首页> 外国专利> PROCESS FOR PRODUCING SPIRO SQUARE BRACKETS OPEN IMIDAZOLIDINE-4,5'(6H)-QUINOLINE SQUARE BRACKETS CLOSED-2,5-DIONE DERIVATIVES

PROCESS FOR PRODUCING SPIRO SQUARE BRACKETS OPEN IMIDAZOLIDINE-4,5'(6H)-QUINOLINE SQUARE BRACKETS CLOSED-2,5-DIONE DERIVATIVES

机译:制备螺旋方括号的过程开咪唑-4,5'(6H)-喹啉方括号闭,-2,5-二酮衍生物

摘要

Spiro-heteroazolone compounds of the formula: CHEM or a pharmaceutically acceptable salt thereof, wherein A is methylene, hydroxymethylene, or methine; Y is methylene, alkylmethylene, methine or alkylmethine, wherein alkyl in each instance has 1-4 carbon atoms; with the proviso that when A is methine, Y is methine or alkylmethine; Z is oxygen, sulfur, or nitrogen substituted by hydrogen; O is nitrogen or nitrogen-N-oxide; and X is in the 3 min -position and is hydrogen, halo, alkyl, alkoxy having 1-4 carbon atoms, alkylthio, alkylsulfinyl, alkylsulfonyl, phenoxy, phenylthio, or nitro; or X is in the 2 min -position and is hydrogen, alkyl, or alkoxy having 1-4 carbon atoms; wherein alkyl in each instance has 1-4 carbon atoms; with the proviso that when O is nitrogen-N-oxide, X is not alkylthio, alkylsulfinyl or phenylthio; and with the further proviso that when O is nitrogen and X is hydrogen and Z is nitrogen subsitituted by hydrogen, at least one of A and Y is always other than methylene. The compounds have utility as aldose reductase inhibitors and as therapeutic agents for the treatment of complications arising from diabetes.
机译:式:的螺-杂唑啉酮化合物或其药学上可接受的盐,其中A为亚甲基,羟甲基或次甲基; Y为亚甲基,亚烷基亚甲基,次甲基或烷基亚甲基,其中烷基在每种情况下均具有1-4个碳原子;前提是当A是次甲基时,Y是次甲基或烷基次甲基; Z是被氢取代的氧,硫或氮; O是氮或氮-N-氧化物; X在3分钟位置,是氢,卤素,烷基,具有1-4个碳原子的烷氧基,烷硫基,烷基亚磺酰基,烷基磺酰基,苯氧基,苯硫基或硝基; X为2分钟位置,为碳原子数1〜4的氢,烷基或烷氧基。其中烷基分别具有1-4个碳原子;前提是当O为氮-N-氧化物时,X不是烷硫基,烷基亚磺酰基或苯硫基;并且进一步的条件是,当O是氮并且X是氢并且Z是被氢取代的氮时,A和Y中的至少一个总是不是亚甲基。该化合物可用作醛糖还原酶抑制剂和用作治疗由糖尿病引起的并发症的治疗剂。

著录项

  • 公开/公告号HU198051B

    专利类型

  • 公开/公告日1989-07-28

    原文格式PDF

  • 申请/专利权人 PFIZER;

    申请/专利号HU19840004630

  • 发明设计人 LIPINSKI CHRISTOPHER A;

    申请日1984-10-30

  • 分类号C07D471/10;A61K31/395;

  • 国家 HU

  • 入库时间 2022-08-22 06:39:12

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