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EA200301110A1 - 2-(замещенный амино) бензоксазолсульфонамидные ингибиторы вич-протеазы широкого спектра - Google Patents

2-(замещенный амино) бензоксазолсульфонамидные ингибиторы вич-протеазы широкого спектра

Info

Publication number
EA200301110A1
EA200301110A1 EA200301110A EA200301110A EA200301110A1 EA 200301110 A1 EA200301110 A1 EA 200301110A1 EA 200301110 A EA200301110 A EA 200301110A EA 200301110 A EA200301110 A EA 200301110A EA 200301110 A1 EA200301110 A1 EA 200301110A1
Authority
EA
Eurasian Patent Office
Prior art keywords
alkyl
amino
aryl
calkandiyl
het
Prior art date
Application number
EA200301110A
Other languages
English (en)
Other versions
EA007383B1 (ru
Inventor
Доминик Луи Нестор Гилэйн Сюрлеро
Сандрин Мари Элен Вендевилль
Вим Гастон Версхюэрен
Мари-Пьер Т.М.М.Дж. Де Бетюн
Херман Аугустинус Де Кок
Абделлах Тахри
Монтсеррат Эрра Сола
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 EA200301110A1 publication Critical patent/EA200301110A1/ru
Publication of EA007383B1 publication Critical patent/EA007383B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58Benzoxazoles; Hydrogenated benzoxazoles 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
    • 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
    • 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы (I)их N-оксидам, солям, стереоизомерным формам, рацемическим смесям, пролекарствам, сложным эфирам и метаболитам, где каждый из Rи Rпредставляет H, необязательно замещенный Cалкил, Cалкенил, Cциклоалкил, арил, Het, Het; Rможет также представлять радикал формулы (RR)NC(RR)CR; t равно 0, 1 или 2; Rпредставляет H или Cалкил; L представляет -C(=O)-, -O-C(=O)-, -NR-C(=O)-, -O-Cалкандиил-C(=O)-, -NR-Cалкандиил-C(=O)-, -S(=O)-, -O-S(=O)-, -NR-S(=O); Rпредставляет Cалкил, арил, Cциклоалкил, Cциклоалкил-Cалкил или арил-Cалкил; Rпредставляет H, Cалкил-OC(=O), карбоксил, амино-C(=O), моно- или ди(Cалкил)амино-C(=O), Cциклоалкил, Cалкенил, Cалкинил или необязательно замещенный Cалкил; A представляет Cалкандиил, -C(=O)-, -C(=S)-, -S(=O)-, Cалкандиил-C(=O)-, Cалкандиил-C(=S)- или Cалкандиил-S(=O)-; Rпредставляет H, OH, Cалкил, HetCалкил, HetCалкил, необязательно замещенный амино-Cалкил; Rпредставляет Cалкил-O, Het, HetO, Het, HetO, арил, арил-O; Cалкилоксикарбониламино или амино; и в случае если -A- отличается от Cалкандиила, то Rможет также представлять Cалкил, HetCалкил, HetOCалкил, HetCалкил, HetCалкил, арил-Cалкил, арил-OCалкил или амино-Cалкил; причем каждая из аминогрупп в определении Rможет быть необязательно замещенной. -A-Rпредставляет гидрокси-Cалкил; Rи -A-R, взятые вместе с атомом азота, к которому они присоединены, могут также образовывать Hetили Het. Изобретение относится также к применению таких соединений в качестве ингибиторов ВИЧ-протеазы широкого спектра, также к способам их получения, а также к фармацевтическим композициям и диагностическим наборам, содержащим такие соединения. Оно относится также к сочетаниям таких соединений с другим антиретровирусным агентом и к их применению в испытаниях в качестве эталонных соединений или реактивов.Отчет о международном поиске был опубликован 2003.05.01.
EA200301110A 2001-04-09 2002-04-09 2-(замещенный амино)бензоксазолсульфонамидные ингибиторы вич-протеазы широкого спектра EA007383B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP01201308 2001-04-09
US28770401P 2001-05-02 2001-05-02
PCT/EP2002/004012 WO2002081478A2 (en) 2001-04-09 2002-04-09 Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide hiv protease inhibitors

