HK1163661A1 - 作為 調節劑的雜芳基衍生物 - Google Patents

作為 調節劑的雜芳基衍生物

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Publication number
HK1163661A1
HK1163661A1 HK12103803.7A HK12103803A HK1163661A1 HK 1163661 A1 HK1163661 A1 HK 1163661A1 HK 12103803 A HK12103803 A HK 12103803A HK 1163661 A1 HK1163661 A1 HK 1163661A1
Authority
HK
Hong Kong
Prior art keywords
cftr
modulators
heteroaryl derivatives
heteroaryl
derivatives
Prior art date
Application number
HK12103803.7A
Other languages
English (en)
Inventor
.哈蒂達-魯哈
.米勒
周競蘭
.貝爾
Original Assignee
沃泰克斯藥物股份有限公司
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 沃泰克斯藥物股份有限公司 filed Critical 沃泰克斯藥物股份有限公司
Publication of HK1163661A1 publication Critical patent/HK1163661A1/zh

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    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
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Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
MXPA06002567A (es) 2003-09-06 2006-09-04 Vertex Pharma Moduladores de transportadores con casete de union de atp.
ES2328824T3 (es) * 2003-11-14 2009-11-18 Vertex Pharmaceuticals Incorporated Tiazoles y oxazoles utiles como moduladores de transportadores de tipo casete de union a atp.
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
WO2005075435A1 (en) * 2004-01-30 2005-08-18 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
ES2656017T3 (es) 2004-06-24 2018-02-22 Vertex Pharmaceuticals Incorporated Moduladores de transportadores del casete de unión a ATP
KR20080053297A (ko) 2005-08-11 2008-06-12 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유종 트랜스막 전도도 조정자의 조절자
EP1945632B1 (en) 2005-11-08 2013-09-18 Vertex Pharmaceuticals Incorporated Heterocyclic modulators of atp-binding cassette transporters
US7671221B2 (en) * 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
DK3219705T3 (da) 2005-12-28 2020-04-14 Vertex Pharma Farmaceutiske sammensætninger af den amorfe form af n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinolin-3-carboxamid
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
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
CA2869945C (en) 2006-04-07 2018-01-23 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US8563573B2 (en) * 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
EP2789606B1 (en) 2007-05-09 2017-11-15 Vertex Pharmaceuticals Incorporated Modulators of CFTR
CA2687764A1 (en) * 2007-05-25 2008-12-04 Vertex Pharmaceuticals Incorporated Ion channel modulators and methods of use
CA2696298C (en) 2007-08-24 2016-09-06 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP2211956A4 (en) 2007-10-10 2014-07-09 Parion Sciences Inc DISPOSAL OF OSMOLYTES WITH A NOSE CANNULA
EP3012250B1 (en) 2007-11-16 2017-11-08 Vertex Pharmaceuticals Incorporated Isoquinoline modulators of atp-binding cassette transporters
JP2011506331A (ja) * 2007-12-07 2011-03-03 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 3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸の処方物
NZ612635A (en) 2007-12-07 2015-06-26 Vertex Pharma Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
EP3683218B1 (en) 2007-12-07 2024-09-18 Vertex Pharmaceuticals Incorporated Solid forms 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
CA2931134C (en) * 2008-02-28 2019-07-30 Vertex Pharmaceuticals Incorporated Heteroaryl derivatives as cftr modulators
SI2615085T1 (sl) 2008-03-31 2015-11-30 Vertex Pharmaceuticals Incorporated Piridilni derivati kot cftr-modulatorji
JP2012504143A (ja) * 2008-09-29 2012-02-16 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 3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸の用量単位
BRPI0919930A2 (pt) * 2008-10-23 2016-02-16 Vertex Pharma moduladores de regulador de condutância transmembrana de fibrose cística
WO2010068863A2 (en) 2008-12-12 2010-06-17 Cystic Fibrosis Foundation Therapeutics, Inc. Pyrimidine compounds and methods of making and using same
EP3330255B1 (en) 2009-03-20 2020-12-09 Vertex Pharmaceuticals Incorporated Process for making modulators of cystic fibrosis transmembrane conductance regulator
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
US8952001B2 (en) * 2009-12-22 2015-02-10 Merck Sharp & Dohme Corp. Amino-heteroaryl derivatives as HCN blockers
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
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
MX2012011655A (es) 2010-04-07 2012-11-23 Vertex Pharma Formas solidas de acido 3-(6-(1-(2,2-difluorobenzo [d][1-3]dioxol-5-il]ciclopropanocarboxamido)-3-metilpiridin-2-il) benzoico.
HRP20211752T1 (hr) 2010-04-07 2022-02-18 Vertex Pharmaceuticals Incorporated Farmaceutski pripravci 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline i njihova primjena
ES2858351T3 (es) 2010-04-22 2021-09-30 Vertex Pharma Compuesto intermedio para proceso de producción de compuestos de cicloalquilcaraboxamido-indol
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
US8334292B1 (en) 2010-06-14 2012-12-18 Cystic Fibrosis Foundation Therapeutics, Inc. Pyrimidine compounds and methods of making and using same
WO2012061926A1 (en) * 2010-11-08 2012-05-18 Zalicus Pharmaceuticals Ltd. Bisarylsulfone and dialkylarylsulfone compounds as calcium channel blockers
AU2012267938B2 (en) 2011-06-07 2017-05-04 Parion Sciences, Inc. Methods of treatment
US8945605B2 (en) 2011-06-07 2015-02-03 Parion Sciences, Inc. Aerosol delivery systems, compositions and methods
AR086745A1 (es) 2011-06-27 2014-01-22 Parion Sciences Inc 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil)carbamimidoil)pirazina-2-carboxamida
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2755652B1 (en) 2011-09-16 2021-06-02 Novartis AG N-substituted heterocyclyl carboxamides
CA2852991C (en) 2011-11-08 2019-12-31 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
AU2013226076B2 (en) 2012-02-27 2017-11-16 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administration thereof
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
TR201809148T4 (tr) 2012-05-29 2018-07-23 Parion Sciences Inc Göz kuruluğu ve diğer mukozal hastalıkların tedavisi için sodyum kanal blokör etkinliğine sahip dendrimer benzeri amino asitler.
AU2013270681A1 (en) 2012-06-08 2014-12-18 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of CFTR -mediated disorders
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
US8729263B2 (en) 2012-08-13 2014-05-20 Novartis Ag 1,4-disubstituted pyridazine analogs there of and methods for treating SMN-deficiency-related conditions
ITMI20122065A1 (it) 2012-12-03 2014-06-04 Univ Padova Uso dei correttori del cftr nel trattamento delle patologie del muscolo striato
AU2013363218B2 (en) 2012-12-17 2018-03-15 Parion Sciences, Inc. Chloro-pyrazine carboxamide derivatives useful for the treatment of diseases favoured by insufficient mucosal hydration
ES2674665T3 (es) 2012-12-17 2018-07-03 Parion Sciences, Inc. Compuestos de 3,5-diamino-6-cloro-N-(N-(4-fenilbutilo)carbamimidoilo)-pirazina-2-carboxamida
KR20150095870A (ko) 2012-12-17 2015-08-21 패리온 사이언스 인코퍼레이티드 3,5-디아미노-6-클로로-n-(n-(4-페닐부틸)카르밤이미도일)피라진-2-카르복스아미드 화합물
CN105636953B (zh) * 2013-07-31 2018-01-02 诺华股份有限公司 1,4‑二取代的哒嗪衍生物及其用于治疗与smn缺乏相关的病症的用途
US10231932B2 (en) 2013-11-12 2019-03-19 Vertex Pharmaceuticals Incorporated Process of preparing pharmaceutical compositions for the treatment of CFTR mediated diseases
RU2744460C2 (ru) 2014-04-15 2021-03-09 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости
JP6746569B2 (ja) 2014-10-07 2020-08-26 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Vertex Pharmaceuticals Incorporated 嚢胞性線維症膜貫通コンダクタンス制御因子のモジュレーターの共結晶
ES2830279T3 (es) * 2014-10-31 2021-06-03 Abbvie Overseas Sarl Cromanos sustituidos y método de uso
SG11201703963QA (en) 2014-11-18 2017-06-29 Vertex Pharma Process of conducting high throughput testing high performance liquid chromatography
CN105153106B (zh) * 2015-09-02 2017-08-25 阜新奥瑞凯新材料有限公司 一种2,2‑二氟胡椒酸甲酯的制备方法
AU2016333908A1 (en) * 2015-10-09 2018-04-26 AbbVie S.à.r.l. Potentiator-corrector combinations useful in the treatment of cystic fibrosis
CN109219602A (zh) 2016-04-26 2019-01-15 艾伯维公司 囊性纤维化跨膜传导调节物蛋白的调节剂
CN110099898B (zh) 2016-10-24 2023-07-25 优曼尼蒂治疗公司 化合物及其用途
EP3700934A4 (en) 2017-10-24 2021-10-27 Yumanity Therapeutics, Inc. COMPOUNDS AND USES OF THESE COMPOUNDS
US11066417B2 (en) * 2018-02-15 2021-07-20 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulators
JP7517992B2 (ja) * 2018-03-23 2024-07-17 ヤンセン ファーマシューティカ エヌ.ベー. 化合物及びその使用
KR20210088532A (ko) 2018-09-09 2021-07-14 카나트파마 아게 뇌혈관 상태를 치료하기 위한 cftr 조절제의 용도
CA3127791A1 (en) 2019-01-24 2020-07-30 Yumanity Therapeutics, Inc. Compounds and uses thereof
TW202115092A (zh) 2019-08-14 2021-04-16 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).
