EA200600699A1 - Способы получения соединений бензоксазолсульфонамида и их промежуточные соединения - Google Patents
Способы получения соединений бензоксазолсульфонамида и их промежуточные соединенияInfo
- Publication number
- EA200600699A1 EA200600699A1 EA200600699A EA200600699A EA200600699A1 EA 200600699 A1 EA200600699 A1 EA 200600699A1 EA 200600699 A EA200600699 A EA 200600699A EA 200600699 A EA200600699 A EA 200600699A EA 200600699 A1 EA200600699 A1 EA 200600699A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- methods
- compounds
- sulfonamide
- benzoxasole
- obtaining
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 3
- BBFZKZROAWKUCD-UHFFFAOYSA-N 1,3-benzoxazole-2-sulfonamide Chemical compound C1=CC=C2OC(S(=O)(=O)N)=NC2=C1 BBFZKZROAWKUCD-UHFFFAOYSA-N 0.000 abstract 2
- SDCCPSGJFZFNPB-UHFFFAOYSA-N 2-amino-3h-1,3-benzoxazole-2-sulfonamide Chemical class C1=CC=C2OC(N)(S(N)(=O)=O)NC2=C1 SDCCPSGJFZFNPB-UHFFFAOYSA-N 0.000 abstract 1
- CBXAWZGFEDZKFR-UHFFFAOYSA-N 2-methylsulfanyl-1,3-benzoxazole Chemical compound C1=CC=C2OC(SC)=NC2=C1 CBXAWZGFEDZKFR-UHFFFAOYSA-N 0.000 abstract 1
- CPMVNLAOBJLSFV-UHFFFAOYSA-N 2-sulfanyl-3h-1,3-benzoxazole-2-sulfonamide Chemical compound C1=CC=C2OC(S(=O)(=O)N)(S)NC2=C1 CPMVNLAOBJLSFV-UHFFFAOYSA-N 0.000 abstract 1
- -1 carbamine ester Chemical class 0.000 abstract 1
- 239000004030 hiv protease inhibitor Substances 0.000 abstract 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- 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
- 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
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Данное изобретение относится к способам получения соединений бензоксазолсульфонамида формулы (9), а также к новым промежуточным соединениям формулы (6) для применения в указанном способе. Более конкретно, данное изобретение относится к способам получения соединений 2-аминобензоксазолсульфонамида, в которых применяются промежуточные соединения 2-меркаптобензоксазолсульфонамида, более конкретно, к способам, в которых применяется промежуточное соединение 1-бензил-2-гидрокси-3-[изобутил(2-метилсульфанилбензоксазол-6-сульфонил)амино]пропил)карбаминовый сложный эфир, и к способам, применяемым в промышленном масштабе. Такие соединения бензоксазолсульфонамида особенно полезны в качестве ингибиторов ВИЧ протеазы. Заместители определены в формуле изобретения.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03103630 | 2003-09-30 | ||
| US50799603P | 2003-10-02 | 2003-10-02 | |
| PCT/EP2004/052382 WO2005030739A1 (en) | 2003-09-30 | 2004-09-30 | Methods for the preparation of benzoxazole sulfonamide compounds and intermediates thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200600699A1 true EA200600699A1 (ru) | 2006-08-25 |
| EA011891B1 EA011891B1 (ru) | 2009-06-30 |
Family
ID=34395298
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200600699A EA011891B1 (ru) | 2003-09-30 | 2004-09-30 | Способы получения соединений бензоксазолсульфонамида и их промежуточные соединения |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US20070123574A1 (ru) |
| EP (1) | EP1670773B1 (ru) |
| JP (1) | JP4919802B2 (ru) |
| KR (1) | KR101090102B1 (ru) |
| CN (1) | CN1860107B (ru) |
| AP (1) | AP1985A (ru) |
| AT (1) | ATE353323T1 (ru) |
| AU (1) | AU2004276017B2 (ru) |
| BR (1) | BRPI0414916A (ru) |
| CA (1) | CA2537877C (ru) |
| DE (1) | DE602004004674T2 (ru) |
| DK (1) | DK1670773T3 (ru) |
| EA (1) | EA011891B1 (ru) |
| ES (1) | ES2281828T3 (ru) |
| IL (1) | IL173891A0 (ru) |
| IN (1) | IN2012DN02301A (ru) |
| MX (1) | MXPA06003575A (ru) |
| NO (1) | NO20061951L (ru) |
| NZ (1) | NZ546279A (ru) |
| PL (1) | PL1670773T3 (ru) |
| PT (1) | PT1670773E (ru) |
| SI (1) | SI1670773T1 (ru) |
| WO (1) | WO2005030739A1 (ru) |
| ZA (1) | ZA200602603B (ru) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2011044134A1 (en) * | 2009-10-05 | 2011-04-14 | Albany Molecular Research, Inc. | Epiminocycloalkyl(b)indole derivatives as serotonin sub-type 6 (5-ht6) modulators and uses thereof |
| AU2012207335A1 (en) | 2011-01-19 | 2013-07-25 | Albany Molecular Research, Inc. | Benzofuro[3,2-c] pyridines and related analogs as serotonin sub-type 6 (5-HT6) modulators for the treatment of obesity, metabolic syndrome, cognition and schizophrenia |
