发明名称 HETEROCYCLIC COMPOUND, ITS INTERMEDIATE AND ELASTASE INHIBITOR
摘要 PROBLEM TO BE SOLVED: To obtain a new heterocyclic compound having excellent human neutrophil elastase inhibiting action and useful for the prevention, treatment, or the like, of acute pulmonary diseases. SOLUTION: The objective compound is expressed by formula I [the mark *represents an asymmetric carbon atom; A and B are each a lower alkylene; D is a monocylic or bicyclic heterocyclic group of formula II (G is present or absent; D1 is methylene or ethylene; the dotted line is a ring-constitution element); R1 and R2 are each a lower alkyl; R3 and R4 are each H, OH or together form an oxo group; R5 is a group of formula III (X1 and X2 are each a halogen; Y1 is H, a halogen, a lower alkoxycarbonyl, or the like; (n) is 0-2; (m) is 0-5)], e.g. S-[2-(3-carboxymethyl-2-oxo-1-imidazolidinyl)acetyl]-valyl- N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)-L-prolinamide. The compound of formula I can be produced e.g. by reacting a compound of formula IV with a compound of formula V (W is a group bondable with amino group) in the presence of a base such as triethylamine.
申请公布号 JP2000256396(A) 申请公布日期 2000.09.19
申请号 JP19990056052 申请日期 1999.03.03
申请人 DAINIPPON PHARMACEUT CO LTD 发明人 SATO FUMINORI;INOUE YASUNAO;MENTANI TOMOYOSHI;SHIRATAKE RYOTARO;HONDA SEIJI;KOMIYA MASANOBU;TAKEMURA TADASHI
分类号 A61K38/00;A61K31/00;A61K31/495;A61K31/506;A61P11/00;A61P11/06;A61P29/00;A61P43/00;C07D403/12;C07D413/14;C07K5/02;C07K5/083;C07K5/097;C07K5/103;C07K5/117;(IPC1-7):C07K5/117 主分类号 A61K38/00
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