WO2024072793A1 (en) * 2022-09-26 2024-04-04 Rectify Pharmaceuticals, Inc. Pyridine carboxamide compounds and their use in treating medical conditions
WO2024072794A1 (en) * 2022-09-26 2024-04-04 Rectify Pharmaceuticals, Inc. Pyridine carboxamide compounds and their use in treating medical conditions
US11993580B1 (en) 2022-12-02 2024-05-28 Neumora Therapeutics, Inc. Methods of treating neurological disorders

Family Cites Families (211)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3758475A (en) 1971-07-20 1973-09-11 Sandoz Ag Pyrido(2,3-d)pyrimidin 2 ones
IT1226048B (it) 1981-12-14 1990-12-10 Medea Res Srl Composti ad attivita'antiinfiammatoria, processo per la loro preparazione e composizioni farmaceutiche relative
DE3263567D1 (en) 1981-12-14 1985-06-20 Medea Res Srl New compounds with antiinflammatory and antitussive activity, process for their preparation and relative pharmaceutical compositions
US4501729A (en) 1982-12-13 1985-02-26 Research Corporation Aerosolized amiloride treatment of retained pulmonary secretions
US5981714A (en) 1990-03-05 1999-11-09 Genzyme Corporation Antibodies specific for cystic fibrosis transmembrane conductance regulator and uses therefor
JP3167762B2 (ja) 1990-11-27 2001-05-21 武田薬品工業株式会社 ピリドピリダジン誘導体およびその用途
US5612360A (en) 1992-06-03 1997-03-18 Eli Lilly And Company Angiotensin II antagonists
CA2107196A1 (en) 1992-09-29 1994-03-30 Mitsubishi Chemical Corporation Carboxamide derivatives
GB9317764D0 (en) 1993-08-26 1993-10-13 Pfizer Ltd Therapeutic compound
CN1077886C (zh) 1993-10-21 2002-01-16 G·D·瑟尔公司 用作一氧化一氮合酶抑制剂的脒基衍生物
DE4405712A1 (de) 1994-02-23 1995-08-24 Basf Ag Substituierte Naphthyridine und deren Verwendung
IL113313A (en) 1994-04-11 1999-09-22 Sankyo Co Heterocyclic compounds and pharmaceutical compositions containing the same
BR9509036A (pt) 1994-09-27 1997-10-14 Janssen Pharmaceutica Nv Derivados biciclicos de benzoato de peperidinila n-substituída
US5656256A (en) 1994-12-14 1997-08-12 The University Of North Carolina At Chapel Hill Methods of treating lung disease by an aerosol containing benzamil or phenamil
US5510379A (en) 1994-12-19 1996-04-23 Warner-Lambert Company Sulfonate ACAT inhibitors
AU715658B2 (en) 1996-04-03 2000-02-10 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
DE69713402T2 (de) 1996-08-23 2002-11-07 Agouron Pharma Liganden des neuropeptids y
AU6013998A (en) 1996-12-30 1998-07-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5948814A (en) 1997-02-20 1999-09-07 The Curators Of The University Of Missouri Genistein for the treatment of cystic fibrosis
WO1998047868A1 (en) 1997-04-18 1998-10-29 Smithkline Beecham Plc Heterocycle-containing urea derivatives as 5ht1a, 5ht1b and 5ht1d receptor antagonists
HUP0003881A3 (en) 1997-10-02 2001-04-28 Sankyo Co Amidocarboxylic acid derivatives
DE69914458T2 (de) 1998-02-17 2004-10-28 G.D. Searle & Co., Chicago Verfahren zur enzymatischen auflösung von laktamen
PE20000564A1 (es) 1998-06-08 2000-07-05 Schering Corp Antagonistas receptores y5 de neuropeptidos
US6426331B1 (en) 1998-07-08 2002-07-30 Tularik Inc. Inhibitors of STAT function
AUPP609198A0 (en) 1998-09-22 1998-10-15 Curtin University Of Technology Use of non-peptidyl compounds for the treatment of insulin related ailments
AU770042B2 (en) 1998-12-18 2004-02-12 Bristol-Myers Squibb Pharma Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
CA2364662C (en) 1999-02-24 2009-10-20 F. Hoffmann-La Roche Ag 3-phenylpyridine derivatives and their use as nk-1 receptor antagonists
AU767123B2 (en) 1999-02-24 2003-10-30 F. Hoffmann-La Roche Ag Phenyl- and pyridinyl derivatives