| WO2014194519A1 (en) | 2013-06-07 | 2014-12-11 | Merck Sharp & Dohme Corp. | Imidazole derivatives and methods of use thereof for improving pharmacokinetics of drug |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5968942A (en) * | 1992-08-25 | 1999-10-19 | G. D. Searle & Co. | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
| ES2190793T3 (es) * | 1995-03-10 | 2003-08-16 | Searle & Co | Inhibidores de proteasas retrovirales de heterociclocarbonil aminoacido hidroxietilamino sulfonamida. |
| 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 |
| CA2372352A1 (en) * | 2000-04-07 | 2001-10-18 | Hyun-Gyu Park | Sulfonamide derivative as a matrix metalloproteinase inhibitor |
| US6455738B1 (en) * | 2000-07-13 | 2002-09-24 | Rhodia Chimie | Process for the sulfonation of an aromatic compound |
| SK287582B6 (sk) * | 2001-02-14 | 2011-03-04 | Tibotec Pharmaceuticals Ltd. | 2-(Substituovaná amino)benztiazolsulfonamidová zlúčenina, spôsob jej prípravy, použitie a farmaceutická zmes s jej obsahom |
| BR0209594A (pt) * | 2001-05-11 | 2004-03-30 | Tibotec Pharm Ltd | Inibidores de protease de hiv de amplo espectro de 2-amino-benzoxazol sulfonamida |
| TWI286476B (en) * | 2001-12-12 | 2007-09-11 | Tibotec Pharm Ltd | Combination of cytochrome P450 dependent protease inhibitors |
| MY142238A (en) * | 2002-03-12 | 2010-11-15 | Tibotec Pharm Ltd | Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors |
-
2004
- 2004-09-30 EP EP04766869A patent/EP1670773B1/en not_active Expired - Lifetime
- 2004-09-30 AP AP2006003603A patent/AP1985A/xx active
- 2004-09-30 DK DK04766869T patent/DK1670773T3/da active
- 2004-09-30 WO PCT/EP2004/052382 patent/WO2005030739A1/en not_active Ceased
- 2004-09-30 AT AT04766869T patent/ATE353323T1/de active
- 2004-09-30 US US10/574,157 patent/US20070123574A1/en not_active Abandoned
- 2004-09-30 PT PT04766869T patent/PT1670773E/pt unknown
- 2004-09-30 EA EA200600699A patent/EA011891B1/ru not_active IP Right Cessation
- 2004-09-30 NZ NZ546279A patent/NZ546279A/en not_active IP Right Cessation
- 2004-09-30 CN CN2004800280971A patent/CN1860107B/zh not_active Expired - Fee Related
- 2004-09-30 AU AU2004276017A patent/AU2004276017B2/en not_active Ceased
- 2004-09-30 KR KR1020067005992A patent/KR101090102B1/ko not_active Expired - Fee Related
- 2004-09-30 BR BRPI0414916-5A patent/BRPI0414916A/pt not_active IP Right Cessation
- 2004-09-30 PL PL04766869T patent/PL1670773T3/pl unknown
- 2004-09-30 IN IN2301DEN2012 patent/IN2012DN02301A/en unknown
- 2004-09-30 CA CA2537877A patent/CA2537877C/en not_active Expired - Fee Related
- 2004-09-30 JP JP2006530265A patent/JP4919802B2/ja not_active Expired - Fee Related
- 2004-09-30 ES ES04766869T patent/ES2281828T3/es not_active Expired - Lifetime
- 2004-09-30 SI SI200430265T patent/SI1670773T1/sl unknown
- 2004-09-30 DE DE602004004674T patent/DE602004004674T2/de not_active Expired - Lifetime
- 2004-09-30 MX MXPA06003575A patent/MXPA06003575A/es active IP Right Grant
-
2006
- 2006-02-22 IL IL173891A patent/IL173891A0/en not_active IP Right Cessation
- 2006-03-29 ZA ZA200602603A patent/ZA200602603B/xx unknown
- 2006-05-02 NO NO20061951A patent/NO20061951L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CN1860107A (zh) | 2006-11-08 |
| NZ546279A (en) | 2008-09-26 |
| DE602004004674T2 (de) | 2007-11-22 |
| JP4919802B2 (ja) | 2012-04-18 |
| AU2004276017B2 (en) | 2010-08-19 |
| KR20060092224A (ko) | 2006-08-22 |
| IL173891A0 (en) | 2006-07-05 |
| CA2537877A1 (en) | 2005-04-07 |
| EA011891B1 (ru) | 2009-06-30 |
| PL1670773T3 (pl) | 2007-06-29 |
| NO20061951L (no) | 2006-05-02 |
| AP2006003603A0 (en) | 2006-04-30 |
| CN1860107B (zh) | 2013-08-21 |
| DK1670773T3 (da) | 2007-05-29 |
| SI1670773T1 (sl) | 2007-06-30 |
| IN2012DN02301A (ru) | 2015-08-14 |
| ZA200602603B (en) | 2008-05-28 |
| EP1670773B1 (en) | 2007-02-07 |
| EP1670773A1 (en) | 2006-06-21 |
| AP1985A (en) | 2009-03-30 |
| AU2004276017A1 (en) | 2005-04-07 |
| BRPI0414916A (pt) | 2006-11-07 |
| MXPA06003575A (es) | 2006-06-05 |
| WO2005030739A1 (en) | 2005-04-07 |
| DE602004004674D1 (de) | 2007-03-22 |
| US20070123574A1 (en) | 2007-05-31 |
| PT1670773E (pt) | 2007-05-31 |
| ES2281828T3 (es) | 2007-10-01 |
| JP2007507468A (ja) | 2007-03-29 |
| CA2537877C (en) | 2015-03-17 |
| ATE353323T1 (de) | 2007-02-15 |
| KR101090102B1 (ko) | 2011-12-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KG MD TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): KZ RU |