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Title:
BISUBSTITUTED CARBOCYCLIC CYCLOPHILIN BINDING COMPOUNDS AND THEIRUS
Document Type and Number:
WIPO Patent Application WO2002044126
Kind Code:
A3
Abstract:
The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins. In the compounds of this invention, at least two carbo-or heterocyclic groups are attached to a central saturated, partially saturated, or aromatic 5-6 membered carbocyclic ring by a combination of straight or branched linker chains. The invention further relates to pharmaceutical compositions comprising one or more of the said compounds, and to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders, such as neurological disorders, hair loss disorders, ischemic disorders, and disorders caused by viral or protozoan infection.

Inventors:
HAMILTON GREGORY S (US)
BELYAKOV SERGEI (US)
VAAL MARK (US)
WEI LING (US)
WU YONG-QIAN (US)
STEINER JOSEPH P (US)
Application Number:
PCT/US2001/044449
Publication Date:
September 26, 2002
Filing Date:
November 28, 2001
Export Citation:
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Assignee:
GUILFORD PHARM INC (US)
HAMILTON GREGORY S (US)
BELYAKOV SERGEI (US)
VAAL MARK (US)
WEI LING (US)
WU YONG-QIAN (US)
STEINER JOSEPH P (US)
International Classes:
C07D249/12; A61K31/18; A61K31/255; A61K31/381; A61K31/41; A61K31/4245; A61K31/433; A61P9/04; A61P9/10; A61P25/02; A61P25/14; A61P25/16; A61P25/28; A61P27/02; A61P27/06; A61P31/08; A61P31/12; A61P31/18; A61P33/02; A61P33/10; A61P43/00; C07C233/65; C07C233/80; C07C235/24; C07C235/56; C07C275/30; C07C275/32; C07C275/36; C07C281/06; C07C309/73; C07C311/37; C07C311/48; C07C311/49; C07C311/51; C07C333/16; C07C335/16; C07C335/18; C07C335/20; C07C335/42; C07C337/06; C07C337/08; C07D207/16; C07D271/10; C07D271/113; C07D285/00; C07D285/12; C07D285/135; C07D333/20; C07D333/24; (IPC1-7): C07C233/65; C07C235/24; C07C235/56; C07C275/30; C07C275/36; C07C281/06; C07C309/73; C07C311/48; C07C311/49; C07C311/51; C07C335/20; C07C333/16; C07C335/18; C07C335/42; C07C337/06; C07C337/08; C07D207/16; C07D271/10; C07D285/12; C07D333/24; A61K31/18; A61K31/17; A61K31/167; A61P25/28
Domestic Patent References:
WO2001017953A12001-03-15
WO1998037882A11998-09-03
Foreign References:
GB921682A1963-03-20
GB1075166A1967-07-12
US3062813A1962-11-06
Other References:
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HITOSHI OINUMA, ET AL.: "Synthesis and biological evaluation of substituted benzenesulphonamides as novel potent membrane-bound phospholipase A2 inhibitors", JOURNAL OF MEDICINAL CHEMISTRY, vol. 34, no. 7, July 1991 (1991-07-01), American Chemical Society, Washington, DC, US, pages 2260 - 2267, XP000602078, ISSN: 0022-2623
M. REIFFEN, ET AL.: "Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a new class of compounds exerting antiischaemic properties", JOURNAL OF MEDICINAL CHEMISTRY, vol. 33, no. 5, May 1990 (1990-05-01), American Chemical Society, Washington, DC, US, pages 1496 - 1504, XP002205593, ISSN: 0022-2623
F.O. RITTER: "Studies in the di-acyl acyl hydrazine series. III. The oxidation of acetylhydrazobenzene", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 56, no. 4, April 1934 (1934-04-01), American Chemical Society, Washington, DC, US, pages 975 - 976, XP002205594, ISSN: 0002-7863
S.G. COHEN, ET AL.: "Preparation and kinetics of decomposition of a bicyclic azo compound. A novel reduction", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 83, no. 7, 5 July 1961 (1961-07-05), American Chemical Society, Washington, DC, US, pages 2895 - 2900, XP002205595, ISSN: 0002-7863
C. KING: "Cyclopolymerisation of aliphatic 1,2-diisocyanates", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 86, no. 3, 5 February 1964 (1964-02-05), American Chemical Society, Washington, DC, US, pages 437 - 440, XP002205596, ISSN: 0002-7863
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