EP1035115B1 (en) 1999-02-24 2004-09-29 F. Hoffmann-La Roche Ag 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists
UA71971C2 (en) 1999-06-04 2005-01-17 Agoron Pharmaceuticals Inc Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases
BR0012291A (pt) 1999-06-18 2002-03-26 Bayer Ag Fenoxifluorpirimidinas
UA74539C2 (en) 1999-12-08 2006-01-16 Pharmacia Corp Crystalline polymorphous forms of celecoxib (variants), a method for the preparation thereof (variants), a pharmaceutical composition (variants)
WO2001046165A2 (en) 1999-12-16 2001-06-28 Novartis Ag N-heteroaryl-amides and their use as parasiticides
EP1248869A2 (en) 2000-01-07 2002-10-16 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
AU2001233069A1 (en) 2000-01-28 2001-08-07 Biogen, Inc. Pharmaceutical compositions containing anti-beta 1 integrin compounds and uses
WO2001056989A2 (en) 2000-02-01 2001-08-09 Cor Therapeutics, Inc. Inhibitors of factor xa
WO2001081317A1 (en) 2000-04-26 2001-11-01 Gliatech, Inc. Chiral imidazoyl intermediates for the synthesis of 2-(4-imidazoyl)-cyclopropyl derivatives
WO2001083517A1 (en) 2000-05-03 2001-11-08 Tularik Inc. Stat4 and stat6 binding dipeptide derivatives
EP1268450A1 (en) 2000-06-01 2003-01-02 Bristol-Myers Squibb Pharma Company Lactams substituted by cyclic succinates as inhibitors of a-beta protein production
TWI259180B (en) 2000-08-08 2006-08-01 Hoffmann La Roche 4-Phenyl-pyridine derivatives
CN100355750C (zh) 2000-09-15 2007-12-19 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡唑化合物
JP4272338B2 (ja) 2000-09-22 2009-06-03 バイエル アクチェンゲゼルシャフト ピリジン誘導体
AU2002211379A1 (en) 2000-10-04 2002-04-15 The Children's Hospital Of Philadelphia Compositions and methods for treatment of cystic fibrosis
GB2367816A (en) 2000-10-09 2002-04-17 Bayer Ag Urea- and thiourea-containing derivatives of beta-amino acids
WO2002034739A1 (en) 2000-10-20 2002-05-02 Merck Patent Gmbh Chiral binaphthol derivatives
US6884782B2 (en) 2000-11-08 2005-04-26 Amgen Inc. STAT modulators
DE60142921D1 (de) 2000-12-01 2010-10-07 Eisai Inc Azaphenanthridone-derivate und deren verwendung als parp-inhibitoren
GB0102687D0 (en) 2001-02-02 2001-03-21 Pharmacia & Upjohn Spa Oxazolyl-pyrazole derivatives active as kinase inhibitors,process for their preparation and pharmaceutical compositions comprising them
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
US6531597B2 (en) 2001-02-13 2003-03-11 Hoffmann-La Roche Inc. Process for preparation of 2-phenyl acetic acid derivatives
AU2002258794A1 (en) 2001-04-10 2003-10-20 Transtech Pharma, Inc. Probes, systems and methods for drug discovery
CA2444395C (en) 2001-04-23 2010-12-21 F. Hoffmann-La Roche Ag Use of nk-1 receptor antagonists against benign prostatic hyperplasia
BR0209920A (pt) 2001-05-22 2004-03-30 Neurogen Corp Composto ou sal farmaceuticamente aceitável do mesmo, métodos de tratar ansiedade, depressão ou estresse e sìndrome do intestino irritável ou doença de crohn, de detectar receptores de crf1 em uma primeira amostra biológica, de demonstrar a presença ou ausência de receptores de crf1 em uma amostra biológica e de inibir a ligação de crf a um receptor de crf1, composição farmacêutica, e, embalagem
US20030083345A1 (en) 2001-07-10 2003-05-01 Torsten Hoffmann Method of treatment and/or prevention of brain, spinal or nerve injury
US6627646B2 (en) 2001-07-17 2003-09-30 Sepracor Inc. Norastemizole polymorphs
WO2003007888A2 (en) 2001-07-20 2003-01-30 Adipogenix, Inc. Fat accumulation-modulating compounds
US6841566B2 (en) 2001-07-20 2005-01-11 Boehringer Ingelheim, Ltd. Viral polymerase inhibitors
