JP5793496B2 - アザ二環式化合物を調製するプロセス - Google Patents

アザ二環式化合物を調製するプロセス Download PDF

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Publication number
JP5793496B2
JP5793496B2 JP2012529933A JP2012529933A JP5793496B2 JP 5793496 B2 JP5793496 B2 JP 5793496B2 JP 2012529933 A JP2012529933 A JP 2012529933A JP 2012529933 A JP2012529933 A JP 2012529933A JP 5793496 B2 JP5793496 B2 JP 5793496B2
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Japan
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compound
formula
solvent
contacted
base
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Expired - Fee Related
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JP2012529933A
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Japanese (ja)
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JP2013505259A5 (https=
JP2013505259A (ja
Inventor
ナレンドラ バーリチャンドラ アムベイカー，
ナレンドラ バーリチャンドラ アムベイカー，
ブライアン リチャード ベア，
ブライアン リチャード ベア，
レブ ティー．ディー． ファニング，
レブ ティー．ディー． ファニング，
ロバート ヒューズ，
ロバート ヒューズ，
ベンジャミン リッター，
ベンジャミン リッター，
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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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

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  • 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)
JP2012529933A 2009-09-17 2010-09-17 アザ二環式化合物を調製するプロセス Expired - Fee Related JP5793496B2 (ja)

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 (3)

Publication Number Publication Date
JP2013505259A JP2013505259A (ja) 2013-02-14
JP2013505259A5 JP2013505259A5 (https=) 2013-11-07
JP5793496B2 true JP5793496B2 (ja) 2015-10-14

Family

ID=43242763

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012529933A Expired - Fee Related JP5793496B2 (ja) 2009-09-17 2010-09-17 アザ二環式化合物を調製するプロセス

Country Status (15)

Country Link
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=)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
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
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
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
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

Family Cites Families (14)

* Cited by examiner, † Cited by third party
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
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

Also Published As

Publication number Publication date
AU2010295461A1 (en) 2012-03-08
AU2010295461B2 (en) 2016-03-03
CN102498112B (zh) 2015-05-20
IL218641A0 (en) 2012-05-31
BR112012006031A2 (pt) 2019-09-24
US8461352B2 (en) 2013-06-11
US8404865B2 (en) 2013-03-26
EP2477991B1 (en) 2015-04-15
CN102498112A (zh) 2012-06-13
US20120259129A1 (en) 2012-10-11
KR20120083416A (ko) 2012-07-25
ES2540810T3 (es) 2015-07-13
NZ598277A (en) 2014-03-28
CA2772792A1 (en) 2011-03-24
MX2012003343A (es) 2012-08-17
RU2012115111A (ru) 2013-10-27
ZA201201252B (en) 2013-05-29
EP2477991A1 (en) 2012-07-25
US20110065928A1 (en) 2011-03-17
WO2011035139A1 (en) 2011-03-24
HK1169106A1 (en) 2013-01-18
RU2543622C2 (ru) 2015-03-10
JP2013505259A (ja) 2013-02-14

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