EA200500350A1 - Замещенные оксиндолсульфонамидные ингибиторы вич-протеазы широкого спектра действия - Google Patents
Замещенные оксиндолсульфонамидные ингибиторы вич-протеазы широкого спектра действияInfo
- Publication number
- EA200500350A1 EA200500350A1 EA200500350A EA200500350A EA200500350A1 EA 200500350 A1 EA200500350 A1 EA 200500350A1 EA 200500350 A EA200500350 A EA 200500350A EA 200500350 A EA200500350 A EA 200500350A EA 200500350 A1 EA200500350 A1 EA 200500350A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- formula
- het
- optionally substituted
- cycloalkyl
- 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
-
- 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
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (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)
Abstract
Настоящее изобретение относится к соединениям, имеющим формулу (I), их N-оксидам, солям, стереоизомерным формам, рацемическим смесям, пролекарствам, сложным эфирам и метаболитам, где Rи Rкаждый означает H, необязательно замещенный Cалкил, Cалкенил, Cциклоалкил, арил, Het, Het; Rможет также обозначать радикал формулы (RR)NC(RR)CR-; t равно 0, 1 или 2; Rозначает H или Cалкил; L означает -C(=O)-, -O-C(=O)-, -NR-C(=O)-, -O-Cалкандиил-C(=O)-, -NR-Cалкандиил-C(=O)-, -S(=O)-, -O-S(=O)-, -NR-S(=O); Rозначает Cалкил, арил, Cциклоалкил, CциклоалкилCалкил или арилCалкил; Rозначает H, CалкилOC(=O), карбоксил, аминоC(=O), моно- или ди(Cалкил)аминоC(=O), Cциклоалкил, Cалкенил, Cалкинил или необязательно замещенный Cалкил; формула (II) представляет формулу (III) или формулу (IV); Rи Rозначают Cалкенил, Cалкинил, Cциклоалкил или Cалкил, необязательно замещенный по одному или нескольким атомам; Rи Rмогут также означать водород, арил, Het, Het; Rозначает водород или Cалкил, необязательно замещенный по одному или нескольким атомам углерода. Оно также относится к применению ингибиторов ВИЧ-протеазы широкого спектра действия, способам их получения, а также содержащим их фармацевтическим композициям и диагностическим наборам. Оно также относится к их комбинациям с другим антиретровирусным агентом и их применению в анализах в качестве соединений для сравнения или в качестве агентов.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02078384 | 2002-08-14 | ||
| PCT/EP2003/050379 WO2004016619A1 (en) | 2002-08-14 | 2003-08-14 | Broadspectrum substituted oxindole sulfonamide hiv protease inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200500350A1 true EA200500350A1 (ru) | 2005-08-25 |
| EA010486B1 EA010486B1 (ru) | 2008-10-30 |
Family
ID=31725465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200500350A EA010486B1 (ru) | 2002-08-14 | 2003-08-14 | Замещенные оксиндолсульфонамидные ингибиторы вич-протеазы широкого спектра действия |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7199148B2 (ru) |
| EP (1) | EP1546153A1 (ru) |
| JP (1) | JP4681296B2 (ru) |
| KR (1) | KR100994759B1 (ru) |
| CN (1) | CN1688586B (ru) |
| AP (1) | AP2126A (ru) |
| AU (1) | AU2003262574B2 (ru) |
| BR (1) | BR0305771A (ru) |
| CA (1) | CA2493940C (ru) |
| EA (1) | EA010486B1 (ru) |
| HR (1) | HRP20050606B1 (ru) |
| IL (1) | IL166462A (ru) |
| MX (1) | MXPA05001792A (ru) |
| NO (1) | NO331846B1 (ru) |
| NZ (1) | NZ538714A (ru) |
| PL (1) | PL375307A1 (ru) |
| WO (1) | WO2004016619A1 (ru) |
| ZA (1) | ZA200501223B (ru) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1472536A4 (en) * | 2002-01-07 | 2007-02-14 | Sequoia Pharmaceuticals | VERSATILE INHIBITORS |
| EP1732891A4 (en) * | 2004-03-11 | 2009-05-06 | Sequoia Pharmaceuticals Inc | RESISTANT PREVENTIVE INHIBITORS FOR RETROVIRAL PROTEASES |
| MXPA06012909A (es) * | 2004-05-07 | 2007-09-06 | Sequoia Pharmaceuticals Inc | Inhibidores de proteasa retroviral repelente de resistencia. |
| TWI482775B (zh) | 2008-09-01 | 2015-05-01 | Tibotec Pharm Ltd | 用於製備（３ｒ，３ａｓ，６ａｒ）－六氫呋喃并〔２，３－ｂ〕呋喃－３－基（１ｓ，２ｒ）－３－〔〔（４－胺基苯基）磺醯基〕（異丁基）胺基〕－１－苯甲基－２－羥基丙基胺基甲酸酯之方法 |
| US8921415B2 (en) | 2009-01-29 | 2014-12-30 | Mapi Pharma Ltd. | Polymorphs of darunavir |
| PL2528923T3 (pl) | 2010-01-28 | 2015-01-30 | Mapi Pharma Ltd | Sposób wytwarzania darunawiru i pochodnych darunawiru |
| US8580294B2 (en) | 2010-10-19 | 2013-11-12 | International Partnership For Microbicides | Platinum-catalyzed intravaginal rings |
| WO2012092168A1 (en) * | 2010-12-27 | 2012-07-05 | Purdue Research Foundation | Fused 6,5 bicyclic ring system p2 ligands, and methods for treating hiv |
| WO2012092188A1 (en) * | 2010-12-27 | 2012-07-05 | Ghosh Arun K | Hydrogen bond forming p1 ligands and methods for treating hiv |
