EA200300891A1 - Ингибиторы протеазы вич широкого спектра действия на основе сульфонамидов 2-(замещенных-амино) бензотиазолов - Google Patents
Ингибиторы протеазы вич широкого спектра действия на основе сульфонамидов 2-(замещенных-амино) бензотиазоловInfo
- Publication number
- EA200300891A1 EA200300891A1 EA200300891A EA200300891A EA200300891A1 EA 200300891 A1 EA200300891 A1 EA 200300891A1 EA 200300891 A EA200300891 A EA 200300891A EA 200300891 A EA200300891 A EA 200300891A EA 200300891 A1 EA200300891 A1 EA 200300891A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- het
- calkandiyl
- amino
- aryl
- Prior art date
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)
Abstract
Настоящее изобретение относится к соединениям, имеющим формулу (I), их N-оксидам, солям, стереоизомерам, рацемическим смесям, пролекарствам, эфирам и метаболитам, в которой Rи R,каждый независимо, представляет H, необязательно замещенный Cалкил, Cалкенил, Cциклоалкил, арил, Het, Het; Rтакже может быть радикалом формулы (RR)NC(RR)CR; t независимо равен 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 Cалкилокси, Het, HetO, Het, HetO, арил, арилокси, Cалкилоксикарбониламино или амино; и в случае, когда -A- представляет другую группу, чем Cалкандиил, то тогда Rможет быть также Cалкилом, HetCалкилом, HetоксиCалкилом, HetCалкилом, HetоксиCалкилом, арилCалкилом, арилоксиCалкилом или аминоCалкилом; где каждая из аминогрупп при определении Rможет быть необязательно замещенной; Rи -A-R, взятые вместе с атомом азота, с которым они связаны, могут также образовать Hetили Het. Также оно относится к применению в качестве ингибиторов протеазы ВИЧ широкого спектра действия, способам их получения, а также фармацевтическим композициям и диагностически наборам, включающим их. Также оно относится к их комбинациям с другими противоретровирусными средствами и к их применению в тестах в качестве стандартов или реагентов.Отчет о международном поиске был опубликован 2003.02.13.
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 |
---|---|
EA200300891A1 true EA200300891A1 (ru) | 2004-02-26 |
EA006096B1 EA006096B1 (ru) | 2005-08-25 |
Family
ID=26076833
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200300891A EA006096B1 (ru) | 2001-02-14 | 2002-02-14 | Ингибиторы протеазы вич широкого спектра действия на основе сульфонамидов 2-(замещенных-амино)бензотиазолов |
Country Status (31)
Country | Link |
---|---|
US (1) | US7659404B2 (ru) |
EP (1) | EP1370543B1 (ru) |
JP (1) | JP4530612B2 (ru) |
KR (1) | KR100870184B1 (ru) |
CN (2) | CN100369904C (ru) |
AP (1) | AP1504A (ru) |
AT (1) | ATE343567T1 (ru) |
AU (1) | AU2002302363B2 (ru) |
BG (1) | BG66301B1 (ru) |
BR (1) | BR0207862A (ru) |
CA (1) | CA2438304C (ru) |
CY (1) | CY1108073T1 (ru) |
CZ (1) | CZ304273B6 (ru) |
DE (1) | DE60215623T2 (ru) |
DK (1) | DK1370543T3 (ru) |
EA (1) | EA006096B1 (ru) |
EE (1) | EE05385B1 (ru) |
ES (1) | ES2275866T3 (ru) |
HK (1) | HK1061233A1 (ru) |
HR (1) | HRP20030735B1 (ru) |
HU (1) | HU229224B1 (ru) |
IL (2) | IL157171A0 (ru) |
MX (1) | MXPA03007236A (ru) |
NO (1) | NO326174B1 (ru) |
NZ (1) | NZ527391A (ru) |
PL (1) | PL213327B1 (ru) |
PT (1) | PT1370543E (ru) |
SI (1) | SI1370543T1 (ru) |
SK (1) | SK287582B6 (ru) |
WO (1) | WO2002083657A2 (ru) |
ZA (1) | ZA200306086B (ru) |
Families Citing this family (21)
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ATE302287T1 (de) | 1999-05-28 | 2005-09-15 | Virco Nv | Neue mutationsprofile der hiv-1 reverse transcriptase in verbindung mit phänotypischem medikamentresistenz |
AU2002226316B2 (en) | 2000-10-20 | 2008-06-26 | Virco Bvba | Mutational profiles in HIV-1 reverse transcriptase correlated with phenotypic drug resistance |
EE05385B1 (et) | 2001-02-14 | 2011-02-15 | Tibotec�Pharmaceuticals�Ltd. | LaiaspektrilisedÁ2-(asendatudÁamino)bensotiasoolsulfoonamiididÁkuiÁHIVÁproteaasiÁinhibiitorid,ÁnendeÁvalmistamismeetodÁjaÁkasutamineÁningÁfarmatseutilineÁkompositsioon |
EP1483254A4 (en) | 2002-01-07 | 2005-06-08 | Sequoia Pharmaceuticals | INHIBITORS OF ANTI-RESISTANCE RETROVIRAL PROTEASE |
US7157489B2 (en) | 2002-03-12 | 2007-01-02 | The Board Of Trustees Of The University Of Illinois | HIV protease inhibitors |
