HRP20030735B1 - Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors - Google Patents
Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitorsInfo
- Publication number
- HRP20030735B1 HRP20030735B1 HR20030735A HRP20030735A HRP20030735B1 HR P20030735 B1 HRP20030735 B1 HR P20030735B1 HR 20030735 A HR20030735 A HR 20030735A HR P20030735 A HRP20030735 A HR P20030735A HR P20030735 B1 HRP20030735 B1 HR P20030735B1
- Authority
- HR
- Croatia
- Prior art keywords
- 4alkyl
- aryl
- het2
- het2c1
- arylc1
- Prior art date
Links
- -1 2-(substituted-amino)-benzothiazole sulfonamide Chemical class 0.000 title abstract 8
- 239000004030 hiv protease inhibitor Substances 0.000 title 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 10
- 125000003118 aryl group Chemical group 0.000 abstract 10
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 4
- 150000002431 hydrogen Chemical class 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 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
-
- 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
-
- 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
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/68—Benzothiazoles 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
- C07D277/82—Nitrogen atoms
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (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)
- Thiazole And Isothizaole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01200529 | 2001-02-14 | ||
| US28775801P | 2001-05-02 | 2001-05-02 | |
| PCT/EP2002/001788 WO2002083657A2 (en) | 2001-02-14 | 2002-02-14 | Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20030735A2 HRP20030735A2 (en) | 2005-08-31 |
| HRP20030735B1 true HRP20030735B1 (en) | 2012-02-29 |
Family
ID=26076833
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20030735A HRP20030735B1 (en) | 2001-02-14 | 2003-09-12 | Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US7659404B2 (zh) |
| EP (1) | EP1370543B1 (zh) |
| JP (1) | JP4530612B2 (zh) |
| KR (1) | KR100870184B1 (zh) |
| CN (2) | CN100369904C (zh) |
| AP (1) | AP1504A (zh) |
| AT (1) | ATE343567T1 (zh) |
| AU (1) | AU2002302363B2 (zh) |
| BG (1) | BG66301B1 (zh) |
| BR (1) | BR0207862A (zh) |
| CA (1) | CA2438304C (zh) |
| CY (1) | CY1108073T1 (zh) |
| CZ (1) | CZ304273B6 (zh) |
| DE (1) | DE60215623T2 (zh) |
| DK (1) | DK1370543T3 (zh) |
| EA (1) | EA006096B1 (zh) |
| EE (1) | EE05385B1 (zh) |
| ES (1) | ES2275866T3 (zh) |
| HK (1) | HK1061233A1 (zh) |
| HR (1) | HRP20030735B1 (zh) |
| HU (1) | HU229224B1 (zh) |
| IL (2) | IL157171A0 (zh) |
| MX (1) | MXPA03007236A (zh) |
| NO (1) | NO326174B1 (zh) |
| NZ (1) | NZ527391A (zh) |
| PL (1) | PL213327B1 (zh) |
| PT (1) | PT1370543E (zh) |
| SI (1) | SI1370543T1 (zh) |
| SK (1) | SK287582B6 (zh) |
| WO (1) | WO2002083657A2 (zh) |
| ZA (1) | ZA200306086B (zh) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU783235B2 (en) | 1999-05-28 | 2005-10-06 | Virco Bvba | New mutational profiles in HIV-1 reverse transcriptase correlated with phenotypic drug resistance |
| AU2631602A (en) | 2000-10-20 | 2002-04-29 | Virco Nv | New mutational profiles in hiv-1 reverse transcriptase correlated with phenotypic drug resistance |
| BR0207862A (pt) | 2001-02-14 | 2004-06-22 | Tibotec Pharm Ltd | Inibidores de protease de hiv 2-(amino-substituìda)-benzotiazol-sulfonamida de amplo espectro |
| AU2003202914A1 (en) | 2002-01-07 | 2003-07-24 | Sequoia Pharmaceuticals | Broad spectrum inhibitors |
| US7157489B2 (en) | 2002-03-12 | 2007-01-02 | The Board Of Trustees Of The University Of Illinois | HIV protease inhibitors |
| CA2490764C (en) | 2002-07-01 | 2011-11-22 | Tibotec Pharmaceuticals Ltd. | New mutational profiles in hiv-1 reverse transcriptase correlated with phenotypic drug resistance |
