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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disease
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tert
cftr
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JP2019513741A (ja
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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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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/695Silicon compounds
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
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    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • 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
    • C07F7/0812Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • CCHEMISTRY; METALLURGY
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    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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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

Publications (3)

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JP2019513741A JP2019513741A (ja) 2019-05-30
JP2019513741A5 JP2019513741A5 (enExample) 2020-05-14
JP7061076B2 true JP7061076B2 (ja) 2022-04-27

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US (5) US10662207B2 (enExample)
EP (1) EP3440057B1 (enExample)
JP (1) JP7061076B2 (enExample)
KR (1) KR102448404B1 (enExample)
CN (1) CN109563047A (enExample)
AR (1) AR108203A1 (enExample)
AU (1) AU2017248253B2 (enExample)
BR (1) BR112018070747B1 (enExample)
CA (1) CA3019663C (enExample)
IL (1) IL262030B (enExample)
MA (1) MA43775A (enExample)
MX (1) MX386698B (enExample)
NZ (1) NZ746793A (enExample)
SA (1) SA518400164B1 (enExample)
SG (1) SG11201808682XA (enExample)
WO (1) WO2017177124A1 (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI735416B (zh) 2014-10-06 2021-08-11 美商維泰克斯製藥公司 囊腫纖維化症跨膜傳導調節蛋白之調節劑
MA42488A (fr) 2015-07-24 2018-05-30 Proteostasis Therapeutics Inc Composés, compositions et procédés pour augmenter l'activité du cftr
CA3000483C (en) 2015-10-06 2024-02-13 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for modulating cftr
BR112018070747B1 (pt) * 2016-04-07 2024-01-09 Proteostasis Therapeutics, Inc Átomos de silicone contendo análogos de ivacaftor, composições farmacêuticas e usos terapêuticos
MA45397A (fr) 2016-06-21 2019-04-24 Proteostasis Therapeutics Inc Composés, compositions et procédés pour augmenter l'activité du cftr
SI3519401T1 (sl) 2016-09-30 2022-01-31 Vertex Pharmaceuticals Incorporated Modulator regulatorja transmembranske prevodnosti pri cistični fibrozi, farmacevtski sestavki, postopki zdravljenja in proces za izdelavo modulatorja
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
AU2018279646B2 (en) 2017-06-08 2023-04-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
WO2018237174A2 (en) * 2017-06-21 2018-12-27 The Johns Hopkins University CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR MODULATORS FOR THE TREATMENT OF DOMINANT AUTOMATIC RENAL POLYKYSTOSIS
MA49631A (fr) 2017-07-17 2020-05-27 Vertex Pharma Méthodes de traitement de la fibrose kystique
TWI799435B (zh) 2017-08-02 2023-04-21 美商維泰克斯製藥公司 製備化合物之製程
AU2018346602B2 (en) * 2017-10-06 2024-10-17 Proteostasis Therapeutics, Inc. Compounds, compositions and methods for increasing CFTR activity
US10654829B2 (en) 2017-10-19 2020-05-19 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of CFTR modulators
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
AU2019222758B2 (en) 2018-02-15 2022-07-07 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cystic fibrosis, and process for making them
US20210139514A1 (en) 2018-04-05 2021-05-13 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP3774825A1 (en) 2018-04-13 2021-02-17 Vertex Pharmaceuticals Incorporated 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
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
TWI899097B (zh) 2019-08-14 2025-10-01 美商維泰克斯製藥公司 製備cftr調節劑之方法
CA3150162A1 (en) 2019-08-14 2021-02-18 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
IL300413A (en) 2020-08-13 2023-04-01 Vertex Pharma Crystal forms of CFTR modulators
EP4225762A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
AU2021397294A1 (en) 2020-12-10 2023-07-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
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
BR9606546A (pt) 1995-08-02 1998-07-14 Uriach & Cia Sa J Novas carboxamidas com atividade fungicida
EP0761654B1 (en) 1995-08-24 2003-06-18 Basf Aktiengesellschaft Isoxazole- and isothiazole-5-carboxamide derivatives, their preparation and their use as herbicides
DE69903992T2 (de) 1998-04-15 2003-08-21 Pfizer Products Inc., Groton 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
MXPA06004005A (es) 2003-10-08 2006-06-28 Vertex Pharma Moduladores de transportadores con casete de union con atp.
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
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)
EP1742627A4 (en) 2004-05-06 2009-08-26 Plexxikon Inc PDE4B HEMMER AND ITS USE
