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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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
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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Withdrawn legal-status Critical Current

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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)
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 (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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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
NZ587549A (en) 2004-06-24 2012-10-26 Vertex Pharma 6-Amino-indole derivatives and processes for their preparation
EP1912983B1 (en) 2005-08-11 2011-06-08 Vertex Pharmaceuticals, Inc. Modulators of cystic fibrosis transmembrane conductance regulator
KR101331768B1 (ko) * 2005-11-08 2013-11-22 버텍스 파마슈티칼스 인코포레이티드 Ａｔｐ 결합 카세트 수송체의 헤테로사이클릭 조정제
CA2635581C (en) 2005-12-28 2017-02-28 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
CA2856037C (en) * 2005-12-28 2017-03-07 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
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
PL2674428T3 (pl) 2006-04-07 2017-01-31 Vertex Pharmaceuticals Incorporated Modulatory transporterów z kasetą wiążącą ATP
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
CA2686838C (en) 2007-05-09 2017-03-14 Vertex Pharmaceuticals Incorporated Modulators of cftr
AU2008302598B2 (en) 2007-08-24 2014-07-17 Vertex Pharmaceuticals Incorporated Isothiazolopyridinones useful for the treatment of (inter alia) Cystic Fibrosis
SI2578571T1 (sl) 2007-11-16 2016-01-29 Vertex Pharmaceuticals Incorporated Izokinolinski modulatorji prenašalcev z atp-vezavno kaseto
HRP20170241T2 (hr) 2007-12-07 2023-03-17 Vertex Pharmaceuticals Incorporated Čvrsti oblici 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline
AU2008335439A1 (en) * 2007-12-07 2009-06-18 Vertex Pharmaceuticals Incorporated Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
DK2639223T3 (en) 2007-12-07 2017-06-19 Vertex Pharma Process for Preparation of Cycloalkylcarboxiamido-pyridine Benzoic Acids
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
NZ736561A (en) 2008-02-28 2018-02-23 Vertex Pharma Heteroaryl derivatives as cftr modulators
DK2615085T3 (en) 2008-03-31 2015-10-05 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
US8716338B2 (en) * 2008-09-29 2014-05-06 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
UA104601C2 (uk) * 2008-10-23 2014-02-25 Вертекс Фармасьютікалз, Інкорпорейтед Модулятори регулятора трансмембранної провідності при муковісцидозі
PL2408750T3 (pl) 2009-03-20 2016-02-29 Vertex Pharma Sposób otrzymywania modulatorów błonowego regulatora przewodnictwa swoistego dla mukowiscydozy
EP2477991B1 (en) * 2009-09-17 2015-04-15 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
DK3150198T3 (da) 2010-04-07 2021-11-01 Vertex Pharma Farmaceutiske sammensætninger af 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioxol-5-yl)-cyclopropancarboxamido)-3-methylpyriodin-2-yl)benzoesyre og indgivelse deraf
RS54783B1 (sr) 2010-04-07 2016-10-31 Vertex Pharma Čvrste forme 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksiamido)-3-metilpiridin-2-il)benzoeve kiseline
NZ603042A (en) 2010-04-22 2015-02-27 Vertex Pharma Pharmaceutical compositions comprising cftr modulators and administrations thereof
CA2797118C (en) 2010-04-22 2021-03-30 Vertex Pharmaceuticals Incorporated Process of producing cycloalkylcarboxamido-indole compounds
WO2011133953A1 (en) 2010-04-22 2011-10-27 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
MX357328B (es) 2011-11-08 2018-07-05 Vertex Pharma Moduladores de trasportadores de casete enlazante de atp.
AU2013226076B2 (en) 2012-02-27 2017-11-16 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
EP2872122A1 (en) 2012-07-16 2015-05-20 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
RU2718044C2 (ru) 2013-11-12 2020-03-30 Вертекс Фармасьютикалз Инкорпорейтед Способ получения фармацевтических композиций для лечения опосредованных cftr заболеваний
RS62140B1 (sr) 2014-04-15 2021-08-31 Vertex Pharma Farmaceutske kompozicije za lečenje bolesti posredovanih transmembranskim regulatorom provodljivosti cistične fibroze
KR20170063954A (ko) 2014-10-07 2017-06-08 버텍스 파마슈티칼스 인코포레이티드 낭성 섬유증 막횡단 전도도 조절자의 조정제의 공-결정
HRP20211194T1 (hr) 2014-11-18 2021-10-29 Vertex Pharmaceuticals Inc. Postupak za provođenje testova velike propusnosti putem tekućinske kromatografije visoke djelotvornosti
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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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
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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
NZ587549A (en) 2004-06-24 2012-10-26 Vertex Pharma 6-Amino-indole derivatives and processes for their preparation
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
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
AU2009308241B2 (en) 2008-10-23 2016-01-07 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
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EP2477991B1 (en) * 2009-09-17 2015-04-15 Vertex Pharmaceuticals Incorporated Process for preparing azabicyclic compounds
BR112012009584A2 (pt) * 2009-10-23 2019-09-24 Vertex Pharma formas sólidas de n-(4-(7-azabiciclo[2.2.1]heptan-7-il)-2-(trifluorometil)fenil)-4-oxo-5-(trifluorometil)-1,4-di-hidroquinolina-3-carboxamida
RU2553989C2 (ru) * 2009-10-23 2015-06-20 Вертекс Фармасьютикалз Инкорпорейтед Способ получения модуляторов регулятора трансмембранной проводимости кистозного фиброза
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
RU2012115111A (ru) 2013-10-27
EP2477991A1 (en) 2012-07-25
CN102498112A (zh) 2012-06-13
NZ598277A (en) 2014-03-28
ZA201201252B (en) 2013-05-29
ES2540810T3 (es) 2015-07-13
CN102498112B (zh) 2015-05-20
IL218641A0 (en) 2012-05-31
AU2010295461B2 (en) 2016-03-03
RU2543622C2 (ru) 2015-03-10
JP5793496B2 (ja) 2015-10-14
AU2010295461A1 (en) 2012-03-08
BR112012006031A2 (pt) 2019-09-24
US8461352B2 (en) 2013-06-11
US8404865B2 (en) 2013-03-26
WO2011035139A1 (en) 2011-03-24
US20120259129A1 (en) 2012-10-11
CA2772792A1 (en) 2011-03-24
JP2013505259A (ja) 2013-02-14
EP2477991B1 (en) 2015-04-15
HK1169106A1 (en) 2013-01-18
MX2012003343A (es) 2012-08-17
US20110065928A1 (en) 2011-03-17

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Patent event date: 20120416

Patent event code: PA01051R01D

Comment text: International Patent Application

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Patent event code: PA02012R01D

Patent event date: 20150916

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Patent event code: PC12021R01D

Patent event date: 20160420

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