Patent ID: 6699887
Filing Date: 2004-03-02
Classification: A61K,A61P,C07D

Abstract:
A compound of the formula whereinR1 is optionally substituted C1-12-alkyl, C3-8-cycloalkyl, acyl, C1-4-alkylsulfonyl, optionally substituted phenylsulfonyl, aryl, heterocyclyl or C1-4-alkyl substituted with phenyl, wherein the heterocycle is furyl, 1-pyrrolyl, 2-pyrrolyl, 1-thiophenyl, 2-thiophenyl, 2-pyridinyl (2-pyridyl), 3-pyridinyl (3-pyridyl), 4-pyridinyl (4-pyridyl), 1H-pyridin-2-one, 1H-pyridin-4-one, 3H-pyrimidine-4-one, pyridazine (1,2-diazine), pyrimidine (1,3-diazine), pyrazine (1,4-diazine), oxazole or isoxazole (iso-oxazole), the substituted C1-12-alkyl is substituted with 1-5 substituents selected from fluorine, chlorine and bromine, and the substituted phenyl is substituted with 1-5 substituents selected from C1-4-alkyl, C1-4-alkoxy, hydroxy, fluorine, chlorine, bromine and cyano; R2â€² is phenyl or phenyl substituted with 1-5 substituents selected from C1-4-alkyl, C1-4-alkoxy, hydroxy, fluorine, chlorine, bromine, cyano and nitro; R3 is C1-12-alkyl or C1-4-alkoxy-C1-4-alkyl; Aâ€² is a group selected from CH2-(aryl-C1-4-alkylamino), CH2-(aryl-C1-4-alkoxy), C1-4-alkyl substituted with unsubstituted aryl, aryl substituted with 1-5 substituents selected from C1-4-alkyl, C1-4-alkoxy, hydroxy, fluorine, chlorine, bromine, cyano, Sâ€”C1-4-alkyl and NRRâ€², unsubstituted 4-pyridyl, or 4-pyridyl substituted with 1-4 substituents selected from C1-4-alkyl, C1-4-alkoxy, hydroxy, fluorine, chlorine, bromine, cyano, Sâ€”C1-4-alkyl and NRRâ€², wherein R and Râ€² are independently of each other hydrogen or C1-4-alkyl, or CH2-(heterocyclyl-C1-4-alkoxy) wherein the heterocycle is furyl, 1-pyrrolyl, 2-pyrrolyl, 1-thiophenyl, 2-thiophenyl, 2-pyridinyl (2-pyridyl), 3-pyridinyl (3-pyridyl), 4-pyridinyl (4-pyridyl), 1H-pyridin-2-one, 1H-pyridin-4-one, 3H-pyrimidine-4-one, pyridazine (1,2-diazine), pyrimidine (1,3-diazine), pyrazine (1,4-diazine), oxazole or isoxazole (iso-oxazole); or Aâ€² is a group of formula CH2-U-heterocyclyl, wherein the heterocycle is furyl, 1-pyrrolyl, 2-pyrrolyl, 1-thiophenyl, 2-thiophenyl, 2-pyridinyl (2-pyridyl), 3-pyridinyl (3-pyridyl), 4-pyridinyl (4-pyridyl), 1H-pyridin-2-one, 1H-pyridin-4-one, 3H-pyrimidine-4-one, pyridazine (1,2-diazine), pyrimidine (1,3-diazine), pyrazine (1,4-diazine), oxazole or isoxazole (iso-oxazole), wherein U is O, S or NRâ€³, wherein Râ€³ is hydrogen or C1-4-alkyl, and wherein heterocyclyl is optionally substituted with 1-4 substituents selected from C1-4-alkyl, fluorine, chlorine, bromine, cyano, nitro and NRRâ€², wherein R and Râ€² are independently of each other hydrogen or C1-4-alkyl; or Aâ€² is a group of formula CH(OH)aryl; or Aâ€² is a group of formula CH&boxH;CHW wherein W is unsubstituted aryl, aryl substituted with 1-5 substituents selected from C1-4-alkyl, C1-4-alkoxy, hydroxy, cyano, fluorine, chlorine and bromine, heterocyclyl, optionally substituted with 1-4 substituents selected from C1-4-alkyl, C1-4-alkoxy, hydroxy, cyano, fluorine, chlorine and bromine, and wherein said heterocycle is furyl, 1-pyrrolyl, 2-pyrrolyl, 1-thiophenyl, 2-thiophenyl, 2-pyridinyl (2-pyridyl), 3-pyridinyl (3-pyridyl), 4-pyridinyl (4-pyridyl), 1H-pyridin-2-one, 1H-pyridin-4-one, 3H-pyrimidine-4-one, pyridazine (1,2-diazine), pyrimidine (1,3-diazine), pyrazine (1,4-diazine), oxazole or isoxazole (iso-oxazole); X is S or O; or the pharmaceutically acceptable hydrolyzable esters or ethers thereof or pharmaceutically acceptable salts thereof.