US2023109104A1PendingUtilityA1
Heterocyclic compounds and uses thereof
Est. expiryOct 9, 2037(~11.2 yrs left)· nominal 20-yr term from priority
Inventors:Sarvajit ChakravartySon Minh PhamJayakanth KankanalaAnil Kumar AgarwalBrahmam PujalaSanjeev SoniSatish K. AryaDeepak PalveAshu GuptaVarun Kumar
C07D 487/04C07D 471/04C07D 519/00A61P 35/00
63
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Claims
Abstract
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Claims
exact text as granted — not AI-modified1 - 61 . (canceled)
62 . A method of treating a cancer in an individual in need thereof comprising administering to the individual a therapeutically effective amount of a compound of Formula (I):
or a tautomer or stereoisomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein:
X 1 is N or CR;
X 2 is N or CR, wherein at least one of X 1 and X 2 is N;
each R is independently hydrogen, C 1 -C 6 alkyl, halogen or CN;
A is phenyl or 5- to 6-membered heteroaryl, each of which is optionally substituted by R 1 ;
B is C 6 -C 14 aryl, 5- to 10-membered heteroaryl, C 3 -C 8 cycloalkyl, or 3- to 12-membered heterocyclyl, each of which is optionally substituted by R 4 , wherein A is fused to B;
m is 0, 1, 2, 3, or 4;
n is 0, 1, 2, 3, or 4;
R 1 is independently halogen, —CN, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, —C(O)R 17 , —C(O)OR 17 , —NR 17 R 18 or —C(O)NR 17 R 18 ;
R 2 is independently hydrogen, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, —(C 1 -C 3 alkylene)CN, —(C 1 -C 3 alkylene)OR 10 , —(C 1 -C 3 alkylene)NR 11 R 12 , —(C 1 -C 3 alkylene)CF3, —(C 1 -C 3 alkylene)C(O)R 10 , —(C 1 -C 3 alkylene)C(O)NR 11 R 12 , —(C 2 -C 3 alkylene)NR 10 C(O)R 11 , —(C 1 -C 3 alkylene)S(O) 2 R 10 , —(C 2 -C 3 alkylene)NR 10 S(O) 2 R 11 , —(C 1 -C 3 alkylene)S(O) 2 NR 11 R 12 , —(C 1 -C 3 alkylene)(3- to 12-membered heterocyclyl), —(C 1 -C 3 alkylene)(5- to 10-membered heteroaryl), or —(C 1 -C 3 alkylene)(C 6 -C 14 aryl), wherein each R 2 is independently optionally substituted by halogen, oxo, —OR 13 , C 1 -C 6 alkyl, or —NR 13 R 14 ;
R 3 is independently hydrogen, C 1 -C 6 alkyl, —C(O)R 10 , —S(O)R 10 , —S(O) 2 R 10 , C 3 -C 6 cycloalkyl, 3- to 12-membered heterocyclyl, 5- to 10-membered heteroaryl, C 6 -C 14 aryl, —(C 1 -C 3 alkylene)(C 3 -C 6 cycloalkyl), —(C 1 -C 3 alkylene)(3- to 12-membered heterocyclyl), —(C 1 -C 3 alkylene)(5- to 10-membered heteroaryl), or —(C 1 -C 3 alkylene)(C 6 -C 14 aryl), wherein each R 3 is independently optionally substituted by halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that the 5- to 10-membered heteroaryl and C 6 -C 14 aryl of R 3 is not substituted by
