1-4 alkyl), CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , —CONH—C 1-4 alkylene-O(C 1-4 alkyl), —CONH—C 1-4 alkylene-N(C 1-4 alkyl) 2 , —CONH—C 1-4 alkylene-N(C 1-4 alkyl) 2 , —C 1-4 alkylene-O—P(O)(OH) 2 , —NHCO 2 (C 1-4 alkyl), —R c , COR c , CO 2 R c , and CONHR c ;
R c , at each occurrence, is independently selected from —(CH 2 ) n —C 3-6 cycloalkyl, —(CH 2 ) n -phenyl, and —(CH 2 ) n -5- to 6-membered heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4 alkyl), O, and S(O) p ; wherein each ring moiety is substituted with 0-2 R d ;
R d , at each occurrence, is independently selected from ═O, halogen, —OH, C 1-4 alkyl, NH 2 , NH(C 1-4 alkyl), N(C 1-4 alkyl) 2 , C 1-4 alkoxy, and —NHCO(C 1-4 alkyl), and heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4 alkyl), O, and S(O) p ;
n, at each occurrence, is independently selected from 0, 1, 2, 3, and 4;
p, at each occurrence, is independently selected from 0, 1, and 2.
3. The compound of claim 2 , wherein:
R 5 is selected from H, C 1-4 alkyl, —(CH 2 ) n —C 3-10 cycloalkyl, —(CH 2 ) n -aryl, —(CH 2 ) n -4-10 membered heterocycle selected from
wherein said alkyl, cycloalkyl, aryl are substituted with 1-4 R 7 .
4. The compound of claim 2 , wherein:
R 5 and R 5 are taken together with the nitrogen atom to which they are attached to form a heterocycle selected from
R 7 , at each occurrence, is independently selected from H, ═O, halogen, C 1-4 alkyl, C 1-4 alkoxy, CN, OH, CF 3 , —(CH 2 ) n —CO 2 H, —(CH 2 ) n —CO 2 (C 1-4 alkyl), —(CH 2 ) n —NR 8 R 8 , —CH 2 NH 2 , —NHCO(C 1-4 alkyl), —NHCOCF 3 , —NHCO 2 (C 1-4 alkyl), —NHC(O)NH 2 , —NHC(O)NH(C 1-4 alkyl), —NHC(O)N(C 1-4 alkyl) 2 , —NHSO 2 (C 1-4 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1-4 alkyl), —SO 2 N(C 1-4 alkyl) 2 , —SO 2 NH(CH 2 ) 2 OH, —SO 2 NH(CH 2 ) 2 O(C 1-4 alkyl), —(CH 2 ) n —CONR 8 R 8 , —O(CH 2 ) n -carbocycle, —O(CH 2 ) n -heterocycle, —NHCO-carbocycle, —NHCO-heterocycle, —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 8 , at each occurrence, is independently selected from H, C 1-4 alkyl, C(O)C 1-4 alkyl, C(O)carbocycle, C(O)heterocycle, —(CH 2 ) n —C(O)NR a R a , C(O)O-alkyl, C(O)O-carbocycle, C(O)O-heterocycle, SO 2 alkyl, SO 2 carbocycle, SO 2 heterocycle, SO 2 NR a R a , —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle, wherein said alkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
alternatively, R 8 and R 8 are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle substituted with 0-4 R 9 ; and
R 9 , at each occurrence, is independently selected from halogen, OH, NO 2 , CHF 2 , CF 3 , C 1-4 alkyl, C 1-4 alkoxy, CH 2 OH, CO 2 H, CO 2 (C 1-4 alkyl), CONH 2 , —(CH 2 ) n NR a R a , —(CH 2 ) n CONR a R a , —O(CH 2 ) n heterocycle, —O(CH 2 ) (2-4) NR a R a , —(CR 10 R 10 ) n -4-10 membered heterocycle, wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R b ;
R a , at each occurrence, is independently selected from H, C 1-4 alkyl, —(CH 2 ) n OH, CO(C 1-4 alkyl), COCF 3 , CO 2 (C 1-4 alkyl), —CONH 2 , —CONH—C 1-4 alkylene-CO 2 (C 1-4 alkyl), C 1-4 alkylene-CO 2 (C 1-4 alkyl), R c , CO 2 R c , and CONHR c ; alternatively, R a and R a are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle, wherein said alkyl, alkylene, and heterocycle are substituted with 0-4 R b ;
R b , at each occurrence, is independently selected from ═O, halogen, C 1-4 alkyl, C 1-4 alkoxy, OCF 3 , NH 2 , NO 2 , N(C 1-4 alkyl) 2 , CO(C 1-4 alkyl), CO(C 1-4 haloalkyl), CO 2 (C 1-4 alkyl), CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , —CONH—C 1-4 alkylene-O(C 1-4 alkyl), —CONH—C 1-4 alkylene-N(C 1-4 alkyl) 2 , —CONH—C 1-4 alkylene-N(C 1-4 alkyl) 2 , —C 1-4 alkylene-O—P(O)(OH) 2 , —NHCO 2 (C 1-4 alkyl), —R c , COR c , CO 2 R c , and CONHR c ;
R c , at each occurrence, is independently selected from —(CH 2 ) n —C 3-6 cycloalkyl, —(CH 2 ) n -phenyl, and —(CH 2 ) n -5- to 6-membered heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4 alkyl), O, and S(O) p ; wherein each ring moiety is substituted with 0-2 R d ; and
R d , at each occurrence, is independently selected from ═O, halogen, —OH, C 1-4 alkyl, NH 2 , NH(C 1-4 alkyl), N(C 1-4 alkyl) 2 , C 1-4 alkoxy, and —NHCO(C 1-4 alkyl), and heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4 alkyl), O, and S(O) p .
