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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (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)
  • 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 (cs)
EP (1) EP1370543B1 (cs)
JP (1) JP4530612B2 (cs)
KR (1) KR100870184B1 (cs)
CN (2) CN100369904C (cs)
AP (1) AP1504A (cs)
AT (1) ATE343567T1 (cs)
AU (1) AU2002302363B2 (cs)
BG (1) BG66301B1 (cs)
BR (1) BR0207862A (cs)
CA (1) CA2438304C (cs)
CY (1) CY1108073T1 (cs)
CZ (1) CZ304273B6 (cs)
DE (1) DE60215623T2 (cs)
DK (1) DK1370543T3 (cs)
EA (1) EA006096B1 (cs)
EE (1) EE05385B1 (cs)
ES (1) ES2275866T3 (cs)
HR (1) HRP20030735B1 (cs)
HU (1) HU229224B1 (cs)
IL (2) IL157171A0 (cs)
MX (1) MXPA03007236A (cs)
NO (1) NO326174B1 (cs)
NZ (1) NZ527391A (cs)
PL (1) PL213327B1 (cs)
PT (1) PT1370543E (cs)
SI (1) SI1370543T1 (cs)
SK (1) SK287582B6 (cs)
WO (1) WO2002083657A2 (cs)
ZA (1) ZA200306086B (cs)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1185712B8 (en) 1999-05-28 2005-10-19 Virco Bvba New mutational profiles in hiv-1 reverse transcriptase correlated with phenotypic drug resistance
RU2318213C2 (ru) 2000-10-20 2008-02-27 Вирко Бвба Новые мутационные профили обратной транскриптазы вич-1, коррелирующие с фенотипической резистентностью к лекарственным средствам
DK1370543T3 (da) 2001-02-14 2007-02-19 Tibotec Pharm Ltd Bredspektrede 2-(substitueret amino) benzothiazol- sulfonamid-HIV-proteaseinhibitorer
CA2473231A1 (en) 2002-01-07 2003-08-07 Sequoia Pharmaceuticals 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
AU2003254500B2 (en) 2002-07-01 2009-11-19 Tibotec Pharmaceuticals Ltd. Mutational profiles in HIV-1 protease correlated with phenotypic drug resistance
ATE397669T1 (de) 2002-07-01 2008-06-15 Tibotec Pharm Ltd Mit phänotypischer medikamentenresistenz korrelierte mutationsprofile in hiv-1-reverse- transkriptase
KR101327772B1 (ko) * 2002-08-02 2013-11-11 얀센 알 앤드 디 아일랜드 광범위 2-아미노-벤조티아졸 설폰아미드 ｈｉｖ 프로테아제 저해제
AU2003262561B2 (en) * 2002-08-02 2008-10-16 Tibotec Pharmaceuticals Ltd. Broadspectrum 2-amino-benzothiazole sulfonamide HIV protease inhibitors
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
US7378441B2 (en) * 2004-05-07 2008-05-27 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
BRPI0607827B8 (pt) 2005-02-25 2021-05-25 Janssen R & D Ireland composto precursor de inibidor de protease, processo para a produção do referido composto e seu uso
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
JP5911638B2 (ja) 2012-04-20 2016-04-27 ギリアード サイエンシーズ， インコーポレイテッド ベンゾチアゾール−６−イル酢酸誘導体およびｈｉｖ感染を処置するためのそれらの使用
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)

* 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

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
DE69332002T2 (de) 1992-08-25 2002-12-19 Monsanto Co Hydroxyethylaminosulfonamide verwendbar als Inhibitoren 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
PL175564B1 (pl) 1993-10-01 1999-01-29 Astra Ab Sposób i urządzenie do formowania leku w proszku oraz lek w proszku
US6143747A (en) 1995-01-20 2000-11-07 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
US5705500A (en) 1995-03-10 1998-01-06 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
US6861539B1 (en) * 1995-03-10 2005-03-01 G. D. Searle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
ES2190793T3 (es) 1995-03-10 2003-08-16 Searle & Co Inhibidores de proteasas retrovirales de heterociclocarbonil aminoacido hidroxietilamino sulfonamida.
US6143788A (en) * 1995-03-10 2000-11-07 G.D. Searle & Co. Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors
US6150556A (en) * 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
JP2000515488A (ja) * 1995-11-15 2000-11-21 ジー．ディー．サール アンド カンパニー 置換スルホニルアルカノイルアミノヒドロキシエチルアミノスルホンアミド レトロウイルスプロテアーゼ阻害剤
DK0904060T3 (da) 1996-05-20 2004-04-13 Janssen Pharmaceutica Nv Antifungale præparater med forbedret biotilgængelighed
HU224217B1 (hu) 1997-03-26 2005-06-28 Janssen Pharmaceutica N.V. Gombaellenes hatóanyaggal és polimerrel bevont magrészt tartalmazó pelletek
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
WO1999033795A1 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
WO1999033792A2 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
TR200002402T2 (tr) * 1997-12-24 2001-01-22 Vertex Pharmaceuticals Incorporated Aspartil proteaz inhibitörü ön-ilaçlar.
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
WO1999067254A2 (en) 1998-06-23 1999-12-29 The United States Of America Represented By The Secretary, Department Of Health And Human Services Multi-drug resistant retroviral protease inhibitors and use thereof
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
DK1370543T3 (da) 2001-02-14 2007-02-19 Tibotec Pharm Ltd Bredspektrede 2-(substitueret amino) benzothiazol- sulfonamid-HIV-proteaseinhibitorer

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

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