each R 4 is independently oxo, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, halogen, —C(O)R 17 , —C(O)OR 17 , —C(O)NR 17 R 18 , —CN, —Si(C 1 -C 6 alkyl) 3 , —OR 17 , —NR 17 R 18 , —OC(O)NR 17 R 18 , —NR 17 C(O)R 18 , —S(O) 2 R 17 , —NR 17 S(O) 2 R 18 , —S(O) 2 NR 17 R 18 , C 3 -C 6 cycloalkyl, 3- to 6-membered heterocyclyl, —(C 1 -C 3 alkylene)CN, —(C 1 -C 3 alkylene)OR 17 , —(C 1 -C 3 alkylene)NR 17 R 18 , —(C 1 -C 3 alkylene)CF 3 , —(C 1 -C 3 alkylene)C(O)R 17 , —(C 1 -C 3 alkylene)C(O)NR 17 R 18 , —(C 1 -C 3 alkylene)NR 17 C(O)R 18 , —(C 1 -C 3 alkylene)S(O) 2 R 17 , —(C 1 -C 3 alkylene)NR 17 S(O) 2 R 18 , —(C 1 -C 3 alkylene)S(O) 2 NR 17 R 18 , —(C 1 -C 3 alkylene)(C 3 -C 6 cycloalkyl) or —(C 1 -C 3 alkylene)(3- to 6-membered heterocyclyl), wherein each R 4 is independently optionally substituted by halogen, oxo, —OR 19 , —NR 19 R 20 , or —C(O)R 19 ,
or two R 4 , when bound to the same carbon or two different carbon atoms, are taken together with the carbon or carbons to which they are attached to form a C 3 -C 6 cycloalkyl or 3- to 7-membered heterocyclyl, each is optionally substituted by R 19 ;
R 10 is independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl, or 3- to 6-membered heterocyclyl, wherein the C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl and 3- to 6-membered heterocyclyl are independently optionally substituted by halogen, oxo, —CN, —OR 1 , —NR 15 R 16 , —P(O)(OR 15 )(OR 16 ), phenyl optionally substituted by halogen, or C 1 -C 6 alkyl optionally substituted by halogen, —OH or oxo;
R 11 and R 12 are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl, or 3- to 6-membered heterocyclyl, wherein the C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl and 3- to 6-membered heterocyclyl are independently optionally substituted by halogen, oxo, —CN, —OR 1 , —NR 15 R 16 , or C 1 -C 6 alkyl optionally substituted by halogen, —OH or oxo,
or R 11 and R 12 are taken together with the atom to which they attached to form a 3- to 6-membered heterocyclyl optionally substituted by halogen, oxo, —OR 1 , —NR 15 R 16 or C 1 -C 6 alkyl optionally substituted by halogen, oxo or —OH;
R 13 and R 14 are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl, 3- to 6-membered heterocyclyl, —C(O)OR 15 , —(C 1 -C 3 alkylene)OR 15 or —C(O)NR 15 R 16 , wherein the C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl and 3- to 6-membered heterocyclyl are independently optionally substituted by halogen, oxo, —CN, —OR 15 , —NR 15 R 16 , or C 1 -C 6 alkyl optionally substituted by halogen, —OH or oxo,
or R 13 and R 14 are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen or C 1 -C 6 alkyl optionally substituted by halogen or oxo;
R 15 and R 16 are each independently hydrogen, C 1 -C 6 alkyl optionally substituted by halogen or oxo, C 2 -C 6 alkenyl optionally substituted by halogen or oxo, or C 2 -C 6 alkynyl optionally substituted by halogen or oxo,
or R 15 and R 16 are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C 1 -C 6 alkyl optionally substituted by oxo or halogen; and
each R 17 , R 18 , R 19 , and R 20 is independently hydrogen, C 3 -C 6 cycloalkyl, 3-6 membered heterocyclyl or C 1 -C 6 alkyl, each of which is optionally substituted by halogen, oxo or —OH,
or R 17 and R 18 are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or —OH.
63 - 66 . (canceled)
67 . The method of claim 62 , wherein the cancer comprises a mutant TP53 gene.
