Novel pyrazolo[4, 3-d]pyrimidines, processes for their preparation and methods for therapy

文件类型：PDF文档
文件大小：5229K
(57) Abstract : The invention relates to 3-, 5-, 7-trisubstituted R7 pyrazolo[4, 3-d]pyrimidines represented by the general formula (I), and H substituted alkyl, cycloalkyl, cycloheteroalkyl, cycloalkyl alkyl, aryl or / N {I} pharmaceutically alkylaryl group; R5 acceptable is halogen, salts -NHNH thereof, 2 , -NHOH, wherein, NHCONH R3 is an 2 optionally , guanylo N (NH-C(NH)NHz) an optionally substituted C 1 -C 6 alkyl, alkenyl, alkinyl, C 3-Cis cycloalkyl, Re (C 3 -Cis cycloalkyl), heterocycle, heteroalkyl, R5 aryl, heteroaryl, arylalkyl, cycloheteroalkyl, cycloheteroalkyl alkyl, R3 heteroarylalkyl group, the group -C(O)-Re, -C(O)NRbR c - SO 3 Rd, or -NHC(O)Re, wherein Re and Rf are an optionally substituted Ci-C 6 alkyl, alkenyl, or alkinyl group, Rb, Re and Rd are independently selected from the group consisting of H, optionally substituted Ct-C 6 alkyl, alkenyl, or alkinyl group, and Re is a hydroxy, amino, alkoxy, alkylamino, optionally substituted C 1 -C 6 alkyl, alkenyl or alkinyl group; or the group -X-R, , wherein X is -NH-, -O-, -Sor -N(alkyl)- and Rs, is hydrogen, an optionally substituted C 1 C 6 alkyl, alkenyl, alkinyl, C 3 C 15 cycloalkyl, Rf(C 3 C 15 cycloalkyl), aryl, heterocycle, hetero C 1 -C, alkyl, arylalkyl, heteroaryl, cycloheteroalkyl, cycloheteroalkyl alkyl, or heteroarylalkyl group, the group -C(O)-Re, -C(O)NRbRc, -SO 3 Rd, or -NHC(O)Re, wherein R., Re, Pc, Rd, Re and Rf have the above meaning, and R7 is halogen, -NHNH> HOH, NHCONHz, guanylo (NH C(NH)NHz) or the group X R 7 , wherein X has the above meaning and the meaning of R 7 , is as defined for Rs, .