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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JP2012529933A
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English (en)
Japanese (ja)
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JP2013505259A (ja
JP2013505259A5 (https=
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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Publication of JP2013505259A publication Critical patent/JP2013505259A/ja
Publication of JP2013505259A5 publication Critical patent/JP2013505259A5/ja
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Publication of JP5793496B2 publication Critical patent/JP5793496B2/ja
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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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (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)

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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
RU2006111093A (ru) 2003-09-06 2007-10-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) Модуляторы атр-связывающих кассетных транспортеров
CN101675928A (zh) * 2003-11-14 2010-03-24 沃泰克斯药物股份有限公司 可用作atp-结合弹夹转运蛋白调控剂的噻唑和噁唑
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
RS56037B1 (sr) 2004-06-24 2017-09-29 Vertex Pharma Modulatori atp-vezujućih kasetnih transportera
US7999113B2 (en) 2005-08-11 2011-08-16 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
CA2856037C (en) 2005-12-28 2017-03-07 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
EP3219705B1 (en) 2005-12-28 2020-03-11 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of the amorphous form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
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
EP2674428B1 (en) 2006-04-07 2016-04-06 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
CN104447716A (zh) 2007-05-09 2015-03-25 沃泰克斯药物股份有限公司 Cftr调节剂
JP5389030B2 (ja) 2007-08-24 2014-01-15 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 （特に）嚢胞性線維症の処置に有用なイソチアゾロピリジノン
SI2578571T1 (sl) 2007-11-16 2016-01-29 Vertex Pharmaceuticals Incorporated Izokinolinski modulatorji prenašalcev z atp-vezavno kaseto
MX365732B (es) * 2007-12-07 2019-06-12 Vertex Pharma Procesos para producir acidos cicloalquilcarboxamido-piridin benzoicos.
EP3683218B1 (en) 2007-12-07 2024-09-18 Vertex Pharmaceuticals Incorporated Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
CN101998854A (zh) * 2007-12-07 2011-03-30 沃泰克斯药物股份有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的制剂
NZ720282A (en) 2008-02-28 2017-12-22 Vertex Pharma Heteroaryl derivatives as cftr modulators
NZ616097A (en) 2008-03-31 2015-04-24 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
AR073709A1 (es) 2008-09-29 2010-11-24 Vertex Pharma Unidades de dosis de acido 3-(6-(1-(2,2-difluorobenzeno (d) (1,3) dioxol-5-il) ciclopropancarboxamido)-3-metilpiridin-2-il) benzoico
EP2349263B1 (en) * 2008-10-23 2014-04-23 Vertex Pharmaceuticals Inc. Modulators of cystic fibrosis transmembrane conductance regulator
PL2408750T3 (pl) 2009-03-20 2016-02-29 Vertex Pharma Sposób otrzymywania modulatorów błonowego regulatora przewodnictwa swoistego dla mukowiscydozy
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
MX2012011655A (es) 2010-04-07 2012-11-23 Vertex Pharma Formas solidas de acido 3-(6-(1-(2,2-difluorobenzo [d][1-3]dioxol-5-il]ciclopropanocarboxamido)-3-metilpiridin-2-il) benzoico.
JP2013523833A (ja) 2010-04-07 2013-06-17 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）安息香酸の医薬組成物およびその投与
MX353408B (es) 2010-04-22 2018-01-11 Vertex Pharma Proceso para producir compuestos de cicloalquilcarboxamido-indol.
CA2796602A1 (en) 2010-04-22 2011-10-27 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
WO2013070961A1 (en) 2011-11-08 2013-05-16 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
NZ727015A (en) 2012-01-25 2017-12-22 Vertex Pharma Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
JP2015511583A (ja) 2012-02-27 2015-04-20 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 薬学的組成物およびその投与
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
AR092857A1 (es) 2012-07-16 2015-05-06 Vertex Pharma Composiciones farmaceuticas de (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)-n-(1-(2,3-dihidroxipropil)-6-fluoro-2-(1-hidroxi-2-metilpropan-2-il)-1h-indol-5-il)ciclopropancarboxamida y administracion de las mismas
AU2014349010C1 (en) 2013-11-12 2020-08-06 Vertex Pharmaceuticals Incorporated Process of preparing pharmaceutical compositions for the treatment of CFTR mediated diseases
RU2744460C2 (ru) 2014-04-15 2021-03-09 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости
CN107250113B (zh) 2014-10-07 2019-03-29 弗特克斯药品有限公司 囊性纤维化跨膜传导调节蛋白的调节剂的共晶
RU2691136C2 (ru) 2014-11-18 2019-06-11 Вертекс Фармасьютикалз Инкорпорейтед Способ проведения высокопроизводительной тестовой высокоэффективной жидкостной хроматографии
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
JP2007523146A (ja) * 2004-02-20 2007-08-16 アストラゼネカ アクチボラグ ＧｎＲＨのアンタゴニストとしてのチエノピロール類
RS56037B1 (sr) * 2004-06-24 2017-09-29 Vertex Pharma Modulatori atp-vezujućih kasetnih transportera
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
CN102224141B (zh) * 2008-10-23 2014-10-08 沃泰克斯药物股份有限公司 N-(4-(7-氮杂双环[2.2.1]庚-7-基)-2-(三氟甲基)苯基)-4-氧代-5-(三氟甲基)-1,4-二氢喹啉-3-甲酰胺的固体形式
EP2349263B1 (en) * 2008-10-23 2014-04-23 Vertex Pharmaceuticals Inc. Modulators of cystic fibrosis transmembrane conductance regulator
BR112012006031A2 (pt) * 2009-09-17 2019-09-24 Vertex Pharma processo para preparação de compostos azabicíclicos.
US8344147B2 (en) * 2009-10-23 2013-01-01 Vertex Pharmaceutical Incorporated Process for preparing modulators of cystic fibrosis transmembrane conductance regulator
CN102666546B (zh) * 2009-10-23 2015-09-09 沃泰克斯药物股份有限公司 N-(4-(7-氮杂双环[2.2.1]庚-7-基)-2-(三氟甲基)苯基)-4-氧代-5-(三氟甲基)-1,4-二氢喹啉-3-甲酰胺的固体形式
AR081920A1 (es) * 2010-05-20 2012-10-31 Vertex Pharma Procesos de produccion de moduladores del regulador de conductancia transmembrana de fibrosis quistica

Also Published As

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

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