EP1425284A2 (en) 2001-09-11 2004-06-09 Smithkline Beecham Corporation Furo- and thienopyrimidine derivatives as angiogenesis inhibitors
PA8557501A1 (es) 2001-11-12 2003-06-30 Pfizer Prod Inc Benzamida, heteroarilamida y amidas inversas
JP2003155285A (ja) 2001-11-19 2003-05-27 Toray Ind Inc 環状含窒素誘導体
JP2003221386A (ja) 2001-11-26 2003-08-05 Takeda Chem Ind Ltd 二環性誘導体、その製造法およびその用途
JP2005518391A (ja) 2001-12-21 2005-06-23 ノボ ノルディスク アクティーゼルスカブ Gk活性化剤としてのアミド誘導体
TW200307539A (en) 2002-02-01 2003-12-16 Bristol Myers Squibb Co Cycloalkyl inhibitors of potassium channel function
TW200304820A (en) 2002-03-25 2003-10-16 Avanir Pharmaceuticals Use of benzimidazole analogs in the treatment of cell proliferation
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
FR2840807B1 (fr) 2002-06-12 2005-03-11 Composition cosmetique de soin et/ou de maquillage, structuree par des polymeres silicones et des organogelateurs, sous forme rigide
GB0221443D0 (en) 2002-09-16 2002-10-23 Glaxo Group Ltd Pyridine derivates
AU2003287160A1 (en) 2002-10-15 2004-05-04 Rigel Pharmaceuticals, Inc. Substituted indoles and their use as hcv inhibitors
CA2503713A1 (en) 2002-10-30 2004-05-21 Merck & Co., Inc. Piperidinyl cyclopentyl aryl benzylamide modulators of chemokine receptor activity
BR0317183A (pt) 2002-12-12 2005-11-01 Pharmacia Corp Método de usar compostos de aminocianopiridina como inibidores de proteìna quinase-2 ativada por proteìna quinase ativada por mitógeno
JP4716734B2 (ja) 2003-01-06 2011-07-06 イーライ リリー アンド カンパニー グルコキナーゼ活性化物質としての置換されたアリールシクロプロピルアセトアミド
EP1603878B1 (en) 2003-02-10 2013-01-02 Vertex Pharmaceuticals Incorporated Processes for the preparation of n-heteroaryl-n-aryl-amines by reacting an n-aryl carbamic acid ester with a halo-heteroaryl and analogous processes
US20050113423A1 (en) 2003-03-12 2005-05-26 Vangoor Frederick F. Modulators of ATP-binding cassette transporters
KR20060006953A (ko) 2003-04-30 2006-01-20 디 인스티튜트스 포 파마슈티컬 디스커버리, 엘엘씨 치환된 카르복실산
DE602004022819D1 (de) 2003-06-06 2009-10-08 Vertex Pharma Von atp-bindende kassette transportern
CA2530075C (en) 2003-06-27 2012-08-21 Harvey Pollard Amphiphilic pyridinium compounds, method of making and use thereof
GB0315111D0 (en) 2003-06-27 2003-07-30 Cancer Rec Tech Ltd Substituted 5-membered ring compounds and their use
JP2005053902A (ja) 2003-07-18 2005-03-03 Nippon Nohyaku Co Ltd フェニルピリジン類、その中間体及びこれを有効成分とする除草剤
EP1680424A2 (en) 2003-09-05 2006-07-19 Neurogen Corporation Heteroaryl fused pyridines, pyrazines and pyrimidines as crf1 receptor ligands
MXPA06002567A (es) 2003-09-06 2006-09-04 Vertex Pharma Moduladores de transportadores con casete de union de atp.
US7534894B2 (en) 2003-09-25 2009-05-19 Wyeth Biphenyloxy-acids
US20050070718A1 (en) 2003-09-30 2005-03-31 Abbott Gmbh & Co. Kg Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them
KR20060121909A (ko) 2003-10-08 2006-11-29 버텍스 파마슈티칼스 인코포레이티드 사이클로알킬 또는 피라닐 그룹을 포함하는 atp-결합카세트 수송자의 조절자
FR2861304B1 (fr) 2003-10-23 2008-07-18 Univ Grenoble 1 Modulateurs des canaux cftr
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
ES2328824T3 (es) 2003-11-14 2009-11-18 Vertex Pharmaceuticals Incorporated Tiazoles y oxazoles utiles como moduladores de transportadores de tipo casete de union a atp.
WO2005049034A2 (en) 2003-11-19 2005-06-02 Glaxo Group Limited Use of cyclooxygenase-2 selective inhibitors for the treatment of schizophrenic disorders
WO2005075435A1 (en) 2004-01-30 2005-08-18 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
CN100567270C (zh) 2004-02-19 2009-12-09 万有制药株式会社 磺酰胺衍生物
ES2241496B1 (es) 2004-04-15 2006-12-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridina.
EP1734820A4 (en) 2004-04-16 2008-01-23 Neurogen Corp Imidazopyrrazine, imidazopyridine, and imidazo-pyrimidine as CRF1 receptor ligands
EP1740575A2 (en) 2004-04-22 2007-01-10 Eli Lilly And Company Pyrrolidine derivatives useful as bace inhibitors
US7585885B2 (en) 2004-04-22 2009-09-08 Eli Lilly And Company Pyrrolidine derivatives useful as BACE inhibitors
AU2005249154B2 (en) 2004-06-01 2011-02-10 Luminex Molecular Diagnostics, Inc. Method of detecting cystic fibrosis associated mutations
US8354427B2 (en) 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
US20140343098A1 (en) 2004-06-24 2014-11-20 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
ES2656017T3 (es) 2004-06-24 2018-02-22 Vertex Pharmaceuticals Incorporated Moduladores de transportadores del casete de unión a ATP
WO2006003504A1 (en) 2004-07-01 2006-01-12 Warner-Lambert Company Llc Preparation of pharmaceutical compositions containing nanoparticles
JP2008505124A (ja) 2004-07-02 2008-02-21 アドバンシス ファーマスーティカル コーポレイション パルス送達用錠剤
CA2573223C (en) 2004-08-06 2013-05-21 Otsuka Pharmaceutical Co., Ltd. Aromatic compound
EP1794135A1 (en) 2004-09-27 2007-06-13 Amgen Inc. Substituted heterocyclic compounds and methods of use
US8153643B2 (en) 2004-10-12 2012-04-10 Astrazeneca Ab Quinazoline derivatives
WO2006051394A1 (en) 2004-11-15 2006-05-18 Pfizer Products Inc. Azabenzoxazoles for the treatment of cns disorders
CA2589495C (en) 2004-12-15 2013-10-01 Dompe Pha.R.Ma. S.P.A. 2-arylpropionic acid derivatives and pharmaceutical compositions containing them
JP4790260B2 (ja) 2004-12-22 2011-10-12 出光興産株式会社 アントラセン誘導体を用いた有機エレクトロルミネッセンス素子
US20080146612A1 (en) 2005-01-27 2008-06-19 Astrazeneca Ab Novel Biaromatic Compounds, Inhibitors of the P2X7-Receptor
US7888374B2 (en) 2005-01-28 2011-02-15 Abbott Laboratories Inhibitors of c-jun N-terminal kinases
EP1845081A4 (en) 2005-02-01 2009-03-25 Takeda Pharmaceutical amide
US8242149B2 (en) 2005-03-11 2012-08-14 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US7402596B2 (en) 2005-03-24 2008-07-22 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
EP1710246A1 (en) 2005-04-08 2006-10-11 Schering Aktiengesellschaft Sulfoximine-pyrimidine Macrocycles and the salts thereof, a process for making them, and their pharmaceutical use against cancer
AR053712A1 (es) 2005-04-18 2007-05-16 Neurogen Corp Heteroarilos sustituidos, antagonistas de cb1 (receptor 1 canabinoide)
MX2007013049A (es) 2005-04-19 2008-01-11 Bayer Pharmaceuticals Corp Preparacion y uso de derivados de aril alquil acido para el tratamiento de la obesidad.
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
EP1891018B1 (en) 2005-05-24 2011-11-16 Vertex Pharmaceuticals, Inc. Modulators of atp-binding cassette transporters
AU2006252768A1 (en) 2005-06-02 2006-12-07 Bayer Cropscience Ag Phenylalkyl substituted heteroaryl devivatives
JP2008543919A (ja) 2005-06-21 2008-12-04 アステックス・セラピューティクス・リミテッド 医薬化合物
CN101287732A (zh) 2005-08-11 2008-10-15 沃泰克斯药物股份有限公司 囊性纤维化跨膜电导调节剂的调控剂
KR20080053297A (ko) 2005-08-11 2008-06-12 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유종 트랜스막 전도도 조정자의 조절자
WO2007028654A1 (en) 2005-09-09 2007-03-15 Smithkline Beecham Corporation Pyridine derivatives and their use in the treatment of psychotic disorders
EP1928427B1 (en) 2005-09-23 2009-12-30 F.Hoffmann-La Roche Ag Novel dosage formulation
US8314256B2 (en) 2005-10-06 2012-11-20 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
BRPI0618417A2 (pt) 2005-10-19 2012-07-31 Gruenenthal Chemie novos ligandos de receptores de vanilàide e seu uso para produzir medicamentos
US20120232059A1 (en) 2005-11-08 2012-09-13 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette Transporters
WO2007054480A1 (en) 2005-11-08 2007-05-18 N.V. Organon 2-(benzimidazol-1-yl)-acetamide biaryl derivatives and their use as inhibitors of the trpv1 receptor
EP1945632B1 (en) 2005-11-08 2013-09-18 Vertex Pharmaceuticals Incorporated Heterocyclic modulators of atp-binding cassette transporters
US7807673B2 (en) 2005-12-05 2010-10-05 Glaxosmithkline Llc 2-pyrimidinyl pyrazolopyridine ErbB kinase inhibitors
WO2007075901A2 (en) 2005-12-24 2007-07-05 Vertex Pharmaceuticals Incorporated Quinolin- 4 - one derivatives as modulators of abc transporters
CA2635214A1 (en) 2005-12-27 2007-07-05 Vertex Pharmaceuticals Incorporated Compounds useful in cftr assays and methods therewith
DK3219705T3 (da) 2005-12-28 2020-04-14 Vertex Pharma Farmaceutiske sammensætninger af den amorfe form af n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinolin-3-carboxamid
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
US7671221B2 (en) 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
CA2869945C (en) * 2006-04-07 2018-01-23 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
ES2377840T3 (es) 2006-05-12 2012-04-02 Vertex Pharmaceuticals, Inc. Composiciones de N-[2,4-bis(1,1-dimetiletil)-5-hidroxifenil]-1,4-dihidro-4-oxoquinolina-3-carboxamida
ES2646175T3 (es) 2006-11-03 2017-12-12 Vertex Pharmaceuticals Incorporated Derivados de azaindol como moduladores de CFTR
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US7754739B2 (en) 2007-05-09 2010-07-13 Vertex Pharmaceuticals Incorporated Modulators of CFTR
WO2008065068A2 (en) 2006-11-27 2008-06-05 Novartis Ag Substituted dihydroimidazoles and their use in the treatment of tumors
