JP7061076B2 - アイバカフトール類似体を含有するケイ素原子 - Google Patents

アイバカフトール類似体を含有するケイ素原子 Download PDF

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JP7061076B2
JP7061076B2 JP2018552693A JP2018552693A JP7061076B2 JP 7061076 B2 JP7061076 B2 JP 7061076B2 JP 2018552693 A JP2018552693 A JP 2018552693A JP 2018552693 A JP2018552693 A JP 2018552693A JP 7061076 B2 JP7061076 B2 JP 7061076B2
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mmol
tert
cftr
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JP2019513741A (ja
JP2019513741A5 (cg-RX-API-DMAC7.html
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ムノーズ,ベニート
パークス,ダニエル
バストス,セシリア,エム.
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プロテオステイシス セラピューティクス,インコーポレイテッド
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    • A61K31/00Medicinal preparations containing organic active ingredients
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    • C07D215/54Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
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    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/081Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
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JP2018552693A 2016-04-07 2017-04-07 アイバカフトール類似体を含有するケイ素原子 Active JP7061076B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662319439P 2016-04-07 2016-04-07
US62/319,439 2016-04-07
PCT/US2017/026579 WO2017177124A1 (en) 2016-04-07 2017-04-07 Silicone atoms containing ivacaftor analogues

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JP2019513741A JP2019513741A (ja) 2019-05-30
JP2019513741A5 JP2019513741A5 (cg-RX-API-DMAC7.html) 2020-05-14
JP7061076B2 true JP7061076B2 (ja) 2022-04-27

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EP (1) EP3440057B1 (cg-RX-API-DMAC7.html)
JP (1) JP7061076B2 (cg-RX-API-DMAC7.html)
KR (1) KR102448404B1 (cg-RX-API-DMAC7.html)
CN (1) CN109563047A (cg-RX-API-DMAC7.html)
AR (1) AR108203A1 (cg-RX-API-DMAC7.html)
AU (1) AU2017248253B2 (cg-RX-API-DMAC7.html)
BR (1) BR112018070747B1 (cg-RX-API-DMAC7.html)
CA (1) CA3019663C (cg-RX-API-DMAC7.html)
IL (1) IL262030B (cg-RX-API-DMAC7.html)
MA (1) MA43775A (cg-RX-API-DMAC7.html)
MX (1) MX386698B (cg-RX-API-DMAC7.html)
NZ (1) NZ746793A (cg-RX-API-DMAC7.html)
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Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016057572A1 (en) 2014-10-06 2016-04-14 Mark Thomas Miller Modulators of cystic fibrosis transmembrane conductance regulator
MA42488A (fr) 2015-07-24 2018-05-30 Proteostasis Therapeutics Inc Composés, compositions et procédés pour augmenter l'activité du cftr
CN108430994B (zh) 2015-10-06 2022-04-12 蛋白质平衡治疗股份有限公司 用于调节cftr的化合物、组合物和方法
AR108203A1 (es) 2016-04-07 2018-07-25 Proteostasis Therapeutics Inc Compuestos, composiciones y métodos para modular cftr (regulador de la conductancia transmembrana de la fibrosis quística)
WO2017223188A1 (en) 2016-06-21 2017-12-28 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
