WO1999067254A3 - Multi-drug resistant retroviral protease inhibitors and use thereof - Google Patents
Multi-drug resistant retroviral protease inhibitors and use thereof Download PDFInfo
- Publication number
- WO1999067254A3 WO1999067254A3 PCT/US1999/014120 US9914120W WO9967254A3 WO 1999067254 A3 WO1999067254 A3 WO 1999067254A3 US 9914120 W US9914120 W US 9914120W WO 9967254 A3 WO9967254 A3 WO 9967254A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- formula
- optionally substituted
- retroviral protease
- resistant retroviral
- multidrug
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/02—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving viable microorganisms
- C12Q1/025—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving viable microorganisms for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
- C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/005—Assays involving biological materials from specific organisms or of a specific nature from viruses
- G01N2333/08—RNA viruses
- G01N2333/15—Retroviridae, e.g. bovine leukaemia virus, feline leukaemia virus, feline leukaemia virus, human T-cell leukaemia-lymphoma virus
- G01N2333/155—Lentiviridae, e.g. visna-maedi virus, equine infectious virus, FIV, SIV
- G01N2333/16—HIV-1, HIV-2
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/81—Protease inhibitors
- G01N2333/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
- G01N2333/8142—Aspartate protease (E.C. 3.4.23) inhibitors, e.g. HIV protease inhibitors
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Immunology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- General Engineering & Computer Science (AREA)
- Physics & Mathematics (AREA)
- Analytical Chemistry (AREA)
- Biophysics (AREA)
- Virology (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Epidemiology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Toxicology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU48281/99A AU4828199A (en) | 1998-06-23 | 1999-06-23 | Multi-drug resistant retroviral protease inhibitors and associated methods |
PCT/US1999/014120 WO1999067254A2 (en) | 1998-06-23 | 1999-06-23 | Multi-drug resistant retroviral protease inhibitors and use thereof |
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US9039398P | 1998-06-23 | 1998-06-23 | |
US60/090,393 | 1998-06-23 | ||
PCT/US1999/014120 WO1999067254A2 (en) | 1998-06-23 | 1999-06-23 | Multi-drug resistant retroviral protease inhibitors and use thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
WO1999067254A2 WO1999067254A2 (en) | 1999-12-29 |
WO1999067254A3 true WO1999067254A3 (en) | 2000-02-10 |
Family
ID=36950030
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US1999/014120 WO1999067254A2 (en) | 1998-06-23 | 1999-06-23 | Multi-drug resistant retroviral protease inhibitors and use thereof |
Country Status (2)
Country | Link |
---|---|
AU (1) | AU4828199A (en) |
WO (1) | WO1999067254A2 (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8143421B2 (en) | 2002-03-12 | 2012-03-27 | Tibotec Pharmaceuticals Ltd. | Broadspectrum substituted benzimidazole sulfonamide HIV protease inhibitors |
Families Citing this family (40)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2336134B1 (en) | 1998-06-23 | 2016-08-31 | The United States of America, represented by the Secretary, Department of Health and Human Services | Fitness assay and methods for reducing resistance of HIV to therapy |
PL204924B1 (en) * | 1999-10-06 | 2010-02-26 | Tibotec Pharm Ltd | Hexahydrofuro'2,3−b!furan−3−yl−n− {3'(1,3−benzodioxol −5− ylsulfonyl) (isobutyl) amino! −1−benzyl−2−hydroxypropyl} carbamate as retroviral protease inhib |
HU229224B1 (en) | 2001-02-14 | 2013-09-30 | Tibotec Pharmaceuticals Ltd Little Island | 2-(substituted-amino)-benzothiazole sulfonamide compounds having broadspectrum hiv protease inhibitor activity and medicaments containing them |
