KR20120083416A - 아자비시클릭 화합물의 제조 방법 - Google Patents

아자비시클릭 화합물의 제조 방법 Download PDF

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Publication number
KR20120083416A
KR20120083416A KR1020127009689A KR20127009689A KR20120083416A KR 20120083416 A KR20120083416 A KR 20120083416A KR 1020127009689 A KR1020127009689 A KR 1020127009689A KR 20127009689 A KR20127009689 A KR 20127009689A KR 20120083416 A KR20120083416 A KR 20120083416A
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KR
South Korea
Prior art keywords
compound
formula
solvent
mixture
base
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KR1020127009689A
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English (en)
Korean (ko)
Inventor
나렌드라 발칸드라 암바이카르
브리안 리차드 베어
레브 티. 디. 패닝
로버트 휴즈
벤자민 리틀러
Original Assignee
버텍스 파마슈티칼스 인코포레이티드
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Publication of KR20120083416A publication Critical patent/KR20120083416A/ko
Withdrawn legal-status Critical Current

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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)
KR1020127009689A 2009-09-17 2010-09-17 아자비시클릭 화합물의 제조 방법 Withdrawn KR20120083416A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24347709P 2009-09-17 2009-09-17
US61/243,477 2009-09-17

Publications (1)

Publication Number Publication Date
KR20120083416A true KR20120083416A (ko) 2012-07-25

Family

ID=43242763

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127009689A Withdrawn KR20120083416A (ko) 2009-09-17 2010-09-17 아자비시클릭 화합물의 제조 방법

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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
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

Also Published As

Publication number Publication date
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
RU2012115111A (ru) 2013-10-27
AU2010295461A1 (en) 2012-03-08
ES2540810T3 (es) 2015-07-13
US8404865B2 (en) 2013-03-26
CA2772792A1 (en) 2011-03-24
US20120259129A1 (en) 2012-10-11

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