Title:
METHOD AND COMPOSITIONS FOR IDENTIFYING ANTI-HIV THERAPEUTIC COMPOUNDS
Document Type and Number:
WIPO Patent Application WO2004096818
Kind Code:
A3
Abstract:
The invention relates to methods and compositions for identifying compounds having therapeutic activity against human immunodeficiency virus (HIV).
Inventors:
BIRKUS GABRIEL (US)
CHEN JAMES M (US)
CHEN XIAOWU (US)
CIHLAR TOMAS (US)
EISENBERG EUGENE J (US)
HATADA MARCOS (US)
HE GONG-XIN (US)
KIM CHOUNG U (US)
LEE WILLIAM A (US)
MCDERMOTT MARTIN J (US)
SWAMINATHAN SUNDARAMOORTHI (US)
CHEN JAMES M (US)
CHEN XIAOWU (US)
CIHLAR TOMAS (US)
EISENBERG EUGENE J (US)
HATADA MARCOS (US)
HE GONG-XIN (US)
KIM CHOUNG U (US)
LEE WILLIAM A (US)
MCDERMOTT MARTIN J (US)
SWAMINATHAN SUNDARAMOORTHI (US)
Application Number:
PCT/EP2003/012423
Publication Date:
April 07, 2005
Filing Date:
November 06, 2003
Export Citation:
Assignee:
GILEAD SCIENCES INC (US)
BIRKUS GABRIEL (US)
CHEN JAMES M (US)
CHEN XIAOWU (US)
CIHLAR TOMAS (US)
EISENBERG EUGENE J (US)
HATADA MARCOS (US)
HE GONG-XIN (US)
KIM CHOUNG U (US)
LEE WILLIAM A (US)
MCDERMOTT MARTIN J (US)
SWAMINATHAN SUNDARAMOORTHI (US)
BIRKUS GABRIEL (US)
CHEN JAMES M (US)
CHEN XIAOWU (US)
CIHLAR TOMAS (US)
EISENBERG EUGENE J (US)
HATADA MARCOS (US)
HE GONG-XIN (US)
KIM CHOUNG U (US)
LEE WILLIAM A (US)
MCDERMOTT MARTIN J (US)
SWAMINATHAN SUNDARAMOORTHI (US)
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; C07F9/6561; G01N33/04
Domestic Patent References:
| WO2001039724A2 | 2001-06-07 | |||
| WO2001096354A1 | 2001-12-20 | |||
| WO2002008241A2 | 2002-01-31 | |||
| WO2002103008A2 | 2002-12-27 |
Foreign References:
| US20040121316A1 | 2004-06-24 |
Other References:
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HAKIMELAHI G H ET AL: "DESIGN, SYNTHESIS, AND STRUCTURE-ACTIVITY RELATIONSHIP OF NOVEL DINUCLEOTIDE ANALOGS AS AGENTS AGAINST HERPES AND HUMAN IMMUNODEFICIENCY VIRUSES", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 38, no. 23, 1995, pages 4648 - 4659, XP001145914, ISSN: 0022-2623
KOFOED T ET AL: "REGIOISOMERS OF 2',3'-DIDEOXYNUCLEOSIDES RELATED TO 2-(PHOSPHONYLMETHOXY)ETHYL NUCLEOSIDES", BULLETIN DE LA SOCIETE CHIMIQUE DE FRANCE, SOCIETE FRANCAISE DE CHIMIE. PARIS, FR, vol. 134, 1997, pages 59 - 65, XP009004947, ISSN: 0037-8968
KRAUS J-L: "NEW PHOSPHONATE ANALOGUES OF 3'-THIA-2',3'-DIDEOXYCYTIDINE (BCH-189) SYNTHESIS AND ANTI-HIV EVALUATION", NUCLEOSIDES & NUCLEOTIDES, DEKKER, NEW YORK,NY,, US, vol. 12, no. 2, 1993, pages 157 - 162, XP009004946, ISSN: 0732-8311
CHARVET ET AL: "Inhibition of Human Immunodefiency Virus Type 1 Replication by Phosphonoformate- and Phosphonoacetate- 2',3'-Dideoxy-3'-thiacytidine Conjugates", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 14, no. 37, 1994, pages 2216 - 2223, XP002072425, ISSN: 0022-2623
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
BALLATORE, C. ET AL.: "Synthesis and Evaluation of Novel Amidate Prodrugs of PMEA and PMPA", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 11, no. 8, 23 April 2001 (2001-04-23), pages 1053 - 1056, XP001180825
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
GORIN B I ET AL: "A Novel Esterification Procedure Applied to Synthesis of Biologically Active Esters of Foscarnet", TETRAHEDRON LETTERS, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 38, no. 16, 21 April 1997 (1997-04-21), pages 2791 - 2794, XP004058495, ISSN: 0040-4039
DATABASE MEDLINE [online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; May 2002 (2002-05-01), POKROVSKII A G ET AL: "Comparative analysis of HIV-1 resistance to AZT and AZT H-phosphonate in a cell culture.", XP002296489, Database accession no. NLM12134511
