RU2543622C2 - Способ получения азабициклических соединений - Google Patents
Способ получения азабициклических соединений Download PDFInfo
- Publication number
- RU2543622C2 RU2543622C2 RU2012115111/04A RU2012115111A RU2543622C2 RU 2543622 C2 RU2543622 C2 RU 2543622C2 RU 2012115111/04 A RU2012115111/04 A RU 2012115111/04A RU 2012115111 A RU2012115111 A RU 2012115111A RU 2543622 C2 RU2543622 C2 RU 2543622C2
- Authority
- RU
- Russia
- Prior art keywords
- compound
- formula
- solvent
- contacting
- mixture
- Prior art date
Links
- AJDUFGPZEKPRSU-MGCOHNPYSA-N CC(C)(C)OC(N[C@H](CC1)CC[C@@H]1OS(C)(=O)=O)=O Chemical compound CC(C)(C)OC(N[C@H](CC1)CC[C@@H]1OS(C)(=O)=O)=O AJDUFGPZEKPRSU-MGCOHNPYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B61/00—Other general methods
- C07B61/02—Generation of organic free radicals; Organic free radicals per se
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C211/00—Compounds containing amino groups bound to a carbon skeleton
- C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
- C07C211/34—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton
- C07C211/35—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing only non-condensed rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24347709P | 2009-09-17 | 2009-09-17 | |
| US61/243,477 | 2009-09-17 | ||
| PCT/US2010/049306 WO2011035139A1 (en) | 2009-09-17 | 2010-09-17 | Process for preparing azabicyclic compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2012115111A RU2012115111A (ru) | 2013-10-27 |
| RU2543622C2 true RU2543622C2 (ru) | 2015-03-10 |
Family
ID=43242763
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2012115111/04A RU2543622C2 (ru) | 2009-09-17 | 2010-09-17 | Способ получения азабициклических соединений |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US8404865B2 (enExample) |
| EP (1) | EP2477991B1 (enExample) |
| JP (1) | JP5793496B2 (enExample) |
| KR (1) | KR20120083416A (enExample) |
| CN (1) | CN102498112B (enExample) |
| AU (1) | AU2010295461B2 (enExample) |
| BR (1) | BR112012006031A2 (enExample) |
| CA (1) | CA2772792A1 (enExample) |
| ES (1) | ES2540810T3 (enExample) |
| IL (1) | IL218641A0 (enExample) |
| MX (1) | MX2012003343A (enExample) |
| NZ (1) | NZ598277A (enExample) |
| RU (1) | RU2543622C2 (enExample) |
| WO (1) | WO2011035139A1 (enExample) |
| ZA (1) | ZA201201252B (enExample) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA200602755B (en) | 2003-09-06 | 2007-06-27 | Vertex Pharma | Modulators of ATP-binding cassette transporters |
| JP4869072B2 (ja) * | 2003-11-14 | 2012-02-01 | 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 | Ａｔｐ結合カセットトランスポーターのモジュレーターとして有用なチアゾールおよびオキサゾール |
| US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| NZ587549A (en) | 2004-06-24 | 2012-10-26 | Vertex Pharma | 6-Amino-indole derivatives and processes for their preparation |
| EP1912983B1 (en) | 2005-08-11 | 2011-06-08 | Vertex Pharmaceuticals, Inc. | Modulators of cystic fibrosis transmembrane conductance regulator |
| KR101331768B1 (ko) * | 2005-11-08 | 2013-11-22 | 버텍스 파마슈티칼스 인코포레이티드 | Ａｔｐ 결합 카세트 수송체의 헤테로사이클릭 조정제 |
