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    • 2. 发明授权
    • AMINOINDANES AND RELATED COMPOUNDS USEFUL AS CALCIUM-CHANNEL ANTAGONISTS
    • AMINOINDANE UND VERWANDTE VERBINDUNGEN ALS CALCIUMKANAL-ANTAGONISTEN
    • EP0711271B1
    • 1998-10-07
    • EP94921664.2
    • 1994-07-21
    • SMITHKLINE BEECHAM PLC
    • HARLING, John, DavidORLEK, Barry, Sidney
    • C07C211/42C07C211/49C07C217/52C07C323/23A61K31/135
    • C07D333/20C07C211/42C07C217/52C07C2601/02C07C2602/08C07C2602/10C07C2602/12
    • Compounds of formula (I) and salts thereof are useful for treating accumulation of calcium in brain cells, wherein X represents O, S, NH or a bond; p and q independently represent 0-4 such that the sum of p + q is at least 1; R?1 and R2¿ each independently represent hydrogen, C¿1-6?alkyl, C3-6cycloalkyl, or C1-4alkyl-C3-6cycloalkyl; n is 1, 2 or 3; and Ar represents phenyl optionally substituted by 1 to 3 substituents selected from: halo, C1-4alkyl, C1-4alkoxy, C1-2alkylenedioxy, trifluoromethyl, trifluoromethoxy, CN, NO2, amino, mono- or di-alkylamino, optionally substituted benzoyl and Ph(CH2)rY(CH2)s- where Ph is optionally substituted phenyl, Y is oxygen or a bond and r and s each independently represent 0-4 provided that the sum of r + s is not greater than 4, or Ar represents an optionally substituted unsaturated monocyclic heteroaryl ring system containing 5 or 6 ring members, or an optionally substituted, unsaturated or partially saturated bicyclic aryl or heteroaryl ring system containing 8-10 ring members.
    • 式(I)化合物及其盐可用于治疗脑细胞中钙的积累,其中X表示O,S,NH或键; p和q独立地表示0-4,使得p + q的和为至少1; R 1和R 2各自独立地表示氢,C 1-6烷基,C 3-6环烷基或C 1-4烷基-C 3-6环烷基; n为1,2或3; 并且Ar表示任选被1至3个选自以下的取代基取代的苯基:卤素,C 1-4烷基,C 1-4烷氧基,C 1-2亚烷基二氧基,三氟甲基,三氟甲氧基,CN,NO 2,氨基,单 - 或二 - 烷基氨基,任选取代的苯甲酰基和Ph (CH 2)r Y(CH 2)s - 其中Ph是任选取代的苯基,Y是氧或键,并且r和s各自独立地代表0-4,条件是r + s之和不大于4,或Ar表示 含有5或6个环成员的任选取代的不饱和单环杂芳环系统,或含有8-10个环成员的任选取代的不饱和或部分饱和的双环芳基或杂芳基环系。