SE0401969D0 (sv) 2004-08-02 2004-08-02 Astrazeneca Ab Piperidine derivatives
US20060100226A1 (en) 2004-09-10 2006-05-11 Sikorski James A 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
DE602006018301D1 (de) 2005-06-22 2010-12-30 Pfizer Prod Inc Histamin-3-rezeptorantagonisten
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
WO2008051757A1 (en) 2006-10-20 2008-05-02 Irm Llc Compositions and methods for modulating c-kit and pdgfr receptors
WO2008070739A1 (en) 2006-12-06 2008-06-12 Cytokinetics, Inc. Ksp activators
CN101778845B (zh) 2007-06-29 2014-06-25 爱思开生物制药株式会社 用于预防和治疗再狭窄的包含异噁唑衍生物的药物组合物
WO2009011850A2 (en) 2007-07-16 2009-01-22 Abbott Laboratories Novel therapeutic compounds
JP2011511756A (ja) 2007-08-02 2011-04-14 ナームローゼ・フエンノートチヤツプ・オルガノン Trpv1モジュレータとしての5−フェニル−イソオキサゾール−3−カルボキサミド誘導体
WO2009086303A2 (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 (enExample) 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
AU2011242454A1 (en) 2010-04-22 2012-11-08 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
JP5996532B2 (ja) 2010-07-15 2016-09-21 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH 有害生物防除剤としての新規複素環式化合物
SG193002A1 (en) 2011-03-10 2013-09-30 Daiichi Sankyo Co Ltd Dispiropyrrolidine derivative
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
JP6006794B2 (ja) 2011-07-29 2016-10-12 カリオファーム セラピューティクス,インコーポレイテッド 核内輸送調節因子およびその使用
ES2882807T3 (es) 2011-09-16 2021-12-02 Novartis Ag Heterociclil carboxamidas N-sustituidas
WO2013038386A1 (en) 2011-09-16 2013-03-21 Novartis Ag Heterocyclic compounds for the treatment of cystic fibrosis
US8623860B2 (en) 2011-12-30 2014-01-07 Boehringer Ingelheim International Gmbh Azetidine derivatives, pharmaceutical compositions and uses thereof
JP6138834B2 (ja) 2012-02-16 2017-05-31 ダウ アグロサイエンシィズ エルエルシー スルフィルイミン化合物の製造方法
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
ES2713988T3 (es) 2012-08-01 2019-05-24 United Therapeutics Corp Tratamiento de hipertensión arterial pulmonar con células progenitoras endoteliales tratadas con prostaciclina
WO2014045283A1 (en) 2012-09-24 2014-03-27 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Restoration of the cftr function by splicing modulation
AU2013348018A1 (en) 2012-11-20 2015-06-04 Discoverybiomed, Inc. Small molecule CFTR correctors
EP2922853A4 (en) 2012-11-20 2016-11-23 Discoverybiomed Inc SMALL MOLECULE BICYCLIC AND TRICYCLIC CFTR CORRECTING DEVICES
CN109364075B (zh) * 2012-11-21 2021-10-29 顶点制药(欧洲)有限公司 氘化cftr增效剂
EP2968285A4 (en) 2013-03-13 2016-12-21 Flatley Discovery Lab COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
EP2968323A4 (en) 2013-03-13 2016-12-14 Flatley Discovery Lab PYRIDAZINONE COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
EP2968987A4 (en) 2013-03-15 2017-04-26 Vertex Pharmaceuticals Inc. Correctors acting through msd1 of cftr protein
US9815825B2 (en) 2013-03-15 2017-11-14 Discoverybiomed, Inc. Coumarin derivatives and methods of use in treating cystic fibrosis, chronic obstructive pulmonary disease, and misfolded protein disorders
US20160074374A1 (en) 2013-04-26 2016-03-17 Vertex Pharmaceuticals Incorporated Correctors acting through msd1 of cftr protein
EP2994463B1 (en) 2013-05-07 2017-10-25 Galapagos NV Novel 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
WO2014210159A1 (en) 2013-06-26 2014-12-31 Proteostasis Therapeutics, Inc. Methods of modulating cftr activity
US9920073B2 (en) 2013-10-04 2018-03-20 Drexel University Compositions useful for inhibiting HIV-1 infection and methods using same
WO2015138934A1 (en) 2014-03-13 2015-09-17 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
CA2942386A1 (en) 2014-03-13 2015-09-17 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
CA2952862A1 (en) 2014-06-19 2015-12-23 Proteostasis Therapeutics, Inc. Compounds, compositions and methods of increasing cftr activity
WO2016054560A1 (en) 2014-10-02 2016-04-07 Flatley Discovery Lab Isoxazole compounds and methods for the treatment of cystic fibrosis
CA2971850A1 (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
WO2016105468A1 (en) 2014-12-23 2016-06-30 Proteostasis Therapeutics, Inc. Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis
US10738011B2 (en) 2014-12-23 2020-08-11 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
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
CA3000483C (en) 2015-10-06 2024-02-13 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for modulating cftr
MA44126A (fr) 2015-12-22 2018-10-31 Proteostasis Therapeutics Inc Méthodes de traitement de maladies et troubles pulmonaires
BR112018070747B1 (pt) 2016-04-07 2024-01-09 Proteostasis Therapeutics, Inc Átomos de silicone contendo análogos de ivacaftor, composições farmacêuticas e usos terapêuticos
CA3023512A1 (en) 2016-05-09 2017-11-16 Proteostasis Therapeutics, Inc. Methods of identifying cftr modulators
MA45397A (fr) 2016-06-21 2019-04-24 Proteostasis Therapeutics Inc Composés, compositions et procédés pour augmenter l'activité du cftr

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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