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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (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 |
|---|---|---|---|---|
| CA2472580A1 (en) * | 2002-01-07 | 2003-07-17 | Sequoia Pharmaceuticals | Broad spectrum inhibitors |
| EP1732891A4 (en) * | 2004-03-11 | 2009-05-06 | Sequoia Pharmaceuticals Inc | RESISTANT PREVENTIVE INHIBITORS FOR RETROVIRAL PROTEASES |
| EP2422780A1 (en) * | 2004-05-07 | 2012-02-29 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
| AR073248A1 (es) | 2008-09-01 | 2010-10-20 | Tibotec Pharm Ltd | Proceso para la preparacion de (1s, 2r)-3- ((4-aminofenil) sulfonil) ( isobutil) amino)-1- bencil-2- hidroxipropilcarbamato de (3r, 3as,6ar)- hexahidrofuro-(2,3-b) furan-3- ilo (darunavir) y compuestos intermediarios utiles en dicho proceso. |
| US8921415B2 (en) | 2009-01-29 | 2014-12-30 | Mapi Pharma Ltd. | Polymorphs of darunavir |
| JP2013518096A (ja) | 2010-01-28 | 2013-05-20 | マピ ファーマ リミテッド | ダルナビル及びダルナビル中間体の調製方法 |
| 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 |
| JPWO2016039403A1 (ja) * | 2014-09-11 | 2017-06-29 | 塩野義製薬株式会社 | 持続性ｈｉｖプロテアーゼ阻害剤 |
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 |
| WO1995006030A1 (en) | 1993-08-24 | 1995-03-02 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
| 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 |
| BR9407686A (pt) | 1993-10-01 | 1997-02-04 | Astra Ab | Processo e aparelho para o tratamento de um medicamento em pó finamente dividido uso do aparelho e aglomerados |
| 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 |
| PL184771B1 (pl) | 1995-03-10 | 2002-12-31 | Searle & Co | Związek stanowiący hydroksyetyloaminosulfonamid pirolidynokarbonyloaminokwasu, kompozycja zawierająca ten związek, jego zastosowanie do wytwarzania kompozycji do leczenia infekcji retrowirusowej i sposób zapobiegania replikacji retrowirusa in vitro |
| EP0861249A1 (en) | 1995-11-15 | 1998-09-02 | G.D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| ATE255883T1 (de) | 1996-05-20 | 2003-12-15 | Janssen Pharmaceutica Nv | Fungizide mittel mit verbesserter bioverfügbarkeit |
| HU224217B1 (hu) | 1997-03-26 | 2005-06-28 | Janssen Pharmaceutica N.V. | Gombaellenes hatóanyaggal és polimerrel bevont magrészt tartalmazó pelletek |
| AU2012199A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
| WO1999033792A2 (en) | 1997-12-24 | 1999-07-08 | Vertex Pharmaceuticals Incorporated | Prodrugs os aspartyl protease inhibitors |
| JP2001527062A (ja) | 1997-12-24 | 2001-12-25 | バーテックス ファーマシューティカルズ インコーポレイテッド | アスパルチルプロテアーゼインヒビターのプロドラッグ |
| CA2335477C (en) * | 1998-06-19 | 2010-11-30 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
| 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 |
| EP1088098B2 (en) | 1998-06-23 | 2015-07-01 | THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES | Fitness assay and methods for reducing resistance of hiv to therapy |
| WO2001072708A2 (en) * | 2000-03-24 | 2001-10-04 | Cor Therapeutics, Inc. | OXINDOLE INHIBITORS OF FACTOR Xa |
-
2003
- 2003-08-14 WO PCT/EP2003/050379 patent/WO2004016619A1/en active Application Filing
- 2003-08-14 CN CN038240955A patent/CN1688586B/zh not_active Expired - Fee Related
- 2003-08-14 AP AP2005003245A patent/AP2126A/xx active
- 2003-08-14 EA EA200500350A patent/EA010486B1/ru not_active IP Right Cessation
- 2003-08-14 AU AU2003262574A patent/AU2003262574B2/en not_active Ceased
- 2003-08-14 MX MXPA05001792A patent/MXPA05001792A/es active IP Right Grant
- 2003-08-14 JP JP2004528524A patent/JP4681296B2/ja not_active Expired - Fee Related
- 2003-08-14 US US10/524,451 patent/US7199148B2/en not_active Expired - Fee Related
- 2003-08-14 PL PL03375307A patent/PL375307A1/xx unknown
- 2003-08-14 EP EP03787818A patent/EP1546153A1/en not_active Withdrawn
- 2003-08-14 CA CA2493940A patent/CA2493940C/en not_active Expired - Fee Related
- 2003-08-14 BR BR0305771-2A patent/BR0305771A/pt not_active IP Right Cessation
