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
-
- 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 (https=) |
| EP (1) | EP2477991B1 (https=) |
| JP (1) | JP5793496B2 (https=) |
| KR (1) | KR20120083416A (https=) |
| CN (1) | CN102498112B (https=) |
| AU (1) | AU2010295461B2 (https=) |
| BR (1) | BR112012006031A2 (https=) |
| CA (1) | CA2772792A1 (https=) |
| ES (1) | ES2540810T3 (https=) |
| IL (1) | IL218641A0 (https=) |
| MX (1) | MX2012003343A (https=) |
| NZ (1) | NZ598277A (https=) |
| RU (1) | RU2543622C2 (https=) |
| WO (1) | WO2011035139A1 (https=) |
| ZA (1) | ZA201201252B (https=) |
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| 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 |
| LT2502911T (lt) | 2004-06-24 | 2017-09-11 | Vertex Pharmaceuticals Incorporated | Atp surišančios kasetės transporterių moduliatoriai |
| ATE512145T1 (de) | 2005-08-11 | 2011-06-15 | Vertex Pharma | Modulatoren des cystic fibrosis transmembrane conductance regulators |
| EP1945632B1 (en) | 2005-11-08 | 2013-09-18 | Vertex Pharmaceuticals Incorporated | Heterocyclic modulators of atp-binding cassette transporters |
| AU2006336504C9 (en) * | 2005-12-28 | 2015-05-14 | Vertex Pharmaceuticals Incorporated | 1-(benzo [D] [1,3] dioxol-5-yl) -N- (phenyl) cyclopropane- carboxamide derivatives and related compounds as modulators of ATP-Binding Cassette transporters for the treatment of Cystic Fibrosis |
| WO2007079139A2 (en) | 2005-12-28 | 2007-07-12 | Vertex Pharmaceuticals, Inc. | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| NZ571803A (en) | 2006-04-07 | 2011-12-22 | Vertex Pharma | Amide indole derivatives as modulators of ATP-binding cassette transporters |
| US10022352B2 (en) | 2006-04-07 | 2018-07-17 | 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 |
| US8563573B2 (en) * | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| US8969386B2 (en) | 2007-05-09 | 2015-03-03 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
| HUE028426T2 (en) | 2007-08-24 | 2016-12-28 | Vertex Pharma | Isothiazolopyridinones for (inter alia) treating cystic fibrosis |
| SI2217572T1 (sl) | 2007-11-16 | 2014-05-30 | Vertex Pharmaceuticals Incorporated | Izokinolinski modulatorji prenaĺ alcev z atp-vezavno kaseto |
| US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| SI2225230T1 (sl) | 2007-12-07 | 2017-03-31 | Vertex Pharmaceuticals Incorporated | Trdne oblike 3-(6-(1-2,2-difluorobenzo(d)(1,3)dioxol-5-il)ciklopropan- karboksamido)-3-metilpiridin-2-il) benzojske kisline |
| WO2009076141A2 (en) * | 2007-12-07 | 2009-06-18 | Vertex Pharmaceuticals Incorporated | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cycklopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| EP2639224B1 (en) | 2007-12-07 | 2016-08-24 | Vertex Pharmaceuticals Incorporated | Process for producing cycloalkylcarboxiamido-pyridine benzoic acids |
| NZ720282A (en) | 2008-02-28 | 2017-12-22 | Vertex Pharma | Heteroaryl derivatives as cftr modulators |
| EP2271621B1 (en) * | 2008-03-31 | 2013-11-20 | Vertex Pharmaceuticals Incorporated | 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 |
| JP2012504143A (ja) * | 2008-09-29 | 2012-02-16 | 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 | ３−（６−（１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）シクロプロパンカルボキサミド）−３−メチルピリジン−２−イル）安息香酸の用量単位 |
| NZ592685A (en) * | 2008-10-23 | 2013-04-26 | Vertex Pharma | Modulators of cystic fibrosis transmembrane conductance regulator |
| SI2408750T1 (sl) | 2009-03-20 | 2015-11-30 | Vertex Pharmaceuticals Incorporated | Postopek za izdelavo modulatorjev cistično-fibroznega transmembranskega regulatorja prevodnosti |
| BR112012006031A2 (pt) * | 2009-09-17 | 2019-09-24 | Vertex Pharma | processo para preparação de compostos azabicíclicos. |
| 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 |
