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Patent Searching and Data


Title:
CARBOXYLIC ACID COMPOUND
Document Type and Number:
WIPO Patent Application WO/2010/123016
Kind Code:
A1
Abstract:
Disclosed is a compound having a GPR40 agonistic activity and useful for use in a pharmaceutical composition or useful as an insulin secretion promoter or a prophylactic or therapeutic agent for diabetes. Extensive studies have been made on compounds having a GPR40 agonistic activity. As a result, it is found that a compound (I) having a carboxylic acid bound to the second or third ring moiety through a methylene group or having a benzene ring bound to the second or third ring moiety through a group –O-methylene -NH-methylene, wherein the benzene ring has been substituted by a 6-membered monocyclic aromatic ring, or a pharmaceutically acceptable salt of the compound (I) has an excellent GPR40 agonistic activity. It is also found that the compound has an excellent insulin secretion-promoting activity and can prevent the increase in a blood glucose level after glucose tolerance aggressively.

Inventors:
NEGORO, Kenji (3-11 Nihonbashi-Honcho 2-chom, Chuo-ku Tokyo 11, 〒1038411, JP)
根来 賢二 (〒11 東京都中央区日本橋本町二丁目3番11号 アステラス製薬株式会社内 Tokyo, 〒1038411, JP)
OHNUKI, Kei (3-11 Nihonbashi-Honcho 2-chom, Chuo-ku Tokyo 11, 〒1038411, JP)
大貫 圭 (〒11 東京都中央区日本橋本町二丁目3番11号 アステラス製薬株式会社内 Tokyo, 〒1038411, JP)
YONETOKU, Yasuhiro (3-11 Nihonbashi-Honcho 2-chom, Chuo-ku Tokyo 11, 〒1038411, JP)
米徳 康博 (〒11 東京都中央区日本橋本町二丁目3番11号 アステラス製薬株式会社内 Tokyo, 〒1038411, JP)
Application Number:
JP2010/057034
Publication Date:
October 28, 2010
Filing Date:
April 21, 2010
Export Citation:
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Assignee:
Astellas Pharma Inc. (3-11, Nihonbashi-Honcho 2-chome Chuo-ku Tokyo, 11, 〒1038411, JP)
アステラス製薬株式会社 (〒11 東京都中央区日本橋本町二丁目3番11号 Tokyo, 〒1038411, JP)
NEGORO, Kenji (3-11 Nihonbashi-Honcho 2-chom, Chuo-ku Tokyo 11, 〒1038411, JP)
根来 賢二 (〒11 東京都中央区日本橋本町二丁目3番11号 アステラス製薬株式会社内 Tokyo, 〒1038411, JP)
OHNUKI, Kei (3-11 Nihonbashi-Honcho 2-chom, Chuo-ku Tokyo 11, 〒1038411, JP)
大貫 圭 (〒11 東京都中央区日本橋本町二丁目3番11号 アステラス製薬株式会社内 Tokyo, 〒1038411, JP)
YONETOKU, Yasuhiro (3-11 Nihonbashi-Honcho 2-chom, Chuo-ku Tokyo 11, 〒1038411, JP)
International Classes:
C07C43/225; A61K31/40; A61K31/4015; A61P3/10; C07C49/417; C07C69/76; C07C235/18; C07C303/36; C07D207/06; C07D207/27; C07D239/34; C07D305/06; C07D307/94; C07D309/06; C07D309/10; C07D317/22; C07D405/12; C07K14/705; C12N15/09
Domestic Patent References:
WO2005087710A12005-09-22
WO2004106276A12004-12-09
WO2008001931A22008-01-03
WO2009111056A12009-09-11
WO2004041266A12004-05-21
WO2005063729A12005-07-14
WO2005063725A12005-07-14
WO2005087710A12005-09-22
WO2004106276A12004-12-09
WO2008001931A22008-01-03
WO2008066097A12008-06-05
Foreign References:
JP2000212174A2000-08-02
JPH072848A1995-01-06
Other References:
See also references of EP 2423176A4
NATURE, vol. 422, 2003, pages 173 - 176
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 36, 2001, pages 31 - 42
PROG. MED., vol. 5, 1995, pages 2157 - 2161
"Drug Design", vol. 7, 1990, HIROKAWA PUBLISHING COMPANY, article "Pharmaceutical Research and Development", pages: 163 - 199
P. G. M. WUTS, T. W. GREENE: "Greene's Protective Groups in Organic Synthesis", 2006
M. HUDLICKY: "Reductions in Organic Chemistry", 1996, ACS
"Courses in Experimental Chemistry", vol. 19, 2005, MARUZEN
B. M. TROST, COMPREHENSIVE ORGANIC SYNTHESIS, vol. 7, 1991
M. HUDLICKY: "Oxidation in Organic Chemistry", 1990, ACS
"Courses in Experimental Chemistry", vol. 17, 2005, MARUZEN
A. R. KATRITZKY, R. J. K. TAYLOR: "Comprehensive Organic Functional Group Transformations II", vol. 2, 2005, ELSEVIER PERGAMON
"Courses in Experimental Chemistry", vol. 14, 2005, MARUZEN
S. R. SANDLER, W. KARO: "Organic Functional Group Preparations", vol. 1, 1991, ACADEMIC PRESS INC.
R. C. LAROCK: "Comprehensive Organic Transformations", 1999, VCH PUBLISHERS, INC.
T. J. DONOHOE: "Oxidation and Reduction in Organic Synthesis (Oxford Chemistry Primers 6", 2000, OXFORD SCIENCE PUBLICATIONS
SYNTHESIS, vol. 4, 2006, pages 629 - 632
NUCLEIC ACIDS RESEARCH, vol. 18, 1990, pages 5322
Attorney, Agent or Firm:
MORITA, Hiroshi et al. (3-11 Nihonbashi-Honcho 2-chom, Chuo-ku Tokyo 11, 〒1038411, JP)
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