US20080260820A1 (en) 2007-04-19 2008-10-23 Gilles Borrelly Oral dosage formulations of protease-resistant polypeptides
EP2789606B1 (en) * 2007-05-09 2017-11-15 Vertex Pharmaceuticals Incorporated Modulators of CFTR
EP2170901B1 (en) 2007-05-25 2015-07-01 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20110177999A1 (en) 2007-08-09 2011-07-21 Vertex Pharmaceuticals Incorporated Therapeutic Combinations Useful in Treating CFTR Related Diseases
CA2696298C (en) 2007-08-24 2016-09-06 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
DE102007042754A1 (de) 2007-09-07 2009-03-12 Bayer Healthcare Ag Substituierte 6-Phenylnikotinsäuren und ihre Verwendung
NZ583878A (en) 2007-09-14 2012-10-26 Vertex Pharma Modulators of ABC transporter and cystic fibrosis transmembrane conductance regulator (CFTR)
CA2699292A1 (en) 2007-09-14 2009-03-26 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
US8118283B2 (en) 2007-09-21 2012-02-21 Lanny Vlasak Apparatus for aerating an aqueous solution
FR2921657A1 (fr) 2007-09-28 2009-04-03 Sanofi Aventis Sa Derives de nicotinamide, leur preparation et leur application en therapeutique
EP3012250B1 (en) 2007-11-16 2017-11-08 Vertex Pharmaceuticals Incorporated Isoquinoline modulators of atp-binding cassette transporters
NZ612635A (en) 2007-12-07 2015-06-26 Vertex Pharma Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
JP2011506331A (ja) 2007-12-07 2011-03-03 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 3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸の処方物
EP3683218B1 (en) 2007-12-07 2024-09-18 Vertex Pharmaceuticals Incorporated Solid forms 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
AU2008335031B2 (en) 2007-12-13 2013-11-28 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
CA2931134C (en) * 2008-02-28 2019-07-30 Vertex Pharmaceuticals Incorporated Heteroaryl derivatives as cftr modulators
SI2615085T1 (sl) 2008-03-31 2015-11-30 Vertex Pharmaceuticals Incorporated Piridilni derivati kot cftr-modulatorji
US8784904B2 (en) 2008-04-10 2014-07-22 U.S. Nutraceuticals, LLC Plant derived seed extract rich in essential fatty acids derived from perilla seed: composition of matter, manufacturing process and use
GB0813709D0 (en) 2008-07-26 2008-09-03 Univ Dundee Method and product
ME03019B (me) 2008-08-13 2018-10-20 Vertex Pharma Farmaceutska kompozicija n-[2,4-bis(1,1- dimeтileтil)-5-hidroksifenil]- 1,4-dihidro-4-oksohinolin-3-karboksamida i njeno ordiniranje
US20100256184A1 (en) 2008-08-13 2010-10-07 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
JP2012504143A (ja) 2008-09-29 2012-02-16 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 3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸の用量単位
BRPI0919930A2 (pt) 2008-10-23 2016-02-16 Vertex Pharma moduladores de regulador de condutância transmembrana de fibrose cística
NZ592687A (en) 2008-10-23 2013-04-26 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
US20110257223A1 (en) 2008-10-23 2011-10-20 Vertex Pharmaceuticals Incorporated Modulators of Cystic Fibrosis Transmembrane Conductance Regulator
MX2011004374A (es) 2008-10-23 2011-05-23 Vertex Pharma Formas solidas de n-(4-(7-azabiciclo[2.2.1]heptan-7-il)-2-(trifluo rometil)fenil)-4-oxo-5-(trifluorometil)-1,4-dihidroquinolin-3-car boxamida.
NZ592694A (en) 2008-11-06 2013-05-31 Vertex Pharma ATP-Binding Cassette (ABC) transporters as modulators of CFTR activity
UA104876C2 (uk) 2008-11-06 2014-03-25 Вертекс Фармасьютікалз Інкорпорейтед Модулятори atф-зв'язувальних касетних транспортерів
US8367660B2 (en) 2008-12-30 2013-02-05 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
CA2755969C (en) 2009-03-20 2018-05-08 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP3330255B1 (en) 2009-03-20 2020-12-09 Vertex Pharmaceuticals Incorporated Process for making modulators of cystic fibrosis transmembrane conductance regulator
US9713575B2 (en) 2009-05-07 2017-07-25 Gea Process Engineering Limited Tablet production module and method for continuous production of tablets
RU2543622C2 (ru) 2009-09-17 2015-03-10 Вертекс Фармасьютикалз Инкорпорейтед Способ получения азабициклических соединений
CA2777245A1 (en) 2009-10-22 2011-04-28 Vertex Pharmaceuticals Incorporated Compositions for treatment of cystic fibrosis and other chronic diseases
JP5877157B2 (ja) 2009-10-23 2016-03-02 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Vertex Pharmaceuticals Incorporated N−(4−(7−アザビシクロ[2.2.1]ヘプタン−7−イル)−2−(トリフルオロメチル)フェニル)−4−オキソ−5−(トリフルオロメチル)−1,4−ジヒドロキノリン−3−カルボキサミドの固体形態
JP5789611B2 (ja) 2009-10-23 2015-10-07 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Vertex Pharmaceuticals Incorporated 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調製するためのプロセス
WO2011116397A1 (en) 2010-03-19 2011-09-22 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
HUE062892T2 (hu) 2010-03-25 2023-12-28 Vertex Pharma (R)-1(2,2-difluorbenzo[d][1,3]dioxol-5-il)-N-(1-(2,3-dihidroxipropil)-6-fluor-2-(1-hidroxi- 2-metilpropán-2-il)-1H-indol-5-il)ciklopropánkarboxamid elõállítása és köztitermékei
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
HRP20211752T1 (hr) 2010-04-07 2022-02-18 Vertex Pharmaceuticals Incorporated Farmaceutski pripravci 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline i njihova primjena
MX2012011655A (es) 2010-04-07 2012-11-23 Vertex Pharma Formas solidas de acido 3-(6-(1-(2,2-difluorobenzo [d][1-3]dioxol-5-il]ciclopropanocarboxamido)-3-metilpiridin-2-il) benzoico.
