Patent ID: 6548495
Filing Date: 2003-04-15
Classification: A61P,C07D

Abstract:
A compound of formula whereinR1 is selected from the group consisting of cyano, fluoro-lower alkyl, lower alkoxy, fluoro-lower alkoxy, unsubstituted pyrrol-1-yl, and pyrrol-1-yl substitued by between one to three substituents selected from the group consisting of fluoro, chloro, cyano, unsubstituted phenyl, or phenyl substituted by a substituent selected from the group consisting of halogen, â€”(CH2)1-4-hydroxy, fluoro-lower alkyl, lower alkyl, â€”(CH2)n-lower alkoxy, â€”(CH2)nâ€”C(O)Oâ€”Râ€³, â€”(CH2)1-4â€”NRâ€²Râ€³, hydroxy-lower alkoxy and â€”(CH2)nâ€”CONRâ€²Râ€³; R2 is selected from the group consisting of halogen, hydroxy, lower alkyl, fluoro-lower alkyl, lower alkoxy, hydroxymethyl, hydroxyethoxy, lower alkoxy-(ethoxy)m, wherein m=1 to 4, lower alkoxymethyl, cyanomethoxy, morpholine-4-yl, thiomorpholine-4-yl, 1-oxothiomorpholine-4-yl, 1,1-dioxothiomorpholine-4-yl, 4-oxo-piperidine-1-yl 4-alkoxy-piperidine-1-yl, 4-hydroxy-piperidine-1-yl, 4-hydroxyethoxy-piperidine-1-yl, 4-lower alkyl-piperazine-1-yl, alkoxycarbonyl, 2-dialkylamino-ethylsulfanyl, N,N-bis lower alkylamino lower alkyl, carbamoylmethyl, alkylsulfonyl lower alkoxycarbonyl-lower alkyl, alkylcarboxy-lower alkyl, carboxy-lower alkyl, alkoxycarbonylmethylsulfanyl, carboxymethylsulfanyl, 1,4-dioxa-8-aza-spiro[4.5]dec-8-yl, carboxy-lower alkoxy, cyano-lower alkyl, 2,3-dihydroxy-lower alkoxy, carbamoylmethoxy, 2-oxo-[1,3]-dioxolan-4-yl-lower alkoxy, N-(2-hydroxy-lower alkyl)-N-lower alkyl amino, hydroxycarbamoyl-lower alkoxy, 2,2-dimethyl-tetrahydro-[1,3]dioxolo[4,5c]-pyrrol-5-yl, lower alkoxy-carbamoyl-lower alkoxy, 3R-hydroxy-pyrrolidin-1-yl, 3,4-dihydroxy-pyrrolidin-1-yl, 2-oxo-oxazolidin-3-yl, lower alkyl-carbamoylmethoxy, aminocarbamoyl-lower alkoxy, and, when R1 is unsubstituted pyrrol-1-yl or pyrrol-1-yl substituted as defined above, hydrogen; Y is â€”CH&boxH; or &boxH;Nâ€”; R3 is halogen, lower alkyl, fluoro-lower alkyl, lower alkoxy, cyano, â€”(CH2)nâ€”C(O)â€”ORâ€³, â€”(CH2)nâ€”C(O)â€”NRâ€²Râ€³, or is an unsubstituted five-membered aromatic heterocycle or a five-membered aromatic heterocycle, substituted by halogen, fluoro-lower alkyl, fluoro-lower alkoxy, cyano, â€”(CH2)nâ€”NRâ€²Râ€³, â€”(CH2)nâ€”C(O)â€”ORâ€³, â€”(CH2)nâ€”C(O)â€”NRâ€²Râ€³, â€”(CH2)nâ€”SO2â€”NRâ€²Râ€³, â€”(CH2)nâ€”C(NH2)&boxH;NRâ€³, hydroxy, lower alkoxy, lower alkylthio, lower alkyl, or lower alkyl substituted by fluoro, hydroxy, lower alkoxy, cyano or carbamoyloxy; Râ€² is selected from the group consisting of hydrogen, lower alkyl, C3-C6-cycloalkyl, fluoro-lower alkyl and 2-lower alkoxy lower alkyl; Râ€³ is selected from the group consisting of hydrogen, lower alkyl, C3-C6-cycloalkyl, fluoro-lower alkyl, 2-lower alkoxy lower alkyl, â€”(CH2)2-4-di-lower alkylamino, â€”(CH2)2-4-morpholinyl, â€”(CH2)2-4-pyrrolidinyl, â€”(CH2)2-4-piperidinyl and 3-hydroxy-lower alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable addition salt thereof.