| DE60327768D1 (de) | 2002-07-01 | 2009-07-09 | Tibotec Pharm Ltd | Mutationsprofile bei mit phänotypischer medikamentenresistenz korrelierter hiv-1-protease |
| KR20050025647A (ko) * | 2002-08-02 | 2005-03-14 | 티보텍 파마슈티칼즈 리미티드 | 광범위 2-아미노-벤조티아졸 설폰아미드 ｈｉｖ프로테아제 저해제 |
| CN101445493A (zh) * | 2002-08-02 | 2009-06-03 | 泰博特克药品有限公司 | 广谱2-氨基-苯并噻唑磺酰胺类hiv蛋白酶抑制剂 |
| ATE353323T1 (de) * | 2003-09-30 | 2007-02-15 | Tibotec Pharm Ltd | Verfahren zur herstellung von benzoxazolsulfonamidverbindungen und zwischenprodukten davon |
| DE10360835A1 (de) * | 2003-12-23 | 2005-07-21 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel |
| EP2422781A1 (en) * | 2004-05-07 | 2012-02-29 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
| AU2006217922B2 (en) | 2005-02-25 | 2012-04-05 | Janssen Sciences Ireland Uc | Protease inhibitor precursor synthesis |
| AR053845A1 (es) | 2005-04-15 | 2007-05-23 | Tibotec Pharm Ltd | 5-tiazolilmetil[(1s,2r)-3-[[(2-amino-6-benzoxazolil)sulfonil)](2-metilpropil)amino]-2-hidroxi-1-(fenilmetil)propil]carbamato como mejorador de farmacos metabolizados por el citocromo p450 |
| JO2841B1 (en) * | 2006-06-23 | 2014-09-15 | تيبوتيك فارماسيوتيكالز ليمتد | 2-(substituted-amino) -benzothiazole sulfonamide as protease inhibitors HIV (HIV) |
| WO2011061590A1 (en) | 2009-11-17 | 2011-05-26 | Hetero Research Foundation | Novel carboxamide derivatives as hiv inhibitors |
| JO3090B1 (ar) * | 2009-12-11 | 2017-03-15 | Janssen Sciences Ireland Uc | 5- امينو-4- هيدروكسي-بنتويل اميدات |
| US9024038B2 (en) * | 2010-12-27 | 2015-05-05 | Purdue Research Foundation | Compunds and methods for treating HIV |
| ES2571479T3 (es) | 2012-04-20 | 2016-05-25 | Gilead Sciences Inc | Derivados del ácido benzotiazol-6-il acético y su uso para tratar una infección por VIH |
| CN104000824B (zh) * | 2014-05-28 | 2016-07-06 | 中山大学 | 苯并五元杂环类化合物在制备抗hiv-1病毒药物中的应用 |
| US11439608B2 (en) | 2017-09-25 | 2022-09-13 | Qun Lu | Roles of modulators of intersectin-CDC42 signaling in Alzheimer's disease |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995006030A1 (en) * | 1993-08-24 | 1995-03-02 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
| WO1996028463A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| WO1999065870A2 (en) * | 1998-06-19 | 1999-12-23 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0445926B1 (en) | 1990-03-09 | 1996-08-21 | Milliken Research Corporation | Organic materials having sulfonamido linked poly(oxyalkylene) moieties and their preparation |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| ES2123065T3 (es) | 1992-08-25 | 1999-01-01 | Searle & Co | Hidroxietilamino-sulfonamidas utiles como inhibidores de proteasas retroviricas. |
| 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 |
| IL111080A (en) | 1993-10-01 | 1999-08-17 | Astra Ab | Method for treating a finely divided powder medicament |
| JP4014220B2 (ja) | 1995-01-20 | 2007-11-28 | ジー．ディー．サール アンド カンパニー | ビス−スルホンアミドヒドロキシエチルアミノ レトロ ウイルスプロテアーゼインヒビター |
| US6140505A (en) * | 1995-03-10 | 2000-10-31 | G. D. Searle & Co. | Synthesis of benzo fused heterocyclic sulfonyl chlorides |
| 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 |
| RU2174519C2 (ru) * | 1995-03-10 | 2001-10-10 | Джи. Ди. Сирл Энд Ко. | Гидроксиэтиламино сульфонамиды гетероциклокарбонил аминокислоты, ингибирующие ретровирусную протеазу |
| US6143788A (en) * | 1995-03-10 | 2000-11-07 | G.D. Searle & Co. | Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors |
| US6861539B1 (en) * | 1995-03-10 | 2005-03-01 | G. D. Searle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| WO1997018205A1 (en) | 1995-11-15 | 1997-05-22 | G.D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| CN1165291C (zh) | 1996-05-20 | 2004-09-08 | 詹森药业有限公司 | 具有改进的生物利用度的抗真菌组合物 |