68 - 71 . (canceled)
72 . A method of inhibiting Wee1 in a cell, comprising administering a compound of Formula (I):
or a tautomer or stereoisomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, to the cell, wherein:
X 1 is N or CR;
X 2 is N or CR, wherein at least one of X 1 and X 2 is N;
each R is independently hydrogen, C 1 -C 6 alkyl, halogen or CN;
A is phenyl or 5- to 6-membered heteroaryl, each of which is optionally substituted by R 1 ;
B is C 6 -C 14 aryl, 5- to 10-membered heteroaryl, C 3 -C 8 cycloalkyl, or 3- to 12-membered heterocyclyl, each of which is optionally substituted by R 4 , wherein A is fused to B;
m is 0, 1, 2, 3, or 4;
n is 0, 1, 2, 3, or 4;
R 1 is independently halogen, —CN, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, —C(O)R 17 , —C(O)OR 17 , —NR 17 R 18 or —C(O)NR 17 R 18 ;
R 2 is independently hydrogen, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, —(C 1 -C 3 alkylene)CN, —(C 1 -C 3 alkylene)OR 10 , —(C 1 -C 3 alkylene)NR 11 R 12 , —(C 1 -C 3 alkylene)CF 3 , —(C 1 -C 3 alkylene)C(O)R 10 , —(C 1 -C 3 alkylene)C(O)NR 11 R 12 , —(C 2 -C 3 alkylene)NR 10 C(O)R 11 , —(C 1 -C 3 alkylene)S(O) 2 R 10 , —(C 2 -C 3 alkylene)NR 10 S(O) 2 R 11 , —(C 1 -C 3 alkylene)S(O) 2 NR 11 R 12 , —(C 1 -C 3 alkylene)(3- to 12-membered heterocyclyl), —(C 1 -C 3 alkylene)(5- to 10-membered heteroaryl), or —(C 1 -C 3 alkylene)(C 6 -C 14 aryl), wherein each R 2 is independently optionally substituted by halogen, oxo, —OR 13 , C 1 -C 6 alkyl, or —NR 13 R 14 ;
R 3 is independently hydrogen, C 1 -C 6 alkyl, —C(O)R 10 , —S(O)R 10 , —S(O) 2 R 10 , C 3 -C 6 cycloalkyl, 3- to 12-membered heterocyclyl, 5- to 10-membered heteroaryl, C 6 -C 14 aryl, —(C 1 -C 3 alkylene)(C 3 -C 6 cycloalkyl), —(C 1 -C 3 alkylene)(3- to 12-membered heterocyclyl), —(C 1 -C 3 alkylene)(5- to 10-membered heteroaryl), or —(C 1 -C 3 alkylene)(C 6 -C 14 aryl), wherein each R 3 is independently optionally substituted by halogen, oxo, —OR 3 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 1 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 1 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 5 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that the 5- to 10-membered heteroaryl and C 6 -C 14 aryl of R 3 is not substituted by
each R 4 is independently oxo, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, halogen, —C(O)R 17 , —C(O)OR 17 , —C(O)NR 17 R 18 , —CN, —Si(C 1 -C 6 alkyl) 3 , —OR 17 , —NR 17 R 18 , —OC(O)NR 17 R 18 , —NR 17 C(O)R 18 , —S(O) 2 R 17 , —NR 17 S(O) 2 R 18 , —S(O) 2 NR 17 R 18 , C 3 -C 6 cycloalkyl, 3- to 6-membered heterocyclyl, —(C 1 -C 3 alkylene)CN, —(C 1 -C 3 alkylene)OR 17 , —(C 1 -C 3 alkylene)NR 17 R 18 , —(C 1 -C 3 alkylene)CF3, —(C 1 -C 3 alkylene)C(O)R 17 , —(C 1 -C 3 alkylene)C(O)NR 17 R 18 , —(C 1 -C 3 alkylene)NR 17 C(O)R 18 , —(C 1 -C 3 alkylene)S(O) 2 R 17 , —(C 1 -C 3 alkylene)NR 17 S(O) 2 R 18 , —(C 1 -C 3 alkylene)S(O) 2 NR 17 R 18 , —(C 1 -C 3 alkylene)(C 3 -C 6 cycloalkyl) or —(C 1 -C 3 alkylene)(3- to 6-membered heterocyclyl), wherein each R 4 is independently optionally substituted by halogen, oxo, —OR 19 , —NR 19 R 20 , or —C(O)R 19 ,
or two R 4 , when bound to the same carbon or two different carbon atoms, are taken together with the carbon or carbons to which they are attached to form a C 3 -C 6 cycloalkyl or 3- to 7-membered heterocyclyl, each is optionally substituted by R 19 ;
