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Title:
新しいチオフェングリコシド誘導体、その製造方法、該化合物を含む医薬及びその使用
Document Type and Number:
Japanese Patent JP4511927
Kind Code:
B2
Abstract:
Thienyl-glycoside compounds (I) are new. Thienyl-glycoside compounds of formula (I) and their salts are new. [Image] R 1, R 2H, halo, OH, NO 2, CN, COOH, COT', COOT', CONH 2, CONHT', CONT' 2, T', 2-6C alkenyl, 2-6C alkynyl, OT', -T'-OH, -T'-OT', Ph,CH 2Ph, (1-4C) alkylcarbonyl (optionally substituted (os) by one or more F), SO 2NH 2, SO 2NHT, SO 2NT 2, ST, S(CH 2) pPh', SOT, SO(CH 2) pPh', SO 2T, SO 2(CH 2) pPh', NH 2, NHT, NT 2, 1-7C acylamino, Ph'' or -O(CH 2) pPh''; T : 1-6C alkyl; T' : 1-6C alkyl (os by one or more F); p : 0-6; Ph' : phenyl (os by 1 or 2 of F, Cl, Br, OH, CF 3, NO 2, CN, OCF 3, OT, T or NH 2); Ph'' : phenyl (os by 1-3 of halo, OH, CF 3, NO 2, CN, OCF 3, OT, T, NH 2, NHT, NT 2, SO 2Me, COOH, COOT or CONH 2); A : direct bond or 1-15C alkanediyl (optionally having one or more C-atom(s) replaced by O, CO, CH=CH, CC, S, CH(OH), CHF, SO, SO 2, N(T), N(-T-Ph) or NH); n : 0-4; Cyc 1>3-7 membered saturated, partially unsaturated or unsaturated ring, optionally having one C-atom replaced by O or S; R 3 - R 5H, halo, OH, NO 2, CN, COOH, COOT', (1-4C) alkylcarbonyl (os by one or more F), CONH 2, CONHT', CONT' 2, T', 2-6C alkenyl, 2-6C alkynyl, 1-12C alkoxy (os by one or more F), -T'-OH, -T'-OT', Ph,CH 2Ph, SO 2NH 2, SO 2NHT, SO 2NT 2, ST, S(CH 2) pPh', SOT, SO(CH 2) pPh', SO 2T, SO 2(CH 2) pPh', NH 2, NHT, NT 2, 1-7C acylamino, Ph'', -(CH 2) pPh'' or -O(CH 2) pPh''; or R 3 + R 4group completing a 5-7 membered saturated, partially unsaturated or unsaturated ring (Cyc 2>), optionally having 1 or 2 C-atom(s) replaced by N, O or S and os by T, 2-5C alkenyl or 2-5C (all optionally having one CH 2 replaced by O) or by F, Cl, OH, CF 3, NO 2, CN, (1-4C) alkoxycarbonyl, CONH 2, (1-4C) alkylaminocarbonyl or OCF 3; and provided that when R 3 and R 4 form a ring, R 5 is H. ACTIVITY : Antidiabetic; nephrotropic; ophthalmological; neuroprotective; anorectic; cardiant; vasotropic; thrombolytic; anticoagulant; antiarteriosclerotic; antiinflammatory; immunosuppressive; anti-HIV; antiasthmatic; osteopathic; cytostatic; antipsoriatic; nootropic; neuroleptic; antibacterial. MECHANISM OF ACTION : Glucose transport regulator. In a glucose transport assay in rabbit renal cortex 'Burstensaum' membrane vesicles, 2-hydroxymethyl-6-(2-(2-(4-chlorophenyl)-ethyl)-thien-3-yloxy)-tetrahydropyran-3,4,5-triol (Ia) (in beta -D-gluco form) had IC 2 5 0.9 MicroM.

Inventors:
Heiner Grombic
Wenderin Flick
Hubert Hoyer
Werner Kramer
Halm Bloomer Hop
Oliver Plettenburg
Application Number:
JP2004520429A
Publication Date:
July 28, 2010
Filing Date:
June 27, 2003
Export Citation:
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Assignee:
Sanofi-Aventis Deutschland Gesellschaft Mitt Beschlenktel Haftung
International Classes:
C07H7/00; C07H17/00; A61K31/7042; A61K31/7048; A61P3/04; A61P3/10; A61P7/00; A61P7/02; A61P9/08; A61P9/10; A61P11/06; A61P13/12; A61P17/06; A61P19/10; A61P25/00; A61P25/18; A61P25/28; A61P27/02; A61P29/00; A61P31/00; A61P31/18; A61P35/00; A61P37/02
Foreign References:
WO2001016147A1
Other References:
H. G. FOUDA,DUG METABOLISM AND DISPOSITION,1997年,V25 N2,P140-148
FUENTES J,TETRAHEDRON : ASYMMETRY,NL,ELSEVIER SCIENCE PUBLISHERS,1998年 7月17日,V9 N14,P2517-2532
Attorney, Agent or Firm:
Chika Takagi
Junji Yuda
Shoji Miwa