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    • 2. 发明授权
    • Substituted cycloalkylamine derivatives and their use as calcium channel
antagonists
    • 取代的环烷基胺衍生物及其作为钙通道拮抗剂的用途
    • US5817698A
    • 1998-10-06
    • US704585
    • 1996-09-20
    • Thomas Henry BrownJohn David HarlingBarry Sidney Orlek
    • Thomas Henry BrownJohn David HarlingBarry Sidney Orlek
    • A61K31/135A61P9/10A61P25/00A61P25/28A61P43/00C07C211/35C07C211/37C07C217/52C07C225/20C07C255/49C07C323/26C07C323/30C07C323/50
    • C07C225/20C07C217/52C07C323/26C07C2101/08
    • A method of treatment of a condition or disease related to the accumulation of calcium in the brain cells of a mammal which comprises administering to a subject in need thereof an effective amount of a compound of formula (I), wherein X is O, S, C.dbd.O or a bond; p and q are independently 0-4; R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkylC.sub.1-4 alkyl; n is 1, 2, 3 or 4; and Ar is phenyl optionally substituted by 1 to 3 substituents selected from; halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-2 alkylenedioxy, trifluoromethyl, trifluoromethoxy, CN, NO.sub.2, amino, mono- or di- alkylamino and Ph(Alk.sup.1).sub.r Y(Alk.sup.2).sub.s -- where Ph is optionally substituted phenyl, Y is a bond, oxygen or a carbonyl group, Alk.sup.1 and Alk.sup.2 are independently C.sub.1-4 alkyl which may be straight or branched and r and s are independently 0 or 1, provided that the length of (Alk.sup.1).sub.r Y(Alk.sup.2).sub.s does not exceed 5 atoms, and pharmaceutically acceptable salts thereof; in the manufacture of a medicament for the treatment of a disorder wherein a calcium channel antagonist is indicated, e.g. ischaemic stroke. Certain novel compounds within formula (I) are also claimed.
    • PCT No.PCT / EP95 / 00964 Sec。 371日期:1996年9月20日 102(e)1996年9月20日PCT PCT 1995年3月14日PCT公布。 公开号WO95 / 26327 日期1995年10月5日式(I)治疗与哺乳动物脑细胞中钙累积相关的病症或疾病的方法,其包括向有需要的受试者施用有效量的化合物 式(I)的化合物,其中X为O,S,C = O或键; p和q独立地为0-4; R 1和R 2各自独立地选自氢,C 1-6烷基,C 3-6环烷基或C 3-6环烷基C 1-4烷基; n为1,2,3或4; 并且Ar是任选被1至3个选自下列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 - 烷基氨基和Ph(Alk 1)rY(Alk 2)s-,其中Ph是任选取代的苯基,Y是 键,氧或羰基,Alk1和Alk2独立地为可以是直链或支链的C 1-4烷基,r和s独立地为0或1,条件是(Alk1)rY(Alk2)s的长度不超过5 原子及其药学上可接受的盐; 在制备用于治疗其中指示钙通道拮抗剂的病症的药物中,例如, 缺血性中风。 还要求公式(I)中的某些新化合物。