MXPA05001792A - Oxindolsulfonamida sustituida como inhibidores de proteasa de virus de inmunodeficiencia humana de amplio espectro. - Google Patents
Oxindolsulfonamida sustituida como inhibidores de proteasa de virus de inmunodeficiencia humana de amplio espectro.Info
- Publication number
- MXPA05001792A MXPA05001792A MXPA05001792A MXPA05001792A MXPA05001792A MX PA05001792 A MXPA05001792 A MX PA05001792A MX PA05001792 A MXPA05001792 A MX PA05001792A MX PA05001792 A MXPA05001792 A MX PA05001792A MX PA05001792 A MXPA05001792 A MX PA05001792A
- Authority
- MX
- Mexico
- Prior art keywords
- 6alkyl
- formula
- het
- optionally substituted
- 6alkenyl
- 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
La presente invencion se refiere a los compuestos que tienen la formula (1) N-oxidos, sales, formas estereoisomericas, mezclas racemicas, profarmacos, esteres y metabolitos de los mismos, en donde R1 y R8, son II, alquilo de C1-6 opcionalmente sustituido, alquenilo de C2-6, cicloalquilo de C3-7, arilo, Het1, Het2 R1 tambien puede ser un radical de la formula (R11aR11b)NC(R10aR10b)CR9 t es 0, 1 o 2; R2 es H o alquilo de C1-6; L es -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-alcanodiilo de C1-6-C(=O)-, -NR8- alcanodiilo de C1-6-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2; R3 es alquilo de C1-6, arilo, cicloalquilo de C3-7, cicloalquilo de C3-7-alquilo de C1-4, o arilo-alquilo de C1-4 R1. es H, alquilo de C1-4OC(=O), carboxi, aminoC(=O), mono- o di(alquilo de C1-4)aminoC(=O), cicloalquilo de C3-7, alquenhlo de C2-6, alquinilo de C2-6 o alquilo de C1-6 opcionalmente sustituido; la formula (II) es la formula (III) o la formula (IV); R5a y R5b es alquenilo de C2-6, alquinilo de C2-6, cicloalquilo de C3-7 o alquilo de C1-6, opcionalmente sustituido en uno o mas atomos; R5a y R5b tambien pueden ser hidrogeno, arilo, Het1, Het2 R6 es hidrogeno o alquilo de C1-6 opcionalmente sustituido, en uno o mas atomos de carbono; ademas, se refiere a su uso como inhibidores de proteasa de VIH de amplio espectro, procedimientos para su preparacion asi como composiciones farmaceuticas y equipos de diagnostico que los comprenden; tambien se refiere a combinaciones de los mismos con otro agente antirretroviral, y a su uso en ensayos como compuestos de referencia o como reactivos.
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 (1)
| Publication Number | Publication Date |
|---|---|
| MXPA05001792A true MXPA05001792A (es) | 2005-04-25 |
Family
ID=31725465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA05001792A MXPA05001792A (es) | 2002-08-14 | 2003-08-14 | Oxindolsulfonamida sustituida como inhibidores de proteasa de virus de inmunodeficiencia humana de amplio espectro. |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7199148B2 (es) |
| EP (1) | EP1546153A1 (es) |
| JP (1) | JP4681296B2 (es) |
| KR (1) | KR100994759B1 (es) |
| CN (1) | CN1688586B (es) |
| AP (1) | AP2126A (es) |
| AU (1) | AU2003262574B2 (es) |
| BR (1) | BR0305771A (es) |
| CA (1) | CA2493940C (es) |
| EA (1) | EA010486B1 (es) |
| HR (1) | HRP20050606B1 (es) |
| IL (1) | IL166462A (es) |
| MX (1) | MXPA05001792A (es) |
| NO (1) | NO331846B1 (es) |
| NZ (1) | NZ538714A (es) |
| PL (1) | PL375307A1 (es) |
| WO (1) | WO2004016619A1 (es) |
| ZA (1) | ZA200501223B (es) |
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 |
| 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 |
| EA200500350A1 (ru) | 2005-08-25 |
| 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 |
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