发明名称 TETRAHYDROPYRROLO(1,2-A)PYRAZINE-4-SPIRO-3'-PYRROLIDINE DERIVATIVE AND DIABETIC COMPLICATION THERAPEUTIC AGENT WITH THE SAME AS ACTIVE INGREDIENT
摘要 <p>PURPOSE:To provide a new, low toxic compound having aldose reductase- inhibitory activity, useful for therapeutic agents for diabetic complications such as cataract, nerve disorder and nephropathy. CONSTITUTION:The objective compound of formula I (R<1> and R<2> are each H, halogen, trifluoromethyl, lower alkyl, lower alkoxy or nitro; R<3> is H, halogen or lower alkyl), e.g. 2-(4-bromo-2-fluorobenzyl)-[1,2,3,4-tetrahydropyrrolo[1,2- a]pyrazine-4-spiro-3'-pyrrolidine]1,2',3,5'-tetraone. The compound of the formula I can be obtained by reaction of a compound of formula II (R<4> is protecting group for carboxyl; X is halogen) with a compound of formula III in a solvent like THF in the presence of a base such as triethylamine.</p>
申请公布号 JPH05186472(A) 申请公布日期 1993.07.27
申请号 JP19920193074 申请日期 1992.06.25
申请人 DAINIPPON PHARMACEUT CO LTD 发明人 NEGORO TOSHIYUKI;MURATA MAKOTO;UEDA SHOZO;FUJITANI BUICHI;ONO YOSHIYUKI
分类号 A61K31/495;A61P3/08;A61P3/10;C07D207/416;C07D487/20;C12N9/99 主分类号 A61K31/495
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