5. The compound of claim 1 , having Formula (III):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof, wherein:
M is N;
R 5 , at each occurrence, is independently selected from H, C 1-4 alkyl, —(CR 6 R 6 ) n —C 3-10 carbocycle, and —(CR 6 R 6 ) n -4-10 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, carbocycle, and heterocycle are substituted with 1-4 R 7 ;
alternatively, R 5 and R 5 are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle substituted with 1-4 R 7 ;
R 6 , at each occurrence, is independently selected from H and C 1-4 alkyl;
R 7 , at each occurrence, is independently selected from H, ═O, NO 2 , halogen, C 1-4 alkyl, C 1-4 alkoxy, CN, OH, CF 3 , —(CH 2 ) n —CO 2 H, —(CH 2 ) n —CO 2 (C 1-4 alkyl), —(CH 2 ) n —NR 8 R 8 , —NHCO(C 1-4 alkyl), —NHCOCF 3 , —NHCO 2 (C 1-4 alkyl), —NHCO 2 (CH 2 ) 2 O(C 1-4 alkyl), —NHCO 2 (CH 2 ) 3 O(C 1-4 alkyl), —NHCO 2 (CH 2 ) 2 OH, —NHCO 2 (CH 2 ) 2 NH 2 , —NHCO 2 (CH 2 ) 2 N(C 1-4 alkyl) 2 , —NHCO 2 CH 2 CO 2 H, —CH 2 NHCO 2 (C 1-4 alkyl), —NHC(O)NR 8 R 8 , —NHSO 2 (C 1-4 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1-4 alkyl), —SO 2 N(C 1-4 alkyl) 2 , —SO 2 NH(CH 2 ) 2 OH, —SO 2 NH(CH 2 ) 2 O(C 1-4 alkyl), —(CH 2 ) n —CONR 8 R 8 , —O(CH 2 ) n -carbocycle, —O(CH 2 ) n -heterocycle, —NHCO-carbocycle, —NHCO-heterocycle, —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 8 , at each occurrence, is independently selected from H, C 1-4 alkyl, C(O)C 1-4 alkyl, C(O)carbocycle, C(O)heterocycle, —(CH 2 ) n —C(O)NR a R a , C(O)O-alkyl, C(O)O-carbocycle, C(O)O-heterocycle, SO 2 alkyl, SO 2 carbocycle, SO 2 heterocycle, SO 2 NR a R a , —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle, wherein said alkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 9 , at each occurrence, is independently selected from halogen, OH, NO 2 , CHF 2 , CF 3 , C 1-4 alkyl, C 1-4 alkoxy, CH 2 OH, CO 2 H, CO 2 (C 1-4 alkyl), CONH 2 , —(CH 2 ) n NR a R a , —(CH 2 ) n CONR a R a , —O(CH 2 ) n heterocycle, —O(CH 2 ) (2-4) NR a R a , —(CR 10 R 10 ) n -4-10 membered heterocycle, wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R b ;
n, at each occurrence, is independently selected from 0, 1, 2, 3, and 4; and
p, at each occurrence, is independently selected from 0, 1, and 2.
6. The compound of claim 1 , wherein:
L is —NR 6 —;
R 1 is heteroaryl substituted with 1-4 R 7 ;
R 7 , at each occurrence, is independently selected from H, halogen, C 1-4 alkyl, C 1-4 alkoxy, CN, OH, —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle, wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R 9 .
7. The compound of claim 6 , wherein:
L is —NR 6 —; and
R 1 is selected from
8. The compound of claim 1 , having Formula (IV):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof, wherein:
R 1 is selected from NR 5 R 5 , C 3-10 carbocycle, and 5- to 10-membered heterocycle, wherein said carbocycle and heterocycle are substituted with 1-4 R 7 ;
R 5 , at each occurrence, is independently selected from H, C 1-4 alkyl, —(CR 6 R 6 ) n —C 3-10 carbocycle, and —(CR 6 R 6 ) n -4-10 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, carbocycle, and heterocycle are substituted with 1-4 R 7 ;
alternatively, R 5 and R 5 are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle substituted with 1-4 R 7 ;
R 6 , at each occurrence, is independently selected from H and C 1-4 alkyl;
R 7 , at each occurrence, is independently selected from H, ═O, NO 2 , halogen, C 1-4 alkyl, C 1-4 alkoxy, CN, OH, CF 3 , —(CH 2 ) n —CO 2 H, —(CH 2 ) n —CO 2 (C 1-4 alkyl), —(CH 2 ) n —NR 8 R 8 , —NHCO(C 1-4 alkyl), —NHCOCF 3 , —NHCO 2 (C 1-4 alkyl), —NHCO 2 (CH 2 ) 2 O(C 1-4 alkyl), —NHCO 2 (CH 2 ) 3 O(C 1-4 alkyl), —NHCO 2 (CH 2 ) 2 OH, —NHCO 2 (CH 2 ) 2 NH 2 , —NHCO 2 (CH 2 ) 2 N(C 1-4 alkyl) 2 , —NHCO 2 CH 2 CO 2 H, —CH 2 NHCO 2 (C 1-4 alkyl), —NHC(O)NR 8 R 8 , —NHSO 2 (C 1-4 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1-4 alkyl), —SO 2 N(C 1-4 alkyl) 2 , —SO 2 NH(CH 2 ) 2 OH, —SO 2 NH(CH 2 ) 2 O(C 1-4 alkyl), —(CH 2 ) n —CONR 8 R 8 , —O(CH 2 ) n -carbocycle, —O(CH 2 ) n -heterocycle, —NHCO-carbocycle, —NHCO-heterocycle, —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 8 , at each occurrence, is independently selected from H, C 1-4 alkyl, C 2-4 alkenyl, C(O)C 1-4 alkyl, C(O)carbocycle, C(O)heterocycle, —(CH 2 ) n —C(O)NR a R a , C(O)O-alkyl, C(O)O-carbocycle, C(O)O-heterocycle, SO 2 alkyl, SO 2 carbocycle, SO 2 heterocycle, SO 2 NR a R a , —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle, wherein said alkyl, alkenyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 9 , at each occurrence, is independently selected from halogen, OH, NO 2 , CHF 2 , CF 3 , C 1-4 alkyl, C 1-4 alkoxy, CH 2 OH, CO 2 H, CO 2 (C 1-4 alkyl), CONH 2 , —(CH 2 ) n NR a R a , —(CH 2 ) n CONR a R a , —O(CH 2 ) n heterocycle, —O(CH 2 ) (2-4) NR a R a , —(CR 10 R 10 ) n -4-10 membered heterocycle, wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R b ;
n, at each occurrence, is independently selected from 0, 1, 2, 3, and 4;
p, at each occurrence, is independently selected from 0, 1, and 2.