WO2004003223A2 (en) | 2002-07-01 | 2004-01-08 | Tibotec Pharmaceuticals Ltd. | New mutational profiles in hiv-1 reverse transcriptase correlated with phenotypic drug resistance |
CA2490862A1 (en) | 2002-07-01 | 2004-01-08 | Tibotec Pharmaceuticals Ltd. | Mutational profiles in hiv-1 protease correlated with phenotypic drug resistance |
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 |
DE602004004674T2 (de) * | 2003-09-30 | 2007-11-22 | Tibotec Pharmaceuticals Ltd. | Verfahren zur herstellung von benzoxazolsulfonamidverbindungen und zwischenprodukten davon |
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 |
JP5260965B2 (ja) | 2005-02-25 | 2013-08-14 | テイボテク・フアーマシユーチカルズ | プロテアーゼ阻害剤前駆体合成 |
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 |
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PL341762A1 (en) | 1997-12-24 | 2001-05-07 | Vertex Pharma | Precursors of aspartil protease inhibitors |
WO1999033795A1 (en) | 1997-12-24 | 1999-07-08 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
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CA2336160C (en) * | 1998-06-23 | 2015-02-17 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Use of compounds for treating hiv |
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 |
EE05385B1 (et) | 2001-02-14 | 2011-02-15 | Tibotec�Pharmaceuticals�Ltd. | LaiaspektrilisedÁ2-(asendatudÁamino)bensotiasoolsulfoonamiididÁkuiÁHIVÁproteaasiÁinhibiitorid,ÁnendeÁvalmistamismeetodÁjaÁkasutamineÁningÁfarmatseutilineÁkompositsioon |
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2002
- 2002-02-14 EE EEP200300381A patent/EE05385B1/xx not_active IP Right Cessation
- 2002-02-14 EA EA200300891A patent/EA006096B1/ru not_active IP Right Cessation
- 2002-02-14 CZ CZ2003-2415A patent/CZ304273B6/cs not_active IP Right Cessation
- 2002-02-14 DE DE60215623T patent/DE60215623T2/de not_active Expired - Lifetime
- 2002-02-14 CN CNB028049829A patent/CN100369904C/zh not_active Expired - Fee Related
- 2002-02-14 BR BR0207862-7A patent/BR0207862A/pt not_active IP Right Cessation
- 2002-02-14 CN CN2007101997173A patent/CN101230067B/zh not_active Expired - Fee Related
- 2002-02-14 PL PL363778A patent/PL213327B1/pl unknown
- 2002-02-14 MX MXPA03007236A patent/MXPA03007236A/es active IP Right Grant
- 2002-02-14 NZ NZ527391A patent/NZ527391A/xx not_active IP Right Cessation
- 2002-02-14 PT PT02729930T patent/PT1370543E/pt unknown
- 2002-02-14 JP JP2002581413A patent/JP4530612B2/ja not_active Expired - Fee Related
- 2002-02-14 IL IL15717102A patent/IL157171A0/xx unknown
- 2002-02-14 SK SK1102-2003A patent/SK287582B6/sk not_active IP Right Cessation
- 2002-02-14 ES ES02729930T patent/ES2275866T3/es not_active Expired - Lifetime
- 2002-02-14 SI SI200230467T patent/SI1370543T1/sl unknown
- 2002-02-14 AP APAP/P/2003/002856A patent/AP1504A/en active
- 2002-02-14 CA CA2438304A patent/CA2438304C/en not_active Expired - Fee Related
- 2002-02-14 DK DK02729930T patent/DK1370543T3/da active
- 2002-02-14 US US10/467,609 patent/US7659404B2/en not_active Expired - Fee Related
- 2002-02-14 EP EP02729930A patent/EP1370543B1/en not_active Expired - Lifetime
- 2002-02-14 WO PCT/EP2002/001788 patent/WO2002083657A2/en active IP Right Grant
- 2002-02-14 AU AU2002302363A patent/AU2002302363B2/en not_active Ceased
- 2002-02-14 HU HU0303257A patent/HU229224B1/hu not_active IP Right Cessation
- 2002-02-14 KR KR1020037010506A patent/KR100870184B1/ko not_active IP Right Cessation
- 2002-02-14 AT AT02729930T patent/ATE343567T1/de active
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2003
- 2003-07-30 IL IL157171A patent/IL157171A/en not_active IP Right Cessation
- 2003-08-06 ZA ZA2003/06086A patent/ZA200306086B/en unknown
- 2003-08-13 NO NO20033584A patent/NO326174B1/no not_active IP Right Cessation
- 2003-09-01 BG BG108143A patent/BG66301B1/bg unknown
- 2003-09-12 HR HR20030735A patent/HRP20030735B1/xx not_active IP Right Cessation
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2004
- 2004-06-03 HK HK04104020A patent/HK1061233A1/xx not_active IP Right Cessation
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2007
- 2007-01-25 CY CY20071100088T patent/CY1108073T1/el unknown
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