EA007383B1 (en) * | 2001-04-09 | 2006-10-27 | Тиботек Фармасьютикалз Лтд. | Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide hiv protease inhibitors |
DK1387842T3 (en) * | 2001-05-11 | 2009-08-10 | Tibotec Pharm Ltd | Wide-spectrum 2-amino-benzoxazole sulfonamide HIV protease inhibitors |
EP1448567B1 (en) * | 2001-09-10 | 2009-12-30 | Tibotec Pharmaceuticals | Method for the preparation of hexahydro-furo 2,3-b furan-3-ol |
TWI286476B (en) * | 2001-12-12 | 2007-09-11 | Tibotec Pharm Ltd | Combination of cytochrome P450 dependent protease inhibitors |
JP4578101B2 (en) * | 2001-12-21 | 2010-11-10 | テイボテク・フアーマシユーチカルズ・リミテツド | Heterocyclic substituted phenyl-containing sulfonamides are broad spectrum HIV protease inhibitors |
US7285566B2 (en) | 2002-01-07 | 2007-10-23 | Erickson John W | Resistance-repellent retroviral protease inhibitors |
US20040009890A1 (en) * | 2002-01-07 | 2004-01-15 | Erickson John W. | Broad spectrum inhibitors |
US7157489B2 (en) | 2002-03-12 | 2007-01-02 | The Board Of Trustees Of The University Of Illinois | HIV protease inhibitors |
PT2767539T (en) | 2002-05-16 | 2017-08-28 | Janssen Sciences Ireland Uc | Pseudopolymorphic forms of a hiv protease inhibitor |
US7462636B2 (en) | 2002-05-17 | 2008-12-09 | Tibotec Pharmaceuticals Ltd | Broadspectrum substituted benzisoxazole sulfonamide HIV protease inhibitors |
NZ538488A (en) * | 2002-08-02 | 2007-10-26 | Tibotec Pharm Ltd | Broadspectrum 2-amino-benzothiazole sulfonamide HIV protease inhibitors |
CN101445493A (en) * | 2002-08-02 | 2009-06-03 | 泰博特克药品有限公司 | Broadspectrum 2-amino-benzothiazole sulfonamide HIV protease inhibitors |
PL375307A1 (en) * | 2002-08-14 | 2005-11-28 | Tibotec Pharmaceuticals Ltd. | Broadspectrum substituted oxindole sulfonamide hiv protease inhibitors |
EP1589018A4 (en) | 2002-12-27 | 2007-03-14 | Sumitomo Chemical Co | Process for producing hexahydrofurofuranol derivative, intermediate thereof and process for producing the same |
GB0310593D0 (en) * | 2003-05-08 | 2003-06-11 | Leuven K U Res & Dev | Peptidic prodrugs |
US7807845B2 (en) | 2004-03-11 | 2010-10-05 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
EP1750696B1 (en) | 2004-05-07 | 2013-06-26 | Sequoia Pharmaceuticals Inc | Resistance-repellent retroviral protease inhibitors |
RU2421459C2 (en) | 2005-02-25 | 2011-06-20 | Тиботек Фармасьютикалз Лтд. | Synthesis of protease inhibitor precursor |
CA2667445A1 (en) * | 2005-06-22 | 2007-01-04 | University Of Massachusetts | Hiv-1 protease inhibitors |
TWI432438B (en) | 2005-11-28 | 2014-04-01 | Tibotec Pharm Ltd | Substituted aminophenylsulfonamide compounds and derivatives as hiv protease inhibitor |
AR057182A1 (en) * | 2005-11-28 | 2007-11-21 | Tibotec Pharm Ltd | AMINOPHENYL SULFONAMIDE COMPOUNDS REPLACED AS HIV PROTEASE INHIBITORS |
US20090312318A1 (en) * | 2006-07-24 | 2009-12-17 | Desai Manoj C | Therapeutic compounds and methods |
DK2089371T3 (en) | 2006-11-09 | 2011-05-16 | Tibotec Pharm Ltd | Preparation method for preparing hexahydrofuro [2,3-b] furan-3-OL |
EP2491785A1 (en) * | 2006-11-21 | 2012-08-29 | Purdue Research Foundation | Method and compositions for treating HIV infections |
CN101702908A (en) * | 2007-03-23 | 2010-05-05 | 麻萨诸塞州大学 | hiv-1 protease inhibitors |
PT2152667E (en) | 2007-04-27 | 2011-04-06 | Tibotec Pharm Ltd | Methods for the preparation of n-isobutyl-n-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives |
GT200800303A (en) | 2007-12-24 | 2009-09-18 | ANTI-RETROVIRAL COMBINATION | |
EP2244571A4 (en) | 2008-01-17 | 2014-02-19 | Purdue Research Foundation | Small molecule inhibitors of hiv proteases |
WO2010002994A1 (en) | 2008-07-01 | 2010-01-07 | Purdue Research Foundation | Nonpeptide hiv-1 protease inhibitors |
US8501961B2 (en) | 2008-07-09 | 2013-08-06 | Purdue Research Foundation | HIV protease inhibitors and methods for using |
TWI482775B (en) * | 2008-09-01 | 2015-05-01 | Tibotec Pharm Ltd | Process for the preparation of (3r,3as,6ar)-hexahydrofuro2,3-bfuran-3-yl(1s,2r)-3-(4-aminophenyl)sulfonyl(isobutyl)amino-1-benzyl-2-hydroxypropylcarbamate |