| HU224217B1 (hu) | 1997-03-26 | 2005-06-28 | Janssen Pharmaceutica N.V. | Gombaellenes hatóanyaggal és polimerrel bevont magrészt tartalmazó pelletek |
| 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 |
| BR9814484A (pt) * | 1997-12-24 | 2000-10-10 | Vertex Pharma | "pró-drogas de inibidores de aspartil protease" |
| AU2012199A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| 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 |
| WO1999067417A2 (en) * | 1998-06-23 | 1999-12-29 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Fitness assay and associated methods |
| 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 |
| BR0207862A (pt) | 2001-02-14 | 2004-06-22 | Tibotec Pharm Ltd | Inibidores de protease de hiv 2-(amino-substituìda)-benzotiazol-sulfonamida de amplo espectro |
-
2002
- 2002-02-14 BR BR0207862-7A patent/BR0207862A/pt not_active IP Right Cessation
- 2002-02-14 HU HU0303257A patent/HU229224B1/hu not_active IP Right Cessation
- 2002-02-14 CN CNB028049829A patent/CN100369904C/zh not_active Expired - Fee Related
- 2002-02-14 SI SI200230467T patent/SI1370543T1/sl unknown
- 2002-02-14 IL IL15717102A patent/IL157171A0/xx unknown
- 2002-02-14 CA CA2438304A patent/CA2438304C/en not_active Expired - Fee Related
- 2002-02-14 SK SK1102-2003A patent/SK287582B6/sk not_active IP Right Cessation
- 2002-02-14 AT AT02729930T patent/ATE343567T1/de active
- 2002-02-14 EA EA200300891A patent/EA006096B1/ru not_active IP Right Cessation
- 2002-02-14 PT PT02729930T patent/PT1370543E/pt unknown
- 2002-02-14 CN CN2007101997173A patent/CN101230067B/zh not_active Expired - Fee Related
- 2002-02-14 JP JP2002581413A patent/JP4530612B2/ja not_active Expired - Fee Related
- 2002-02-14 US US10/467,609 patent/US7659404B2/en not_active Expired - Fee Related
- 2002-02-14 AU AU2002302363A patent/AU2002302363B2/en not_active Ceased
- 2002-02-14 MX MXPA03007236A patent/MXPA03007236A/es active IP Right Grant
- 2002-02-14 DK DK02729930T patent/DK1370543T3/da active
- 2002-02-14 WO PCT/EP2002/001788 patent/WO2002083657A2/en active IP Right Grant
- 2002-02-14 EP EP02729930A patent/EP1370543B1/en not_active Expired - Lifetime
- 2002-02-14 NZ NZ527391A patent/NZ527391A/xx not_active IP Right Cessation
- 2002-02-14 ES ES02729930T patent/ES2275866T3/es not_active Expired - Lifetime
- 2002-02-14 KR KR1020037010506A patent/KR100870184B1/ko not_active IP Right Cessation
- 2002-02-14 PL PL363778A patent/PL213327B1/pl unknown
- 2002-02-14 DE DE60215623T patent/DE60215623T2/de not_active Expired - Lifetime
- 2002-02-14 EE EEP200300381A patent/EE05385B1/xx not_active IP Right Cessation
- 2002-02-14 AP APAP/P/2003/002856A patent/AP1504A/en active
- 2002-02-14 CZ CZ2003-2415A patent/CZ304273B6/cs not_active IP Right Cessation
-
2003
- 2003-07-30 IL IL157171A patent/IL157171A/en not_active IP Right Cessation
- 2003-08-06 ZA ZA2003/06086A patent/ZA200306086B/en unknown
- 2003-08-13 NO NO20033584A patent/NO326174B1/no not_active IP Right Cessation
- 2003-09-01 BG BG108143A patent/BG66301B1/bg unknown
- 2003-09-12 HR HR20030735A patent/HRP20030735B1/xx not_active IP Right Cessation
-
2004
- 2004-06-03 HK HK04104020A patent/HK1061233A1/xx not_active IP Right Cessation
-
2007
- 2007-01-25 CY CY20071100088T patent/CY1108073T1/el unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995006030A1 (en) * | 1993-08-24 | 1995-03-02 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
| WO1996028463A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| WO1999065870A2 (en) * | 1998-06-19 | 1999-12-23 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
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