ES2540810T3 - Proceso para preparar compuestos azabicíclicos - Google Patents
Proceso para preparar compuestos azabicíclicos Download PDFInfo
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- ES2540810T3 ES2540810T3 ES10757544.1T ES10757544T ES2540810T3 ES 2540810 T3 ES2540810 T3 ES 2540810T3 ES 10757544 T ES10757544 T ES 10757544T ES 2540810 T3 ES2540810 T3 ES 2540810T3
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 92
- 238000004519 manufacturing process Methods 0.000 title abstract description 8
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims abstract description 21
- DYHSDKLCOJIUFX-UHFFFAOYSA-N tert-butoxycarbonyl anhydride Chemical compound CC(C)(C)OC(=O)OC(=O)OC(C)(C)C DYHSDKLCOJIUFX-UHFFFAOYSA-N 0.000 claims abstract description 16
- IMLXLGZJLAOKJN-UHFFFAOYSA-N 4-aminocyclohexan-1-ol Chemical compound NC1CCC(O)CC1 IMLXLGZJLAOKJN-UHFFFAOYSA-N 0.000 claims abstract description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 claims abstract description 7
- 150000003839 salts Chemical class 0.000 claims abstract description 7
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- QARBMVPHQWIHKH-UHFFFAOYSA-N methanesulfonyl chloride Chemical compound CS(Cl)(=O)=O QARBMVPHQWIHKH-UHFFFAOYSA-N 0.000 claims abstract description 6
- 239000000203 mixture Substances 0.000 claims description 57
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 41
- 238000000034 method Methods 0.000 claims description 40
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Classifications
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- 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)
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| US24347709P | 2009-09-17 | 2009-09-17 | |
| US243477P | 2009-09-17 | ||
| PCT/US2010/049306 WO2011035139A1 (en) | 2009-09-17 | 2010-09-17 | Process for preparing azabicyclic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2540810T3 true ES2540810T3 (es) | 2015-07-13 |
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| ES10757544.1T Active ES2540810T3 (es) | 2009-09-17 | 2010-09-17 | Proceso para preparar compuestos azabicíclicos |
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|---|---|
| US (2) | US8404865B2 (OSRAM) |
| EP (1) | EP2477991B1 (OSRAM) |
| JP (1) | JP5793496B2 (OSRAM) |
| KR (1) | KR20120083416A (OSRAM) |
| CN (1) | CN102498112B (OSRAM) |
| AU (1) | AU2010295461B2 (OSRAM) |
| BR (1) | BR112012006031A2 (OSRAM) |
| CA (1) | CA2772792A1 (OSRAM) |
| ES (1) | ES2540810T3 (OSRAM) |
| IL (1) | IL218641A0 (OSRAM) |
| MX (1) | MX2012003343A (OSRAM) |
| NZ (1) | NZ598277A (OSRAM) |
| RU (1) | RU2543622C2 (OSRAM) |
| WO (1) | WO2011035139A1 (OSRAM) |
| ZA (1) | ZA201201252B (OSRAM) |
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| CN1898221A (zh) | 2003-09-06 | 2007-01-17 | 沃泰克斯药物股份有限公司 | Atp－结合弹夹转运蛋白的调控剂 |
| ZA200604578B (en) * | 2003-11-14 | 2008-05-28 | Vertex Pharma | Thiazoles and oxazoles.useful as modulators of ATP Binding cassette transporters |
| US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| PT1773816E (pt) | 2004-06-24 | 2015-04-29 | Vertex Pharma | Moduladores de transportadores de cassete de ligação de atp |
| CA2618057A1 (en) | 2005-08-11 | 2007-02-22 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| CN102775396B (zh) | 2005-11-08 | 2014-10-08 | 沃泰克斯药物股份有限公司 | Atp-结合弹夹转运蛋白的杂环调控剂 |
| US7691902B2 (en) | 2005-12-28 | 2010-04-06 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| RS55940B1 (sr) | 2005-12-28 | 2017-09-29 | Vertex Pharma | Čvrsti oblici n-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksohinolin-3-karboksamida |