MA46357B1 (fr) * 2016-09-30 2021-10-29 Vertex Pharma Modulateur de régulateur de conductance transmembranaire de fibrose kystique, compositions pharmaceutiques, procédés de traitement et procédé de fabrication du modulateur
CN110267948B (zh) 2016-12-09 2023-12-08 弗特克斯药品有限公司 囊性纤维化跨膜传导调控剂的调节剂、药物组合物、治疗方法和制备所述调节剂的方法
MA54105A (fr) 2017-06-08 2021-09-15 Vertex Pharma Méthodes de traitement de la fibrose kystique
EP3641763A4 (en) * 2017-06-21 2021-03-24 The Johns Hopkins University CYSTIC FIBROSIS TRANSMEMBRANARY CONDUCTANCE REGULATOR MODULATORS FOR THE TREATMENT OF AUTOSOMIC DOMINANT RENAL POLYKYSTOSIS
CA3069226A1 (en) 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
MA49752A (fr) 2017-08-02 2021-04-21 Vertex Pharma Procédés de préparation de composés de pyrrolidine
IL273752B2 (en) * 2017-10-06 2023-12-01 Proteostasis Therapeutics Inc Ingredients, compounds and methods for increasing CFTR activity
TWI719349B (zh) 2017-10-19 2021-02-21 美商維泰克斯製藥公司 Cftr調節劑之結晶形式及組合物
KR102716244B1 (ko) 2017-12-08 2024-10-14 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유증 막횡단 전도 조절자의 조정제의 제조 방법
TWI810243B (zh) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
SI3752510T1 (sl) 2018-02-15 2023-03-31 Vertex Pharmaceuticals Incorporated Makrocikli kot modulatorji regulatorja transmembranske prevodnosti pri cistični fibrozi, farmacevtski sestavki iz le-teh, njihova uporaba pri zdravljenju cistične fibroze in postopek za njihovo proizvodnjo
US20210139514A1 (en) 2018-04-05 2021-05-13 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2019200246A1 (en) 2018-04-13 2019-10-17 Alexander Russell Abela Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
WO2020006269A1 (en) 2018-06-27 2020-01-02 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
CN109663129B (zh) * 2019-02-27 2021-05-11 四川大学华西第二医院 扩张型心肌病治疗药物及其应用
TWI848092B (zh) 2019-04-03 2024-07-11 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白調節劑
HUE066896T2 (hu) 2019-08-14 2024-09-28 Vertex Pharma Eljárás CFTR modulátorok elõállítására
TWI867024B (zh) 2019-08-14 2024-12-21 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白之調節劑
MX2022001828A (es) 2019-08-14 2022-06-08 Vertex Pharma Formas cristalinas de moduladores del regulador de conductancia transmembrana de la fibrosis quistica (cftr).
MX2023006770A (es) 2020-12-10 2023-08-14 Vertex Pharma Metodos de tratamiento para fibrosis quistica.
CN116425642B (zh) * 2023-04-06 2025-06-10 浙江科聚生物医药有限公司 2-甲氧基-4-氟-5-胺基苯酚的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012521362A (ja) 2009-03-20 2012-09-13 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 嚢胞性線維症膜コンダクタンス制御因子のモジュレーターを作製する方法
JP2014515351A (ja) 2011-05-18 2014-06-30 コンサート ファーマシューティカルズ インコーポレイテッド 重水素化されたイバカフトルの誘導体

Family Cites Families (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3812225A1 (de) 1988-04-13 1989-10-26 Basf Ag Isoxazol(isothiazol)-5-carbonsaeureamide
EP0783502A1 (en) 1995-08-02 1997-07-16 J. URIACH & CIA. S.A. New carboxamides with antifungal activity
