NO20051291L - Bredspektrede substituerte oksindol-sulfonamid HIV-proteaseinhibitorer - Google Patents
Bredspektrede substituerte oksindol-sulfonamid HIV-proteaseinhibitorerInfo
- Publication number
- NO20051291L NO20051291L NO20051291A NO20051291A NO20051291L NO 20051291 L NO20051291 L NO 20051291L NO 20051291 A NO20051291 A NO 20051291A NO 20051291 A NO20051291 A NO 20051291A NO 20051291 L NO20051291 L NO 20051291L
- Authority
- NO
- Norway
- Prior art keywords
- alkyl
- protease inhibitors
- cycloalkyl
- hiv protease
- wide
- Prior art date
Links
- 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 abstract 2
- 239000004030 hiv protease inhibitor Substances 0.000 title abstract 2
- 238000001228 spectrum Methods 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- -1 C-cycloalkyl Chemical group 0.000 abstract 1
- 238000009007 Diagnostic Kit Methods 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 229940121375 antifungal agent Drugs 0.000 abstract 1
- 239000003429 antifungal agent Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 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
- 239000000137 peptide hydrolase inhibitor 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- Medicinal Chemistry (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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (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
Substituerte oksindol-sulfonamid HIV-. proteaseinhibitorer.oreliggende oppfinnelse vedrører forbindelsene med. formelen. N-oksider, salter, stereoisomere former, racemiske blandinger, promedikamenter, estere og metabolitter derav, hvori Ri og Rhver er H, eventuelt substituert C-alkyl, C.alkenyl, C-cykloalkyl, aryl. Ht, HetRi kan også være et radikal med formel (RiuRub) NC (R10lRiob) CR9-; t er 0, 1 eller 2; Rer H eller C_alkyl; L er -C(=0)-, -0-C{=0)-, -NRa-C (=0) -, -0-Ci-6alkandiyl-C(=0) -, -NR-C-alkandiyl-C(=0)-, -S(=0)-, -0-S(=0)-, -NR-S(=0); Rer Ci-6alkyl, aryl, C.cykloalkyl, C-cykloalkylC-alkyl, eller arylC--alkyl; Rt er H, C1.<alkylOC(=0) , karboksyl, aminoC(=0) , mono- eller di (Cnalkyl) aminoC (=0) , C.cykloalkyl, C.-alkenyl, C.alkynyl eller eventuelt substituert C-alkyl;. Rog Rer C.alkenyl, C.alkynyl, C3_7cykioalkyl eller C-(alkyl, eventuelt substituert på et eller flere atomer; Rog Rkan også være hydrogen, aryl, Het, Het; Rér hydrogen eller C_alkyl eventuelt substituert på et eller flere karbonatomer. Den vedrører videre deres anvendelse som HIV-proteaseinhibitorer i et vidt spekter, fremgangsmåter ved deres fremstilling samt farmasøytiske sammensetninger og diagnostiske utstyrssett omfattende dem. Den vedrører også kombinasjoner derav med et annet anti-
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 |
|---|---|
| NO20051291L true NO20051291L (no) | 2005-05-18 |
| NO331846B1 NO331846B1 (no) | 2012-04-23 |
Family
ID=31725465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20051291A NO331846B1 (no) | 2002-08-14 | 2005-03-14 | Bredspektrede, substituerte oksindol-sulfonamid HIV-proteaseinhibitorer. |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7199148B2 (no) |
| EP (1) | EP1546153A1 (no) |
| JP (1) | JP4681296B2 (no) |
| KR (1) | KR100994759B1 (no) |
| CN (1) | CN1688586B (no) |
| AP (1) | AP2126A (no) |
| AU (1) | AU2003262574B2 (no) |
| BR (1) | BR0305771A (no) |
| CA (1) | CA2493940C (no) |
| EA (1) | EA010486B1 (no) |
| HR (1) | HRP20050606B1 (no) |
| IL (1) | IL166462A (no) |
| MX (1) | MXPA05001792A (no) |
| NO (1) | NO331846B1 (no) |
| NZ (1) | NZ538714A (no) |
| PL (1) | PL375307A1 (no) |
| WO (1) | WO2004016619A1 (no) |
| ZA (1) | ZA200501223B (no) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7109230B2 (en) * | 2002-01-07 | 2006-09-19 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
| WO2005087728A1 (en) * | 2004-03-11 | 2005-09-22 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
| AU2005244121B2 (en) * | 2004-05-07 | 2012-01-19 | 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 |
| 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 |
| US20170253607A1 (en) * | 2014-09-11 | 2017-09-07 | Shionogi & Co., Ltd. | Long-acting 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 |
| ES2127938T3 (es) | 1993-08-24 | 1999-05-01 | Searle & Co | Hidroxietilamino sulfonamidas utiles como inhibidores de proteasas retroviricas. |
| ES2166786T3 (es) | 1993-10-01 | 2002-05-01 | Astrazeneca Ab | Procedimiento i. |
| 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 |
| US5705500A (en) | 1995-03-10 | 1998-01-06 | G.D. Searle & Co. | Sulfonylalkanoylamino 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 |
| US5753660A (en) | 1995-11-15 | 1998-05-19 | G. D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| US6509038B2 (en) | 1996-05-20 | 2003-01-21 | Janssen Pharmaceutica N.V. | Antifungal compositions with improved bioavailability |
| 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 |
| AU2010299A (en) | 1997-12-24 | 1999-07-19 | 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 |
| BR9912169A (pt) * | 1998-06-19 | 2001-04-10 | Vertex Pharma | Inibidores de sulfonamida de protease de aspartil |
| PT2336134T (pt) | 1998-06-23 | 2016-10-19 | The Board Of Trustees Of The Univ Of Illionis | Ensaio de aptidão e métodos para reduzir a resistência do hiv à terapia |
| 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 |
| US6548517B2 (en) * | 2000-03-24 | 2003-04-15 | Millennium Pharmaceuticals, Inc. | Oxindole inhibitors of factor Xa |
-
2003
- 2003-08-14 NZ NZ538714A patent/NZ538714A/en not_active IP Right Cessation
- 2003-08-14 BR BR0305771-2A patent/BR0305771A/pt 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 CN CN038240955A patent/CN1688586B/zh not_active Expired - Fee Related
- 2003-08-14 EP EP03787818A patent/EP1546153A1/en not_active Withdrawn
- 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 WO PCT/EP2003/050379 patent/WO2004016619A1/en not_active Ceased
- 2003-08-14 US US10/524,451 patent/US7199148B2/en 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 KR KR1020057001812A patent/KR100994759B1/ko not_active Expired - Fee Related
- 2003-08-14 JP JP2004528524A patent/JP4681296B2/ja not_active Expired - Fee Related
- 2003-08-14 HR HRP20050606AA patent/HRP20050606B1/hr 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
Also Published As
| Publication number | Publication date |
|---|---|
| AP2005003245A0 (en) | 2005-03-31 |
| HRP20050606B1 (hr) | 2014-04-25 |
| PL375307A1 (en) | 2005-11-28 |
| JP2005537305A (ja) | 2005-12-08 |
| CA2493940C (en) | 2011-11-22 |
| EA200500350A1 (ru) | 2005-08-25 |
| HRP20050606A2 (en) | 2006-02-28 |
| WO2004016619A1 (en) | 2004-02-26 |
| CN1688586A (zh) | 2005-10-26 |
| CA2493940A1 (en) | 2004-02-26 |
| IL166462A0 (en) | 2006-01-15 |
| IL166462A (en) | 2012-04-30 |
| NZ538714A (en) | 2007-03-30 |
| US7199148B2 (en) | 2007-04-03 |
| US20060058368A1 (en) | 2006-03-16 |
| BR0305771A (pt) | 2004-10-05 |
| KR20050042141A (ko) | 2005-05-04 |
| AU2003262574A1 (en) | 2004-03-03 |
| EP1546153A1 (en) | 2005-06-29 |
| KR100994759B1 (ko) | 2010-11-16 |
| CN1688586B (zh) | 2012-05-09 |
| AP2126A (en) | 2010-06-03 |
| ZA200501223B (en) | 2006-07-26 |
| NO331846B1 (no) | 2012-04-23 |
| MXPA05001792A (es) | 2005-04-25 |
| AU2003262574B2 (en) | 2009-07-09 |
| EA010486B1 (ru) | 2008-10-30 |
| JP4681296B2 (ja) | 2011-05-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM1K | Lapsed by not paying the annual fees |