| CA2635581C (en) | 2005-12-28 | 2017-02-28 | Vertex Pharmaceuticals Incorporated | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| CA2856037C (en) * | 2005-12-28 | 2017-03-07 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| USRE50453E1 (en) | 2006-04-07 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| US7645789B2 (en) * | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| US10022352B2 (en) | 2006-04-07 | 2018-07-17 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| PL2674428T3 (pl) | 2006-04-07 | 2017-01-31 | Vertex Pharmaceuticals Incorporated | Modulatory transporterów z kasetą wiążącą ATP |
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| CA2686838C (en) | 2007-05-09 | 2017-03-14 | Vertex Pharmaceuticals Incorporated | Modulators of cftr |
| AU2008302598B2 (en) | 2007-08-24 | 2014-07-17 | Vertex Pharmaceuticals Incorporated | Isothiazolopyridinones useful for the treatment of (inter alia) Cystic Fibrosis |
| SI2578571T1 (sl) | 2007-11-16 | 2016-01-29 | Vertex Pharmaceuticals Incorporated | Izokinolinski modulatorji prenašalcev z atp-vezavno kaseto |
| HRP20170241T2 (hr) | 2007-12-07 | 2023-03-17 | Vertex Pharmaceuticals Incorporated | Čvrsti oblici 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline |
| AU2008335439A1 (en) * | 2007-12-07 | 2009-06-18 | Vertex Pharmaceuticals Incorporated | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| DK2639223T3 (en) | 2007-12-07 | 2017-06-19 | Vertex Pharma | Process for Preparation of Cycloalkylcarboxiamido-pyridine Benzoic Acids |
| US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| NZ736561A (en) | 2008-02-28 | 2018-02-23 | Vertex Pharma | Heteroaryl derivatives as cftr modulators |
| DK2615085T3 (en) | 2008-03-31 | 2015-10-05 | Vertex Pharma | Pyridyl derivatives as CFTR modulators |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| US12458635B2 (en) | 2008-08-13 | 2025-11-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| US8716338B2 (en) * | 2008-09-29 | 2014-05-06 | Vertex Pharmaceuticals Incorporated | Dosage units of 3-(6-(1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| UA104601C2 (uk) * | 2008-10-23 | 2014-02-25 | Вертекс Фармасьютікалз, Інкорпорейтед | Модулятори регулятора трансмембранної провідності при муковісцидозі |
| PL2408750T3 (pl) | 2009-03-20 | 2016-02-29 | Vertex Pharma | Sposób otrzymywania modulatorów błonowego regulatora przewodnictwa swoistego dla mukowiscydozy |
| EP2477991B1 (en) * | 2009-09-17 | 2015-04-15 | Vertex Pharmaceuticals Incorporated | Process for preparing azabicyclic compounds |
| US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
| DK3150198T3 (da) | 2010-04-07 | 2021-11-01 | Vertex Pharma | Farmaceutiske sammensætninger af 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioxol-5-yl)-cyclopropancarboxamido)-3-methylpyriodin-2-yl)benzoesyre og indgivelse deraf |
| RS54783B1 (sr) | 2010-04-07 | 2016-10-31 | Vertex Pharma | Čvrste forme 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksiamido)-3-metilpiridin-2-il)benzoeve kiseline |
| NZ603042A (en) | 2010-04-22 | 2015-02-27 | Vertex Pharma | Pharmaceutical compositions comprising cftr modulators and administrations thereof |
| CA2797118C (en) | 2010-04-22 | 2021-03-30 | Vertex Pharmaceuticals Incorporated | Process of producing cycloalkylcarboxamido-indole compounds |