9. The compound of claim 8 , wherein:
R 1 is selected from
R 7 , at each occurrence, is independently selected from H, ═O, NO 2 , halogen, C 1-4 alkyl, C 1-4 alkoxy, CN, OH, CF 3 , —(CH 2 ) n —CO 2 H, —(CH 2 ) n —CO 2 (C 1-4 alkyl), —(CH 2 ) n —NR 8 R 8 , —NHCO(C 1-4 alkyl), —NHCOCF 3 , —NHCO 2 (C 1-4 alkyl), —NHCO 2 (CH 2 ) 2 O(C 1-4 alkyl), —NHCO 2 (CH 2 ) 3 O(C 1-4 alkyl), —NHCO 2 (CH 2 ) 2 OH, —NHCO 2 (CH 2 ) 2 NH 2 , —NHCO 2 (CH 2 ) 2 N(C 1-4 alkyl) 2 , —NHCO 2 CH 2 CO 2 H, —CH 2 NHCO 2 (C 1-4 alkyl), —NHC(O)NR 8 R 8 , —NHSO 2 (C 1-4 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1-4 alkyl), —SO 2 N(C 1-4 alkyl) 2 , —SO 2 NH(CH 2 ) 2 OH, —SO 2 NH(CH 2 ) 2 O(C 1-4 alkyl), —(CH 2 ) n —CONR 8 R 8 , —O(CH 2 ) n -carbocycle, —O(CH 2 ) n -heterocycle, —NHCO-carbocycle, —NHCO-heterocycle, —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 8 , at each occurrence, is independently selected from H, C 1-4 alkyl, C(O)C 1-4 alkyl, C(O)carbocycle, C(O)heterocycle, —(CH 2 ) n —C(O)NR a R a , C(O)O-alkyl, C(O)O-carbocycle, C(O)O-heterocycle, SO 2 alkyl, SO 2 carbocycle, SO 2 heterocycle, SO 2 NR a R a , —(CH 2 ) n -carbocycle, and —(CH 2 ) n -heterocycle, wherein said alkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
alternatively, R 8 and R 8 are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle substituted with 0-4 R 9 ; and
R 9 , at each occurrence, is independently selected from halogen, OH, NO 2 , CHF 2 , CF 3 , C 1-4 alkyl, C 1-4 alkoxy, CH 2 OH, CO 2 H, CO 2 (C 1-4 alkyl), CONH 2 , —(CH 2 ) n NR a R a , —(CH 2 ) n CONR a R a , —O(CH 2 ) n heterocycle, —O(CH 2 ) (2-4) NR a R a , —(CR 10 R 10 ) n -4-10 membered heterocycle, wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R b ;
R a , at each occurrence, is independently selected from H, C 1-4 alkyl, —(CH 2 ) n OH, CO(C 1-4 alkyl), COCF 3 , CO 2 (C 1-4 alkyl), —CONH 2 , —CONH—C 1-4 alkylene-CO 2 (C 1-4 alkyl), C 1-4 alkylene-CO 2 (C 1-4 alkyl), R c , CO 2 R c , and CONHR c ; alternatively, R a and R a are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle, wherein said alkyl, alkylene, and heterocycle are substituted with 0-4 R b ;
R b , at each occurrence, is independently selected from ═O, halogen, C 1-4 alkyl, C 1-4 alkoxy, OCF 3 , NH 2 , NO 2 , N(C 1-4 alkyl) 2 , CO(C 1-4 alkyl), CO(C 1-4 haloalkyl), CO 2 (C 1-4 alkyl), CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , —CONH—C 1-4 alkylene-O(C 1-4 alkyl), —CONH—C 1-4 alkylene-N(C 1-4 alkyl) 2 , —CONH—C 1-4 alkylene-N(C 1-4 alkyl) 2 , —C 1-4 alkylene-O—P(O)(OH) 2 , —NHCO 2 (C 1-4 alkyl), —R c , COR c , CO 2 R c , and CONHR c ;
R c , at each occurrence, is independently selected from —(CH 2 ) n —C 3-6 cycloalkyl, —(CH 2 ) n -phenyl, and —(CH 2 ) n -5- to 6-membered heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4 alkyl), O, and S(O) p ; wherein each ring moiety is substituted with 0-2 R d ; and
R d , at each occurrence, is independently selected from ═O, halogen, —OH, C 1-4 alkyl, NH 2 , NH(C 1-4 alkyl), N(C 1-4 alkyl) 2 , C 1-4 alkoxy, and —NHCO(C 1-4 alkyl), and heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4 alkyl), O, and S(O) p .
10. The compound of claim 8 , wherein:
R 1 is NR 5 R 5 ;
R 5 and R 5 are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle substituted with 1-4 R 7 ;
R 7 , at each occurrence, is independently selected from H, ═O, halogen, C 1-4 alkyl, C 1-4 alkoxy, CN, OH, CF 3 , —(CH 2 ) n —CO 2 H, —(CH 2 ) n —CO 2 (C 1-4 alkyl), —(CH 2 ) n —NR 8 R 8 , —NHCO(C 1-4 alkyl), —NHCOCF 3 , —NHCO 2 (C 1-4 alkyl), —NHC(O)NH 2 , —NHC(O)NH(C 1-4 alkyl), —NHC(O)N(C 1-4 alkyl) 2 , —NHSO 2 (C 1-4 alkyl), —SO 2 NH 2 , —SO 2 NH(C 1-4 alkyl), —SO 2 N(C 1-4 alkyl) 2 , —SO 2 NH(CH 2 ) 2 OH, —SO 2 NH(CH 2 ) 2 O(C 1-4 alkyl), —CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , —CH 2 CONH 2 , —(CH 2 ) n -carbocycle, —O(CH 2 ) n -carbocycle, —O(CH 2 ) n -heterocycle, and —(CH 2 ) n -heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ;
R 8 , at each occurrence, is independently selected from H, C 1-4 alkyl, C(O)C 1-4 alkyl, C(O)carbocycle, C(O)heterocycle, —(CH 2 ) n —C(O)NR a R a , C(O)O-alkyl, C(O)O-carbocycle, C(O)O-heterocycle, SO 2 alkyl, SO 2 carbocycle, SO 2 heterocycle, SO 2 NR a R a , —(CH 2 ) n -cycloalkyl, —(CH 2 ) n -phenyl, and —(CH 2 ) n -heterocycle, wherein said alkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ; and
R 9 , at each occurrence, is independently selected from halogen, OH, NO 2 , CHF 2 , CF 3 , C 1-4 alkyl, C 1-4 alkoxy, CH 2 OH, CO 2 H, CO 2 (C 1-4 alkyl), CONH 2 , —(CH 2 ) n NR a R a , —(CH 2 ) n CONR a R a , —O(CH 2 ) n heterocycle, —O(CH 2 ) (2-4) NR a R a , —(CR 10 R 10 ) n -4-10 membered heterocycle, wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R b .
11. The compound of claim 1 selected from the group consisting of:
4-(4-(2-(isoindolin-2-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (1);
4-(4-(2-(5-fluoroisoindolin-2-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (2);
4-(4-(2-(5-methoxyisoindolin-2-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (3);
4-{4-[2-oxo-2-(1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]phenyl}-1,2-dihydrophthalazin-1-one (4);
2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-N-(pyridin-3-yl)acetamide (5);
N-benzyl-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (6);
2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-N-(pyridin-4-yl)acetamide (7);
N-benzyl-N-methyl-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (8);
N-(1H-1,3-benzodiazol-2-yl)-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (9);
N-(1,3-benzoxazol-2-yl)-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (10);
4-{4-[2-oxo-2-(4-phenylpiperidin-1-yl)ethyl]phenyl}-1,2-dihydrophthalazin-1-one (11);
4-{4-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (12);
4-(4-{2-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]-2-oxoethyl}phenyl)-1,2-dihydrophthalazin-1-one (13);
N-(cyclopropylmethyl)-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (14);
4-(4-{2-oxo-2-[4-(pyrimidin-2-yl)piperazin-1-yl]ethyl}phenyl)-1,2-dihydrophthalazin-1-one (15);
4-(4-{2-[4-(4-methoxyphenyl)piperazin-1-yl]-2-oxoethyl}phenyl)-1,2-dihydrophthalazin-1-one (16);
4-{4-[2-(4-benzylpiperidin-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (17);
2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-N-[(1S,2R)-2-phenylcyclopropyl]acetamide (18);
N-cyclobutyl-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (19);
2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-N-phenylacetamide (20);
N-(1,3-benzothiazol-6-yl)-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (21);
N-methyl-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-N-phenylacetamide (22);
4-{4-[2-(2,3-dihydro-1H-indol-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (23);
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (24);
4-[4-(2-{5-[(4-methylpiperazin-1-yl)methyl]-2,3-dihydro-1H-isoindol-2-yl}-2-oxoethyl)phenyl]-1,2-dihydrophthalazin-1-one (25);
N-(3-methyl-1,2-oxazol-5-yl)-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (26);
N-(5-methyl-1,2-oxazol-3-yl)-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (27);
2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-N-(1,3-thiazol-2-yl)acetamide (28);
2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-N-(1,3,4-thiadiazol-2-yl)acetamide (29);
N-(6-chloropyridazin-3-yl)-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (30);
N-(5-methyl-1,3,4-thiadiazol-2-yl)-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (31);
4-{4-[2-(5-methyl-2,3-dihydro-1H-indol-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (32);
4-{4-[2-(6-ethoxy-2,3-dihydro-1H-indol-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (33);
4-{4-[2-oxo-2-(1,2,3,4-tetrahydroquinolin-1-yl)ethyl]phenyl}-1,2-dihydrophthalazin-1-one (34);
4-(4-{2-oxo-2-[6-(trifluoromethyl)-2,3-dihydro-1H-indol-1-yl]ethyl}phenyl)-1,2-dihydrophthalazin-1-one (35);
2-(2-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-1-(isoindolin-2-yl)ethanone (36);
4-(2-fluoro-4-(2-(isoindolin-2-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (37);
4-{4-[2-(3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (39);
4-{4-[2-(2-methyl-2,3-dihydro-1H-indol-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (40);
4-{4-[2-(6-methoxy-2,3-dihydro-1H-indol-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (41);
4-(4-(1-(indolin-1-yl)-1-oxopropan-2-yl)phenyl)phthalazin-1(2H)-one (42);
4-(4-(1-(isoindolin-2-yl)-1-oxopropan-2-yl)phenyl)phthalazin-1(2H)-one (43);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-2,3-dihydro-1H-indene-2-carboxamide (44);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-2-(pyridin-4-yl)thiazole-4-carboxamide (45);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2-phenyl-1,3-thiazole-4-carboxamide (46);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-(pyridin-4-yl)-1,3-thiazole-2-carboxamide (47);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2-[4-(trifluoromethyl)phenyl]-1,3-thiazole-4-carboxamide (48);
2-(3,5-difluorophenyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-thiazole-4-carboxamide (49);
4-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-thiazole-2-carboxamide (50);
5-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-4H,5H,6H, 7H-[1,3]thiazolo[5,4-c]pyridine-2-carboxamide (51);
1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-imidazole-2-carboxamide (52);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-4,5,6,7-tetrahydro-1,3-benzothiazole-2-carboxamide (53);
1-(4-nitrophenyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]piperidine-4-carboxamide (54); 1-acetyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]piperidine-4-carboxamide (55);
1-benzyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]piperidine-4-carboxamide (56);
1-(2-methoxyethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrrolidine-3-carboxamide (57);
4-(dimethylamino)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]benzamide (58);
1-benzyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrrolidine-3-carboxamide (59); N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-4-(pyrrolidin-1-yl)benzamide (60);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-4-(piperidin-1-yl)benzamide (61);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-3-(pyrrolidin-1-yl)benzamide (62);
4-(morpholin-4-yl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]benzamide (63);
4-(4-methylpiperazin-1-yl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]benzamide (64);
4-(1H-imidazol-1-yl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]benzamide (65);
3-(dimethylamino)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]benzamide (66);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]benzamide (67);
4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl isoindoline-2-carboxylate (68);
4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl3-phenylpyrrolidine-1-carboxylate (69);
4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl5-methoxyisoindoline-2-carboxylate (70);
4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl5-fluoroisoindoline-2-carboxylate (71);
4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl5-((4-methylpiperazin-1-yl)methyl)isoindoline-2-carboxylate, (72);
4-(4-((5-phenyloxazol-2-yl)amino)phenyl)phthalazin-1(2H)-one (73);
4-(4-((4-phenylthiazol-2-yl)amino)phenyl)phthalazin-1(2H)-one (74);
4-(4-(benzo[d]oxazol-2-ylamino)phenyl)phthalazin-1(2H)-one (75);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)indoline-1-carboxamide (76);
4-{4-[(quinazolin-2-yl)amino]phenyl}-1,2-dihydrophthalazin-1-one (78);
4-(4-(quinazolin-2-ylamino)phenyl)phthalazin-1(2H)-one (79);
(R)-N-(2,3-dihydro-1H-inden-1-yl)-2-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)acetamide (81);
(S)-N-(2,3-dihydro-1H-inden-1-yl)-2-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)acetamide (82);
4-(4-(2-(6-(benzyloxy)indolin-1-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (83);
4-(4-(benzo[d]thiazol-2-ylamino)phenyl)phthalazin-1(2H)-one (84);
4-(4-(phthalazin-1-ylamino)phenyl)phthalazin-1(2H)-one (85);
4-{4-[(5-methyl-1,3-benzoxazol-2-yl)amino]phenyl}-1,2-dihydrophthalazin-1-one (86);
4-(4-((5-phenyl-1,3,4-thiadiazol-2-yl)amino)phenyl)phthalazin-1(2H)-one (87);
4-(4-((5-phenylthiazol-2-yl)amino)phenyl)phthalazin-1(2H)-one (88);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyridine-2-carboxamide (89);
1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (90);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2,3-dihydro-1H-indene-1-carboxamide (91);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-4-(1H-1,2,4-triazol-1-yl)benzamide (92);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2,1-benzoxazole-3-carboxamide (93);
6-(dimethylamino)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (94);
2-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyridine-3-carboxamide (95);
5-chloro-1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (96);
5,5-dimethyl-4-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-indole-3-carboxamide (97);
1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (98);
1-benzyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (99);
5-ethoxy-2-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-benzofuran-3-carboxamide (100);
5-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (101);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidine-2-carboxamide (102);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (103);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyridine-3-carboxamide (104);
5-(benzyloxy)-2-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-benzofuran-3-carboxamide (105);
5-hydroxy-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2,3-dihydro-1-benzofuran-2-carboxamide (106);
1-ethyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (107);
4-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-(propan-2-yl)-3H,4H-pyrrolo[2,1-f][1,2,4]triazine-6-carboxamide (108);
4-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-indazole-3-carboxamide (109);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazolo[3,4-b]pyridine-3-carboxamide (110);
6-methyl-4-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-4H,5H,6H,7H-furo[2,3-c]pyridine-3-carboxamide (111);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-[1,2,4]triazolo[1,5-a]pyrimidine-2-carboxamide (112);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide (113);
5-chloro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (114);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-benzothiazole-2-carboxamide (115);
2-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-4,5,6,7-tetrahydro-2H-indazole-3-carboxamide (116);
4-methoxy-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-3-carboxamide (117);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,2-benzoxazole-3-carboxamide (118);
5-chloro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrrolo[2,3-b]pyridine-2-carboxamide (119);
5-fluoro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrrolo[2,3-b]pyridine-3-carboxamide (120);
6-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyrazine-2-carboxamide (121);
1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-3-carboxamide (122);
5-methoxy-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (123);
8-chloro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyrazine-2-carboxamide (124);
5-methoxy-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (125);
7-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyridine-2-carboxamide (126);
6-methoxy-1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (127);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-6-(propan-2-yloxy)-1H-indole-2-carboxamide (128);
7-methoxy-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (129);
5-ethoxy-1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (130);
2-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2H-indazole-3-carboxamide (131);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(propan-2-yl)-1H-indazole-3-carboxamide (132);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyrazine-2-carboxamide (133);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5H,6H,7H,8H-imidazo[1,2-a]pyridine-2-carboxamide (134);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrrolo[2,3-b]pyridine-3-carboxamide (135);
1-benzyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (136);
1-(2-hydroxy-2-methylpropyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (137);
1-(2-hydroxy-2-methylpropyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-3-carboxamide (138);
2,7-dimethyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyridine-3-carboxamide (139);
2-ethyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyrimidine-3-carboxamide (140);
6-methoxy-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (141);
1-[2-(dimethylamino)ethyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (142);
2-(oxetan-3-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2H-indazole-3-carboxamide (143);
1-(oxetan-3-ylmethyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (144);
1-[(3-methyloxetan-3-yl)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (145);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(oxolan-3-ylmethyl)-1H-indazole-3-carboxamide (146);
1-[3-(benzyloxy)-2-hydroxypropyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (147);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(oxolan-2-ylmethyl)-1H-indazole-3-carboxamide (148);
1-(2,3-dihydroxypropyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (149);
1-(oxan-4-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (150);
1-(2-methoxyethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (151);
1-(oxetan-2-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (152);
1-(2-hydroxypropyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (153);
1-[2-(2-methoxyethoxy)ethyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (154);
1-(2-hydroxyethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (155);
1-[2-(oxan-4-yl)ethyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (156);
1-[2-(benzyloxy)ethyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (157);
6-fluoro-1-(2-hydroxy-2-methylpropyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (158);
6-fluoro-1-(oxetan-3-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (159);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(pyridin-2-ylmethyl)-1H-indazole-3-carboxamide (160);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(pyridin-3-ylmethyl)-1H-indazole-3-carboxamide (161);
1-[3-(benzyloxy)propyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (162);
1-(3-methoxypropyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (163);
1-(3-hydroxypropyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (164);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(pyridin-4-ylmethyl)-1H-indazole-3-carboxamide (165);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrrolo[3,2-c]pyridine-3-carboxamide (166);
5-fluoro-1-(2-hydroxy-2-methylpropyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (167);
1-(oxan-2-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (168);
1-(2-hydroxy-2-methylpropyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrrolo[2,3-b]pyridine-3-carboxamide (169);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-[3-ylmethyl]-1H-indazole-3-carboxamide (170);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-[oxolan-3-ylmethyl]-1H-indazole-3-carboxamide (171);
6-(2-hydroxy-2-methylpropoxy)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (172);
5-fluoro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(oxolan-3-ylmethyl)-1H-indazole-3-carboxamide (173);
6-fluoro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(oxolan-3-ylmethyl)-1H-indazole-3-carboxamide (174);
6-(2-methoxyethoxy)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (175);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-6-[2-(pyrrolidin-1-yl)ethoxy]pyrazolo[1,5-a]pyridine-3-carboxamide (176);
6-[2-(dimethylamino)ethoxy]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (177);
5-fluoro-1-(2-methylprop-1-en-1-yl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (178);
6-fluoro-1-(2-methylprop-1-en-1-yl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (179);
6-fluoro-5-methoxy-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-benzofuran-2-carboxamide (180);
5-(2-hydroxy-2-methylpropoxy)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (181);
5-methoxy-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (182);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-[2-(pyrrolidin-1-yl)ethoxy]pyrazolo[1,5-a]pyridine-3-carboxamide (183);
5-(2-methoxyethoxy)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (184);
5-(2-hydroxypropoxy)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (185);
5-(2-hydroxyethoxy)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (186);
5-[2-(morpholin-4-yl)ethoxy]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (187);
6-[2-(morpholin-4-yl)ethoxy]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (188);
5-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-1H-pyrazole-4-carboxamide (189);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-5-(trifluoromethyl)-1H-pyrazole-4-carboxamide (190);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-1H-pyrazole-4-carboxamide (191);
1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-phenyl-1H-pyrazole-4-carboxamide (192);
3-(3-chloro-2-fluorophenyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-4,5-dihydro-1,2-oxazole-5-carboxamide (193);
5-(2-hydroxy-3-methoxypropoxy)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (194);
1-(3-methylphenyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-imidazole-4-carboxamide (195);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-3-phenyl-4,5-dihydro-1,2-oxazole-5-carboxamide (196);
1-(2-methoxyphenyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-4-carboxamide (197);
1-(3-chlorophenyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-4-carboxamide (198);
5-chloro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-1H-pyrazole-4-carboxamide (199);
1-benzyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-4-carboxamide (200);
5-(adamantan-1-yl)-1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-3-carboxamide (201);
1-(3-chloro-2-fluorophenyl)-5-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-4-carboxamide (202);
1-(3-methoxyphenyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-4-carboxamide (203);
1-ethyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-3-carboxamide (204);
1,5-dimethyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-3-carboxamide (205);
5-tert-butyl-1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-3-carboxamide (206);
1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-phenyl-1H-pyrazole-3-carboxamide (207);
1-benzyl-5-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-3-carboxamide (208);
1-(3-methylphenyl)-2-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrrolidine-3-carboxamide (209);
1-(4-methylphenyl)-5-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrrolidine-3-carboxamide (210);
1-(3-chloro-2-fluorophenyl)-5-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrrolidine-3-carboxamide (211);
1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-4-carboxamide (212);
5-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-1H-pyrazole-3-carboxamide (213);
5-methyl-1-(2-methylphenyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-4-carboxamide (214);
2-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenylpyrrolidine-3-carboxamide (215);
1-(2-methoxyphenyl)-2-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrrolidine-3-carboxamide (216);
5-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenylpyrrolidine-3-carboxamide (217);
5-oxo-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(propan-2-yl)pyrrolidine-3-carboxamide (218);
3,5-dimethyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-1H-pyrazole-4-carboxamide (219);
1-(2-chlorophenyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-4-carboxamide (220);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-5-(propan-2-yl)-1H-1,2,3-triazole-4-carboxamide (221);
1-(2-fluorophenyl)-5-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-1,2,3-triazole-4-carboxamide (222);
5-[4-(2-hydroxypropan-2-yl)phenyl]-3-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,2-oxazole-4-carboxamide (223);
5-[4-(hydroxymethyl)phenyl]-3-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,2-oxazole-4-carboxamide (224);
1-(3-chlorophenyl)-5-ethyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-1,2,3-triazole-4-carboxamide (225);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-1H-pyrazole-3-carboxamide (226);
1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-3-carboxamide (227);
3-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-1H-pyrazole-4-carboxamide (228);
1-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-propyl-1H-pyrazole-3-carboxamide (229);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2-phenyl-1H-imidazole-4-carboxamide (230);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-5-propyl-1H-1,2,3-triazole-4-carboxamide (231);
5-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-[3-(trifluoromethyl)phenyl]-1H-1,2,3-triazole-4-carboxamide (232);
1-ethyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-imidazole-5-carboxamide (233);
N-(1-tert-butyl-3-{[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]carbamoyl}-1H-pyrazol-4-yl)pyridine-4-carboxamide (234);
1-tert-butyl-5-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrazole-3-carboxamide (235);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-phenyl-1H-pyrazole-5-carboxamide (236);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-(pyridin-2-yl)-1H-1,2,4-triazole-3-carboxamide (237);
2-(2,3-dichlorophenyl)-5-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2H-1,2,3-triazole-4-carboxamide (238);
1-(2-cyano-5-methoxyphenyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-1,2,4-triazole-3-carboxamide (239);
N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(pyridin-2-yl)-1H-1,2,4-triazole-3-carboxamide (240);
4-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2-(1,2,3,4-tetrahydroquinolin-1-yl)-1,3-thiazole-5-carboxamide (241);
2-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-imidazole-4-carboxamide (242);
4-methyl-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2-(phenylamino)-1,3-thiazole-5-carboxamide (243);
4-(4-(2-(5-methoxy-7-methylindolin-1-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (252);
4-(4-(2-(7-bromo-5-(trifluoromethoxy)indolin-1-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (253);
4-(4-(2-(6-isopropoxyindolin-1-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (258);
4-(4-(2-(indolin-1-yl)-2-oxoethyl)-2-methylphenyl)phthalazin-1(2H)-one (259);
4-(4-(2-(isoindolin-2-yl)-2-oxoethyl)-2-methylphenyl)phthalazin-1(2H)-one (260);
4-(2-fluoro-4-(2-(indolin-1-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (261);
4-(4-(2-(6-(2-hydroxy-2-methylpropoxy)indolin-1-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (265);
4-(4-{2-oxo-2-[6-(pyridin-3-ylmethoxy)-2,3-dihydro-1H-indol-1-yl]ethyl}phenyl)-1,2-dihydrophthalazin-1-one (270);
4-(4-{2-oxo-2-[6-(pyridin-2-ylmethoxy)-2,3-dihydro-1H-indol-1-yl]ethyl}phenyl)-1,2-dihydrophthalazin-1-one (271);