- 2003-08-14 NZ NZ538714A patent/NZ538714A/en not_active IP Right Cessation
- 2003-08-14 KR KR1020057001812A patent/KR100994759B1/ko not_active IP Right Cessation
-
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 |
|---|---|
| AP2126A (en) | 2010-06-03 |
| ZA200501223B (en) | 2006-07-26 |
| NO20051291L (no) | 2005-05-18 |
| HRP20050606A2 (en) | 2006-02-28 |
| IL166462A0 (en) | 2006-01-15 |
| MXPA05001792A (es) | 2005-04-25 |
| WO2004016619A1 (en) | 2004-02-26 |
| HRP20050606B1 (hr) | 2014-04-25 |
| NZ538714A (en) | 2007-03-30 |
| AP2005003245A0 (en) | 2005-03-31 |
| EA010486B1 (ru) | 2008-10-30 |
| IL166462A (en) | 2012-04-30 |
| CA2493940C (en) | 2011-11-22 |
| CN1688586A (zh) | 2005-10-26 |
| NO331846B1 (no) | 2012-04-23 |
| EP1546153A1 (en) | 2005-06-29 |
| KR20050042141A (ko) | 2005-05-04 |
| JP2005537305A (ja) | 2005-12-08 |
| CN1688586B (zh) | 2012-05-09 |
| AU2003262574B2 (en) | 2009-07-09 |
| US7199148B2 (en) | 2007-04-03 |
| PL375307A1 (en) | 2005-11-28 |
| BR0305771A (pt) | 2004-10-05 |
| CA2493940A1 (en) | 2004-02-26 |
| US20060058368A1 (en) | 2006-03-16 |
| KR100994759B1 (ko) | 2010-11-16 |
| JP4681296B2 (ja) | 2011-05-11 |
| AU2003262574A1 (en) | 2004-03-03 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EA200400387A1 (ru) | Азабициклические замещённые конденсированные гетероарильные соединения для лечения заболеваний | |
| AR040773A1 (es) | Pirazoles utiles como inhibidores de gsk-3 | |
| BG93979A (bg) | Производни на n-(4-пиперидинил)(дихидробензофуран или дихидро-2н-бензопиран)карбоксамид, фармацевтичен състав, който ги съдържа, метод за получаване на производните и приложението им | |
| PE20040164A1 (es) | Mimeticos de glucocorticoides, procedimientos para su preparacion y composiciones farmaceuticas | |
| AR047076A1 (es) | Compuestos de pirrolotriazina como inhibidores de tirosina quinasas, composiciones farmaceuticas | |
| ATE349417T1 (de) | 5-aminolaevulinsäure-ester als mittel zur photosensibilisierung in der chemotherapie | |
| AR047744A1 (es) | Compuestos de triazol y su uso como antagonistas del receptor de glutamato metabotropico | |
| AR052458A1 (es) | Amino-imidazolonas para la inhibicion de beta-secretasa | |
| HUP0402454A2 (hu) | Szubsztituált kinazolinszármazékok mint az aurora kinázok inhibitorai, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények | |
| EA200870321A1 (ru) | Способ получения 4-оксохинолинового соединения | |
| EA200500350A1 (ru) | Замещенные оксиндолсульфонамидные ингибиторы вич-протеазы широкого спектра действия | |
| AR047339A1 (es) | Derivados de difenilazetidona.proceso de obtencion. | |
| AR054482A1 (es) | Derivados de azetidinona para el tratamiento de hiperlipidemias | |
| EA200300891A1 (ru) | Ингибиторы протеазы вич широкого спектра действия на основе сульфонамидов 2-(замещенных-амино) бензотиазолов | |
| EA200601178A1 (ru) | Морфолинилсодержащие бензимидазолы в качестве ингибиторов репликации респираторно-синцитиального вируса | |
| DE602006008962D1 (de) | Verfahren zur herstellung von valsartan | |
| EA200301234A1 (ru) | 2-аминобензоксазолсульфонамидные ингибиторы вич-протеазы широкого спектра | |
| BRPI0408160B1 (pt) | Processo para o preparo de ésteres do ácido nicotínico substituído e intermediários de enamina para uso nesse processo | |
| EA200500122A1 (ru) | Новые соединения, фармацевтические композиции, содержащие их, и способы их использования | |
| PE20040929A1 (es) | Amidas de acido 5-aminometil-1h-pirrol-2-carboxilico substituidas | |
| RU2008143546A (ru) | Тиазолилдигидрохиназолины | |
| MY135226A (en) | Broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors | |
| MXPA04008926A (es) | Inhibidores de entrada a moleculas pequenas. | |
| EA200301110A1 (ru) | 2-(замещенный амино) бензоксазолсульфонамидные ингибиторы вич-протеазы широкого спектра | |
| EA200500298A1 (ru) | 2-аминобензотиазолсульфонамидные ингибиторы протеазы вич широкого спектра действия |
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 |
|
| 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 |