R 10 is independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl, or 3- to 6-membered heterocyclyl, wherein the C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl and 3- to 6-membered heterocyclyl are independently optionally substituted by halogen, oxo, —CN, —OR 15 , —NR 15 R 16 , —P(O)(OR 15 )(OR 16 ), phenyl optionally substituted by halogen, or C 1 -C 6 alkyl optionally substituted by halogen, —OH or oxo;
R 11 and R 12 are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl, or 3- to 6-membered heterocyclyl, wherein the C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl and 3- to 6-membered heterocyclyl are independently optionally substituted by halogen, oxo, —CN, —OR 15 , —NR 15 R 16 , or C 1 -C 6 alkyl optionally substituted by halogen, —OH or oxo,
or R 11 and R 12 are taken together with the atom to which they attached to form a 3- to 6-membered heterocyclyl optionally substituted by halogen, oxo, —OR 15 , —NR 15 R 16 or C 1 -C 6 alkyl optionally substituted by halogen, oxo or —OH;
R 13 and R 14 are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl, 3- to 6-membered heterocyclyl, —C(O)OR 15 , —(C 1 -C 3 alkylene)OR 15 or —C(O)NR 15 R 16 , wherein the C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl and 3- to 6-membered heterocyclyl are independently optionally substituted by halogen, oxo, —CN, —OR 15 , —NR 15 R 16 , or C 1 -C 6 alkyl optionally substituted by halogen, —OH or oxo,
or R 13 and R 14 are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen or C 1 -C 6 alkyl optionally substituted by halogen or oxo;
R 15 and R 16 are each independently hydrogen, C 1 -C 6 alkyl optionally substituted by halogen or oxo, C 2 -C 6 alkenyl optionally substituted by halogen or oxo, or C 2 -C 6 alkynyl optionally substituted by halogen or oxo,
or R 15 and R 16 are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C 1 -C 6 alkyl optionally substituted by oxo or halogen; and
each R 17 , R 18 , R 19 , and R 20 is independently hydrogen, C 3 -C 6 cycloalkyl, 3-6 membered heterocyclyl or C 1 -C 6 alkyl, each of which is optionally substituted by halogen, oxo or —OH,
or R 17 and R 18 are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or —OH.
73 - 75 . (canceled)
76 . The method of claim 62 , comprising administering to the individual a therapeutically effective amount of a compound of Formula (Ia),
or a tautomer or stereoisomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein:
A is phenyl or 6-membered heteroraryl, each of which is optionally substituted by R 1 ;
B is C 6 aryl, 5- to 6-membered heteroaryl, C 3 -C 8 cycloalkyl, or 3- to 8-membered heterocyclyl, each of which is optionally substituted by R 4 , wherein A is fused with B;
m is 0, 1, 2, 3, or 4;
n is 0, 1, 2, 3, or 4;
R 1 is independently halogen, —CN, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, —C(O)R 17 , —C(O)OR 17 , or —C(O)NR 17 R 18 ;
R 2 is independently hydrogen, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, —(C 1 -C 3 alkylene)CN, —(C 1 -C 3 alkylene)OR 10 , —(C 1 -C 3 alkylene)NR 11 R 12 , —(C 1 -C 3 alkylene)CF3, —(C 1 -C 3 alkylene)C(O)R 10 , —(C 1 -C 3 alkylene)C(O)NR 11 R 12 , —(C 2 -C 3 alkylene)NR 10 C(O)R 11 , —(C 1 -C 3 alkylene)S(O) 2 R 10 , —(C 2 -C 3 alkylene)NR 10 S(O) 2 R 11 , —(C 1 -C 3 alkylene)S(O) 2 NR 11 R 12 , —(C 1 -C 3 alkylene)(3- to 12-membered heterocyclyl), —(C 1 -C 3 alkylene)(5- to 10-membered heteroaryl), or —(C 1 -C 3 alkylene)(C 6 -C 14 aryl), wherein each R 2 is independently optionally substituted by halogen, oxo, —OR 13 , C 1 -C 6 alkyl, or —NR 13 R 14 ;
