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Title:
NOVEL COMPOUND HAVING 3-HETEROARYLPYRIMIDIN-4-(3H)-ONE STRUCTURE AND PHARMACEUTICAL PREPARATION CONTAINING SAME
Document Type and Number:
WIPO Patent Application WO/2010/119700
Kind Code:
A1
Abstract:
Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPARγ activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R1 and R2 independently represent a C1-6 alkyl group; and each of R3 to R5 is absent or represents H, a halogen atom, OH, NO2, a halo-C1-6 alkyl group, a (substituted) C1-6 alkoxy group, a (substituted) C3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.]

Inventors:
MIURA TORU (JP)
ONOGI KAZUHIRO (JP)
SATO SEIICHI (JP)
TAGASHIRA JUNYA (JP)
WATANABE GEN (JP)
SEKIMOTO RYOHEI (JP)
ISHIDA RIE (JP)
AOKI HITOMI (JP)
OHGIYA TADAAKI (JP)
Application Number:
PCT/JP2010/002766
Publication Date:
October 21, 2010
Filing Date:
April 16, 2010
Export Citation:
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Assignee:
KOWA CO (JP)
MIURA TORU (JP)
ONOGI KAZUHIRO (JP)
SATO SEIICHI (JP)
TAGASHIRA JUNYA (JP)
WATANABE GEN (JP)
SEKIMOTO RYOHEI (JP)
ISHIDA RIE (JP)
AOKI HITOMI (JP)
OHGIYA TADAAKI (JP)
International Classes:
C07D401/14; A61K31/506; A61K31/53; A61P3/00; A61P3/04; A61P3/06; A61P3/10; A61P9/00; A61P9/10; A61P9/12; A61P13/12; A61P25/00; A61P27/02; A61P43/00; C07D403/14; C07D413/14; C07D417/14
Domestic Patent References:
WO2008062905A22008-05-29
WO2008084303A12008-07-17
WO2008096820A12008-08-14
WO2008096829A12008-08-14
Foreign References:
JPH04230370A1992-08-19
JPH05505609A1993-08-19
JPH06199811A1994-07-19
JPH06509349A1994-10-20
JPH06509349A1994-10-20
JPH04230370A1992-08-19
Other References:
NICOLAIE, E. ET AL.: "Synthesis and angiotensin II receptor antagonist activity of C-linked pyrimidine derivatives", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 30, no. 5, 1995, pages 365 - 75, XP000602152
AMER. J. HYPERTENSION, vol. 18, 2005, pages 720
CURRENT HYPERTENSION REPORT, vol. 10, 2008, pages 261
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FASEB J., vol. 20, no. 8, 2006, pages 1203
HYPERTENSION, vol. 43, 2004, pages 993
CIRCULATION, vol. 109, 2004, pages 2054
PROGRESS IN MEDICINE, vol. 5, 1985, pages 2157 - 2161
"Molecular Designs", vol. 7, 1990, HIROKAWA SHOTEN, article "Development of Drugs", pages: 163 - 198
"Protective Groups in Organic Synthesis", JOHN WILEY & SONS, INC
JOURNAL OF MEDICINAL CHEMISTRY, vol. 38, no. 24, 1995, pages 4806
SYNTHESIS, 2004, pages 2825
See also references of EP 2420501A4
Attorney, Agent or Firm:
SAEKI, NORIO (JP)
Norio Saeki (JP)
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