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Title:
PYRAZOLE DERIVATIVES, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF
Document Type and Number:
WIPO Patent Application WO/2004/018491
Kind Code:
A1
Abstract:
A pyrazole derivative represented by the general formula (I) [wherein R1 is H, optionally substituted C1-6 alkyl, etc.; either of Q and T is the group of the formula (II) or the formula (III) and the other is optionally substituted C1-6 alkyl, etc.; R2 is H, halogeno, OH, optionally substituted C1-6 alkyl, etc.; X is a single bond, O, or S; Y is optionally substituted C1-6 alkylene, etc.; Z is -RB, -CORC, etc. (RB is optionally substituted C1-6 alkyl, etc.; and RC is optionally substituted C1-6 alkyl, etc.); R4 is H, optionally substituted C1-6 alkyl, etc.; and R3, R5, and R6 each is H, halogeno, etc.], a pharmacologically acceptable salt of the derivative, or a prodrug of either. They have excellent human SGLT1 inhibitory activity and are useful as a preventive or therapeutic agent for diseases attributable to hyperglycemia such as diabetes, impaired glucose tolerance, fasting blood sugar abnormality, complications of diabetes, and obesity and for diseases attributable to an increased blood galactose level such as galactosemia.

Inventors:
FUSHIMI NOBUHIKO (JP)
SHIMIZU KAZUO (JP)
YONEKUBO SHIGERU (JP)
TERANISHI HIROTAKA (JP)
TOMAE MASAKI (JP)
ISAJI MASAYUKI (JP)
Application Number:
PCT/JP2003/010551
Publication Date:
March 04, 2004
Filing Date:
August 21, 2003
Export Citation:
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Assignee:
KISSEI PHARMACEUTICAL (JP)
FUSHIMI NOBUHIKO (JP)
SHIMIZU KAZUO (JP)
YONEKUBO SHIGERU (JP)
TERANISHI HIROTAKA (JP)
TOMAE MASAKI (JP)
ISAJI MASAYUKI (JP)
International Classes:
A61K31/00; A61K31/10; A61K31/205; A61K31/37; A61K31/4166; A61K31/7056; A61K31/7072; A61K31/737; A61K38/18; A61K38/28; A61K45/00; A61K45/06; A61P3/04; A61P3/06; A61P3/10; A61P5/48; A61P7/10; A61P9/04; A61P9/10; A61P9/12; A61P19/06; A61P43/00; C07H17/02; (IPC1-7): C07H17/02; A61K31/7056; A61K31/10; A61K31/205; A61K31/37; A61K31/4166; A61K31/7072; A61K31/737; A61K38/00; A61K38/26; A61K38/27; A61K38/28; A61K45/00; A61P3/04; A61P3/06; A61P3/10; A61P5/48; A61P7/10; A61P9/04; A61P9/10; A61P9/12; A61P19/06; A61P43/00
Domestic Patent References:
WO2002036602A12002-05-10
WO2002053573A12002-07-11
Foreign References:
EP1213296A12002-06-12
Other References:
DYER JANE ET AL.: "Sugar analogues as potential inhibitors of the intestinal Na+/glucose co-transporter(SGLT1)", BIOCHEMICAL SOCIETY TRANSACTIONS, vol. 26, no. 2, 1998, pages S180, XP002973976
See also references of EP 1548024A4
J. DYER, AMERICAN JOURNAL OF PHYSIOLOGY, vol. 282, no. 2, February 2002 (2002-02-01), pages G241 - G248
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