R 3 is independently hydrogen, C 1 -C 6 alkyl, —C(O)R 10 , —S(O)R 10 , —S(O) 2 R 10 , C 3 -C 6 cycloalkyl, 3- to 12-membered heterocyclyl, 5- to 10-membered heteroaryl, C 6 -C 14 aryl, —(C 1 -C 3 alkylene)(C 3 -C 6 cycloalkyl), —(C 1 -C 3 alkylene)(3- to 12-membered heterocyclyl), —(C 1 -C 3 alkylene)(5- to 10-membered heteroaryl), or —(C 1 -C 3 alkylene)(C 6 -C 14 aryl), wherein each R 3 is independently optionally substituted by halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —S(O)R 13 , —S(O) 2 R 13 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH or halogen, with the proviso that the 5- to 10-membered heteroaryl and C 6 -C 14 aryl of R 3 is not substituted by
each R 4 is independently oxo, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, —C(O)R 17 , —C(O)OR 17 , or —C(O)NR 17 R 18 , wherein each R 4 is independently optionally substituted by halogen, oxo, —OR 19 , —NR 19 R 20 , or —C(O)R 19 ;
or two R 4 are taken together with the carbon to which they attach to form a C 3 -C 6 cycloalkyl;
R 10 is independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl, or 3- to 6-membered heterocyclyl, wherein the C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl and 3- to 6-membered heterocyclyl are independently optionally substituted by halogen, oxo, —CN, —OR 15 , —NR 15 R 16 , —P(O)(OR 15 )(OR 16 ), phenyl optionally substituted by halogen, or C 1 -C 6 alkyl optionally substituted by halogen, —OH or oxo;
R 11 and R 12 are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl, or 3- to 6-membered heterocyclyl, wherein the C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl and 3- to 6-membered heterocyclyl are independently optionally substituted by halogen, oxo, —CN, —OR 15 , —NR 15 R 16 , or C 1 -C 6 alkyl optionally substituted by halogen, —OH or oxo,
or R 11 and R 12 are taken together with the atom to which they attached to form a 3- to 6-membered heterocyclyl optionally substituted by halogen, oxo, —OR 15 , —NR 15 R 16 or C 1 -C 6 alkyl optionally substituted by halogen, oxo or —OH;
R 13 and R 14 are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl, or 3- to 6-membered heterocyclyl, wherein the C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 6 -C 14 aryl, 5- to 6-membered heteroaryl and 3- to 6-membered heterocyclyl are independently optionally substituted by halogen, oxo, —CN, —OR 1 , —NR 15 R 16 , or C 1 -C 6 alkyl optionally substituted by halogen, —OH or oxo,
or R 13 and R 14 are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen or C 1 -C 6 alkyl optionally substituted by halogen or oxo;
R 15 and R 16 are each independently hydrogen, C 1 -C 6 alkyl optionally substituted by halogen or oxo, C 2 -C 6 alkenyl optionally substituted by halogen or oxo, or C 2 -C 6 alkynyl optionally substituted by halogen or oxo,
or R 15 and R 16 are taken together with the atom to which they attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C 1 -C 6 alkyl optionally substituted by oxo or halogen; and
each R 17 , R 18 , R 19 , and R 20 is independently hydrogen or C 1 -C 6 alkyl.
77 . The method of claim 62 , wherein the compound is of Formula (Ib) or Formula (Ic);
78 . The method of claim 62 , wherein A is phenyl fused with B and is optionally substituted by R 1 .
79 . The method of claim 62 , wherein A is 5- to 6-membered heteroaryl fused with B and is optionally substituted by R 1 .
80 . The method of claim 62 , wherein A is 6-membered heteroaryl fused with B and is optionally substituted by R 1 .
81 . The method of claim 62 , wherein A is selected from the group consisting of:
wherein the wavy lines denote attachment points to the parent molecule and each is fused with B and is optionally substituted by R 1 .
82 . The method of claim 62 , wherein B is C 6 aryl optionally substituted by R 4 .
