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    • 105. 发明授权
    • Pharmacologically active pyrimidineamine derivatives and processes for
the preparation thereof
    • 药理活性嘧啶胺衍生物及其制备方法
    • US5705502A
    • 1998-01-06
    • US446742
    • 1995-05-31
    • Jurg Zimmermann
    • Jurg Zimmermann
    • A61K31/505A61P35/00C07D239/42C07D401/04C07D403/04C07D417/04
    • C07D239/42C07D401/04
    • Described are N-phenyl-2-pyrimidineamine derivatives of formula I ##STR1## wherein R.sub.1 is a substituted cyclic radical, the cyclic radical being bonded at a ring carbon atom in each case and being selected from phenyl, pyridyl, pyrazinyl, thiazolyl, pyrimidinyl, pyridazinyl and imidazolyl, and the substituents of the above-mentioned cyclic radical being selected from one or more of the groups halogen, cyano, carbamoyl, --C(.dbd.O)--OR.sub.3, --C(.dbd.O)--R.sub.4, --SO.sub.2 --N(R.sub.5)--R.sub.6, --N(R.sub.7)--R.sub.8, --OR.sub.9 and fluorine-substituted lower alkyl, wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are each independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino; and R.sub.2 is selected from halogen, cyano, carbamoyl, --C(.dbd.O)--OR.sub.10, --C(.dbd.O)--R.sub.11, --SO.sub.2 --N(R.sub.12)--R.sub.13, --N(R.sub.14)--R.sub.15, --OR.sub.16 and fluorine-substituted lower alkyl, wherein R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15 and R.sub.16 are each independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino. Those compounds can be used, for example, in the treatment of tumour diseases.
    • PCT No.PCT / EP94 / 03148 Sec。 371日期:1995年5月31日 102(e)日期1995年5月31日PCT 1994年9月21日PCT PCT。 WO95 / 09851 PCT出版物 日期1995年04月13日描述了式I的N-苯基-2-嘧啶胺衍生物,其中R1是取代的环状基团,环状基团在环状碳原子上键合,并且选自苯基 吡啶基,噻唑基,嘧啶基,哒嗪基和咪唑基,上述环状基团的取代基选自一个或多个卤素,氰基,氨基甲酰基,-C(= O)-OR 3,-C( = O)-R4,-SO2-N(R5)-R6,-N(R7)-R8,-OR9和氟取代的低级烷基,其中R3,R4,R5,R6,R7,R8和R9各自独立地 的其它氢或未被取代或被一或二低级烷基氨基取代的低级烷基; 且R 2选自卤素,氰基,氨基甲酰基,-C(= O)-OR 10,-C(= O)-R 11,-SO 2 -N(R 12)-R 13,-N(R 14)-R 15,-OR 16和 氟取代的低级烷基,其中R10,R11,R12,R13,R14,R15和R16各自独立地为氢或未被取代或被一或二低级烷基氨基取代的低级烷基。 那些化合物可用于例如治疗肿瘤疾病。