| PL2007756T3 (pl) | 2006-04-07 | 2016-01-29 | Vertex Pharma | Modulatory transporterów posiadających kasetę wiążącą ATP |
| US7645789B2 (en) * | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| USRE50453E1 (en) | 2006-04-07 | 2025-06-10 | 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 |
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| JP5497633B2 (ja) | 2007-05-09 | 2014-05-21 | 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 | Ｃｆｔｒのモジュレーター |
| AU2008302598B2 (en) | 2007-08-24 | 2014-07-17 | Vertex Pharmaceuticals Incorporated | Isothiazolopyridinones useful for the treatment of (inter alia) Cystic Fibrosis |
| CN101952254B (zh) | 2007-11-16 | 2012-09-05 | 沃泰克斯药物股份有限公司 | Atp结合盒转运蛋白的异喹啉调节剂 |
| NZ614151A (en) | 2007-12-07 | 2015-04-24 | Vertex Pharma | Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| EP2231606B1 (en) | 2007-12-07 | 2013-02-13 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxiamido-pyridine benzoic acids |
| US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| EA201070699A1 (ru) * | 2007-12-07 | 2011-02-28 | Вертекс Фармасьютикалз Инкорпорейтед | Композиции 3-(6-(1-2,2-дифторбензо[d][1,3]диоксол-5-ил)циклопропанкарбоксамидо)-3-метилпиридин-2-ил)бензойной кислоты |
| ES2647531T3 (es) | 2008-02-28 | 2017-12-22 | Vertex Pharmaceuticals Incorporated | Derivados de heteroarilo como moduladores de CFTR |
| NZ616097A (en) * | 2008-03-31 | 2015-04-24 | Vertex Pharma | Pyridyl derivatives as cftr modulators |
| US12458635B2 (en) | 2008-08-13 | 2025-11-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| CA2736545A1 (en) * | 2008-09-29 | 2010-04-01 | 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 |
| PL2349263T3 (pl) * | 2008-10-23 | 2014-11-28 | Vertex Pharma | Modulatory mukowiscydozowego regulatora przewodnictwa przezbłonowego |
| EP2821400B1 (en) | 2009-03-20 | 2017-09-27 | Vertex Pharmaceuticals Incorporated | Process for making modulators of cystic fibrosis transmembrane conductance regulator |
| WO2011035139A1 (en) * | 2009-09-17 | 2011-03-24 | 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 |
| ME02446B (me) | 2010-04-07 | 2016-09-20 | Vertex Pharma | Čvrste forme 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksiamido)-3-metilpiridin-2-il)benzoeve kiseline |
| ES3017582T3 (en) | 2010-04-07 | 2025-05-13 | Vertex Pharma | Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyriodin-2-yl)benzoic acid and administration thereof |
| KR20190061096A (ko) | 2010-04-22 | 2019-06-04 | 버텍스 파마슈티칼스 인코포레이티드 | 시클로알킬카르복스아미도-인돌 화합물의 제조 방법 |
| EP2560650A1 (en) | 2010-04-22 | 2013-02-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| EP2560649A1 (en) | 2010-04-22 | 2013-02-27 | 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 |
| HRP20170458T1 (hr) | 2011-11-08 | 2017-05-19 | Vertex Pharmaceuticals Inc. | Modulatori atp - vezujućih kasetnih transportera |
| MX2014010253A (es) | 2012-02-27 | 2014-11-12 | Vertex Pharma | Composicion farmaceutica y administraciones de la misma. |
| 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 |
| CA2878057A1 (en) | 2012-07-16 | 2014-01-23 | Rossitza Gueorguieva Alargova | Pharmaceutical compositions 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 and administration thereof |
| CN105848657B (zh) | 2013-11-12 | 2020-05-22 | 沃泰克斯药物股份有限公司 | 制备用于治疗cftr介导的疾病的药物组合物的方法 |
| PL3925607T3 (pl) | 2014-04-15 | 2023-10-30 | Vertex Pharmaceuticals Incorporated | Kompozycje farmaceutyczne do leczenia chorób, w których pośredniczy mukowiscydozowy przezbłonowy regulator przewodnictwa |
| RU2749213C2 (ru) | 2014-10-07 | 2021-06-07 | Вертекс Фармасьютикалз Инкорпорейтед | Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе |
| SI3221692T1 (sl) | 2014-11-18 | 2021-11-30 | Vertex Pharmaceuticals Inc. | Postopek za izvajanje testov visoke prepustnosti z visoko zmogljivostno tekočinsko kromatografijo |
| 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 |
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| 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 |
| PT1773816E (pt) | 2004-06-24 | 2015-04-29 | Vertex Pharma | Moduladores de transportadores de cassete de ligação de atp |
| 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 |
| 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 |
| PL2349263T3 (pl) | 2008-10-23 | 2014-11-28 | Vertex Pharma | Modulatory mukowiscydozowego regulatora przewodnictwa przezbłonowego |
| RU2518479C2 (ru) | 2008-10-23 | 2014-06-10 | Вертекс Фармасьютикалз Инкорпорейтед | Твердые формы n-(7-азабицикло[2.2.1]гептан-7-ил-)-2-(трифторметил)фенил)-4-оксо-5-(трифторметил)-1,4-дигидрохинолин-3-карбоксамида |
| WO2011035139A1 (en) * | 2009-09-17 | 2011-03-24 | Vertex Pharmaceuticals Incorporated | Process for preparing azabicyclic compounds |
| CA2778492A1 (en) * | 2009-10-23 | 2011-04-28 | Vertex Pharmaceuticals Incorporated | Process for preparing modulators of cystic fibrosis transmembrane conductance regulator |
| KR20120102645A (ko) * | 2009-10-23 | 2012-09-18 | 버텍스 파마슈티칼스 인코포레이티드 | Ｎ-(4-(7-아자비시클로［2.2.1］헵탄-7-일)-2-(트리플루오로메틸)페닐)-4-옥소-5-(트리플루오로메틸)-1,4-디히드로퀴놀린-3-카르복사미드의 고체 형태 |
| US8404849B2 (en) * | 2010-05-20 | 2013-03-26 | Vertex Pharmaceuticals | Processes for producing modulators of cystic fibrosis transmembrane conductance regulator |
-
2010
- 2010-09-17 WO PCT/US2010/049306 patent/WO2011035139A1/en not_active Ceased
- 2010-09-17 CA CA2772792A patent/CA2772792A1/en not_active Abandoned
- 2010-09-17 RU RU2012115111/04A patent/RU2543622C2/ru not_active IP Right Cessation
- 2010-09-17 US US12/884,925 patent/US8404865B2/en active Active
- 2010-09-17 BR BR112012006031A patent/BR112012006031A2/pt not_active IP Right Cessation
- 2010-09-17 KR KR1020127009689A patent/KR20120083416A/ko not_active Withdrawn
- 2010-09-17 JP JP2012529933A patent/JP5793496B2/ja not_active Expired - Fee Related
- 2010-09-17 CN CN201080041222.8A patent/CN102498112B/zh not_active Expired - Fee Related
- 2010-09-17 EP EP10757544.1A patent/EP2477991B1/en not_active Not-in-force
- 2010-09-17 MX MX2012003343A patent/MX2012003343A/es active IP Right Grant
- 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 NZ NZ598277A patent/NZ598277A/en not_active IP Right Cessation
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- 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
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| EP2477991A1 (en) | 2012-07-25 |
| BR112012006031A2 (pt) | 2019-09-24 |
| EP2477991B1 (en) | 2015-04-15 |
| AU2010295461B2 (en) | 2016-03-03 |
| RU2543622C2 (ru) | 2015-03-10 |
| ZA201201252B (en) | 2013-05-29 |
| NZ598277A (en) | 2014-03-28 |
| JP2013505259A (ja) | 2013-02-14 |
| US8461352B2 (en) | 2013-06-11 |
| MX2012003343A (es) | 2012-08-17 |
| WO2011035139A1 (en) | 2011-03-24 |
| IL218641A0 (en) | 2012-05-31 |
| JP5793496B2 (ja) | 2015-10-14 |
| US20110065928A1 (en) | 2011-03-17 |
| HK1169106A1 (en) | 2013-01-18 |
| CN102498112A (zh) | 2012-06-13 |
| CN102498112B (zh) | 2015-05-20 |
| KR20120083416A (ko) | 2012-07-25 |
| RU2012115111A (ru) | 2013-10-27 |
| AU2010295461A1 (en) | 2012-03-08 |
| US8404865B2 (en) | 2013-03-26 |
| CA2772792A1 (en) | 2011-03-24 |
| US20120259129A1 (en) | 2012-10-11 |
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