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US 10,766,879 B2Granted
Pyrimidine derivatives as kinase inhibitors and their therapeutical applications
AssigneeNantBioScience, Inc.
InventorsChunlin Tao, Qinwei Wang, Laxman Nallan, David Ho, Tulay Polat, Forrest Arp, Paul Weingarten
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Abstract
The present invention provides antitumor agents comprising substituted pyrimidine derivatives and pharmaceutically-acceptable formulations thereof, methods for making novel compounds and methods for using the compounds. The compounds and compositions in accordance with the invention have utility in treatment of a variety of diseases and have kinase inhibitory activities.
Claims9
A compound of the formula
- or a pharmaceutically acceptable salt thereof, wherein:
- W is selected from the group consisting of:
- Cl, Br, I, CN, and CONH2;
- Ar represents heteroaryl or aryl, each of which is substituted with from 0 to 4 substituents independently chosen from the group consisting of:
- (1) halogen, hydroxy, amino, amide, cyano, —COOH, —SO2NH2, oxo, nitro or alkoxycarbonyl;
- (2) NR1;
- and
- (3) groups of the formula
- wherein:
- R1 represents hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, alkylthio, aryl, or arylalkyl;
- R4 represents hydrogen, C1-C4 alkyl, or oxo;
- X—R3 is CH;
- or X—R3 is O;
- or X is N, and R3 represents hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C10 aryl or heteroaryl, (C3-C7 cycloalkyl)C1-C4 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 alkylthio, C2-C6 alkanoyl, C1-C6 alkoxycarbonyl, C2-C6 alkanoyloxy, mono- and di-(C3-C8 cycloalkyl)aminoC0-C4alkyl, (4- to 7-membered heterocycle)C0-C4alkyl, C1-C6 alkylsulfonyl, mono- and di-(C1-C6 alkyl) sulfonamido, and mono- and di-(C1-C6 alkyl)aminocarbonyl, each of which is substituted with from 0 to 4 substituents independently chosen from halogen, hydroxy, cyano, amino, —COOH or oxo;
- R5 and R6 are independently selected from the group consisting of:
- hydrogen, F, Cl, and Br;
- and
- R7, R8 and R9 are independently selected from the group consisting of:
- hydrogen and CH3.
16 more elements
Dependencies are inferred from the claim text.