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
- 239000004030 hiv protease inhibitor Substances 0.000 title abstract 2
- SPKYQJAFIYJJOX-UHFFFAOYSA-N 2-oxo-3h-indole-1-sulfonamide Chemical class C1=CC=C2N(S(=O)(=O)N)C(=O)CC2=C1 SPKYQJAFIYJJOX-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 238000009007 Diagnostic Kit Methods 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 229940124522 antiretrovirals Drugs 0.000 abstract 1
- 239000003903 antiretrovirus agent Substances 0.000 abstract 1
- 238000003556 assay Methods 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Tropical Medicine & Parasitology (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)
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 |
| MXPA06010365A (es) * | 2004-03-11 | 2007-05-04 | Sequoia Pharmaceuticals Inc | Inhibidores de proteasa retrovirales repelentes a la resistencia. |
| AU2005244121B2 (en) * | 2004-05-07 | 2012-01-19 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
| 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 |
| US8829208B2 (en) | 2010-01-28 | 2014-09-09 | Mapi Pharma Ltd. | Process for the preparation of darunavir and darunavir intermediates |
| 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 |
| CN1110300C (zh) | 1993-10-01 | 2003-06-04 | 阿斯特拉公司 | 工艺技术ⅰ |
| EP0804428B1 (en) * | 1995-01-20 | 2007-12-26 | G.D. Searle LLC. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
| US5756533A (en) | 1995-03-10 | 1998-05-26 | G.D. Searle & Co. | Amino acid 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 |
| US5705500A (en) | 1995-03-10 | 1998-01-06 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| WO1996028465A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| AU7722296A (en) | 1995-11-15 | 1997-06-05 | 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 |
| AP1227A (en) | 1997-03-26 | 2003-11-24 | Janssen Pharmaceutica Nv | Pellets having a core coated with an antifungal and a polymer. |
| 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 |
| AU2012199A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| AP2000001856A0 (en) | 1997-12-24 | 2000-09-30 | Vertex Pharma | Prodrugs of aspartyl protease inhibitors. |
| CA2335477C (en) * | 1998-06-19 | 2010-11-30 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
| 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 |
| 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 |
| EP1272483A2 (en) | 2000-03-24 | 2003-01-08 | Millenium Pharmaceuticals, Inc. | OXINDOLE INHIBITORS OF FACTOR Xa |
-
2003
- 2003-08-14 KR KR1020057001812A patent/KR100994759B1/ko not_active Expired - Fee Related
- 2003-08-14 MX MXPA05001792A patent/MXPA05001792A/es active IP Right Grant
- 2003-08-14 US US10/524,451 patent/US7199148B2/en not_active Expired - Fee Related
- 2003-08-14 EA EA200500350A patent/EA010486B1/ru not_active IP Right Cessation
- 2003-08-14 CA CA2493940A patent/CA2493940C/en not_active Expired - Fee Related
- 2003-08-14 NZ NZ538714A patent/NZ538714A/en not_active IP Right Cessation
- 2003-08-14 EP EP03787818A patent/EP1546153A1/en not_active Withdrawn
- 2003-08-14 AP AP2005003245A patent/AP2126A/xx active
- 2003-08-14 CN CN038240955A patent/CN1688586B/zh not_active Expired - Fee Related
- 2003-08-14 AU AU2003262574A patent/AU2003262574B2/en not_active Ceased
- 2003-08-14 HR HRP20050606AA patent/HRP20050606B1/hr not_active IP Right Cessation
- 2003-08-14 JP JP2004528524A patent/JP4681296B2/ja not_active Expired - Fee Related
- 2003-08-14 BR BR0305771-2A patent/BR0305771A/pt not_active IP Right Cessation
- 2003-08-14 WO PCT/EP2003/050379 patent/WO2004016619A1/en not_active Ceased
- 2003-08-14 PL PL03375307A patent/PL375307A1/xx unknown
-
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
Also Published As
| Publication number | Publication date |
|---|---|
| JP2005537305A (ja) | 2005-12-08 |
| KR100994759B1 (ko) | 2010-11-16 |
| CN1688586A (zh) | 2005-10-26 |
| BR0305771A (pt) | 2004-10-05 |
| CA2493940C (en) | 2011-11-22 |
| NO20051291L (no) | 2005-05-18 |
| AU2003262574A1 (en) | 2004-03-03 |
| HRP20050606B1 (hr) | 2014-04-25 |
| ZA200501223B (en) | 2006-07-26 |
| NO331846B1 (no) | 2012-04-23 |
| AP2126A (en) | 2010-06-03 |
| CA2493940A1 (en) | 2004-02-26 |
| KR20050042141A (ko) | 2005-05-04 |
| WO2004016619A1 (en) | 2004-02-26 |
| IL166462A0 (en) | 2006-01-15 |
| HRP20050606A2 (en) | 2006-02-28 |
| PL375307A1 (en) | 2005-11-28 |
| IL166462A (en) | 2012-04-30 |
| EA010486B1 (ru) | 2008-10-30 |
| AP2005003245A0 (en) | 2005-03-31 |
| US20060058368A1 (en) | 2006-03-16 |
| CN1688586B (zh) | 2012-05-09 |
| EA200500350A1 (ru) | 2005-08-25 |
| EP1546153A1 (en) | 2005-06-29 |
| JP4681296B2 (ja) | 2011-05-11 |
| NZ538714A (en) | 2007-03-30 |
| AU2003262574B2 (en) | 2009-07-09 |
| US7199148B2 (en) | 2007-04-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |