CN102498112B - 制备氮杂二环化合物的方法 - Google Patents

制备氮杂二环化合物的方法 Download PDF

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Publication number
CN102498112B
CN102498112B CN201080041222.8A CN201080041222A CN102498112B CN 102498112 B CN102498112 B CN 102498112B CN 201080041222 A CN201080041222 A CN 201080041222A CN 102498112 B CN102498112 B CN 102498112B
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compound
solvent
contacted
formula
mixture
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Expired - Fee Related
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English (en)
Chinese (zh)
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CN102498112A (zh
Inventor
N·B·安部海卡
B·R·比尔
L·T·D·凡宁
R·胡格赫斯
B·利特勒
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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)
CN201080041222.8A 2009-09-17 2010-09-17 制备氮杂二环化合物的方法 Expired - Fee Related CN102498112B (zh)

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 (2)

Publication Number Publication Date
CN102498112A CN102498112A (zh) 2012-06-13
CN102498112B true CN102498112B (zh) 2015-05-20

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CN201080041222.8A Expired - Fee Related CN102498112B (zh) 2009-09-17 2010-09-17 制备氮杂二环化合物的方法

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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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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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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
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
KR20120083416A (ko) 2012-07-25
HK1169106A1 (en) 2013-01-18
AU2010295461B2 (en) 2016-03-03
EP2477991B1 (en) 2015-04-15

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