83 . The method of claim 62 , wherein B is 5- to 6-membered heteroaryl optionally substituted by R 4 .
84 . The method of claim 62 , wherein B is 3- to 8-membered heterocyclyl optionally substituted by R 4 .
85 . The method of claim 62 , wherein B is C 3 -C 8 cycloalkyl optionally substituted by R 4 .
86 . The method of claim 62 , wherein the compound is of:
wherein Y is hydrogen or R 4 ;
wherein Y is hydrogen or R 4 ;
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 1 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 1 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13, —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 1 R 16 , —OR 1 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein Y is hydrogen or R 4 ;
wherein Y is hydrogen or R 4 ;
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 5 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 1 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein Y is hydrogen or R 4 ;
or a salt thereof, wherein Y is hydrogen or R 4
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 5 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 1 R 16 , —C(O)OR 5 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4;
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
wherein:
Y is hydrogen or R 4 ;
n and p are independently 0, 1, 2, 3, or 4; and
R 3a is independently hydrogen, halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —C(O)OR 13 , —C(O)NR 13 R 14 , —NR 13 C(O)R 14 , —CN, —SR 13 , —S(O)R 13 , —S(O) 2 R 13 , —Si(C 1 -C 6 alkyl) 3 , —P(O)R 13 R 14 , —NR 13 S(O) 2 R 14 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl optionally substituted by C 1 -C 6 alkyl, CN, CF 3 , oxo, —OH, —NR 15 R 16 , —OR 15 or halogen, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, —NR 15 R 16 , —C(O)OR 15 , —OR 15 or halogen, with the proviso that R 3a is not
87 . The method of claim 62 , wherein A, B, R 1 and R 4 together are selected from the group consisting of:
wherein the wavy lines denote attachment points to the parent molecule.
88 . The method of claim 62 , wherein R 2 is C 1 -C 6 alkyl.
89 . The method of claim 62 , wherein R 2 is C 3 -C 6 cycloalkyl.
90 . The method of claim 62 , wherein R 2 is selected from the group consisting of: methyl, ethyl, isopropyl, cyclopropyl, cyclobutyl,
91 . The method of claim 62 , wherein R 3 is C 1 -C 6 alkyl, —C(O)R 10 , —(C 1 -C 3 alkylene)(C 3 -C 6 cycloalkyl), —(C 1 -C 3 alkylene)(3- to 12-membered heterocyclyl), —(C 1 -C 3 alkylene)(5- to 10-membered heteroaryl), —S(O)R 10 , —S(O) 2 R 10 , or 5- to 10-membered heteroaryl, each of which is optionally substituted by halogen, oxo, —OR 13 , —NR 13 R 14 , —C(O)R 13 , —CN, —S(O)R 13 , —S(O) 2 R 13 , —(C 1 -C 3 alkylene)OR 13 , —(C 1 -C 3 alkylene)NR 13 R 14 , —(C 1 -C 3 alkylene)C(O)R 13 , C 3 -C 8 cycloalkyl, 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, or halogen, or C 1 -C 6 alkyl optionally substituted by oxo, —OH, or halogen, with the proviso that the 5- to 10-membered heteroaryl of R 3 is not substituted by
92 . The method of claim 62 , wherein R 3 is 5- to 10-membered heteroaryl substituted by 3- to 12-membered heterocyclyl optionally substituted by oxo, —OH, or halogen, —CN, —(C 1 -C 3 alkylene)NR 13 R 14 , C 3 -C 8 cycloalkyl, —C(O)R 13 , —NR 13 R 14 , —OR 13 , or C 1 -C 6 alkyl optionally substituted by —OH or halogen, with the proviso that the 5- to 10-membered heteroaryl of R 3 is not substituted by
93 . The method of claim 62 , wherein R 3 is selected from the group consisting of:
94 . The method of claim 62 , wherein the compound is selected from the group consisting of Compound Nos. 1.2, 1.3, 1.6-1.8, and 1.10-3.136 in Tables 1A and 1B, or a tautomer or stereoisomer thereof, or a pharmaceutically acceptable salt of any of the foregoing.Join the waitlist — get patent alerts
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