EP0761654B1 (en) 1995-08-24 2003-06-18 Basf Aktiengesellschaft Isoxazole- and isothiazole-5-carboxamide derivatives, their preparation and their use as herbicides
ATE228119T1 (de) 1998-04-15 2002-12-15 Pfizer Prod Inc Heterocyclische carboxamide
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
EP1501514B1 (en) 2002-05-03 2012-12-19 Exelixis, Inc. Protein kinase modulators and methods of use
WO2005035514A2 (en) 2003-10-08 2005-04-21 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters containing cycloalkyl or pyranyl groups
CN1925854A (zh) 2003-11-14 2007-03-07 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
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
JP2008503446A (ja) 2004-05-06 2008-02-07 プレキシコン,インコーポレーテッド Pde4b阻害剤及びその使用
SE0401969D0 (sv) 2004-08-02 2004-08-02 Astrazeneca Ab Piperidine derivatives
WO2006031806A2 (en) 2004-09-10 2006-03-23 Atherogenics, Inc. 2-thiopyrimidinones as therapeutic agents
DE102004051277A1 (de) 2004-10-21 2006-04-27 Merck Patent Gmbh Heterocyclische Carbonylverbindungen
JP2006176443A (ja) 2004-12-22 2006-07-06 Shionogi & Co Ltd メラニン凝集ホルモン受容体アンタゴニスト
WO2006136924A1 (en) 2005-06-22 2006-12-28 Pfizer Products Inc. Histamine-3 receptor antagonists
JP4822406B2 (ja) 2005-09-26 2011-11-24 ルネサスエレクトロニクス株式会社 表示制御駆動装置および表示システム
WO2007075896A2 (en) 2005-12-22 2007-07-05 Kemia, Inc. Heterocyclic cytokine inhibitors
KR101394245B1 (ko) 2005-12-30 2014-05-14 에스케이바이오팜 주식회사 아이속사졸 유도체 및 이의 용도
WO2007086584A1 (ja) 2006-01-30 2007-08-02 Meiji Seika Kaisha, Ltd. 新規FabKおよびFabI/K阻害剤
TW200815351A (en) 2006-05-02 2008-04-01 Astrazeneca Ab Novel compounds
US8193225B2 (en) 2006-10-13 2012-06-05 The Board Of Regents Of The University Of Texas System Isoxazole amides, derivatives and methods of chemical induction of neurogenesis
WO2008046072A2 (en) 2006-10-13 2008-04-17 The Board Of Regents Of The University Of Texas System Chemical inducers of neurogenesis
US7678792B2 (en) 2006-10-20 2010-03-16 Irm Llc Compositions and methods for modulating c-kit and PDGFR receptors
WO2008070739A1 (en) 2006-12-06 2008-06-12 Cytokinetics, Inc. Ksp activators
KR101464302B1 (ko) 2007-06-29 2014-11-26 에스케이바이오팜 주식회사 아이속사졸 유도체를 포함하는 혈관재협착 예방 및 치료용약학 조성물
US20090069288A1 (en) 2007-07-16 2009-03-12 Breinlinger Eric C Novel therapeutic compounds
CN101796036A (zh) 2007-08-02 2010-08-04 欧加农股份有限公司 作为trpv1调节剂的5-苯基异噁唑-3-甲酰胺衍生物
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
US8236838B2 (en) 2008-04-21 2012-08-07 Institute For Oneworld Health Compounds, compositions and methods comprising isoxazole derivatives
US20090318429A1 (en) 2008-04-28 2009-12-24 Institute For Oneworld Health Compounds, Compositions and Methods Comprising Heteroaromatic Derivatives
AU2010211114A1 (en) 2009-02-04 2011-06-30 Msd Oss B.V. Isoxazole-5-carboxamide derivatives
MX2011009414A (es) 2009-03-11 2011-10-19 Kyorin Seiyaku Kk 7-cicloalquiloaminoquinolonas como inhibidores de gsk-3.