4-(4-{2-oxo-2-[6-(pyridin-4-ylmethoxy)-2,3-dihydro-1H-indol-1-yl]ethyl}phenyl)-1,2-dihydrophthalazin-1-one (272);
4-(4-{2-oxo-2-[5-(propan-2-yloxy)-2,3-dihydro-1H-indol-1-yl]ethyl}phenyl)-1,2-dihydrophthalazin-1-one (273);
4-[4-(2-oxo-2-{6-[(3R)-oxolan-3-yloxy]-2,3-dihydro-1H-indol-1-yl}ethyl)phenyl]-1,2-dihydrophthalazin-1-one (274);
4-[4-(2-oxo-2-{6-[(3S)-oxolan-3-yloxy]-2,3-dihydro-1H-indol-1-yl}ethyl)phenyl]-1,2-dihydrophthalazin-1-one (275);
2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-N-(4,5,6,7-tetrahydro-1,2-benzoxazol-3-yl)acetamide (276);
4-{4-[2-(6-{[(3R)-1-methylpyrrolidin-3-yl]oxy }-2,3-dihydro-1H-indol-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (277);
N-(5-tert-butyl-1,2-oxazol-3-yl)-2[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (278);
4-[4-(2-{6-[2-(dimethylamino)ethoxy]-2,3-dihydro-1H-indol-1-yl}-2-oxoethyl)phenyl]-1,2-dihydrophthalazin-1-one (279);
N-(dimethyl-1,2-oxazol-3-yl)-2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetamide (280);
4-{4[2(6-{[(3S)-1-methylpyrrolidin-3-yl]oxy }-2,3-dihydro-1H-indol-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (281);
4-[4-(2-{6-[(1-methylpiperidin-4-yl)oxy]-2,3-dihydro-1H-indol-1-yl}-2-oxoethyl)phenyl]-1,2-dihydrophthalazin-1-one (282);
methyl 2-[(1-{2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetyl}-2,3-dihydro-1H-indol-6-yl)oxy]acetate (283);
4-(4-{2-[6-(oxetan-3-ylmethoxy)-2,3-dihydro-1H-indol-1-yl]-2-oxoethyl}phenyl)-1,2-dihydrophthalazin-1-one (284);
4-{4-[2-(6-nitro-2,3-dihydro-1H-indol-1-yl)-2-oxoethyl]phenyl}-1,2-dihydrophthalazin-1-one (285);
4-[4-(2-oxo-2-{6-[2-(pyrrolidin-1-yl)ethoxy]-2,3-dihydro-1H-indol-1-yl}ethyl)phenyl]-1,2-dihydrophthalazin-1-one (286);
2-((1-(2-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)acetyl)indolin-6-yl)oxy)acetic acid (290);
N,N-dimethyl-1-{2-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]acetyl}-2,3-dihydro-1H-indole-6-carboxamide (291);
4-(4-{2-[6-(4-methylpiperazine-1-carbonyl)-2,3-dihydro-1H-indo1-1-yl]-2-oxoethyl}phenyl)-1,2-dihydrophthalazin-1-one (292);
4-(4-{2-[6-(morpholine-4-carbonyl)-2,3-dihydro-1H-indol-1-yl]-2-oxoethyl}phenyl)-1,2-dihydrophthalazin-1-one (293);
4-(4-{2-[5-(4-hydroxypiperidine-1-carbonyl)-2,3-dihydro-1H-indol-1-yl]-2-oxoethyl}phenyl)-1,2-dihydrophthalazin-1-one (294);
4-(4-{2-[6-(4-hydroxypiperidine-1-carbonyl)-2,3-dihydro-1H-indol-1-yl]-2-oxoethyl}phenyl)-1,2-dihydrophthalazin-1-one (295);
4-(4-{2-[5-(morpholine-4-carbonyl)-2,3-dihydro-1H-indol-1-yl]-2-oxoethyl}phenyl)-1,2-dihydrophthalazin-1-one (296);
4-(4-(2-(6-(2-morpholino-2-oxoethoxy)indolin-1-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (297);
2-((1-(2-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)acetyl)indolin-6-yl)oxy)acetamide (298);
4-(4-(2-(6-(2-(4-methylpiperazin-1-yl)-2-oxoethoxy)indolin-1-yl)-2-oxoethyl)phenyl)phthalazin-1(2H)-one (299);
4-(dimethylamino)-N-(1-(2-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)acetyl)indolin-6-yl)benzamide (300);
1-(2-hydroxy-2-methylpropyl)-N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (301);
1-(2-hydroxy-2-methylpropyl)-N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-3-carboxamide (302);
1-[2-(dimethylamino)ethyl]-N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (303);
2-[2-(dimethylamino)ethyl]-N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2H-indazole-3-carboxamide (304);
N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2-(oxetan-3-ylmethyl)-2H-indazole-3-carboxamide (305);
N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-2,1-benzoxazole-3-carboxamide (306);
benzyl4-[(3-{[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]carbamoyl}-1H-indazol-1-yl)methyl]piperidine-1-carboxylate (307);
5-fluoro-N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-pyrrolo[2,3-b]pyridine-3-carboxamide (308);
7-methoxy-N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indole-2-carboxamide (309);
N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]pyrazolo[1,5-a]pyridine-3-carboxamide (310);
2-methyl-N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyridine-3-carboxamide (311);
N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyridine-3-carboxamide (312);
N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(oxan-4-ylmethyl)-1H-indazole-3-carboxamide (313);
N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1[(3-methyloxetan-3-yl)methyl]-1H-indazole-3-carboxamide (314);
N-[3-chloro-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(2-hydroxy-2-methylpropyl)-1H-indazole-3-carboxamide (315);
tert-butyl3-[(3-{[3-chloro-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]carbamoyl}-1H-indazol-1-yl)methyl]azetidine-1-carboxylate (316);
N-[3-chloro-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]imidazo[1,2-a]pyridine-3-carboxamide (317);
N-[3-chloro-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(oxan-4-ylmethyl)-1H-indazole-3-carboxamide (318);
N-[3-chloro-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-(oxolan-3-ylmethyl)-1H-indazole-3-carboxamide (319);
N-[3-chloro-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1-[(3-methyloxetan-3-yl)methyl]-1H-indazole-3-carboxamide (320);
1-((1-(4-hydroxybutyl)piperidin-4-yl)methyl)-N-(3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (321);
1-((1-(4-hydroxybutyl)piperidin-4-yl)methyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (322);
N-(3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)indoline-1-carboxamide (324);
N-[3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-6-[2-(pyrrolidin-1-yl)ethoxy]pyrazolo[1,5-a]pyridine-3-carboxamide (325);
1-(azetidin-3-ylmethyl)-N-(3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (326);
1-(azetidin-3-ylmethyl)-N-[3-chloro-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1H-indazole-3-carboxamide (327);
2-(3-{[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]carbamoyl}-1H-indazol-1-yl)acetic acid (328);
1-((1-acetylazetidin-3-yl)methyl)-N-(3-chloro-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (329);
N-(3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-((1-methylazetidin-3-yl)methyl)-1H-indazole-3-carboxamide (330);
3-(3-((4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)carbamoyl)-1H-indazol-1-yl)propanoic acid (331);
methyl 3-(3-((4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)carbamoyl)-1H-indazol-1-yl)propanoate (332);
1-(3-hydroxy-3-methylbutyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (333);
1-(2-((2-hydroxy-2-methylpropyl)amino)-2-oxoethyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (334);
1-(2-(((1-hydroxycyclobutyl)methyl)amino)-2-oxoethyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (335);
1-(3-((2-hydroxy-2-methylpropyl)amino)-3-oxopropyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (336);
1-(3-morpholino-3-oxopropyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (337);
1-(azetidin-3-ylmethyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (338);
1-((1-acetylazetidin-3-yl)methyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (339);
1-((1-methylazetidin-3-yl)methyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (340);
methyl 3-((3-((4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)carbamoyl)-1H-indazol-1-yl)methyl)azetidine-1-carboxylate (341);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(piperidin-4-ylmethyl)-1H-indazole-3-carboxamide (342);
1-((1-acetylpiperidin-4-yl)methyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (343);
methyl 4-((3-((4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)carbamoyl)-1H-indazol-1-yl)methyl)piperidine-1-carboxylate (344);
