发明名称 Amine derivatives as calcium channel antagonists
摘要 Compounds of formula (I), wherein R<1> and R<2> each independently represent: hydrogen, C1-8alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-4alkyl, arylC1-4alkyl, C2-6hydroxyalkyl or R<3>R<4>NC2-6alkyl (where R<3> and R<4> independently represent H or C1-4alkyl) or NR<1>R<2> represents a saturated heterocyclic ring containing 4 to 9 ring members, one of which may optionally be a further heteroatom selected from O, S or NR<5>, (where R<5> is H, C1-4alkyl or arylC1-4alkyl), which ring may optionally be substituted by one or two substituents selected from C1-6alkyl and C1-6alkoxy; X represents O, S or NR<6> (where R<6> is hydrogen, C1-4alkyl or arylC1-4alkyl); Y represents O, S, C=O or a bond; n is 2 to 5; m is 1 to 5 (providing that when m is 1, Y represents a bond); and Ar represents phenyl optionally substituted by 1-3 substituents selected from halo, C1-8alkyl, C1-8alkoxy, C1-2alkylenedioxy e.g. methylenedioxy, trifluoromethyl, trifluoromethyloxy, or by a group Ph(Alk<1>)pA(Alk<2>)q- where Ph isoptionally substituted phenyl, A is a bond, O, S, -C=O or CH=CH, Alk<1> and Alk<2> independently represent C1-4alkyl which may be straight or branched and p and q are independently 0 or 1, provided that the length of -(Alk<1>)pA(Alk<2>)q- does not exceed 5 atoms, or Ar is an optionally substitued tricyclic heteroaryl group (a) in which Y<1> is Y<2>(CH2)r where r is 0 or 1 and Y<2> is O, S or NR<7> where R<7> is hydrogen or C1-4alkyl, Z is (CH2)s or -CH=CH-, s is 0, 1 or 2 or Ar is the corresponding tricyclic dehydro ring system; and pharmaceutically acceptable salts thereof are useful as atherapeutic agents, e.g. for the treatment of ischaemic stroke.
申请公布号 ZA9408232(B) 申请公布日期 1996.04.22
申请号 ZA19940008232 申请日期 1994.10.20
申请人 SMITHKLINE BEECHAM PLC. 发明人 DAVID GWYN COOPER;RONALD JOSEPH KING;THOMAS HENRY BROWN
分类号 C07D295/08;A61K31/397;A61K31/40;A61K31/435;A61K31/495;A61P3/00;A61P3/14;A61P9/00;A61P25/00;A61P25/08;A61P25/28;A61P25/30;C07D205/04;C07D205/08;C07D295/088;C07D295/12;C07D295/13 主分类号 C07D295/08
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