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 (OSRAM
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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B61/00Other general methods
    • C07B61/02Generation of organic free radicals; Organic free radicals per se
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/34Compounds 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
    • C07C211/35Compounds 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 (OSRAM) 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 (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)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA200602755B (en) 2003-09-06 2007-06-27 Vertex Pharma Modulators of ATP-binding cassette transporters
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

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
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
UA104601C2 (uk) 2008-10-23 2014-02-25 Вертекс Фармасьютікалз, Інкорпорейтед Модулятори регулятора трансмембранної провідності при муковісцидозі
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
AU2010295461A1 (en) 2012-03-08
BR112012006031A2 (pt) 2019-09-24
US8461352B2 (en) 2013-06-11
US8404865B2 (en) 2013-03-26
KR20120083416A (ko) 2012-07-25
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

Similar Documents

Publication Publication Date Title
JP5793496B2 (ja) アザ二環式化合物を調製するプロセス
KR101612642B1 (ko) 테노포비어 알라펜아미드 헤미푸마레이트
JP5368089B2 (ja) Hcvインヒビター
AU721325B2 (en) 1H-4(5)-substituted imidazole derivatives
WO1997028130A1 (en) Isoquinoline derivatives and drugs
KR20150028971A (ko) 항바이러스성 화합물의 고체 형태
JP2021506920A (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
WO2017040606A1 (en) Isoxazole derivatives for use in the treatment of pulmonary diseases and disorders
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
CN118178369A (zh) 氨基硫醇类化合物作为脑神经或心脏保护剂的用途
KR20250111317A (ko) 중추 신경계 손상 질환을 처치 또는 예방하기 위한 고리형 펩티드 유도체 조성물
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
JP2023549962A (ja) Pu.1阻害剤としての化合物
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
CN107663202A (zh) 3-(脲基-甲基) -4-芳基-吡啶衍生物及其制备方法和作为抗肝癌药物的应用
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

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