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    • 10. 发明授权
    • Succinamic acid compound, production method thereof and use thereof
    • 琥珀酸化合物及其制备方法及用途
    • US5688818A
    • 1997-11-18
    • US617824
    • 1996-03-14
    • Hiroshi HosonoToshiyuki NishioHiromichi IshikawaYoshiyuki NakamuraTetsuo Matsui
    • Hiroshi HosonoToshiyuki NishioHiromichi IshikawaYoshiyuki NakamuraTetsuo Matsui
    • A61K31/425A61K31/428A61P3/08A61P3/10A61P13/02A61P15/00A61P25/00A61P27/02A61P27/12A61P43/00C07D277/64C07D277/68C07D277/62
    • C07D277/64
    • Provision of a succinamic acid compound of the formula (1) ##STR1## wherein R.sup.1 is an alkyl or a lower alkenyl and R.sup.2 is an optionally esterified carboxyl, a pharmaceutically acceptable salt thereof, an agent for the prophylaxis and/or treatment of the complications of diabetes, comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, an aldose reductase inhibitor comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, and a method for producing the succinamic acid compound or a pharmaceutically acceptable salt thereof. The novel succinamic acid compounds of the formula (1) of the present invention and pharmaceutically acceptable salts thereof have a strong aldose reductase activity-inhibitory in mammals such as human, and show superior safety. Hence, they are useful as pharmaceutical agents for the treatment of the complications of diabetes such as faulty union of corneal injury, cataract, neurosis, retinopathy and nephropathy, in particular, cataract and neurosis. According to the production method of the present invention, efficient production of such useful compounds of the present invention can be provided.
    • PCT No.PCT / JP94 / 01266 Sec。 371日期:1996年3月14日 102(e)1996年3月14日PCT PCT 1994年8月1日PCT公布。 WO95 / 07898 PCT出版物 日期1995年3月23日提供式(1)的琥珀酰胺酸化合物其中R1是烷基或低级烯基,R2是任选酯化的羧基,其药学上可接受的盐, 预防和/或治疗糖尿病的并发症,其包含作为活性成分的琥珀酰胺酸化合物或其药学上可接受的盐,醛糖还原酶抑制剂,其包含作为活性成分的琥珀酰胺酸化合物或其药学上可接受的盐 ,以及琥珀酰胺酸化合物或其药学上可接受的盐的制造方法。 本发明式(1)的新型琥珀酰胺酸化合物及其药学上可接受的盐在哺乳动物如人中具有很强的醛糖还原酶活性,并且具有优异的安全性。 因此,它们可用作治疗糖尿病并发症的药剂,例如角膜损伤,白内障,神经症,视网膜病变和肾病,尤其是白内障和神经症的联合失调。 根据本发明的制造方法,能够有效地制造本发明的有用化合物。