HRP20030735B1 - Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors - Google Patents

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

Info

Publication number
HRP20030735B1
HRP20030735B1 HR20030735A HRP20030735A HRP20030735B1 HR P20030735 B1 HRP20030735 B1 HR P20030735B1 HR 20030735 A HR20030735 A HR 20030735A HR P20030735 A HRP20030735 A HR P20030735A HR P20030735 B1 HRP20030735 B1 HR P20030735B1
Authority
HR
Croatia
Prior art keywords
4alkyl
aryl
het2
het2c1
arylc1
Prior art date
Application number
HR20030735A
Other languages
English (en)
Croatian (hr)
Inventor
Louis Nestor Ghislai Surleraux Dominique
Tom Bert Paul Wigerinck Piet
Getman Daniel
Gaston Verschueren Wim
Marie Helene Vendeville Sandrine
T.M.M.G De Bethune Marie-Pierre
Octaaf Antoon De Kerpel Jan
Leo Christiaan Moors Samuel
Augustinus De Kock Herman
Christiane Johanna Voets Marieke
Original Assignee
Tibotec Pharmaceuticals 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 Pharmaceuticals Ltd. filed Critical Tibotec Pharmaceuticals Ltd.
Publication of HRP20030735A2 publication Critical patent/HRP20030735A2/xx
Publication of HRP20030735B1 publication Critical patent/HRP20030735B1/xx

Links

Classifications

    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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
    • C07D277/82—Nitrogen atoms

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (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)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
HR20030735A 2001-02-14 2002-02-14 Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors HRP20030735B1 (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
HRP20030735A2 HRP20030735A2 (en) 2005-08-31
HRP20030735B1 true HRP20030735B1 (en) 2012-02-29

Family

ID=26076833

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20030735A HRP20030735B1 (en) 2001-02-14 2002-02-14 Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors

Country Status (30)

