Patent classifications
C07D241/20
PD-1/PD-L1 inhibitors
- Evangelos Aktoudianakis ,
- Aesop Cho ,
- Zhimin Du ,
- Michael Graupe ,
- Lateshkumar Thakorlal Lad ,
- Paulo A. Machicao Tello ,
- Jonathan William Medley ,
- Samuel E. Metobo ,
- Prasenjit Kumar Mukherjee ,
- Devan Naduthambi ,
- Eric Q. Parkhill ,
- Barton W. Phillips ,
- Scott Preston Simonovich ,
- Neil H. Squires ,
- Peiyuan Wang ,
- William J. Watkins ,
- Jie Xu ,
- Kin Shing Yang ,
- Christopher Allen Ziebenhaus
Compounds of Formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
PD-1/PD-L1 INHIBITORS
- Evangelos Aktoudianakis ,
- Aesop Cho ,
- Zhimin Du ,
- Michael Graupe ,
- Lateshkumar Thakorlal Lad ,
- Paulo A. Machicao Tello ,
- Jonathan William Medley ,
- Samuel E. Metobo ,
- Prasenjit Kumar Mukherjee ,
- Devan Naduthambi ,
- Eric Q. Parkhill ,
- Barton W. Phillips ,
- Scott Preston Simonovich ,
- Neil H. Squires ,
- Peiyuan Wang ,
- William J. Watkins ,
- Jie Xu ,
- Kin Shing Yang ,
- Christopher Allen Ziebenhaus
Compounds of Formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
PD-1/PD-L1 INHIBITORS
- Evangelos Aktoudianakis ,
- Aesop Cho ,
- Zhimin Du ,
- Michael Graupe ,
- Lateshkumar Thakorlal Lad ,
- Paulo A. Machicao Tello ,
- Jonathan William Medley ,
- Samuel E. Metobo ,
- Prasenjit Kumar Mukherjee ,
- Devan Naduthambi ,
- Eric Q. Parkhill ,
- Barton W. Phillips ,
- Scott Preston Simonovich ,
- Neil H. Squires ,
- Peiyuan Wang ,
- William J. Watkins ,
- Jie Xu ,
- Kin Shing Yang ,
- Christopher Allen Ziebenhaus
Compounds of Formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
AMINOPYRAZINE DERIVATIVES AS PI3K-y INHIBITORS
This application relates to compounds of Formula (I):
##STR00001##
or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
AMINOPYRAZINE DERIVATIVES AS PI3K-y INHIBITORS
This application relates to compounds of Formula (I):
##STR00001##
or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
1,2,4-OXADIAZOL-5-ONE DERIVATIVES FOR THE TREATMENT OF CANCER
The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein A1 is —N═ or —C(R3)=; A2 is —N═ or —CH═; L is —NH—; B1 and B2 are independently —N═ or —C(R2b)=; B3 and B4 are independently —C(R2b)=; no more than one R2b on B1, B2, B3 and B4 is other than hydrogen; R1a is hydrogen, halogen, C1-C3alkyl (n-alkyl) optionally substituted with one R4, or R1a is —NH.sub.2, —NH(C1-C3alkyl (n-alkyl)), —NH(C(═O)—C1-C2alkyl), —N(C1-C3alkyl (n-alkyl)).sub.2, —OC1-C3alkyl (n-alkyl), C1-C3haloalkyl (n-alkyl) or —OC1-C3haloalkyl (n-alkyl); R1b is hydrogen, halogen, C1-C3alkyl (n-alkyl), —OC1-C3alkyl (n-alkyl), —NH.sub.2, —NH(C1-C3alkyl (n-alkyl)) or —N(C1-C3alkyl (n-alkyl)).sub.2; R1a and R1b may together form a —CH═CH—CH═CH— moiety in which one or two non-adjacent CH are optionally replaced by N; R2a is halogen, C1-C6alkyl, C1-C6haloalkyl, cyclopropyl, cyclobutyl, —OR6, —NHC(═O)—C3-C6cycloalkyl, Cycle Q, —SF.sub.5 or group Y (formula (Y)); wherein X is a 3- or 4-membered carbocyclic ring and R8 is halogen, cyano, C1-C6alkyl, C1-C6haloalkyl or —C1-C6alkyl-CN; and wherein R2b, R3, R4, R6 and R8 are as defined in the claims; as well as methods of using the compounds to treat neoplastic diseases, in particular cancer.
##STR00001##
SMALL MOLECULE PROSTAGLADIN TRANSPORT INHIBITORS
The disclosure provides compounds of Formula 1, and the pharmaceutically acceptable salts thereof. The variables in Formula 1, e.g. X.sup.1-X.sup.5, A.sup.1, A.sup.2, and R.sup.1-R.sup.4 are described herein. Such compounds are useful as prostaglandin transport (PGT) inhibitors. The disclosure further includes pharmaceutical compositions comprising a compound of Formula 1 or salt thereof and methods of using compounds of Formula 1 and salts thereof to treat diseases and disorders mediated, at least in part, by prostaglandin levels or cyclooxygenase activity. Such diseases and disorders include painful and inflammatory conditions.
##STR00001##
SMALL MOLECULE PROSTAGLADIN TRANSPORT INHIBITORS
The disclosure provides compounds of Formula 1, and the pharmaceutically acceptable salts thereof. The variables in Formula 1, e.g. X.sup.1-X.sup.5, A.sup.1, A.sup.2, and R.sup.1-R.sup.4 are described herein. Such compounds are useful as prostaglandin transport (PGT) inhibitors. The disclosure further includes pharmaceutical compositions comprising a compound of Formula 1 or salt thereof and methods of using compounds of Formula 1 and salts thereof to treat diseases and disorders mediated, at least in part, by prostaglandin levels or cyclooxygenase activity. Such diseases and disorders include painful and inflammatory conditions.
##STR00001##
HETEROARYL COMPOUNDS AS KINASE INHIBITOR
Provided herein are compounds of formula (I) having activity on a receptor protein tyrosine kinase, wherein R.sup.1, R.sup.2, R.sup.3, A, Q, Z, X and W are set forth in the description, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof.
##STR00001##
HETEROARYL COMPOUNDS AS KINASE INHIBITOR
Provided herein are compounds of formula (I) having activity on a receptor protein tyrosine kinase, wherein R.sup.1, R.sup.2, R.sup.3, A, Q, Z, X and W are set forth in the description, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof.
##STR00001##