发明名称 1'-AMINO-2-[(BENZOTHIAZOLYL)METHYL]SPIRO [ISOQUINOLINE-4(1H),3'-PYRROLIDINE]-1,2',3,5'(2H)-TETRONES AND ANALOGS THEREOF USEFUL AS ALDOSE REDUCTASE INHIBITORS
摘要 The invention concerns compounds of formula (I) wherein: R<1>, R<2> and R<3> are independently hydrogen, alkyl containing 1 to 6 carbon atoms, halogen, lower alkoxy containing 1 to 6 carbon atoms, trifluoromethyl or nitro; R<6> is (a), (b) or (c) wherein R<4> and R<5> are independently hydrogen, alkyl containing 1 to 6 carbon atoms, aryl, aryl (lower alkyl) wherein aryl contains 6 to 10 carbons atoms and lower alkyl contains 1 to 6 carbon atoms, alkanoyl of 2 to 5 carbon atoms or carboalkoxy, or R<4> and R<5> are joined to form alicyclic or heterocyclic rings selected from the group consisting of (d) wherein n = 1-10; (e) wherein X = O, S, SO, SO2; (f) wherein X = O, S; and (g) wherein R<9> = H, lower alkyl containing 1 to 6 carbon atoms, aryl or aryl (lower alkyl) wherein aryl contains 6 to 10 carbon atoms and lower alkyl contains 1 to 6 carbon atoms, and R<7> and R<8> are independently alkylsulfoxy, arylsulfoxy, alkylsulfonyl, arylsulfonyl wherein aryl contains 6 to 10 carbon atoms and alkyl contains 1 to 6 carbon atoms or R<8> may also represent one of the values for R<5> above, and the pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
申请公布号 WO9311126(A1) 申请公布日期 1993.06.10
申请号 WO1992US10268 申请日期 1992.11.25
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 MALAMAS, MICHAEL, SOTIRIOS
分类号 A61K31/54;A61P3/08;A61P3/10;C07D471/10 主分类号 A61K31/54
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