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US 7,605,154 B2Granted
Substituted Thiazolo [4,5-d]pyrimidines as protein kinase inhibitors
AssigneeJanssen Pharmaceutica NV
InventorsEva Binnun, Peter J. Connolly, Sigmond G. Johnson, Ronghui Lin, Steven A. Middleton, Sandra J. Moreno-Mazza, Niranjan B. Pandey, Steven K. Wetter
Life of this patent
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Abstract
The present invention is directed to novel thiazolopyrimidine compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions.
Claims5
The compound of the following formula:
- wherein
- p is 0, 1, 2 or 3,
- R5 is hydrogen or C1-8alkyl,
- Ar1 is phenyl,
- R1 and R2 is each independently selected from the group consisting of
- (1) hydrogen,
- (2) C1-8alkyl,
- (3) C1-8alkoxy,
- wherein (2) and (3) is each optionally substituted with a substituent selected from the group consisting of
- (i) heteroaryl,
- (ii) heterocyclyl,
- wherein (i) and (ii) are optionally substituted with one or two substituents independently selected from the group consisting of
- (a) C1-8alkyl,
- (c) C1-8alkyl(C1-8alkoxy),
- (d) C1-8alkyl(hydroxy)1-3,
- (e) CO2(C1-8alkyl),
- (g) C1-8alkyl(amino), and
- (h) aryl optionally substituted with halogen, and
- (iii) amino optionally mono or disubstituted with a substituent independently selected from the group consisting of
- (a) C1-8alkyl,
- (b) C1-8alkyl(C1-8alkoxy),
- (c) C1-8alkyl(hydroxy)1-3,
- (d) C3-8cycloalkyl,
- (e) heterocyclyl optionally substituted with one or two C1-8alkyl substituents, and
- (f) C1-8alkyl(heterocyclyl) optionally substituted on heterocyclyl with one or two C1-8alkyl substituents,
- (4) amino optionally mono or disubstituted with C1-8alkyl(heterocyclyl),
- (5) cyano,
- (6) hydroxy,
- (7) heterocyclyl,
- (8) SO2(heterocyclyl),
- (9) C(O)amino optionally mono or disubstituted on amino with C1-8alkyl, and
- (10) SO2(amino) optionally mono or disubstituted on amino with a substituent independently selected from the group consisting of
- (i) C1-8alkyl(C1-8alkoxy),
- (ii) C1-8alkyl(amino) optionally mono or disubstituted on amino with C1-8alkyl,
- (iii) C1-8alkyl(hydroxy)1-3, and
- (iv) C1-8alkyl(heterocyclyl),
- Ar2 is phenyl, and
- R3 and R4 is each independently selected from the group consisting of
- (1) hydrogen,
- (2) C1-8alkyl,
- (3) C2-8alkynyl,
- (4) C1-8alkoxy,
- (5) C1-8alkoxy(aryl), wherein aryl is optionally substituted with one, two or three halogen substinients,
- (5) cyano,
- (6) halogen,
- (7) nitro, and
- (8) heterocyclyl.
44 more elements
Dependencies are inferred from the claim text.