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

Info

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
Authority
JP
Japan
Prior art keywords
compound
formula
solvent
contacted
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.)
Expired - Fee Related
Application number
JP2012529933A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013505259A5 (enExample
JP2013505259A (ja
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,
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2013505259A publication Critical patent/JP2013505259A/ja
Publication of JP2013505259A5 publication Critical patent/JP2013505259A5/ja
Application granted granted Critical
Publication of JP5793496B2 publication Critical patent/JP5793496B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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)
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 (enExample) 2013-11-07
JP5793496B2 true JP5793496B2 (ja) 2015-10-14

Family

ID=43242763

Family Applications (1)

Application Number Title Priority Date Filing Date
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 (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 (48)

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

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
EP1730155A1 (en) * 2004-02-20 2006-12-13 AstraZeneca AB Thienopyrroles as antagonists of gnrh
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
TW201202250A (en) * 2010-05-20 2012-01-16 Vertex Pharma Processes for producing modulators of cystic fibrosis transmembrane conductance regulator

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

Similar Documents

Publication Publication Date Title
JP2013505259A (ja) アザ二環式化合物を調製するプロセス
KR101612642B1 (ko) 테노포비어 알라펜아미드 헤미푸마레이트
AU721325B2 (en) 1H-4(5)-substituted imidazole derivatives
TW202222786A (zh) 苯并吡唑化合物及其類似物
WO1997028130A1 (en) Isoquinoline derivatives and drugs
JP2012176973A (ja) Hcvインヒビター
KR20150028971A (ko) 항바이러스성 화합물의 고체 형태
JP2024050607A (ja) 結晶性の置換シクロヘキシルピラゾロ[1,5-a]ピリミジニルカルボキサミド化合物およびその治療的使用
CA2322051A1 (en) New salt forms of (2e)- 5-amino-5- methylhex-2- enoic acid n-methyl-n-((1r)-1-(n- methyl-n-((1r)-1-(methylcarbamoyl)-2- phenylethyl)carbamoyl)-2- (2-naphthyl)ethyl)amide
CN100436414C (zh) 作为毒蕈碱受体拮抗剂的氮杂双环衍生物
US6448282B1 (en) 1H-4(5)-substituted imidazole derivatives
EP0869956B1 (en) Pharmaceutical compositions
JPH07500604A (ja) 高血圧治療用エチルアラニンアミノジオール化合物
RU2007143025A (ru) Полиморфизм додекагидроклопента[а]фенантренилового эфира тиофенкарбоновой кислоты
KR20250111317A (ko) 중추 신경계 손상 질환을 처치 또는 예방하기 위한 고리형 펩티드 유도체 조성물
JP2023549962A (ja) Pu.1阻害剤としての化合物
HK1169106B (zh) 製備氮雜二環化合物的方法
AU2017329111A1 (en) Compositions for the treatment of hypertension and/or fibrosis
CN107056819A (zh) 一种预防和治疗心肌缺血的药物及其制备方法
CN101861330A (zh) 多肽化合物
JPH09110691A (ja) 医薬組成物
CZ20003152A3 (cs) Soli N-methyi-N-((lR)-l-(N-methyl-N-((lR)-l- (methylkarbamoyl)-2-fenylethyl)karbamoyl)-2 (2-naftyl)ethyl)amidu (2E)-5-amino-5-methylhex- 2-enové kyseliny
MXPA00008576A (es) Nuevas formas salinas de la n-metil-n-( (1r)-1-(n-metil-n- ( (1r)-1-(metilcarbamoil)- 2-feniletil)carbamoil)-2- (2-naftil)etil)amida del acido (2e)-5-metilhex- 2-enoico
HK1181769A (en) Process for the preparation of glycopyrronium chloride
HK1209413A1 (en) 5-aminotetrahydroquinoline-2-carboxylic acids and use thereof

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130913

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20130913

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20141117

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20141125

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20150729

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20150810

R150 Certificate of patent or registration of utility model

Ref document number: 5793496

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees