ATE497494T1 - Substituierte benzimidazol-sulfonamid-derivate als breitspectrum hiv- protease- inhibitoren - Google Patents
Substituierte benzimidazol-sulfonamid-derivate als breitspectrum hiv- protease- inhibitorenInfo
- Publication number
- ATE497494T1 ATE497494T1 AT03714954T AT03714954T ATE497494T1 AT E497494 T1 ATE497494 T1 AT E497494T1 AT 03714954 T AT03714954 T AT 03714954T AT 03714954 T AT03714954 T AT 03714954T AT E497494 T1 ATE497494 T1 AT E497494T1
- Authority
- AT
- Austria
- Prior art keywords
- broad
- protease inhibitors
- hiv protease
- sulfonamide derivatives
- substituted benzimidazole
- Prior art date
Links
- XRGHQBXKSHAQRB-UHFFFAOYSA-N 1h-benzimidazole-2-sulfonamide Chemical class C1=CC=C2NC(S(=O)(=O)N)=NC2=C1 XRGHQBXKSHAQRB-UHFFFAOYSA-N 0.000 title 1
- 239000004030 hiv protease inhibitor Substances 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/08—Radicals containing only hydrogen and carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
-
- 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
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
- C07D235/30—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
- C07D235/30—Nitrogen atoms not forming part of a nitro radical
- C07D235/32—Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02075999 | 2002-03-12 | ||
| PCT/EP2003/050057 WO2003076413A1 (en) | 2002-03-12 | 2003-03-12 | Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE497494T1 true ATE497494T1 (de) | 2011-02-15 |
Family
ID=27798870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT03714954T ATE497494T1 (de) | 2002-03-12 | 2003-03-12 | Substituierte benzimidazol-sulfonamid-derivate als breitspectrum hiv- protease- inhibitoren |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US20050171175A1 (de) |
| EP (1) | EP1485358B1 (de) |
| JP (1) | JP4557552B2 (de) |
| KR (3) | KR20040093119A (de) |
| CN (2) | CN1653053A (de) |
| AP (1) | AP2111A (de) |
| AR (1) | AR038928A1 (de) |
| AT (1) | ATE497494T1 (de) |
| AU (1) | AU2003219159B2 (de) |
| BR (1) | BR0303373A (de) |
| CA (1) | CA2479012C (de) |
| DE (1) | DE60335939D1 (de) |
| DK (1) | DK1485358T3 (de) |
| EA (1) | EA011946B1 (de) |
| HR (1) | HRP20040936B1 (de) |
| IL (1) | IL163960A0 (de) |
| MX (1) | MXPA04008929A (de) |
| MY (1) | MY142238A (de) |
| NO (1) | NO326702B1 (de) |
| NZ (1) | NZ535439A (de) |
| PL (1) | PL213645B1 (de) |
| SI (1) | SI1485358T1 (de) |
| TW (1) | TWI329639B (de) |
| WO (1) | WO2003076413A1 (de) |
| ZA (1) | ZA200407242B (de) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL1670773T3 (pl) * | 2003-09-30 | 2007-06-29 | Tibotec Pharm Ltd | Sposób wytwarzania sulfonamidów benzoksazolu i ich związków pośrednich |
| MXPA06012909A (es) * | 2004-05-07 | 2007-09-06 | Sequoia Pharmaceuticals Inc | Inhibidores de proteasa retroviral repelente de resistencia. |
| AU2006217922B2 (en) | 2005-02-25 | 2012-04-05 | Janssen Sciences Ireland Uc | Protease inhibitor precursor synthesis |
| UA103013C2 (uk) * | 2007-12-06 | 2013-09-10 | Тиботек Фармасьютикелз | Амідні сполуки як активатори противірусних препаратів |
| WO2011061590A1 (en) | 2009-11-17 | 2011-05-26 | Hetero Research Foundation | Novel carboxamide derivatives as hiv inhibitors |
| WO2013011485A1 (en) * | 2011-07-20 | 2013-01-24 | Ranbaxy Laboratories Limited | Process for the preparation of sulfonamides useful as retroviral protease inhibitors |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| JP3657002B2 (ja) * | 1992-08-25 | 2005-06-08 | ジー．ディー．サール アンド カンパニー | レトロウイルスプロテアーゼ阻害剤として有用なα−およびβ−アミノ酸ヒドロキシエチルアミノスルホンアミド |
| PH30929A (en) | 1992-09-03 | 1997-12-23 | Janssen Pharmaceutica Nv | Beads having a core coated with an antifungal and a polymer. |
| US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
| AU7669794A (en) | 1993-08-24 | 1995-03-21 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
| SK283569B6 (sk) | 1993-10-01 | 2003-09-11 | Astra Aktiebolag | Spôsob spracovania jemne deleného práškového liečiva, zariadenie na vykonávanie tohto spôsobu a aglomeráty vyrobené týmto spôsobom |
| WO1996022287A1 (en) * | 1995-01-20 | 1996-07-25 | G.D. Searle & Co. | 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 |
| US6140505A (en) * | 1995-03-10 | 2000-10-31 | G. D. Searle & Co. | Synthesis of benzo fused heterocyclic sulfonyl chlorides |
| US5776971A (en) * | 1995-03-10 | 1998-07-07 | G.D. Searle & Co. | Heterocyclecarbonyl 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 |
| AU717598B2 (en) * | 1995-03-10 | 2000-03-30 | G.D. Searle & Co. | Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| JP2000515488A (ja) | 1995-11-15 | 2000-11-21 | ジー．ディー．サール アンド カンパニー | 置換スルホニルアルカノイルアミノヒドロキシエチルアミノスルホンアミド レトロウイルスプロテアーゼ阻害剤 |
| DK0904060T3 (da) | 1996-05-20 | 2004-04-13 | Janssen Pharmaceutica Nv | Antifungale præparater med forbedret biotilgængelighed |
| WO1998042318A1 (en) | 1997-03-26 | 1998-10-01 | Janssen Pharmaceutica N.V. | Pellets having a core coated with an antifungal and a polymer |
| CA2297070A1 (en) * | 1997-08-01 | 1999-02-11 | Morphosys Ag | Novel method and phage for the identification of nucleic acid sequences encoding members of a multimeric (poly)peptide complex |
| WO1999033795A1 (en) | 1997-12-24 | 1999-07-08 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| BR9814484A (pt) | 1997-12-24 | 2000-10-10 | Vertex Pharma | "pró-drogas de inibidores de aspartil protease" |
| 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 |
| NZ508855A (en) * | 1998-06-19 | 2003-10-31 | Vertex Pharma | Sulfonamide inhibitors of HIV aspartyl protease |
| 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 |
| AR031520A1 (es) * | 1999-06-11 | 2003-09-24 | Vertex Pharma | Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion |
-
2003
- 2003-03-10 MY MYPI20030825A patent/MY142238A/en unknown
- 2003-03-11 AR ARP030100829A patent/AR038928A1/es not_active Application Discontinuation
- 2003-03-11 TW TW092105142A patent/TWI329639B/zh not_active IP Right Cessation
- 2003-03-12 HR HRP20040936AA patent/HRP20040936B1/xx not_active IP Right Cessation
- 2003-03-12 KR KR10-2004-7014171A patent/KR20040093119A/ko not_active Ceased
- 2003-03-12 EP EP03714954A patent/EP1485358B1/de not_active Expired - Lifetime
- 2003-03-12 CN CNA038104725A patent/CN1653053A/zh active Pending
- 2003-03-12 KR KR1020127028481A patent/KR20120136411A/ko not_active Ceased
- 2003-03-12 NZ NZ535439A patent/NZ535439A/en not_active IP Right Cessation
- 2003-03-12 MX MXPA04008929A patent/MXPA04008929A/es active IP Right Grant
- 2003-03-12 AU AU2003219159A patent/AU2003219159B2/en not_active Ceased
- 2003-03-12 EA EA200401188A patent/EA011946B1/ru not_active IP Right Cessation
- 2003-03-12 IL IL16396003A patent/IL163960A0/xx unknown
- 2003-03-12 AP APAP/P/2004/003151A patent/AP2111A/en active
- 2003-03-12 KR KR1020107018927A patent/KR101302421B1/ko not_active Expired - Fee Related
- 2003-03-12 WO PCT/EP2003/050057 patent/WO2003076413A1/en not_active Ceased
- 2003-03-12 AT AT03714954T patent/ATE497494T1/de not_active IP Right Cessation
- 2003-03-12 DE DE60335939T patent/DE60335939D1/de not_active Expired - Lifetime
- 2003-03-12 SI SI200331984T patent/SI1485358T1/sl unknown
- 2003-03-12 CN CN201010251011.9A patent/CN101935303B/zh not_active Expired - Fee Related
- 2003-03-12 BR BR0303373-2A patent/BR0303373A/pt not_active IP Right Cessation
- 2003-03-12 JP JP2003574633A patent/JP4557552B2/ja not_active Expired - Fee Related
- 2003-03-12 DK DK03714954.9T patent/DK1485358T3/da active
- 2003-03-12 CA CA2479012A patent/CA2479012C/en not_active Expired - Fee Related
- 2003-03-12 US US10/508,561 patent/US20050171175A1/en not_active Abandoned
- 2003-03-12 PL PL374152A patent/PL213645B1/pl unknown
- 2003-11-12 NO NO20035023A patent/NO326702B1/no not_active IP Right Cessation
-
2004
- 2004-09-09 ZA ZA2004/07242A patent/ZA200407242B/en unknown
-
2009
- 2009-04-27 US US12/430,547 patent/US8143421B2/en not_active Expired - Fee Related
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |