发明授权
- 专利标题: Indolinone derivatives
- 专利标题(中): 吲哚啉酮衍生物
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申请号: US346115申请日: 1988-12-16
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公开(公告)号: US4960785A公开(公告)日: 1990-10-02
- 发明人: Harry R. Howard, Jr. , Reinhard Sarges
- 申请人: Harry R. Howard, Jr. , Reinhard Sarges
- 申请人地址: NY New York
- 专利权人: Pfizer Inc.
- 当前专利权人: Pfizer Inc.
- 当前专利权人地址: NY New York
- 主分类号: C07D209/34
- IPC分类号: C07D209/34 ; C07D209/96 ; C07D491/056
摘要:
A series of novel 3-mono(substituted methyl)- and 3,3-di(substituted methyl)-2-oxo-indoline-1-alkanoic acid compounds have been prepared, including their lower alkyl esters and unsubstituted amide derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Said oxindole-1-alkanoic acid compounds are of the formulae: ##STR1## wherein X is hydrogen and X.sup.1 is hydrogen, hydroxy, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; or X and X.sup.1, when taken separately, are each chlorine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and when taken together are --OCH.sub.2 (CH.sub.2).sub.n O-- at the 4,5-, 5,6- or 6,7-positions of the molecule wherein n is zero or one; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or phenylalkyl having up to three carbon atoms in the alkyl moiety wherein said phenylalkyl is optionally substituted with up to two chlorine substituents on the phenyl ring; R.sub.3 is naphthylmethyl, furfuryl, thenyl, benzothienylmethyl, benzoxazolylmethyl, benzothiazolylmethyl or phenylalkyl having up to three carbon atoms in the alkyl moiety wherein said phenylalkyl is optionally substituted with up to two identical or non-identical substituents on the phenyl ring, said identical substituents being fluorine, chlorine, bromine, trifluoromethyl, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy and said non-identical substituents being chlorine, methyl, methoxy or trifluoromethyl; and Y is hydrogen, fluorine, chlorine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 -alkoxy.
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