GB0910003D0 (en) 2009-06-11 2009-07-22 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
IN2012DN00352A (cg-RX-API-DMAC7.html) 2009-06-16 2015-08-21 Bikam Pharmaceuticals Inc
WO2011008931A2 (en) 2009-07-15 2011-01-20 Cystic Fibrosis Foundation Therapeutics, Inc. Arylpyrimidine compounds and combination therapy comprising same for treating cystic fibrosis & related disorders
US9212177B2 (en) 2009-08-05 2015-12-15 Versitech Limited Antiviral compounds and methods of making and using thereof
GB2474120B (en) 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists
US8569899B2 (en) 2009-12-30 2013-10-29 Stmicroelectronics, Inc. Device and method for alignment of vertically stacked wafers and die
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
WO2011133953A1 (en) 2010-04-22 2011-10-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
WO2012007500A2 (de) 2010-07-15 2012-01-19 Bayer Cropscience Ag Neue heterocyclische verbindungen als schädlingsbekämpfungsmittel
MY172862A (en) 2011-03-10 2019-12-13 Daiichi Sankyo Co Ltd Dispiropyrrolidine derivatives
CA2736441A1 (en) 2011-04-06 2012-10-06 The Regents Of The University Of California Pyrazolylthiazole compounds as .delta.f508-cystic fibrosis transmembrane conductance regulator correctors
HUE047354T2 (hu) * 2011-05-18 2020-04-28 Vertex Pharmaceuticals Europe Ltd Ivacaftor deuterizált származékai
WO2013019561A1 (en) 2011-07-29 2013-02-07 Karyopharm Therapeutics, Inc. Nuclear transport modulators and uses thereof
ES2882807T3 (es) 2011-09-16 2021-12-02 Novartis Ag Heterociclil carboxamidas N-sustituidas
US9034879B2 (en) 2011-09-16 2015-05-19 Novartis Ag Heterocyclic compounds for the treatment of CF
US8623860B2 (en) 2011-12-30 2014-01-07 Boehringer Ingelheim International Gmbh Azetidine derivatives, pharmaceutical compositions and uses thereof
UA116628C2 (uk) 2012-02-16 2018-04-25 ДАУ АГРОСАЙЄНСІЗ ЕлЕлСі Спосіб отримання сульфілімінових сполук
UA110436C2 (en) 2012-03-06 2015-12-25 Zoetis Llc Antibacterial phenol compounds
WO2013146970A1 (ja) 2012-03-29 2013-10-03 第一三共株式会社 新規キノリン誘導体
EP3492084B1 (en) 2012-08-01 2021-02-17 United Therapeutics Corporation Treatment of pulmonary arterial hypertension with prostacyclin-treated endothelial progenitor cells
EP2898072A1 (en) 2012-09-24 2015-07-29 Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. Restoration of the cftr function by splicing modulation
AU2013348019A1 (en) 2012-11-20 2015-06-04 Discoverybiomed, Inc. Small molecule bicyclic and tricyclic CFTR correctors
CA2891962A1 (en) 2012-11-20 2014-05-03 Discoverybiomed, Inc. Small molecule cftr correctors
CN103833630B (zh) * 2012-11-21 2018-11-13 顶点制药(欧洲)有限公司 氘化cftr增效剂
US9783529B2 (en) 2013-03-13 2017-10-10 Flatley Discovery Lab, Llc Pyridazinone compounds and methods for the treatment of cystic fibrosis
WO2014160478A1 (en) 2013-03-13 2014-10-02 Flatley Discovery Lab Compounds and methods for the treatment of cystic fibrosis
AU2014240026B2 (en) 2013-03-15 2018-06-14 Discoverybiomed, Inc. Coumarin derivatives and methods of use in treating cystic fibrosis, chronic obstructive pulmonary disease, and misfolded protein disorders
US20160030406A1 (en) 2013-03-15 2016-02-04 Vertex Pharmaceuticals Incorporated Correctors acting through msd1 of cftr protein
WO2014176553A1 (en) 2013-04-26 2014-10-30 Vertex Pharmaceuticals Incorporated Correctors acting through msd1 of cftr protein
US9382254B2 (en) 2013-05-07 2016-07-05 Galapagos Nv Compounds and pharmaceutical compositions thereof for the treatment of cystic fibrosis
WO2014181287A1 (en) 2013-05-09 2014-11-13 Piramal Enterprises Limited Heterocyclyl compounds and uses thereof
EP3013341A4 (en) 2013-06-26 2017-02-08 Proteostasis Therapeutics, Inc. Methods of modulating cftr activity
