公开(公告)号：EP0719767B1

公开(公告)日：2000-05-03

申请号：EP94921848.1

申请日：1994-08-01

申请人： Senju Pharmaceutical Co., Ltd. ,  YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

发明人： HOSONO, Hiroshi 305, Furatto-Fiirudo ,  NISHIO, Toshiyuki ,  ISHIKAWA, Hiromichi 966, Gurandohaitsu-Uozaki ,  NAKAMURA, Yoshiyuki 105, Haitsu-Toro ,  MATSUI, Tetsuo 403, Etowaru-Kasuga 2-35-2, Kasuga

IPC分类号： C07D277/64 ,  A61K31/425

CPC分类号： C07D277/64

摘要： A novel succinamic acid compound represented by general formula (1) or a pharmaceutically acceptable salt thereof; a preventive and/or a remedy for complications of diabetes containing the compound or the salt as the active ingredient; an aldose reductase inhibitor containing the compound or the salt as the active ingredient; and a process for producing the compound or the salt. In said formula, R1 represents alkyl or lower alkenyl, and R2 represents carboxyl which may be esterified. The invention compound (1) and the salt have a potent aldose reductase inhibitor activity on mammals including humans and an excellent safety, and hence are useful as a remedy for therapeutic treatment of complications of diabetes, such as failure of corneal lesion union, cataract, neurosis, retinopathy and nephropathy, especially cataract and neurosis. The invention process can provide the invention compounds having such a usefulness efficiently.

公开(公告)号：EP0719767A1

公开(公告)日：1996-07-03

申请号：EP94921848.1

申请日：1994-08-01

申请人： Senju Pharmaceutical Co., Ltd. ,  THE GREEN CROSS CORPORATION

发明人： HOSONO, Hiroshi 305, Furatto-Fiirudo ,  NISHIO, Toshiyuki ,  ISHIKAWA, Hiromichi 966, Gurandohaitsu-Uozaki ,  NAKAMURA, Yoshiyuki 105, Haitsu-Toro ,  MATSUI, Tetsuo 403, Etowaru-Kasuga 2-35-2, Kasuga

IPC分类号： C07D277/64 ,  A61K31/425

CPC分类号： C07D277/64

摘要： Provision of a succinamic acid compound of the formula (1)

wherein R 1 is an alkyl or a lower alkenyl and R 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 inhibitory activity 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.

摘要翻译： 提供式（1）的琥珀酰胺酸化合物，其中R 1是烷基或低级烯基，R 2是任选酯化的羧基，其药学上可接受的盐，用于预防和/ /或治疗糖尿病并发症，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备方法。 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强烈的醛糖还原酶抑制活性，并表现出优异的安全性。 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。 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。