AP1504A - Broadspectrum 2- (substituted-amino) -benzothiazole sulfonamide HIV protease inhibitors - Google Patents

Broadspectrum 2- (substituted-amino) -benzothiazole sulfonamide HIV protease inhibitors

Info

Publication number
AP1504A
AP1504A APAP/P/2003/002856A AP2003002856A AP1504A AP 1504 A AP1504 A AP 1504A AP 2003002856 A AP2003002856 A AP 2003002856A AP 1504 A AP1504 A AP 1504A
Authority
AP
ARIPO
Prior art keywords
4alkyl
6alkyl
aryl
het2
substituted
Prior art date
Application number
APAP/P/2003/002856A
Other languages
English (en)
Other versions
AP2003002856A0 (en
Inventor
Dominique Louis Nestor Ghislain Surleraux
Piet Tom Bert Paul Wigerinck
Daniel P Getman
Wim Gaston Verschueren
Sandrine Marie Hélène Vendeville
Bethune Marie-Pierre T M M G De
Kerpel Jan Octaaf Antoon De
Samuel Leo Christiaan Moors
Kock Herman Augustinus De
Marieke Christiane Johanna Voets
Original Assignee
Tibotec Pharm Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Publication of AP2003002856A0 publication Critical patent/AP2003002856A0/xx
Application granted granted Critical
Publication of AP1504A publication Critical patent/AP1504A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82Nitrogen atoms

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
APAP/P/2003/002856A 2001-02-14 2002-02-14 Broadspectrum 2- (substituted-amino) -benzothiazole sulfonamide HIV protease inhibitors AP1504A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP01200529 2001-02-14
US28775801P 2001-05-02 2001-05-02
PCT/EP2002/001788 WO2002083657A2 (en) 2001-02-14 2002-02-14 Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors

Publications (2)

Publication Number Publication Date
AP2003002856A0 AP2003002856A0 (en) 2003-09-30
AP1504A true AP1504A (en) 2005-12-10

Family

ID=26076833

Family Applications (1)

Application Number Title Priority Date Filing Date
APAP/P/2003/002856A AP1504A (en) 2001-02-14 2002-02-14 Broadspectrum 2- (substituted-amino) -benzothiazole sulfonamide HIV protease inhibitors

Country Status (30)

Country Link
US (1) US7659404B2 (https=)
EP (1) EP1370543B1 (https=)
JP (1) JP4530612B2 (https=)
KR (1) KR100870184B1 (https=)
CN (2) CN100369904C (https=)
AP (1) AP1504A (https=)
AT (1) ATE343567T1 (https=)
AU (1) AU2002302363B2 (https=)
BG (1) BG66301B1 (https=)
BR (1) BR0207862A (https=)
CA (1) CA2438304C (https=)
CY (1) CY1108073T1 (https=)
CZ (1) CZ304273B6 (https=)
DE (1) DE60215623T2 (https=)
DK (1) DK1370543T3 (https=)
EA (1) EA006096B1 (https=)
EE (1) EE05385B1 (https=)
ES (1) ES2275866T3 (https=)
HR (1) HRP20030735B1 (https=)
HU (1) HU229224B1 (https=)
IL (2) IL157171A0 (https=)
MX (1) MXPA03007236A (https=)
NO (1) NO326174B1 (https=)
NZ (1) NZ527391A (https=)
PL (1) PL213327B1 (https=)
PT (1) PT1370543E (https=)
SI (1) SI1370543T1 (https=)
SK (1) SK287582B6 (https=)
WO (1) WO2002083657A2 (https=)
ZA (1) ZA200306086B (https=)

