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EA200401524A1 - Ингибиторы вич-протеазы на основе замещённых бензизоксазолсульфонамидов широкого спектра действия - Google Patents

Ингибиторы вич-протеазы на основе замещённых бензизоксазолсульфонамидов широкого спектра действия

Info

Publication number
EA200401524A1
EA200401524A1 EA200401524A EA200401524A EA200401524A1 EA 200401524 A1 EA200401524 A1 EA 200401524A1 EA 200401524 A EA200401524 A EA 200401524A EA 200401524 A EA200401524 A EA 200401524A EA 200401524 A1 EA200401524 A1 EA 200401524A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
benzyazoxasolusulphonamides
substituted
action
protease inhibitors
Prior art date
Application number
EA200401524A
Other languages
English (en)
Other versions
EA010908B1 (ru
Inventor
Доминик Луи Нестор Гилейн Сюрлеро
Бернхард Йоанна Бернард Фергаувен
Херман Августинус Де Кок
Original Assignee
Тиботек Фармасьютикалз Лтд.
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 Тиботек Фармасьютикалз Лтд. filed Critical Тиботек Фармасьютикалз Лтд.
Publication of EA200401524A1 publication Critical patent/EA200401524A1/ru
Publication of EA010908B1 publication Critical patent/EA010908B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • 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
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/20—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Virology (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Настоящее изобретение относится к соединениям, имеющим формы N-оксидов, солей, стереоизомерные формы, формы рацемических смесей, пролекарств, сложных эфиров и метаболитов. Также изобретение относится к использованию таких соединений в качестве ингибиторов ВИЧ-протеазы широкого спектра действия, способам получения этих соединений, а также к включающим такие соединения фармацевтическим композициям и диагностическим наборам. Также изобретение относится к комбинациям таких соединений с другим антиретровирусным средством и к их использованию в анализах в качестве контрольных соединений или реагентов.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200401524A 2002-05-17 2003-05-16 Ингибиторы вич-протеазы на основе замещённых бензизоксазолсульфонамидов широкого спектра действия EA010908B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02076957 2002-05-17
PCT/EP2003/050173 WO2003097616A1 (en) 2002-05-17 2003-05-16 Broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors

Publications (2)

Publication Number Publication Date
EA200401524A1 true EA200401524A1 (ru) 2005-06-30
EA010908B1 EA010908B1 (ru) 2008-12-30

Family

ID=29433159

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200401524A EA010908B1 (ru) 2002-05-17 2003-05-16 Ингибиторы вич-протеазы на основе замещённых бензизоксазолсульфонамидов широкого спектра действия

Country Status (28)

Country Link
US (1) US7462636B2 (ru)
EP (1) EP1517899B1 (ru)
JP (2) JP4674084B2 (ru)
KR (2) KR20100130234A (ru)
CN (1) CN100582097C (ru)
AP (1) AP2004003190A0 (ru)
AR (1) AR039887A1 (ru)
AT (1) ATE371652T1 (ru)
AU (1) AU2003238074B2 (ru)
BR (1) BR0310089A (ru)
CA (1) CA2485903C (ru)
CY (1) CY1107040T1 (ru)
DE (1) DE60315984T2 (ru)
DK (1) DK1517899T3 (ru)
EA (1) EA010908B1 (ru)
ES (1) ES2292976T3 (ru)
HR (1) HRP20050607B1 (ru)
IL (1) IL165043A0 (ru)
MX (1) MXPA04011466A (ru)
MY (1) MY135226A (ru)
NO (1) NO330184B1 (ru)
NZ (1) NZ536496A (ru)
PL (1) PL373425A1 (ru)
PT (1) PT1517899E (ru)
SI (1) SI1517899T1 (ru)
TW (1) TWI356700B (ru)
WO (1) WO2003097616A1 (ru)
ZA (1) ZA200410156B (ru)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1517899E (pt) * 2002-05-17 2007-11-16 Tibotec Pharm Ltd ¿inibidores da protease do hiv de largo espectro benzisoxazolossulfonamidas substituídas¿
CN1953964A (zh) * 2004-03-11 2007-04-25 塞阔伊亚药品公司 抗耐药性反转录病毒蛋白酶抑制剂
WO2005110428A2 (en) * 2004-05-07 2005-11-24 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
CA2595295C (en) 2005-02-25 2014-07-08 Tibotec Pharmaceuticals Ltd. Protease inhibitor precursor synthesis
CN101702908A (zh) * 2007-03-23 2010-05-05 麻萨诸塞州大学 Hiv-1蛋白酶抑制剂
WO2009118356A2 (en) * 2008-03-25 2009-10-01 Formac Pharmaceuticals N.V. Preparation method for solid disupersions
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
DE102010004957A1 (de) * 2010-01-14 2011-07-21 Universitätsklinikum Jena, 07743 Biologisch wirksame Moleküle zur Beeinflussung von Virus-, Bakterien-, Parasiten-infizierten Zellen und/oder Tumorzellen und Verfahren zu deren Anwendung
JP2016503395A (ja) 2012-10-31 2016-02-04 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 病害生物防除剤としての複素環化合物
EP2964204B1 (en) 2013-03-07 2017-01-04 Dow Global Technologies LLC Novel esterified cellulose ethers of very low viscosity

