Title:
CELLULAR ACCUMULATION OF PHOSPHONATE ANALOGS OF HIV PROTEASE INHIBITOR COMPOUNDS AND THE COMPOUNDS AS SUCH
Document Type and Number:
WIPO Patent Application WO2003090690
Kind Code:
A3
Abstract:
Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.
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Inventors:
ARIMILLI MURTY N (US)
BECKER MARK M (US)
BRYANT CLIFFORD (US)
CHEN JAMES M (US)
CHEN XIAOWU
BECKER MARK M (US)
BRYANT CLIFFORD (US)
CHEN JAMES M (US)
CHEN XIAOWU
Application Number:
PCT/US2003/012901
Publication Date:
June 24, 2004
Filing Date:
April 25, 2003
Export Citation:
Assignee:
GILEAD SCIENCES INC (US)
ARIMILLI MURTY N (US)
BECKER MARK M (US)
BRYANT CLIFFORD (US)
CHEN JAMES M (US)
CHEN XIAOWU
ARIMILLI MURTY N (US)
BECKER MARK M (US)
BRYANT CLIFFORD (US)
CHEN JAMES M (US)
CHEN XIAOWU
International Classes:
C12N9/99; A61K31/4155; A61K31/66; A61K31/665; A61K31/675; A61P31/18; A61P43/00; C07D213/75; C07D213/85; C07D231/12; C07D231/20; C07D233/42; C07D239/48; C07D239/80; C07D243/04; C07D265/18; C07D307/68; C07D401/06; C07D403/06; C07D471/14; C07D491/04; C07F9/02; C07F9/38; C07F9/40; C07F9/44; C07F9/58; C07F9/62; C07F9/645; C07F9/6506; C07F9/6509; C07F9/6512; C07F9/653; C07F9/6533; C07F9/655; C07F9/6558; C07F9/6561; C07F9/6584; C12N9/16; C12Q1/18; C12Q1/37; C12Q1/44; C12Q1/70; G01N33/04; G01N33/50; C07F; (IPC1-7): C07F9/40; C07F9/02; C07F9/38
Domestic Patent References:
| WO2000004033A1 | 2000-01-27 | |||
| WO1998011906A1 | 1998-03-26 | |||
| WO2002014344A2 | 2002-02-21 | |||
| WO2002006292A1 | 2002-01-24 | |||
| WO1996014314A2 | 1996-05-17 |
Foreign References:
| US5750493A | 1998-05-12 | |||
| EP0441192A2 | 1991-08-14 | |||
| US5914332A | 1999-06-22 | |||
| US5670497A | 1997-09-23 | |||
| US20010031773A1 | 2001-10-18 |
Other References:
MENENDEZ-ARIAS L: "Targeting HIV: antiretroviral therapy and development of drug resistance", TRENDS IN PHARMACOLOGICAL SCIENCES, ELSEVIER, AMSTERDAM, NL, vol. 23, no. 8, 1 August 2002 (2002-08-01), pages 381 - 388, XP004386181, ISSN: 0165-6147
ABDEL-MEGUID S S ET AL: "Inhibition of human immunodeficiency virus-1 protease by a C2-symmetric phosphinate. Synthesis and crystallographic analysis", BIOCHEMISTRY 1993 UNITED STATES, vol. 32, no. 31, 1993, pages 7972 - 7980, XP002257745, ISSN: 0006-2960
CLERCQ DE E: "NEW DEVELOPMENTS IN ANTI-HIV CHEMOTHERAPY", CURRENT MEDICINAL CHEMISTRY, BENTHAM SCIENCE PUBLISHERS BV, BE, vol. 8, no. 13, November 2001 (2001-11-01), pages 1543 - 1572, XP009012547, ISSN: 0929-8673
DVORAKOVA, HANA ET AL: "Synthesis of 2'-Aminomethyl Derivatives of 9-(2- (Phosphonomethoxy)ethyl) Nucleotide Analogs as Potential Antiviral Agents", JOURNAL OF MEDICINAL CHEMISTRY , 39(17), 3263-3268 CODEN: JMCMAR; ISSN: 0022-2623, 1996, XP002273095
ABDEL-MEGUID S S ET AL: "Inhibition of human immunodeficiency virus-1 protease by a C2-symmetric phosphinate. Synthesis and crystallographic analysis", BIOCHEMISTRY 1993 UNITED STATES, vol. 32, no. 31, 1993, pages 7972 - 7980, XP002257745, ISSN: 0006-2960
CLERCQ DE E: "NEW DEVELOPMENTS IN ANTI-HIV CHEMOTHERAPY", CURRENT MEDICINAL CHEMISTRY, BENTHAM SCIENCE PUBLISHERS BV, BE, vol. 8, no. 13, November 2001 (2001-11-01), pages 1543 - 1572, XP009012547, ISSN: 0929-8673
DVORAKOVA, HANA ET AL: "Synthesis of 2'-Aminomethyl Derivatives of 9-(2- (Phosphonomethoxy)ethyl) Nucleotide Analogs as Potential Antiviral Agents", JOURNAL OF MEDICINAL CHEMISTRY , 39(17), 3263-3268 CODEN: JMCMAR; ISSN: 0022-2623, 1996, XP002273095
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