| WO2011133953A1 (en) | 2010-04-22 | 2011-10-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| US8563593B2 (en) | 2010-06-08 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Formulations of (R)-1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide |
| MX357328B (es) | 2011-11-08 | 2018-07-05 | Vertex Pharma | Moduladores de trasportadores de casete enlazante de atp. |
| AU2013226076B2 (en) | 2012-02-27 | 2017-11-16 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administration thereof |
| CN102633804B (zh) * | 2012-04-19 | 2014-09-24 | 中南大学 | 一种制备7-氮杂双环[2.2.1]庚烷的方法 |
| US8674108B2 (en) | 2012-04-20 | 2014-03-18 | Vertex Pharmaceuticals Incorporated | Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| EP2872122A1 (en) | 2012-07-16 | 2015-05-20 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of (r)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide and administration thereof |
| RU2718044C2 (ru) | 2013-11-12 | 2020-03-30 | Вертекс Фармасьютикалз Инкорпорейтед | Способ получения фармацевтических композиций для лечения опосредованных cftr заболеваний |
| RS62140B1 (sr) | 2014-04-15 | 2021-08-31 | Vertex Pharma | Farmaceutske kompozicije za lečenje bolesti posredovanih transmembranskim regulatorom provodljivosti cistične fibroze |
| KR20170063954A (ko) | 2014-10-07 | 2017-06-08 | 버텍스 파마슈티칼스 인코포레이티드 | 낭성 섬유증 막횡단 전도도 조절자의 조정제의 공-결정 |
| HRP20211194T1 (hr) | 2014-11-18 | 2021-10-29 | Vertex Pharmaceuticals Inc. | Postupak za provođenje testova velike propusnosti putem tekućinske kromatografije visoke djelotvornosti |
| CR20230120A (es) | 2020-08-07 | 2023-09-01 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| US12324802B2 (en) | 2020-11-18 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006077497A1 (en) * | 2005-01-21 | 2006-07-27 | Pfizer Limited | Crystalline forms cis-5-fluoro-n-[4-(2-hydroxy-4-methylbenzamido) cyclohexyl]-2-(tetrahydrothiopyran-a-yloxy) nicotinamide |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6060473A (en) | 1993-04-01 | 2000-05-09 | Ucb S.A. - Dtb | 7-azabicyclo[2.2.1]-heptane and -heptene derivatives as cholinergic receptor ligands |
| JPH06312989A (ja) * | 1993-04-30 | 1994-11-08 | Nippon Chemiphar Co Ltd | （１ｒｓ，２ｒｓ，４ｓｒ）−２−（６−クロロ−３−ピリジル）−７−アザビシクロ［２．２．１］ヘプタンの製造方法 |
| US6117889A (en) | 1994-04-01 | 2000-09-12 | University Of Virginia | 7-Azabicyclo-[2.2.1]-heptane and -heptene derivatives as analgesics and anti-inflammatory agents |
| TW200407127A (en) * | 2002-08-21 | 2004-05-16 | Astrazeneca Ab | Chemical compounds |
| CN1942479A (zh) * | 2004-02-20 | 2007-04-04 | 阿斯利康(瑞典)有限公司 | 用作GnRH拮抗剂的噻吩并吡咯类化合物 |
| NZ587549A (en) | 2004-06-24 | 2012-10-26 | Vertex Pharma | 6-Amino-indole derivatives and processes for their preparation |
| JP5126856B2 (ja) * | 2007-03-28 | 2013-01-23 | 国立大学法人 長崎大学 | 含窒素レドックス触媒 |
| AU2009308241B2 (en) | 2008-10-23 | 2016-01-07 | Vertex Pharmaceuticals Incorporated | Solid forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl) phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide |
| UA104601C2 (uk) | 2008-10-23 | 2014-02-25 | Вертекс Фармасьютікалз, Інкорпорейтед | Модулятори регулятора трансмембранної провідності при муковісцидозі |