DE CLERCQ E: "Chemotherapy of human immunodeficiency virus (HIV) infection: anti-HIV agents targeted at early stages in the virus replicative cycle", BIOMEDICINE AND PHARMACOTHERAPY, vol. 50, no. 5, 1996, pages 207 - 215, XP002296486, ISSN: 0753-3322
SAUBER K ET AL: "A new esterase for the cleavage of pivalic acid-containing prodrug esters of cephalosporins.", ENZYME AND MICROBIAL TECHNOLOGY. JUL 1996, vol. 19, no. 1, July 1996 (1996-07-01), pages 15 - 19, XP002296487, ISSN: 0141-0229
MENDES EDUARDA ET AL: "Synthesis, stability and in vitro dermal evaluation of aminocarbonyloxymethyl esters as prodrugs of carboxylic acid agents.", BIOORGANIC & MEDICINAL CHEMISTRY. MAR 2002, vol. 10, no. 3, March 2002 (2002-03-01), pages 809 - 816, XP002296488, ISSN: 0968-0896
HAKIMELAHI G H ET AL: "DESIGN, SYNTHESIS, AND STRUCTURE-ACTIVITY RELATIONSHIP OF NOVEL DINUCLEOTIDE ANALOGS AS AGENTS AGAINST HERPES AND HUMAN IMMUNODEFICIENCY VIRUSES", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 38, no. 23, 1995, pages 4648 - 4659, XP001145914, ISSN: 0022-2623
KOFOED T ET AL: "REGIOISOMERS OF 2',3'-DIDEOXYNUCLEOSIDES RELATED TO 2-(PHOSPHONYLMETHOXY)ETHYL NUCLEOSIDES", BULLETIN DE LA SOCIETE CHIMIQUE DE FRANCE, SOCIETE FRANCAISE DE CHIMIE. PARIS, FR, vol. 134, 1997, pages 59 - 65, XP009004947, ISSN: 0037-8968
KRAUS J-L: "NEW PHOSPHONATE ANALOGUES OF 3'-THIA-2',3'-DIDEOXYCYTIDINE (BCH-189) SYNTHESIS AND ANTI-HIV EVALUATION", NUCLEOSIDES & NUCLEOTIDES, DEKKER, NEW YORK,NY,, US, vol. 12, no. 2, 1993, pages 157 - 162, XP009004946, ISSN: 0732-8311
CHARVET ET AL: "Inhibition of Human Immunodefiency Virus Type 1 Replication by Phosphonoformate- and Phosphonoacetate- 2',3'-Dideoxy-3'-thiacytidine Conjugates", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 14, no. 37, 1994, pages 2216 - 2223, XP002072425, ISSN: 0022-2623
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
BALLATORE, C. ET AL.: "Synthesis and Evaluation of Novel Amidate Prodrugs of PMEA and PMPA", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 11, no. 8, 23 April 2001 (2001-04-23), pages 1053 - 1056, XP001180825
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
GORIN B I ET AL: "A Novel Esterification Procedure Applied to Synthesis of Biologically Active Esters of Foscarnet", TETRAHEDRON LETTERS, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 38, no. 16, 21 April 1997 (1997-04-21), pages 2791 - 2794, XP004058495, ISSN: 0040-4039
DATABASE MEDLINE [online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; May 2002 (2002-05-01), POKROVSKII A G ET AL: "Comparative analysis of HIV-1 resistance to AZT and AZT H-phosphonate in a cell culture.", XP002296489, Database accession no. NLM12134511
DE CLERCQ E: "Chemotherapy of human immunodeficiency virus (HIV) infection: anti-HIV agents targeted at early stages in the virus replicative cycle", BIOMEDICINE AND PHARMACOTHERAPY, vol. 50, no. 5, 1996, pages 207 - 215, XP002296486, ISSN: 0753-3322
SAUBER K ET AL: "A new esterase for the cleavage of pivalic acid-containing prodrug esters of cephalosporins.", ENZYME AND MICROBIAL TECHNOLOGY. JUL 1996, vol. 19, no. 1, July 1996 (1996-07-01), pages 15 - 19, XP002296487, ISSN: 0141-0229
MENDES EDUARDA ET AL: "Synthesis, stability and in vitro dermal evaluation of aminocarbonyloxymethyl esters as prodrugs of carboxylic acid agents.", BIOORGANIC & MEDICINAL CHEMISTRY. MAR 2002, vol. 10, no. 3, March 2002 (2002-03-01), pages 809 - 816, XP002296488, ISSN: 0968-0896
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