HRP20050606B1 - Supstituirani oksindol sulfonamid hiv proteazni inhibitori širokog spektra - Google Patents
Supstituirani oksindol sulfonamid hiv proteazni inhibitori širokog spektraInfo
- Publication number
- HRP20050606B1 HRP20050606B1 HRP20050606AA HRP20050606A HRP20050606B1 HR P20050606 B1 HRP20050606 B1 HR P20050606B1 HR P20050606A A HRP20050606A A HR P20050606AA HR P20050606 A HRP20050606 A HR P20050606A HR P20050606 B1 HRP20050606 B1 HR P20050606B1
- Authority
- HR
- Croatia
- Prior art keywords
- formula
- het
- calkyl
- optionally substituted
- compounds
- 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
- 150000001875 compounds Chemical class 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- -1 Ccycloalkyl Chemical group 0.000 abstract 1
- 238000009007 Diagnostic Kit Methods 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003342 alkenyl 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
- 229910052799 carbon Inorganic materials 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
- 150000002431 hydrogen 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
- 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
Prikazani izum odnosi se na spojeve formule (I) njihove N-okside, soli, stereoizomerske oblike, racemične smjese, prolijekove, estere i metabolite. gdje su R1 i R8 oba vodik moguće supstituiran sa Calkil, C,alkenil, Ccikloalkil, aril, Het, Het; Rtakođer može biti radikal formule (RR)NC(RR)CR-; t je 0, 1 ili 2; R2 je H ili Calkil; L je -C(=O)-, -O-C(=O)-, -NR-C(=O)-, -O-Calkanediil-C(=O)-, -NR-Calkanediyl-C(=O)-, -S(=O)-, -O-S(=O), -NR-S(=O); Rje Calkil, aril, Ccikloalkil, CcikloalkilCalkil, ili arilCalkil; Rje H, CalkilOC(=O), karboksil, aminoC(=O), mono- ili di(Calkil)aminoC(=O), Ccikloalkil, Calkenil, Calkinil ili moguće supstituiran Calkil; formula (II) je formula (III) ili formula (IV); Ri Rsu Calkenil, Calkinil, Ccikloalkil ili Calkil, moguće supstituiran najednom ili više atoma; Ri Rtakođer mogu biti vodik, aril, Het, Het; R6 je vodik ili Calkil moguće supstituiran na jednom ih više ugljikovih atoma. Nadalje se odnosi na uporabu tih spojeva kao inhibitora HIV proteaze širokog spektra, postupke njihove priprave kao i pripravljanje farmaceutskih pripravaka i dijagnostičkih kitova koji ih sadrže. Također se odnosi na kombiniranje navedenih spojeva sa drugim antiretrovirusnim agensima, i na njihovu uporabu kao referentnih spojeva ili kao reagensa u analizama.
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 |
|---|---|
| HRP20050606A2 HRP20050606A2 (en) | 2006-02-28 |
| HRP20050606B1 true HRP20050606B1 (hr) | 2014-04-25 |
Family
ID=31725465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20050606AA HRP20050606B1 (hr) | 2002-08-14 | 2005-06-29 | Supstituirani oksindol sulfonamid hiv proteazni inhibitori širokog spektra |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7199148B2 (hr) |
| EP (1) | EP1546153A1 (hr) |
| JP (1) | JP4681296B2 (hr) |
| KR (1) | KR100994759B1 (hr) |
| CN (1) | CN1688586B (hr) |
| AP (1) | AP2126A (hr) |
| AU (1) | AU2003262574B2 (hr) |
| BR (1) | BR0305771A (hr) |
| CA (1) | CA2493940C (hr) |
| EA (1) | EA010486B1 (hr) |
| HR (1) | HRP20050606B1 (hr) |
| IL (1) | IL166462A (hr) |
| MX (1) | MXPA05001792A (hr) |
| NO (1) | NO331846B1 (hr) |
| NZ (1) | NZ538714A (hr) |
| PL (1) | PL375307A1 (hr) |
| WO (1) | WO2004016619A1 (hr) |
| ZA (1) | ZA200501223B (hr) |
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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996022287A1 (en) * | 1995-01-20 | 1996-07-25 | G.D. Searle & Co. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
| WO1999065870A2 (en) * | 1998-06-19 | 1999-12-23 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
| WO2001072708A2 (en) * | 2000-03-24 | 2001-10-04 | Cor Therapeutics, Inc. | OXINDOLE INHIBITORS OF FACTOR Xa |
Family Cites Families (19)
| 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 |
| 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 |
| 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 |
-
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
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996022287A1 (en) * | 1995-01-20 | 1996-07-25 | G.D. Searle & Co. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
| WO1999065870A2 (en) * | 1998-06-19 | 1999-12-23 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
| WO2001072708A2 (en) * | 2000-03-24 | 2001-10-04 | Cor Therapeutics, Inc. | OXINDOLE INHIBITORS OF FACTOR Xa |
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 |
| 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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