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    Substituted isoquinoline-3-carboxamides, their preparation and their use as pharmaceuticals
    15.
    发明授权
    Substituted isoquinoline-3-carboxamides, their preparation and their use as pharmaceuticals 有权
    取代的异喹啉-3-甲酰胺，其制备及其作为药物的用途

    公开(公告)号：US6093730A

    公开(公告)日：2000-07-25

    申请号：US174558

    申请日：1998-10-19

    申请人： Klaus Weidmann ,  Karl-Heinz Baringhaus ,  Georg Tschank ,  Ulrich Werner

    发明人： Klaus Weidmann ,  Karl-Heinz Baringhaus ,  Georg Tschank ,  Ulrich Werner

    IPC分类号： A61K31/00 ,  A61K31/47 ,  A61K31/472 ,  A61K38/00 ,  A61K38/05 ,  A61P1/00 ,  A61P1/16 ,  A61P11/00 ,  A61P15/00 ,  A61P17/00 ,  A61P43/00 ,  C07D217/26 ,  C07K5/078 ,  C07D217/00

    CPC分类号： C07K5/06139 ,  C07D217/26 ,  A61K38/00

    摘要： Novel isoquinoline-3-carboxamides of the formula I: ##STR1## in which R.sub.1 is hydrogen or chlorine, R.sup.2 is hydrogen, alkyl, alkoxy, chlorine, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the formula O--[CH.sub.2 ].sub.x --C.sub.f H.sub.(2f+1-g) F.sub.g, where x=0 or 1, f=1-5, and g=1 to (2f+1), R.sup.3 is hydrogen, alkyl, alkoxy, fluorine, chlorine, cyano, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the above formula, R.sup.4 and R.sup.5 are hydrogen, alkyl, fluorine, chlorine, bromine, trifluoromethyl, cyano, alkoxy, or fluoroalkoxy of the above formula, including the physiologically active salts, are strong prolyl-4-hydroxylase inhibitors which do not cause steatosis.

    摘要翻译： 式I的新型异喹啉-3-甲酰胺：其中R 1是氢或氯，R 2是氢，烷基，烷氧基，氯，三氟甲基，羟基或任选被取代的苄氧基，或式O - [CH 2] x-CfH（2f + 1-g）Fg，其中x = 0或1，f = 1-5，g = 1至（2f + 1），R3为氢，烷基，烷氧基，氟，氯，氰基， 三氟甲基，羟基或任选取代的苄氧基，或上式的氟代烷氧基，R4和R5是上式的氢，烷基，氟，氯，溴，三氟甲基，氰基，烷氧基或氟代烷氧基，包括生理活性盐 是不引起脂肪变性的强脯氨酰-4-羟化酶抑制剂。