| US10137031B2 (en) | 2013-11-14 | 2018-11-27 | International Partnership For Microbicides, Inc. | Combination therapy intravaginal rings |
| EP3192794A4 (en) * | 2014-09-11 | 2018-06-27 | Shionogi & Co., Ltd. | Sustained hiv protease inhibitor |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| 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 |
| US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
| DK0715618T3 (da) | 1993-08-24 | 1999-08-23 | Searle & Co | Hydroxyethylaminosulfonamider til anvendelse som inhibitorer af retrovirale proteaser |
| IL111080A (en) | 1993-10-01 | 1999-08-17 | Astra Ab | Method for treating a finely divided powder medicament |
| DE69637380T2 (de) * | 1995-01-20 | 2009-09-17 | G.D. Searle Llc, Chicago | Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen |
| US5756533A (en) | 1995-03-10 | 1998-05-26 | G.D. Searle & Co. | 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 |
| US6150556A (en) | 1995-03-10 | 2000-11-21 | G. D. Dearle & Co. | Bis-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 |
| 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 |
| KR19990044257A (ko) | 1996-05-20 | 1999-06-25 | 디르크 반테 | 생체이용율이 개선된 항진균성 조성물 |
| 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 |
| EP1042280A2 (en) | 1997-12-24 | 2000-10-11 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| AU2012199A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| WO1999033792A2 (en) | 1997-12-24 | 1999-07-08 | Vertex Pharmaceuticals Incorporated | Prodrugs os aspartyl protease inhibitors |
| US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
| AP1717A (en) * | 1998-06-19 | 2007-01-30 | Vertex Pharma | Sulfonamide inhibitors of aspartyl protease. |
| 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 |
| ES2362404T5 (es) | 1998-06-23 | 2015-11-25 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Ensayo de aptitud y métodos para reducir la resistencia del VIH a terapia |
| EP1272483A2 (en) * | 2000-03-24 | 2003-01-08 | Millenium Pharmaceuticals, Inc. | OXINDOLE INHIBITORS OF FACTOR Xa |
-
2003
- 2003-08-14 NZ NZ538714A patent/NZ538714A/en not_active IP Right Cessation
- 2003-08-14 WO PCT/EP2003/050379 patent/WO2004016619A1/en active Application Filing
- 2003-08-14 MX MXPA05001792A patent/MXPA05001792A/es active IP Right Grant
- 2003-08-14 BR BR0305771-2A patent/BR0305771A/pt not_active IP Right Cessation
- 2003-08-14 CN CN038240955A patent/CN1688586B/zh not_active Expired - Fee Related
- 2003-08-14 EA EA200500350A patent/EA010486B1/ru not_active IP Right Cessation
- 2003-08-14 PL PL03375307A patent/PL375307A1/xx unknown
- 2003-08-14 CA CA2493940A patent/CA2493940C/en not_active Expired - Fee Related
- 2003-08-14 EP EP03787818A patent/EP1546153A1/en not_active Withdrawn
- 2003-08-14 AP AP2005003245A patent/AP2126A/xx active
- 2003-08-14 JP JP2004528524A patent/JP4681296B2/ja not_active Expired - Fee Related
- 2003-08-14 KR KR1020057001812A patent/KR100994759B1/ko not_active IP Right Cessation
- 2003-08-14 US US10/524,451 patent/US7199148B2/en not_active Expired - Fee Related
- 2003-08-14 AU AU2003262574A patent/AU2003262574B2/en not_active Ceased
-
2005
- 2005-01-24 IL IL166462A patent/IL166462A/en not_active IP Right Cessation
- 2005-02-10 ZA ZA200501223A patent/ZA200501223B/en unknown
- 2005-03-14 NO NO20051291A patent/NO331846B1/no not_active IP Right Cessation
- 2005-06-29 HR HRP20050606AA patent/HRP20050606B1/hr not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003262574B2 (en) | 2009-07-09 |
| HRP20050606B1 (hr) | 2014-04-25 |
| US20060058368A1 (en) | 2006-03-16 |
| NZ538714A (en) | 2007-03-30 |
| US7199148B2 (en) | 2007-04-03 |
| PL375307A1 (en) | 2005-11-28 |
| ZA200501223B (en) | 2006-07-26 |
| IL166462A (en) | 2012-04-30 |
| CA2493940A1 (en) | 2004-02-26 |
| HRP20050606A2 (en) | 2006-02-28 |
| IL166462A0 (en) | 2006-01-15 |
| WO2004016619A1 (en) | 2004-02-26 |
| EA010486B1 (ru) | 2008-10-30 |
| EP1546153A1 (en) | 2005-06-29 |
| MXPA05001792A (es) | 2005-04-25 |
| NO20051291L (no) | 2005-05-18 |
| KR20050042141A (ko) | 2005-05-04 |
| CA2493940C (en) | 2011-11-22 |
| KR100994759B1 (ko) | 2010-11-16 |
| NO331846B1 (no) | 2012-04-23 |
| AU2003262574A1 (en) | 2004-03-03 |
| CN1688586A (zh) | 2005-10-26 |
| AP2005003245A0 (en) | 2005-03-31 |
| CN1688586B (zh) | 2012-05-09 |
| JP2005537305A (ja) | 2005-12-08 |
| JP4681296B2 (ja) | 2011-05-11 |
| AP2126A (en) | 2010-06-03 |
| BR0305771A (pt) | 2004-10-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 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 |
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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): KZ RU |