AU2011242452A1 (en) 2010-04-22 2012-11-08 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
ES2858351T3 (es) 2010-04-22 2021-09-30 Vertex Pharma Compuesto intermedio para proceso de producción de compuestos de cicloalquilcaraboxamido-indol
WO2011133956A1 (en) 2010-04-22 2011-10-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
NZ603043A (en) 2010-04-22 2015-02-27 Vertex Pharma Pharmaceutical compositions comprising cftr modulators and administrations thereof
TW201202250A (en) 2010-05-20 2012-01-16 Vertex Pharma Processes for producing modulators of cystic fibrosis transmembrane conductance regulator
NZ603386A (en) 2010-05-20 2015-02-27 Vertex Pharma 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
JP2013536231A (ja) 2010-08-23 2013-09-19 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 (r)−1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)−n−(1−(2,3−ジヒドロキシプロピル)−6−フルオロ−2−(1−ヒドロキシ−2−メチルプロパン−2−イル)−1h−インドール−5−イル)シクロプロパンカルボキサミドを含む医薬組成物およびその投与
JP2013536251A (ja) 2010-08-27 2013-09-19 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 薬学的組成物およびその投与
US8802700B2 (en) 2010-12-10 2014-08-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
WO2013067410A1 (en) 2011-11-02 2013-05-10 Vertex Pharmaceuticals Incorporated Use of (n- [2, 4 -bis (1, 1 -dimethylethyl) - 5 - hydroxyphenyl] - 1, 4 - dihydro - 4 - oxoquinoline - 3 - ca rboxamide) for treating cftr mediated diseases
US20140127901A1 (en) 2012-11-08 2014-05-08 Taiwan Semiconductor Manufacturing Company, Ltd. Low-k damage free integration scheme for copper interconnects
CA2852991C (en) 2011-11-08 2019-12-31 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
SG10201606135TA (en) 2012-01-25 2016-09-29 Vertex Pharma Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
AU2013226076B2 (en) 2012-02-27 2017-11-16 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administration thereof
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
AU2013270681A1 (en) 2012-06-08 2014-12-18 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of CFTR -mediated disorders
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
SI2914248T2 (sl) 2012-11-02 2023-12-29 Vertex Pharmaceuticals Incorporated, Farmacevtski sestavki za zdravljenje bolezni, pri katerih posreduje CFTR
US20140221424A1 (en) 2013-01-30 2014-08-07 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for use in the treatment of cystic fibrosis
RU2744460C2 (ru) 2014-04-15 2021-03-09 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости
CN112250627B (zh) 2014-10-06 2024-02-02 弗特克斯药品有限公司 囊性纤维化跨膜转导调节因子调节剂
JP6746569B2 (ja) 2014-10-07 2020-08-26 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Vertex Pharmaceuticals Incorporated 嚢胞性線維症膜貫通コンダクタンス制御因子のモジュレーターの共結晶
WO2016086136A1 (en) 2014-11-26 2016-06-02 Catabasis Pharmaceuticals, Inc. Fatty acid cysteamine conjugates of cftr modulators and their use in treating medical disorders
MA41031A (fr) 2014-11-26 2017-10-03 Catabasis Pharmaceuticals Inc Conjugués cystéamine-acide gras et leur utilisation comme activateurs de l'autophagie
EP3226861A2 (en) 2014-12-05 2017-10-11 Centre National de la Recherche Scientifique (CNRS) Compounds for treating cystic fibrosis
EP3250565B1 (en) 2015-01-26 2019-07-03 Rigel Pharmaceuticals, Inc. Tetrazolones as carboxylic acid bioisosteres
UY36680A (es) 2015-05-19 2016-12-30 Glaxosmithkline Ip Dev Ltd Amidas heterocíclicas como inhibidores de quinasa

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