| EP2477991B1 (en) * | 2009-09-17 | 2015-04-15 | Vertex Pharmaceuticals Incorporated | Process for preparing azabicyclic compounds |
| BR112012009584A2 (pt) * | 2009-10-23 | 2019-09-24 | Vertex Pharma | formas sólidas de n-(4-(7-azabiciclo[2.2.1]heptan-7-il)-2-(trifluorometil)fenil)-4-oxo-5-(trifluorometil)-1,4-di-hidroquinolina-3-carboxamida |
| RU2553989C2 (ru) * | 2009-10-23 | 2015-06-20 | Вертекс Фармасьютикалз Инкорпорейтед | Способ получения модуляторов регулятора трансмембранной проводимости кистозного фиброза |
| AR081920A1 (es) * | 2010-05-20 | 2012-10-31 | Vertex Pharma | Procesos de produccion de moduladores del regulador de conductancia transmembrana de fibrosis quistica |
-
2010
- 2010-09-17 EP EP10757544.1A patent/EP2477991B1/en not_active Not-in-force
- 2010-09-17 CA CA2772792A patent/CA2772792A1/en not_active Abandoned
- 2010-09-17 NZ NZ598277A patent/NZ598277A/en not_active IP Right Cessation
- 2010-09-17 US US12/884,925 patent/US8404865B2/en active Active
- 2010-09-17 MX MX2012003343A patent/MX2012003343A/es active IP Right Grant
- 2010-09-17 RU RU2012115111/04A patent/RU2543622C2/ru not_active IP Right Cessation
- 2010-09-17 CN CN201080041222.8A patent/CN102498112B/zh not_active Expired - Fee Related
- 2010-09-17 JP JP2012529933A patent/JP5793496B2/ja not_active Expired - Fee Related
- 2010-09-17 BR BR112012006031A patent/BR112012006031A2/pt not_active IP Right Cessation
- 2010-09-17 ES ES10757544.1T patent/ES2540810T3/es active Active
- 2010-09-17 AU AU2010295461A patent/AU2010295461B2/en not_active Expired - Fee Related
- 2010-09-17 WO PCT/US2010/049306 patent/WO2011035139A1/en not_active Ceased
- 2010-09-17 KR KR1020127009689A patent/KR20120083416A/ko not_active Withdrawn
-
2012
- 2012-02-20 ZA ZA2012/01252A patent/ZA201201252B/en unknown
- 2012-03-09 US US13/416,157 patent/US8461352B2/en not_active Expired - Fee Related
- 2012-03-14 IL IL218641A patent/IL218641A0/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006077497A1 (en) * | 2005-01-21 | 2006-07-27 | Pfizer Limited | Crystalline forms cis-5-fluoro-n-[4-(2-hydroxy-4-methylbenzamido) cyclohexyl]-2-(tetrahydrothiopyran-a-yloxy) nicotinamide |
Non-Patent Citations (1)
| Title |
|---|
| Canadion J. of Chemistry, 1970, 48, 13, p.2065-2074. * |
Also Published As
| Publication number | Publication date |
|---|---|
| RU2012115111A (ru) | 2013-10-27 |
| EP2477991A1 (en) | 2012-07-25 |
| CN102498112A (zh) | 2012-06-13 |
| NZ598277A (en) | 2014-03-28 |
| ZA201201252B (en) | 2013-05-29 |
| ES2540810T3 (es) | 2015-07-13 |
| CN102498112B (zh) | 2015-05-20 |
| IL218641A0 (en) | 2012-05-31 |
| AU2010295461B2 (en) | 2016-03-03 |
| JP5793496B2 (ja) | 2015-10-14 |
| AU2010295461A1 (en) | 2012-03-08 |
| BR112012006031A2 (pt) | 2019-09-24 |
| US8461352B2 (en) | 2013-06-11 |
| US8404865B2 (en) | 2013-03-26 |
| KR20120083416A (ko) | 2012-07-25 |
| WO2011035139A1 (en) | 2011-03-24 |
| US20120259129A1 (en) | 2012-10-11 |
| CA2772792A1 (en) | 2011-03-24 |
| JP2013505259A (ja) | 2013-02-14 |
| EP2477991B1 (en) | 2015-04-15 |
| HK1169106A1 (en) | 2013-01-18 |
| MX2012003343A (es) | 2012-08-17 |
| US20110065928A1 (en) | 2011-03-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20160918 |