公开(公告)号：US07514452B2

公开(公告)日：2009-04-07

申请号：US10503215

申请日：2003-01-30

申请人： Akihito Fujii ,  Toshiyuki Negoro ,  Chiaki Migihashi ,  Makoto Murata ,  Keiji Nakamura ,  Takashi Nukuda ,  Takafumi Matsumoto ,  Kiyomi Imano

发明人： Akihito Fujii ,  Toshiyuki Negoro ,  Chiaki Migihashi ,  Makoto Murata ,  Keiji Nakamura ,  Takashi Nukuda ,  Takafumi Matsumoto ,  Kiyomi Imano

IPC分类号： A61K31/47 ,  C07D307/02 ,  C07D405/00

CPC分类号： C07D405/12 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/443 ,  A61K31/4709 ,  A61K31/5377 ,  C07D307/68 ,  C07D405/04 ,  C07D407/12 ,  C07D407/14 ,  C07D409/04 ,  C07D409/12

摘要： The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula (I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof: wherein A is a group represented by Formula (a) or the like: (wherein either R4 or R5 represents cyano, nitro or the like, and the other represents a hydrogen atom or the like); either R1 or R2 represents a group: -D-(X)m-R6 or the like, and the other represents a group: -E-(Y)n-R7, hydrogen atom, aryl or the like; R3 is a hydrogen atom or the like; D and E independently represent aryl; X and Y independently represent O or the like; R6 and R7 independently represent alkyl, aryl, arylalkyl or the like; and m and n are independently 0 or 1, provided that the aryl is optionally substituted.

摘要翻译： 本发明提供由下述通式（I）表示的2-呋喃甲酰肼化合物及其前药，生理学上可接受的盐，水合物，溶剂合物：其中A为由式（a）等表示的基团：（其中R 4 或R 5表示氰基，硝基等，另一个表示氢原子等）。 R 1或R 2表示基团：-D-（X）m -R 6等，另一个表示基团：-E-（Y）n -R 7，氢原子，芳基等; R3是氢原子等; D和E独立地表示芳基; X和Y独立地表示O等; R6和R7独立地表示烷基，芳基，芳烷基等; 并且m和n独立地为0或1，条件是芳基任选被取代。

公开(公告)号：US20050171196A1

公开(公告)日：2005-08-04

申请号：US10503215

申请日：2003-01-30

申请人： Akihito Fujii ,  Toshiyuki Negoro ,  Chiaki Migihashi ,  Makoto Murata ,  Keiji Nakamura ,  Takashi Nukuda ,  Takafumi Matsumoto ,  Kiyomi Imano

发明人： Akihito Fujii ,  Toshiyuki Negoro ,  Chiaki Migihashi ,  Makoto Murata ,  Keiji Nakamura ,  Takashi Nukuda ,  Takafumi Matsumoto ,  Kiyomi Imano

IPC分类号： A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/443 ,  A61K31/4709 ,  A61K31/5377 ,  A61P1/00 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P43/00 ,  C07D307/68 ,  A61K31/34 ,  C07D307/02

CPC分类号： C07D405/12 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/443 ,  A61K31/4709 ,  A61K31/5377 ,  C07D307/68 ,  C07D405/04 ,  C07D407/12 ,  C07D407/14 ,  C07D409/04 ,  C07D409/12

摘要： The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula (I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof, methods for producing them and pharmaceutical compositions containing them: wherein A is a group represented by Formula (a) or the like: (wherein either R4 or R5 represents cyano, nitro or the like, and the other represents a hydrogen atom or the like); either R1 or R2 represents a group: -D-(X)m-R6 or the like, and the other represents a group: -E-(Y)n-R7, hydrogen atom, aryl or the like; R3 is a hydrogen atom or the like; D and E independently represent aryl; X and Y independently represent O or the like; R6 and R7 independently represent alkyl, aryl, arylalkyl or the like; and m and n are independently 0 or 1, provided that the aryl is optionally substituted. Such compounds exhibit a potent antagonistic activity on glucagon receptor and are of use as preventive and/or therapeutic agents for symptoms and diseases in which glucagon is involved.

摘要翻译： 本发明提供由下述通式（I）表示的2-呋喃甲酰肼化合物及其前体药物，生理学上可接受的盐，水合物，溶剂化物，其制备方法和含有它们的药物组合物：其中A是由式 a）等：（其中R 4或R 5或R 5表示氰基，硝基等，另一个表示氢原子等）; R 1或R 2 2代表基团：-D-（X）m R 6等，另一个表示一个基团： -E-（Y）nR 7，氢原子，芳基等; R 3是氢原子等; D和E独立地表示芳基; X和Y独立地表示O等; R 6和R 7独立地代表烷基，芳基，芳烷基等; 并且m和n独立地为0或1，条件是芳基任选被取代。 这些化合物对胰高血糖素受体表现出有效的拮抗活性，并且可用作涉及胰高血糖素的症状和疾病的预防和/或治疗剂。