US8921415B2 (en) | 2009-01-29 | 2014-12-30 | Mapi Pharma Ltd. | Polymorphs of darunavir |
WO2010132494A1 (en) * | 2009-05-11 | 2010-11-18 | Ghosh Arun K | Compounds and methods for treating aids and hiv infections |
WO2011092687A1 (en) | 2010-01-28 | 2011-08-04 | Mapi Pharma Hk Limited | Process for the preparation of darunavir and darunavir intermediates |
CN102584844B (en) * | 2011-01-11 | 2016-04-13 | 浙江九洲药业股份有限公司 | A kind of Prezista crystal formation and preparation method thereof |
WO2013011485A1 (en) | 2011-07-20 | 2013-01-24 | Ranbaxy Laboratories Limited | Process for the preparation of sulfonamides useful as retroviral protease inhibitors |
WO2013105118A1 (en) | 2012-01-10 | 2013-07-18 | Council Of Scientific & Industrial Research | A process for synthesis of syn azido epoxide and its use as intermediate the synthesis of amprenavir & saquinavir |
Citations (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1994014793A1 (en) * | 1992-12-29 | 1994-07-07 | G. D. Searle & Co. | Cyclic sulfone containing retroviral protease inhibitors |
WO1995006030A1 (en) * | 1993-08-24 | 1995-03-02 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
US5502060A (en) * | 1991-10-23 | 1996-03-26 | Merck & Co., Inc. | HIV protease inhibitors |
WO1996028463A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
WO1997019055A1 (en) * | 1995-11-21 | 1997-05-29 | Novartis Ag | Azahexane derivatives as substrate isosters of retroviral asparate proteases |
US5703076A (en) * | 1990-11-19 | 1997-12-30 | G. D. Searle & Co. | Retroviral protease inhibitors |
US5705500A (en) * | 1995-03-10 | 1998-01-06 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
US5728718A (en) * | 1994-12-20 | 1998-03-17 | The United States Of America As Represented By The Department Of Health And Human Services | 2,5-diamino-3,4-disubstituted-1,6-diphenylhexane isosteres comprising benzamide, sulfonamide and anthranilamide subunits and methods of using same |
US5753660A (en) * | 1995-11-15 | 1998-05-19 | G. D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
-
1999
- 1999-06-23 WO PCT/US1999/014120 patent/WO1999067254A2/en active Application Filing
- 1999-06-23 AU AU48281/99A patent/AU4828199A/en not_active Abandoned
Patent Citations (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5703076A (en) * | 1990-11-19 | 1997-12-30 | G. D. Searle & Co. | Retroviral protease inhibitors |
US5502060A (en) * | 1991-10-23 | 1996-03-26 | Merck & Co., Inc. | HIV protease inhibitors |
US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
WO1994014793A1 (en) * | 1992-12-29 | 1994-07-07 | G. D. Searle & Co. | Cyclic sulfone containing retroviral protease inhibitors |
WO1995006030A1 (en) * | 1993-08-24 | 1995-03-02 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
US5728718A (en) * | 1994-12-20 | 1998-03-17 | The United States Of America As Represented By The Department Of Health And Human Services | 2,5-diamino-3,4-disubstituted-1,6-diphenylhexane isosteres comprising benzamide, sulfonamide and anthranilamide subunits and methods of using same |
WO1996028463A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
US5705500A (en) * | 1995-03-10 | 1998-01-06 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
US5753660A (en) * | 1995-11-15 | 1998-05-19 | G. D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
WO1997019055A1 (en) * | 1995-11-21 | 1997-05-29 | Novartis Ag | Azahexane derivatives as substrate isosters of retroviral asparate proteases |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8143421B2 (en) | 2002-03-12 | 2012-03-27 | Tibotec Pharmaceuticals Ltd. | Broadspectrum substituted benzimidazole sulfonamide HIV protease inhibitors |
Also Published As
Publication number | Publication date |
---|---|
AU4828199A (en) | 2000-01-10 |
WO1999067254A2 (en) | 1999-12-29 |
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