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5004751A (en) * 1987-08-28 1991-04-02 Mochida Pharmaceutical Co., Ltd. Hydantoin derivatives
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
KR100296463B1 (ko) * 1992-08-25 2001-10-24 죤 에이치. 뷰센 레트로바이러스프로테아제저해제로서유용한히드록시에틸아미노술폰아미드
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
DK0715618T3 (da) 1993-08-24 1999-08-23 Searle & Co Hydroxyethylaminosulfonamider til anvendelse som inhibitorer af retrovirale proteaser
DK0721331T3 (da) 1993-10-01 2002-02-11 Astrazeneca Ab Fremgangsmåde
EP1586558A3 (en) * 1995-01-20 2005-10-26 G.D. Searle LLC. Bis-sulfonamide hydroxyethylamino retroviral protease inhinitors
US5756533A (en) * 1995-03-10 1998-05-26 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
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
US5753660A (en) 1995-11-15 1998-05-19 G. D. Searle & Co. Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
CZ293841B6 (cs) 1996-05-20 2004-08-18 Janssenápharmaceuticaán@Áv Částice s obsahem itrakonazolu
ID21477A (id) 1997-03-26 1999-06-17 Janssen Pharmaceutica Nv Pelet-pelet yang mempunyai inti yang dilapisi dengan suatu anti jamur dan suatu polimer
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
TR200002402T2 (tr) 1997-12-24 2001-01-22 Vertex Pharmaceuticals Incorporated Aspartil proteaz inhibitörü ön-ilaçlar.
AU2010299A (en) 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
WO1999033795A1 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
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
DK1088098T4 (en) * 1998-06-23 2015-09-14 Us Of America Represented By The Secretary Dept Of Health And Human Services Fitnessassay and methods for reducing HIV resistance to therapy
WO2001025240A1 (en) 1999-10-06 2001-04-12 Tibotec Pharmaceuticals 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 INHIBITOR
US7244752B2 (en) * 2001-04-09 2007-07-17 Tibotec Pharmaceuticals Ltd. Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide HIV protease inhibitors
PT1517899E (pt) * 2002-05-17 2007-11-16 Tibotec Pharm Ltd ¿inibidores da protease do hiv de largo espectro benzisoxazolossulfonamidas substituídas¿

Also Published As

Publication number Publication date
AU2003238074B2 (en) 2009-04-30
PT1517899E (pt) 2007-11-16
ATE371652T1 (de) 2007-09-15
EP1517899B1 (en) 2007-08-29
EA010908B1 (ru) 2008-12-30
US20050171173A1 (en) 2005-08-04
ES2292976T3 (es) 2008-03-16
NO330184B1 (no) 2011-02-28
JP4674084B2 (ja) 2011-04-20
JP2005527607A (ja) 2005-09-15
HK1076099A1 (en) 2006-01-06
PL373425A1 (en) 2005-08-22
NZ536496A (en) 2006-06-30
TWI356700B (en) 2012-01-21
AR039887A1 (es) 2005-03-09
DK1517899T3 (da) 2007-12-03
IL165043A0 (en) 2005-12-18
EP1517899A1 (en) 2005-03-30
WO2003097616A1 (en) 2003-11-27
JP2011051999A (ja) 2011-03-17
CY1107040T1 (el) 2012-09-26
HRP20050607A2 (en) 2006-02-28
TW200404538A (en) 2004-04-01
KR20100130234A (ko) 2010-12-10
MY135226A (en) 2008-02-29
DE60315984D1 (de) 2007-10-11
AU2003238074A1 (en) 2003-12-02
HRP20050607B1 (hr) 2014-07-04
DE60315984T2 (de) 2008-05-29
AP2004003190A0 (en) 2004-12-31
US7462636B2 (en) 2008-12-09
KR101019648B1 (ko) 2011-03-07
CN1668605A (zh) 2005-09-14
SI1517899T1 (sl) 2008-02-29
NO20045444L (no) 2005-02-16
MXPA04011466A (es) 2005-02-14
ZA200410156B (en) 2005-11-30
KR20050013549A (ko) 2005-02-04
BR0310089A (pt) 2005-02-15
CA2485903A1 (en) 2003-11-27
CA2485903C (en) 2011-08-16
CN100582097C (zh) 2010-01-20

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): KZ RU