WO2015051230A1 (en) 2013-10-04 2015-04-09 Drexel University Novel compositions useful for inhibiting hiv-1 infection and methods using same
CA2942387A1 (en) 2014-03-13 2015-09-17 Proteostasis Therapeutics, Inc. Compounds, compositions and methods of increasing cftr actvity
EP3116501A1 (en) 2014-03-13 2017-01-18 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
WO2015196071A1 (en) 2014-06-19 2015-12-23 Proteostasis Therapeutics, Inc. Compounds, compositions and methods of increasing cftr activity
US9855249B2 (en) 2014-10-02 2018-01-02 Flatley Discovery Lab, Llc Isoxazole compounds and methods for the treatment of cystic fibrosis
US10344023B2 (en) 2014-12-23 2019-07-09 Proteostasis Therapeutics, Inc. Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis
CA2971855A1 (en) 2014-12-23 2016-06-30 Proteostasis Therapeutics, Inc. Derivatives of 5-(hetero)arylpyrazol-3-carboxylic amide or 1-(hetero)aryltriazol-4-carboxylic amide useful for the treatment of inter alia cystic fibrosis
MA41253A (fr) 2014-12-23 2017-10-31 Proteostasis Therapeutics Inc Composés, compositions et procédés pour augmenter l'activité du cftr
WO2016105477A1 (en) 2014-12-23 2016-06-30 Proteostasis Therapeutics, Inc Derivatives of 5-phenyl- or 5-heteroarylthiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis
US20180147187A1 (en) 2015-01-12 2018-05-31 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
MA42488A (fr) 2015-07-24 2018-05-30 Proteostasis Therapeutics Inc Composés, compositions et procédés pour augmenter l'activité du cftr
WO2017040606A1 (en) 2015-08-31 2017-03-09 Proteostasis Therapeutics, Inc. Isoxazole derivatives for use in the treatment of pulmonary diseases and disorders
CN108430994B (zh) 2015-10-06 2022-04-12 蛋白质平衡治疗股份有限公司 用于调节cftr的化合物、组合物和方法
WO2017112853A1 (en) 2015-12-22 2017-06-29 Proteostasis Therapeutics, Inc. Methods of treating pulmonary diseases and disorders
AR108203A1 (es) 2016-04-07 2018-07-25 Proteostasis Therapeutics Inc Compuestos, composiciones y métodos para modular cftr (regulador de la conductancia transmembrana de la fibrosis quística)
WO2017196843A1 (en) 2016-05-09 2017-11-16 Proteostasis Therapeutics, Inc. Methods of identifying cftr modulators
WO2017223188A1 (en) 2016-06-21 2017-12-28 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012521362A (ja) 2009-03-20 2012-09-13 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 嚢胞性線維症膜コンダクタンス制御因子のモジュレーターを作製する方法
JP2014515351A (ja) 2011-05-18 2014-06-30 コンサート ファーマシューティカルズ インコーポレイテッド 重水素化されたイバカフトルの誘導体

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
DAVIES, J. et al.,Efficacy and Safety of Ivacaftor in Patients Aged 6 to 11 Years with Cystic Fibrosis with a G551D Mutation,,American Journal of Respiratory and Critical Care Medicine,2013年,Vol.187, No.11,pp.1219-1225
FRANZ, A. et al.,Organosilicon Molecules with Medicinal Applications,Journal of Medicinal Chemistry,2013年,Vol.56, No.2,pp.388-405
HEINONEN, P. et al.,Synthesis and pharmacological properties of 4(5)-(2-ethyl-2,3-dihydro-2 silainden-2-yl)imidazole, a silicon analogue of atipamezole,European Journal of Medicinal Chemistry,1996年,Vol.31, No.9,pp.725-729
SHOWELL, G. et al.,Chemistry challenges in lead optimization: silicon isosteres in drug discovery,Drug Discovery Today,2003年,Vol.8, No.12,pp.551-556
TACKE, R. et al.,Sila-haloperidol: A Silicon Analogue of the Dopamine (D2) Receptor Antagonist Haloperidol,Organometallics,2004年,Vol.23, No.19,pp.4468-4477
TACKE, R. et al.,Synthesis and Pharmacological Characterization of Disila‐AM80 (Disila‐tamibarotene) and Disila‐AM580, Silicon Analogues of the RARα‐Selective Retinoid Agonists AM80 (Tamibarotene) and AM580,ChemMedChem,2009年,Vol.4, No.11,pp.1797-1802

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