| 摘要 |
4-Substituted amino-2-aryl-cyclopenta(d)pyrimidine derivatives (I), their stereoisomeric forms, and mixtures in any proportion, and their salts are new. 4-Substituted amino-2-aryl-cyclopenta(d)pyrimidine derivatives of formula (I), their stereoisomeric forms, and mixtures in any proportion, and their salts are new. R<1>, R<2> = H (but not both H); 1-8C alkyl (optionally substituted by one or more of hydroxy, 1-4C alkoxy, 1-4C alkyl-S(O)m, phenyl, naphthyl or pyridyl) or 3-9C cycloalkyl (optionally substituted by 1-4C alkyl, hydroxy, amino or benzyl); a 5-7 membered saturated heterocycle which may include one or more O, NR<10> or S(O)m and is optionally substituted by 1-4C alkyl, hydroxy or aryl(1-4C)alkyl; the phenyl, naphthyl, pyridyl and benzyl groups may be substituted in the aromatic rings by one or more of halo, 1-4C alkyl, 1-4C alkoxy, phenyl, trifluoromethyl, nitro, hydroxy, 1-4C alkoxy(2-4C)alkoxy, 1-2C alkylenedioxy, amino (optionally substituted by one or two 1-4C alkyl, one formyl, or one 1-4C alkylcarbonyl), cyano, carbonylamino (optionally N-substituted by one or two 1-4C alkyl) carboxy, 1-4C alkoxycarbonyl, formyl or 1-4C alkylcarbonyl; or NR<1>R<2> = a 5-7 membered saturated heterocycle, optionally containing an additional O or S(O)m and optionally substituted by one or more of 1-4C alkyl, 1-4C alkoxy, hydroxy or R<11>R<12>N; R<11>, R<12> = H or 1-4C alkyl; R<10> = H, 1-4C alkyl (optionally substituted by aryl, hydroxy, hydroxycarbonyl, 1-4C alkoxycarbonyl or R<11>R<12>NCO), R<13>SO2 or aryl; R<3> = aryl but cannot be unsubstituted phenyl; aryl = phenyl, naphthyl or heteroaryl, all optionally substituted by halo, 1-4C alkyl, phenyl, CF3, NO2, OH, 1-4C alkoxy, 2-4C alkoxy-1-4C alkoxy, 1-2C alkylenedioxy, NH2, NH-1-4C alkyl, N(1-4C alkyl)2, NHCHO, NHCO-1-4C alkyl, CN, CONH2, CONH-1-4C alkyl, CON(1-4C alkyl)2, COOH, COO-1-4C alkyl, CHO or CO-1-4C alkyl; R<13> = 1-4C alkyl, aryl or R<11>R<12>N; m = 0-2; heteroaryl = monocyclic 5-6 membered aromatic heterocycle or a bicyclic 8-10 membered aromatic heterocycle which may contain one or more N, O or S. An Independent claim is also included for a method for production of (I).
|