1-(2-hydroxy-2-methylpropyl)-N-(3-methoxy-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (345);
N-(3-ethoxy-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(2-hydroxy-2-methylpropyl)-1H-indazole-3-carboxamide (346);
N-(3-ethoxy-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-((tetrahydrofuran-3-yl)methyl)-1H-indazole-3-carboxamide (347);
N-(3-methoxy-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-((tetrahydrofuran-3-yl)methyl)-1H-indazole-3-carboxamide (348);
propan-2-yl4-[(3-{[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]carbamoyl}-1H-indazol-1-yl)methyl]piperidine-1-carboxylate (349);
2-fluoroethyl4-[(3-{[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]carbamoyl}-1H-indazol-1-yl)methyl]piperidine-1-carboxylate (350);
2,2,2-trifluoroethyl 4-[(3-{[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]carbamoyl}-1H-indazol-1-yl)methyl]piperidine-1-carboxylate (351);
N-(2-methoxy-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-((tetrahydrofuran-3-yl)methyl)-1H-indazole-3-carboxamide (352);
1-(2-hydroxy-2-methylpropyl)-N-(2-hydroxy-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (353);
N-(2-hydroxy-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-((tetrahydrofuran-3-yl)methyl)-1H-indazole-3-carboxamide (354);
N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-((tetrahydrofuran-3-yl)methyl)-1H-indazole-3-carboxamide (355);
1-((1-methylpiperidin-4-yl)methyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (356);
1-(2-hydroxy-2-methylpropyl)-N-(2-methoxy-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (357);
N-(2-fluoro-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(2-hydroxy-2-methylpropyl)-1H-indazole-3-carboxamide (358);
1-(2-hydroxyethyl)-N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (359);
1-(2-hydroxy-2-methylpropyl)-N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxami de (360);
N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(2-(tetrahydro-2H-pyran-4-yl)ethyl)-1H-indazole-3-carboxamide (361);
N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)pyrazolo[1,5-a]pyridine-3-carboxamide (362);
N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-methyl-1H-indazole-3-carboxamide (363);
N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-isopropyl-1H-indazole-3-carboxamide (364);
N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)imidazo[1,2-a]pyridine-3-carboxamide (365);
5-fluoro-N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-((tetrahydrofuran-3-yl)methyl)-1H-indazole-3-carboxamide (366);
N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-((tetrahydrofuran-2-yl)methyl)-1H-indazole-3-carboxamide (367);
6-fluoro-N-(3-(hydroxymethyl)-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-((tetrahydrofuran-3-yl)methyl)-1H-indazole-3-carboxamide (368);
1-(2-hydroxy-2-methylpropyl)-N-(4-(6-methoxy-4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-indazole-3-carboxamide (369);
N-(4-(6-methoxy-4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)imidazo[1,2-a]pyridine-2-carboxamide (370);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)spiro[indoline-3,4′-piperidine]-1-carboxamide (371);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(piperidin-4-yl)-1H-1,2,3-triazole-4-carboxamide (372);
1-cyclohexyl-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (373);
1-cyclopentyl-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (374);
1-(cyclopropylmethyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (375);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazole-4-carboxamide (376);
1-(2-hydroxy-2-methylpropyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (377);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(3,3,3-trifluoro-2-hydroxypropyl)-1H-pyrazole-4-carboxamide (378);
1-(2-hydroxy-3-methoxypropyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (379);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(3,3,3-trifluoro-2-hydroxy-2-(trifluoromethyl)propyl)-1H-pyrazole-4-carboxamide (380);
1-(tert-butyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (381);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-propyl-1H-pyrazole-4-carboxamide (382);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(2,2,3,3-tetrafluoropropyl)-1H-pyrazole-4-carboxamide (383);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxamide (384);
1-(cyclopropylmethyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (385);
1-(2,2-difluoroethyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (386);
1-(2-hydroxypropyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (387);
1-(4-chlorophenyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (388);
1-(oxetan-3-yl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (389); N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(tetrahydrofuran-3-yl)-1H-pyrazole-4-carboxamide (390);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (391);
1-(bicyclo[2.2.1]heptan-7-yl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (392);
1-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-yl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (393);
5-methyl-N-(3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-phenyl-1H-pyrazole-4-carboxamide (394);
5-(tert-butyl)-1-methyl-N-(3-methyl-4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (395);
1-(1,1-dioxidotetrahydrothiophen-3-yl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-4-carboxamide (396);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(pyrrolidin-3-yl)-1H-pyrazole-4-carboxamide (397);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(3,3,3-trifluoropropyl)-1H-pyrazole-4-carboxamide (398);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(3-(pyrrolidin-1-yl)propyl)-1H-pyrazole-4-carboxamide (399);
5-methyl-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-phenyl-1H-1,2,3-triazole-4-carboxamide (400);
1-(4-methoxyphenyl)-5-methyl-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-1,2,3-triazole-4-carboxamide (401);
1-(4-methoxyphenyl)-4-methyl-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-1,2,3-triazole-5-carboxamide (402);
5-(difluoromethoxy)-1-methyl-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (403);
1-(3-methoxyphenyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-1,2,3-triazole-4-carboxamide (404);
1-(2-methoxyphenyl)-5-methyl-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-1,2,3-triazole-4-carboxamide (405);
1-(2-methoxyphenyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-1,2,3-triazole-4-carboxamide (406);
3-cyclopropyl-1-methyl-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-5-carboxamide (407);
1-methyl-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (408);
N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazole-3-carboxamide (409);
1-(difluoromethyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (410);
1-(2,2-difluoroethyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-5-carboxamide (411); and
1-(2,2-difluoroethyl)-N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (412), or a pharmaceutically acceptable salt thereof.
12. A pharmaceutical composition comprising one or more compounds according to claim 1 and a pharmaceutically acceptable carrier or diluent.
13. A method for inhibiting Rho kinase activity, comprising (a) providing target cells and a composition comprising a compound described in claim 1 ; and (b) exposing said target cells to said composition under conditions such that said composition binds to said target cells so as to inhibit Rho kinase activity within said target cells.Cited by (0)
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