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US 8,008,340 B2Granted
3-arylthioindole-2-carboxamide derivatives and analogs thereof as inhibitors of casein kinase I
AssigneeAventis Pharmaceuticals Inc.
InventorWilliam Arthur Metz, Jr.
Life of this patent
Estimating the term…
Abstract
A method for inhibiting casein kinase Iε activity, comprising administering to said patient a therapeutically effective amount of a compound of formula I. its stereoisomer, enantiomer, racemate, tautomer or pharmaceutically acceptable salt thereof.
Claims12
A method for inhibiting casein kinase Iε activity in a patient comprising the administration to said patient a therapeutically effective amount of a compound of formula I, or a stereoisomer, enantiomer, racemate, tautomer or a pharmaceutically acceptable salt thereof,
- wherein
- X is H, Cl, F, Br, NO2, CN, OR2, NR2R2, HNSO2—C1-3alkyl, or NHCO—C1-3alkyl;
- Y is —S— or —O—;
- R1 is
- 1) aryl, unsubstituted or substituted with one or more:
- a) C1-5alkoxy,
- b) OH,
- c) halogen,
- d) NR2R2,
- e) C1-5alkyl, unsubstituted or substituted with one or more:
- i) OH or
- ii) C1-5alkoxy;
- 2) a heterocycle, substituted or un-substituted with one or more:
- a) C1-5alkyl, substituted or un-substituted with one or more:
- i) OH or
- ii) C1-5alkoxy,
- b) C1-5alkoxy,
- c) OH,
- d) halogen, or
- e) NR2R2;
- 3) C1-5alkyl, substituted or un-substituted with one or more of:
- a) C1-5alkyl,
- b) C1-5alkoxy,
- c) OH, or
- d) aryl, substituted or un-substituted with one or more of:
- i) C1-5alkyl,
- ii) C1-5alkoxy,
- iii) OH,
- iv) halogen, or
- v) NR2R2;
- Z is
- 1) C(═O)NR2R3 or
- 2) C(═O)R4;
- R2 is hydrogen or C1-3alkyl;
- R3 is hydrogen, C1-5alkyl, or C3-6cycloalkyl;
- and
- R4 is 1-piperidinyl, 1-pyrrolidinyl, 1-piperazinyl or 4-morpholinyl, unsubstituted or substituted with one or more of:
- 1) C1-5alkyl,
- 2) C1-5alkoxy,
- 3) OH,
- 4) halogen, or
- 5) NR2R2.
39 more elements
Dependencies are inferred from the claim text.