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ES2246859T3 (es) 1999-05-28 2006-03-01 Virco Bvba Nuevos perfiles mutacionales en la transcriptasa inversa del vih-1 correlacionadas con una resistencia fenotipica a farmacos.
EP1356082A2 (en) 2000-10-20 2003-10-29 Virco Bvba Mutational profiles in hiv-1 reverse transcriptase correlated with phenotypic drug resistance
US7659404B2 (en) 2001-02-14 2010-02-09 Tibotec Pharmaceuticals Ltd. Broad spectrum 2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors
AU2003202914A1 (en) 2002-01-07 2003-07-24 Sequoia Pharmaceuticals Broad spectrum inhibitors
US7157489B2 (en) 2002-03-12 2007-01-02 The Board Of Trustees Of The University Of Illinois HIV protease inhibitors
DE60321466D1 (de) 2002-07-01 2008-07-17 Tibotec Pharm Ltd Mit phänotypischer medikamentenresistenz korrelierte mutationsprofile in hiv-1-reverse-transkriptase
EP1520247B1 (en) 2002-07-01 2009-05-27 Tibotec Pharmaceuticals Ltd. Mutational profiles in hiv-1 protease correlated with phenotypic drug resistance
CN1671380B (zh) * 2002-08-02 2010-05-26 泰博特克药品有限公司 广谱2-氨基-苯并噻唑磺酰胺类hiv蛋白酶抑制剂
OA12893A (en) * 2002-08-02 2006-10-13 Tibotec Pharm Ltd Broadspectrum 2-Amino-Benzothiazole Sulfonamide HIV Protease Inhibitors.
BRPI0414916A (pt) * 2003-09-30 2006-11-07 Tibotec Pharm Ltd métodos para a preparação de compostos de sulfonamida de benzoxazol e intermediários dos mesmos
DE10360835A1 (de) * 2003-12-23 2005-07-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel
US7378441B2 (en) * 2004-05-07 2008-05-27 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
DK1856125T3 (da) 2005-02-25 2009-12-07 Tibotec Pharm Ltd Syntese af proteasehæmmerforstadie
AR053845A1 (es) 2005-04-15 2007-05-23 Tibotec Pharm Ltd 5-tiazolilmetil[(1s,2r)-3-[[(2-amino-6-benzoxazolil)sulfonil)](2-metilpropil)amino]-2-hidroxi-1-(fenilmetil)propil]carbamato como mejorador de farmacos metabolizados por el citocromo p450
JO2841B1 (en) * 2006-06-23 2014-09-15 تيبوتيك فارماسيوتيكالز ليمتد 2-(substituted-amino) -benzothiazole sulfonamide as protease inhibitors HIV (HIV)
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
JO3090B1 (ar) * 2009-12-11 2017-03-15 Janssen Sciences Ireland Uc 5- امينو-4- هيدروكسي-بنتويل اميدات
US9024038B2 (en) 2010-12-27 2015-05-05 Purdue Research Foundation Compunds and methods for treating HIV
UY34750A (es) 2012-04-20 2013-11-29 Gilead Sciences Inc ?compuestos para el tratamiento del hiv, composiciones,métodos de preparación, intermediarios y métodos terapéuticos?.
CN104000824B (zh) * 2014-05-28 2016-07-06 中山大学 苯并五元杂环类化合物在制备抗hiv-1病毒药物中的应用
US11439608B2 (en) 2017-09-25 2022-09-13 Qun Lu Roles of modulators of intersectin-CDC42 signaling in Alzheimer's disease
CN116354903B (zh) * 2021-12-28 2025-09-09 南京药石科技股份有限公司 一种6-苯并噻唑磺酰氯的制备方法
WO2024206093A1 (en) * 2023-03-24 2024-10-03 Purdue Research Foundation Hiv-1p rotease inhibitors and uses thereof

Citations (3)

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WO1995006030A1 (en) * 1993-08-24 1995-03-02 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
WO1996028463A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1999065870A2 (en) * 1998-06-19 1999-12-23 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease

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EP0445926B1 (en) 1990-03-09 1996-08-21 Milliken Research Corporation Organic materials having sulfonamido linked poly(oxyalkylene) moieties and their preparation
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
ES2123065T3 (es) * 1992-08-25 1999-01-01 Searle & Co Hidroxietilamino-sulfonamidas utiles como inhibidores de proteasas retroviricas.
PH30929A (en) 1992-09-03 1997-12-23 Janssen Pharmaceutica Nv Beads having a core coated with an antifungal and a polymer.
IS2334B (is) 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
PT721331E (pt) 1993-10-01 2002-05-31 Astrazeneca Ab Processo i
CA2210889C (en) 1995-01-20 2007-08-28 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
US6140505A (en) * 1995-03-10 2000-10-31 G. D. Searle & Co. Synthesis of benzo fused heterocyclic sulfonyl chlorides
US6861539B1 (en) * 1995-03-10 2005-03-01 G. D. Searle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6150556A (en) * 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-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
BR9607625A (pt) 1995-03-10 1999-06-15 Searle & Co Inibidores de protease retroviral sulfonamida hidroxietilamino de aminoácido heterociclocarbonila
US6143788A (en) * 1995-03-10 2000-11-07 G.D. Searle & Co. Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors
US5753660A (en) 1995-11-15 1998-05-19 G. D. Searle & Co. Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1997044014A1 (en) 1996-05-20 1997-11-27 Janssen Pharmaceutica N.V. Antifungal compositions with improved bioavailability
SK284813B6 (sk) 1997-03-26 2005-12-01 Janssen Pharmaceutica N. V. Peleta obsahujúca itrakonazol, spôsob jej prípravy a farmaceutická dávková forma s jej obsahom
AU2012199A (en) 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
WO1999033792A2 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
EA200000702A1 (ru) * 1997-12-24 2000-12-25 Вертекс Фармасьютикалз Инкорпорейтед Пролекарства ингибиторов аспартилпротеаз
AU4828199A (en) 1998-06-23 2000-01-10 Board Of Trustees Of The University Of Illinois, The Multi-drug resistant retroviral protease inhibitors and associated methods
CA2872424C (en) * 1998-06-23 2017-03-07 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Bisfuran derivatives useful in preventing the emergence of multidrug resistant hiv strains and treatment of hiv
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion
US7659404B2 (en) 2001-02-14 2010-02-09 Tibotec Pharmaceuticals Ltd. Broad spectrum 2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
WO1995006030A1 (en) * 1993-08-24 1995-03-02 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
WO1996028463A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1999065870A2 (en) * 1998-06-19 1999-12-23 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease

Also Published As

Publication number Publication date
CN1525962A (zh) 2004-09-01
PT1370543E (pt) 2007-02-28
WO2002083657A3 (en) 2003-02-13
JP4530612B2 (ja) 2010-08-25
EE05385B1 (et) 2011-02-15
NZ527391A (en) 2005-04-29
EE200300381A (et) 2003-12-15
CA2438304C (en) 2011-04-12
CY1108073T1 (el) 2014-02-12
HU229224B1 (en) 2013-09-30
NO326174B1 (no) 2008-10-13
CZ304273B6 (cs) 2014-02-12
EA200300891A1 (ru) 2004-02-26
EA006096B1 (ru) 2005-08-25
CN101230067A (zh) 2008-07-30
SI1370543T1 (sl) 2007-04-30
US20040116485A1 (en) 2004-06-17
PL213327B1 (pl) 2013-02-28
SK11022003A3 (sk) 2004-07-07
EP1370543B1 (en) 2006-10-25
HRP20030735B1 (en) 2012-02-29
PL363778A1 (en) 2004-11-29
AP2003002856A0 (en) 2003-09-30
AU2002302363B2 (en) 2008-05-01
NO20033584L (no) 2003-10-14
US7659404B2 (en) 2010-02-09
NO20033584D0 (no) 2003-08-13
BG66301B1 (bg) 2013-03-29
WO2002083657A2 (en) 2002-10-24
HUP0303257A2 (hu) 2004-01-28
DE60215623T2 (de) 2007-08-30
HRP20030735A2 (en) 2005-08-31
CZ20032415A3 (cs) 2004-04-14
EP1370543A2 (en) 2003-12-17
CN100369904C (zh) 2008-02-20
JP2004518767A (ja) 2004-06-24
ES2275866T3 (es) 2007-06-16
KR20030077017A (ko) 2003-09-29
CN101230067B (zh) 2011-06-15
IL157171A (en) 2012-10-31
CA2438304A1 (en) 2002-10-24
DK1370543T3 (da) 2007-02-19
MXPA03007236A (es) 2003-12-04
ATE343567T1 (de) 2006-11-15
IL157171A0 (en) 2004-02-08
SK287582B6 (sk) 2011-03-04
ZA200306086B (en) 2005-01-26
KR100870184B1 (ko) 2008-11-24
BR0207862A (pt) 2004-06-22
HK1061233A1 (en) 2004-09-10
DE60215623D1 (de) 2006-12-07
BG108143A (en) 2004-07-30

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