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
Prior art date
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Withdrawn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Withdrawn legal-status Critical Current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 (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)

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US7973169B2 (en) 2003-09-06 2011-07-05 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
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
CA2881078C (en) 2004-06-24 2018-10-02 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
RU2008109031A (ru) 2005-08-11 2009-09-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Модуляторы муковисцидозного трансмембранного регулятора проводимости
PT2404919E (pt) 2005-11-08 2013-10-22 Vertex Pharma Composto heterocíclico útil como um modulador de transportadores de cassete de ligação a atp
EP2016065B1 (en) 2005-12-28 2012-09-19 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
LT1993360T (lt) 2005-12-28 2017-06-12 Vertex Pharmaceuticals Incorporated N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksochinolin-3-karboksamido kieta forma
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
JP5420395B2 (ja) 2006-04-07 2014-02-19 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結合カセット輸送体の調節剤
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
EP2164840A2 (en) 2007-05-09 2010-03-24 Vertex Pharmaceuticals Incorporated Modulators of cftr
CA2696298C (en) 2007-08-24 2016-09-06 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
CN102743385B (zh) 2007-11-16 2014-09-17 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
HUE049642T2 (hu) 2007-12-07 2020-09-28 Vertex Pharma 3-(6-(1-(2,2-Difluorbenzo[d][1,3]dioxol-5-il)-ciklopropánkarboxamido)-3-metilpiridin-2-il)-benzoesav szilárd formái
CA2989620C (en) 2007-12-07 2022-05-03 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
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
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
CA2716109C (en) 2008-02-28 2016-07-19 Vertex Pharmaceuticals Incorporated 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
WO2010037066A2 (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
MX2011004375A (es) 2008-10-23 2013-03-07 Vertex Pharma Moduladores del regulador de conductancia transmembrana de fibrosis quistica.
SI3330255T1 (sl) 2009-03-20 2021-03-31 Vertex Pharmaceuticals Incorporated Postopek izdelave regulatorja transmembranske prevodnosti pri cistični fibrozi
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
ES2900353T3 (es) 2010-04-07 2022-03-16 Vertex Pharma Composiciones farmacéuticas de ácido 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)ciclopropanocarboxamido)-3-metilpiriidin-2-il)benzoico y administración de las mismas
TWI549950B (zh) 2010-04-07 2016-09-21 維泰克斯製藥公司 3-(6-(1-(2,2-二氟苯并[d][1,3]二氧雜環戊烯-5-基)環丙烷甲醯胺基)-3-甲基吡啶-2-基)苯甲酸之固體形式
RU2569678C2 (ru) 2010-04-22 2015-11-27 Вертекс Фармасьютикалз Инкорпорейтед Способ получения циклоалкилкарбоксамидо-индольных соединений
NZ603042A (en) 2010-04-22 2015-02-27 Vertex Pharma Pharmaceutical compositions comprising cftr modulators and administrations thereof
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
CA2852991C (en) 2011-11-08 2019-12-31 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
EP2819670B1 (en) 2012-02-27 2026-05-20 Vertex Pharmaceuticals Incorporated Pharmaceutical Composition and Their Administration
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
AU2013290444B2 (en) 2012-07-16 2018-04-26 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
CA2930199C (en) 2013-11-12 2022-10-25 Vertex Pharmaceuticals Incorporated Process of preparing pharmaceutical compositions for the treatment of cftr mediated diseases
PL3925607T5 (pl) 2014-04-15 2026-06-01 Vertex Pharmaceuticals Incorporated Kompozycje farmaceutyczne do leczenia chorób, w których pośredniczy mukowiscydozowy przezbłonowy regulator przewodnictwa
CA2963945C (en) 2014-10-07 2023-01-10 Vertex Pharmaceuticals Incorporated Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator
HUE055423T2 (hu) 2014-11-18 2021-11-29 Vertex Pharma Eljárás nagy áteresztõképességû tesztelõ nagy teljesítményû folyadék-kromatográfia elvégzésére
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
US12655863B2 (en) 2023-06-16 2026-06-16 Frank V. Patterson Hollow wall mounting device

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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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CA2881078C (en) * 2004-06-24 2018-10-02 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US20080194635A1 (en) * 2005-01-21 2008-08-14 Pfizer Inc. 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
MX2011004375A (es) * 2008-10-23 2013-03-07 Vertex Pharma Moduladores del regulador de conductancia transmembrana de fibrosis quistica.
NZ592504A (en) * 2008-10-23 2013-04-26 Vertex Pharma 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
WO2011035139A1 (en) * 2009-09-17 2011-03-24 Vertex Pharmaceuticals Incorporated Process for preparing azabicyclic compounds
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
NZ600172A (en) * 2009-10-23 2014-07-25 Vertex Pharma Process for preparing modulators of cystic fibrosis transmembrane conductance regulator
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Also Published As

Publication number Publication date
MX2012003343A (es) 2012-08-17
RU2543622C2 (ru) 2015-03-10
AU2010295461A1 (en) 2012-03-08
EP2477991A1 (en) 2012-07-25
JP5793496B2 (ja) 2015-10-14
US8461352B2 (en) 2013-06-11
US20110065928A1 (en) 2011-03-17
ZA201201252B (en) 2013-05-29
JP2013505259A (ja) 2013-02-14
US20120259129A1 (en) 2012-10-11
US8404865B2 (en) 2013-03-26
RU2012115111A (ru) 2013-10-27
BR112012006031A2 (pt) 2019-09-24
WO2011035139A1 (en) 2011-03-24
CN102498112B (zh) 2015-05-20
CA2772792A1 (en) 2011-03-24
ES2540810T3 (es) 2015-07-13
IL218641A0 (en) 2012-05-31
NZ598277A (en) 2014-03-28
CN102498112A (zh) 2012-06-13
HK1169106A1 (en) 2013-01-18
AU2010295461B2 (en) 2016-03-03
EP2477991B1 (en) 2015-04-15

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Patent event date: 20120416

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Patent event date: 20150916

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Patent event date: 20160420

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