| HRP20211752T1 (hr) | 2010-04-07 | 2022-02-18 | Vertex Pharmaceuticals Incorporated | Farmaceutski pripravci 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline i njihova primjena |
| HRP20160682T1 (hr) | 2010-04-07 | 2016-07-29 | Vertex Pharmaceuticals Incorporated | Čvrsti oblici 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksiamido)-3-metilpiridin-2-il)benzojeve kiseline |
| ES2608474T3 (es) | 2010-04-22 | 2017-04-11 | Vertex Pharmaceuticals Incorporated | Proceso de producción de compuestos indol cycloalkylcarboxamido |
| CA2796642A1 (en) | 2010-04-22 | 2011-10-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| AU2011242454A1 (en) | 2010-04-22 | 2012-11-08 | 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 |
| IN2014KN00885A (https=) | 2011-11-08 | 2015-10-02 | Vertex Pharma | |
| WO2013112804A1 (en) | 2012-01-25 | 2013-08-01 | Vertex Pharmaceuticals Incorporated | Formulations of 3-(6-(1-(2.2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| EP2819670A1 (en) | 2012-02-27 | 2015-01-07 | 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 |
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| WO2014014841A1 (en) | 2012-07-16 | 2014-01-23 | 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 |
| JP6963896B2 (ja) | 2013-11-12 | 2021-11-10 | 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Vertex Pharmaceuticals Incorporated | Ｃｆｔｒ媒介性疾患の処置のための医薬組成物を調製する方法 |
| ES2885181T3 (es) | 2014-04-15 | 2021-12-13 | Vertex Pharma | Composiciones farmacéuticas para el tratamiento de enfermedades mediadas por el regulador de la conductancia transmembrana de fibrosis quística |
| KR20170063954A (ko) | 2014-10-07 | 2017-06-08 | 버텍스 파마슈티칼스 인코포레이티드 | 낭성 섬유증 막횡단 전도도 조절자의 조정제의 공-결정 |
| PT3221692T (pt) | 2014-11-18 | 2021-09-10 | Vertex Pharma | Processo de realização de testagem de alta produtividade por cromatografia líquida de alta eficiência |
| 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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| 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 |
| EP1730155A1 (en) * | 2004-02-20 | 2006-12-13 | AstraZeneca AB | Thienopyrroles as antagonists of gnrh |
| LT2502911T (lt) | 2004-06-24 | 2017-09-11 | Vertex Pharmaceuticals Incorporated | Atp surišančios kasetės transporterių moduliatoriai |
| EP1844040A1 (en) * | 2005-01-21 | 2007-10-17 | Pfizer Limited | Crystalline forms of cis-5-fluoro-n-[4-(2-hydroxy-4-methylbenzamido)cyclohexyl]-2-(tetrahydrothiopyran-4-yloxy)nicotinamide |
| WO2008117871A1 (ja) * | 2007-03-28 | 2008-10-02 | Nagasaki University | 含窒素レドックス触媒 |
| NZ592685A (en) | 2008-10-23 | 2013-04-26 | Vertex Pharma | Modulators of cystic fibrosis transmembrane conductance regulator |
| PT2358680E (pt) | 2008-10-23 | 2013-05-14 | Vertex Pharma | Formas sólidas de n-(4-(7-azabiciclo[2.2.1]heptan-7-il)-2- (trifluorometil)fenil)-4-oxo- 5-(trifluorometil)-1,4- dihidroquinolina-3-carboxamida |
| BR112012006031A2 (pt) * | 2009-09-17 | 2019-09-24 | Vertex Pharma | processo para preparação de compostos azabicíclicos. |
| WO2011050220A1 (en) * | 2009-10-23 | 2011-04-28 | 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 |
| CN102648182A (zh) * | 2009-10-23 | 2012-08-22 | 沃泰克斯药物股份有限公司 | 用于制备囊性纤维化跨膜传导调节因子的调节剂的方法 |
| TW201202250A (en) * | 2010-05-20 | 2012-01-16 | Vertex Pharma | Processes for producing modulators of cystic fibrosis transmembrane conductance regulator |
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- 2010-09-17 KR KR1020127009689A patent/KR20120083416A/ko not_active Withdrawn
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| EP2477991A1 (en) | 2012-07-25 |
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| WO2011035139A1 (en) | 2011-03-24 |
| HK1169106A1 (en) | 2013-01-18 |
| RU2543622C2 (ru) | 2015-03-10 |
| JP2013505259A (ja) | 2013-02-14 |
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