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Title:
ANTIPICORNAVIRAL COMPOUNDS AND COMPOSITIONS, THEIR PHARMACEUTICAL USES, AND MATERIALS FOR THEIR SYNTHESIS
Document Type and Number:
WIPO Patent Application WO2001096297
Kind Code:
A3
Abstract:
Compounds of the formula (I), where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

Inventors:
JOHNSON THEODORE O JR
CHU SHAO SONG
HUA YE
LUU HIEP THE
REICH SIEGFRIED HEINZ
SKALITZKY DONALD JAMES
YANG YI
CHAN FORA P
EASTMAN BRIAN WALTER
HENDRICKSON THOMAS F
Application Number:
PCT/US2001/019139
Publication Date:
July 10, 2003
Filing Date:
June 13, 2001
Export Citation:
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Assignee:
AGOURON PHARMA (US)
International Classes:
A61K31/216; A61K31/235; A61K31/381; A61K31/4015; A61K31/404; A61K31/415; A61K31/4184; A61K31/4192; A61K31/427; A61K31/4439; A61K31/47; A61K31/498; A61P31/14; A61P43/00; C07C233/85; C07C237/22; C07C237/36; C07C275/16; C07D207/26; C07D209/42; C07D215/48; C07D231/14; C07D241/44; C07D249/06; C07D333/70; C07D401/12; C07D403/12; C07D405/12; C07D417/12; (IPC1-7): C07D207/26; C07D401/12; C07D403/12; C07D405/12; C07D417/12; C07D333/70; C07D241/44; C07D215/48; C07C237/16; C07D249/06; C07D231/14; C07D209/42; A61K31/40
Domestic Patent References:
WO1999057135A11999-11-11
WO1999031122A11999-06-24
WO1998043950A11998-10-08
WO1997043305A11997-11-20
WO2001040189A12001-06-07
WO2001010894A22001-02-15
Other References:
DRAGOVICH P S ET AL: "Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 2. Peptide structure-activity studies", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 41, no. 15, 16 July 1998 (1998-07-16), pages 2819 - 2834, XP002100727, ISSN: 0022-2623
DRAGOVICH P S ET AL: "Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 3. Structure-activity studies of ketomethylene-containing peptidomimetics", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 42, no. 7, 8 April 1999 (1999-04-08), pages 1203 - 1212, XP002153927, ISSN: 0022-2623
DRAGOVICH P S ET AL: "STRUCTURE-BASED DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF IRREVERSIBLE HUMAN RHINOVIRUS 3C PROTEASE INHIBITORS. 4. INCORPORATION OF P1 LACTAM MOIEITES AS L-GLUTAMINE REPLACEMENTS", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 42, no. 7, 8 April 1999 (1999-04-08), pages 1213 - 1224, XP002153221, ISSN: 0022-2623
MATTHEWS, D. A. ET AL: "Structure-assisted design of mechanism-based irreversible inhibitors of human rhinovirus 3C protease with potent antiviral activity against multiple rhinovirus serotypes", PROC. NATL. ACAD. SCI. U. S. A. (1999), 96(20), 11000-11007, 1999, XP002187093
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; VAN DER BENT, ARIE ET AL: "Synthesis and biological evaluation of lorglumide-like hybrid cholecystokinin-A receptor antagonists", XP002187094, retrieved from STN Database accession no. 121:34962 CA
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