Publications (2)

Publication Number Publication Date
EA200301110A1 true EA200301110A1 (ru) 2004-04-29
EA007383B1 EA007383B1 (ru) 2006-10-27

Family

ID=26076876

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200301110A EA007383B1 (ru) 2001-04-09 2002-04-09 2-(замещенный амино)бензоксазолсульфонамидные ингибиторы вич-протеазы широкого спектра

Country Status (25)

Country Link
US (2) US7244752B2 (ru)
EP (1) EP1397367A2 (ru)
JP (1) JP4417010B2 (ru)
KR (1) KR100872029B1 (ru)
CN (1) CN100491360C (ru)
AP (1) AP1544A (ru)
AR (1) AR035819A1 (ru)
AU (1) AU2002257774B2 (ru)
BG (1) BG66371B1 (ru)
BR (1) BR0208796A (ru)
CA (1) CA2442870C (ru)
CZ (1) CZ303139B6 (ru)
EA (1) EA007383B1 (ru)
EE (1) EE05384B1 (ru)
HR (1) HRP20030905B1 (ru)
HU (1) HUP0303744A3 (ru)
IL (1) IL158092A0 (ru)
MX (1) MXPA03009179A (ru)
NO (1) NO328896B1 (ru)
NZ (1) NZ528954A (ru)
OA (1) OA12464A (ru)
PL (1) PL367084A1 (ru)
SK (1) SK288232B6 (ru)
WO (1) WO2002081478A2 (ru)
ZA (1) ZA200307683B (ru)

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WO2005110428A2 (en) * 2004-05-07 2005-11-24 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
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Also Published As

Publication number Publication date
JP4417010B2 (ja) 2010-02-17
EP1397367A2 (en) 2004-03-17
CA2442870A1 (en) 2002-10-17
KR100872029B1 (ko) 2008-12-05
ZA200307683B (en) 2005-03-30
BG108218A (bg) 2004-09-30
AR035819A1 (es) 2004-07-14
HUP0303744A3 (en) 2008-03-28
MXPA03009179A (es) 2004-11-22
CN100491360C (zh) 2009-05-27
SK13392003A3 (en) 2004-10-05
US7595334B2 (en) 2009-09-29
WO2002081478A3 (en) 2003-05-01
EE05384B1 (et) 2011-02-15
AP2003002882A0 (en) 2003-12-31
US20070135447A1 (en) 2007-06-14
NO20034505D0 (no) 2003-10-08
CN1636006A (zh) 2005-07-06
CA2442870C (en) 2011-08-02
US20040132791A1 (en) 2004-07-08
PL367084A1 (en) 2005-02-21
CZ20032936A3 (cs) 2004-05-12
CZ303139B6 (cs) 2012-04-25
SK288232B6 (sk) 2014-11-04
NO328896B1 (no) 2010-06-07
HRP20030905B1 (en) 2012-03-31
US7244752B2 (en) 2007-07-17
JP2004529144A (ja) 2004-09-24
EE200300494A (et) 2003-12-15
NO20034505L (no) 2003-12-08
AU2002257774B2 (en) 2007-08-30
WO2002081478A2 (en) 2002-10-17
HUP0303744A2 (hu) 2004-03-01
EA007383B1 (ru) 2006-10-27
BR0208796A (pt) 2004-03-09
AP1544A (en) 2006-01-12
BG66371B1 (bg) 2013-10-31
OA12464A (en) 2006-05-24
NZ528954A (en) 2005-04-29
KR20030090719A (ko) 2003-11-28
HRP20030905A2 (en) 2005-08-31
IL158092A0 (en) 2004-03-28

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