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

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA01012270A (es) 1999-05-28 2003-06-24 Virco Nv Nuevos perfiles mutacionales en la transcriptasa reversa de vih-1 correlacionadas con resistencia fenotipica a farmacos.
AU2002226316B2 (en) 2000-10-20 2008-06-26 Virco Bvba Mutational profiles in HIV-1 reverse transcriptase correlated with phenotypic drug resistance
EP1370543B1 (en) 2001-02-14 2006-10-25 Tibotec Pharmaceuticals Ltd. Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors
US7109230B2 (en) 2002-01-07 2006-09-19 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
US7157489B2 (en) 2002-03-12 2007-01-02 The Board Of Trustees Of The University Of Illinois HIV protease inhibitors
CA2490764C (en) 2002-07-01 2011-11-22 Tibotec Pharmaceuticals Ltd. New mutational profiles in hiv-1 reverse transcriptase correlated with phenotypic drug resistance
EP1520247B1 (en) 2002-07-01 2009-05-27 Tibotec Pharmaceuticals Ltd. Mutational profiles in hiv-1 protease correlated with phenotypic drug resistance
OA12893A (en) * 2002-08-02 2006-10-13 Tibotec Pharm Ltd Broadspectrum 2-Amino-Benzothiazole Sulfonamide HIV Protease Inhibitors.
BR0305717A (pt) * 2002-08-02 2004-09-28 Tibotec Pharm Ltd Inibidores da protease do hiv 2-amino-benzotiazol sulfonamida de amplo espectro
WO2005030739A1 (en) * 2003-09-30 2005-04-07 Tibotec Pharmaceuticals Ltd. Methods for the preparation of benzoxazole sulfonamide compounds and intermediates thereof
DE10360835A1 (de) * 2003-12-23 2005-07-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel
AU2005244121B2 (en) * 2004-05-07 2012-01-19 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
ES2331257T3 (es) 2005-02-25 2009-12-28 Tibotec Pharmaceuticals Sintesis de precursores de inhibidores de proteasas.
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
ES2571479T3 (es) 2012-04-20 2016-05-25 Gilead Sciences Inc Derivados del ácido benzotiazol-6-il acético y su uso para tratar una infección por VIH
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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DE69121436T2 (de) 1990-03-09 1997-01-09 Milliken Res Corp Organische Materialien, die sulfonamidogebundene Poly(oxyalkylen)gruppen tragen und ihre Herstellung
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
DE122007000045I2 (de) 1992-08-25 2011-07-21 Gd Searle Llc Gd Searle Llc Darunavir oder pharmazeutisch vertragliche Salze, Hydroxyethylaminosulfonamide verwendbar als InhibiEster oder Prodrugs davon. toren retroviraler Proteasen.
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
ES2166786T3 (es) 1993-10-01 2002-05-01 Astrazeneca Ab Procedimiento i.
DE69637380T2 (de) 1995-01-20 2009-09-17 G.D. Searle Llc, Chicago Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen
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
CN1149223C (zh) * 1995-03-10 2004-05-12 G·D·瑟尔公司 杂环羰基氨基酸羟乙氨基磺酰胺逆转录病毒蛋白酶抑制剂
US6143788A (en) * 1995-03-10 2000-11-07 G.D. Searle & Co. Bis-amino acid hydroxyethlamino 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
US6509038B2 (en) 1996-05-20 2003-01-21 Janssen Pharmaceutica N.V. Antifungal compositions with improved bioavailability
CZ295502B6 (cs) 1997-03-26 2005-08-17 Janssen Pharmaceutica N. V. Antifungální peleta, způsob její přípravy a farmaceutická dávková forma s obsahem těchto pelet
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
AU2012199A (en) 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
EP1042280A2 (en) 1997-12-24 2000-10-11 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
AU2010299A (en) 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
PT2336134T (pt) * 1998-06-23 2016-10-19 The Board Of Trustees Of The Univ Of Illionis Ensaio de aptidão e métodos para reduzir a resistência do hiv à terapia
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
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
EP1370543B1 (en) 2001-02-14 2006-10-25 Tibotec Pharmaceuticals Ltd. Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
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
ATE343567T1 (de) 2006-11-15
AU2002302363B2 (en) 2008-05-01
PT1370543E (pt) 2007-02-28
DK1370543T3 (da) 2007-02-19
MXPA03007236A (es) 2003-12-04
BR0207862A (pt) 2004-06-22
NO326174B1 (no) 2008-10-13
HK1061233A1 (en) 2004-09-10
WO2002083657A2 (en) 2002-10-24
HU229224B1 (en) 2013-09-30
AP1504A (en) 2005-12-10
AP2003002856A0 (en) 2003-09-30
ES2275866T3 (es) 2007-06-16
CY1108073T1 (el) 2014-02-12
JP4530612B2 (ja) 2010-08-25
IL157171A (en) 2012-10-31
CN1525962A (zh) 2004-09-01
NO20033584D0 (no) 2003-08-13
CN101230067B (zh) 2011-06-15
JP2004518767A (ja) 2004-06-24
CA2438304C (en) 2011-04-12
PL213327B1 (pl) 2013-02-28
SK11022003A3 (sk) 2004-07-07
PL363778A1 (en) 2004-11-29
IL157171A0 (en) 2004-02-08
BG66301B1 (bg) 2013-03-29
CA2438304A1 (en) 2002-10-24
KR100870184B1 (ko) 2008-11-24
HRP20030735A2 (en) 2005-08-31
BG108143A (en) 2004-07-30
CN101230067A (zh) 2008-07-30
EE05385B1 (et) 2011-02-15
EA200300891A1 (ru) 2004-02-26
EA006096B1 (ru) 2005-08-25
CZ20032415A3 (cs) 2004-04-14
ZA200306086B (en) 2005-01-26
SI1370543T1 (sl) 2007-04-30
KR20030077017A (ko) 2003-09-29
SK287582B6 (sk) 2011-03-04
NZ527391A (en) 2005-04-29
US20040116485A1 (en) 2004-06-17
HUP0303257A2 (hu) 2004-01-28
US7659404B2 (en) 2010-02-09
EP1370543A2 (en) 2003-12-17
NO20033584L (no) 2003-10-14
CN100369904C (zh) 2008-02-20
DE60215623D1 (de) 2006-12-07
EE200300381A (et) 2003-12-15
CZ304273B6 (cs) 2014-02-12
EP1370543B1 (en) 2006-10-25
WO2002083657A3 (en) 2003-02-13
DE60215623T2 (de) 2007-08-30

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