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RU2014139006A - Фармацевтическая композиция и ее введения - Google Patents

Фармацевтическая композиция и ее введения Download PDF

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Publication number
RU2014139006A
RU2014139006A RU2014139006A RU2014139006A RU2014139006A RU 2014139006 A RU2014139006 A RU 2014139006A RU 2014139006 A RU2014139006 A RU 2014139006A RU 2014139006 A RU2014139006 A RU 2014139006A RU 2014139006 A RU2014139006 A RU 2014139006A
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Russia
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weight
disease
pharmaceutical composition
dosage form
unit dosage
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RU2014139006A
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English (en)
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RU2692779C2 (ru
Inventor
Элени ДОКОУ
Шахла ДЖАМЗАД
Джон П. Мл. КАЕСАР
Маджед ФАВАЗ
Лаура ДАС
Чун-Хой ГУ
Патрисия Нелл ХЕРТЕР
Мегхна Джай ИСРАНИ
Меган М. ДЖОНСТОН
Драгутин КНЕЗИЧ
Эндрю Г. КУЗМИССИОН
Хунжэнь ВАН
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Вертекс Фармасьютикалз Инкорпорейтед
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Abstract

1. Фармацевтическая композиция, содержащаяприблизительно 35 мас.% твердой дисперсии по массе композиции, где указанная дисперсия содержит приблизительно 80 мас.%, по существу, аморфного или аморфного соединения 1 по массе дисперсии, приблизительно 19,5 мас.% HPMCAS по массе дисперсии и приблизительно 0,5 мас.% SLS по массе дисперсии;приблизительно 13,5 мас.% маннита по массе композиции;приблизительно 41 мас.% лактозы по массе композиции;приблизительно 2 мас.% сукралозы по массе композиции;приблизительно 6 мас.% кроскармеллозы натрия по массе композиции;приблизительно 1 мас.% коллоидного диоксида кремния по массе композиции; иприблизительно 1,5 мас.% стеарата магния по массе композиции.2. Фармацевтическая композиция по п. 1, где фармацевтическая композиция представляет собой единичную дозированную форму, включающую одно или множество из гранул, пеллет, частиц или мини-таблеток, и где единичная дозированная форма содержит от приблизительно 1 мг до приблизительно 100 мг, по существу, аморфного или аморфного соединения 1.3. Фармацевтическая композиция по п. 2, где единичная дозированная форма содержит от приблизительно 50 мг, по существу, аморфного или аморфного соединения 1.4. Фармацевтическая композиция по п. 2, где единичная дозированная форма содержит от приблизительно 75 мг, по существу, аморфного или аморфного соединения 1.5. Фармацевтическая композиция по п. 2, где единичная дозированная форма содержит от приблизительно 25 до приблизительно 40 гранул.6. Фармацевтическая композиция по п. 2, где твердая дисперсия присутствует в количестве приблизительно 35 мас.% фармацевтической композиции и единичная дозированная форма содержит от приблизительно 26 гранул.7. Фармацевтическая композиция по п. 6, где

Claims (23)

1. Фармацевтическая композиция, содержащая
приблизительно 35 мас.% твердой дисперсии по массе композиции, где указанная дисперсия содержит приблизительно 80 мас.%, по существу, аморфного или аморфного соединения 1 по массе дисперсии, приблизительно 19,5 мас.% HPMCAS по массе дисперсии и приблизительно 0,5 мас.% SLS по массе дисперсии;
приблизительно 13,5 мас.% маннита по массе композиции;
приблизительно 41 мас.% лактозы по массе композиции;
приблизительно 2 мас.% сукралозы по массе композиции;
приблизительно 6 мас.% кроскармеллозы натрия по массе композиции;
приблизительно 1 мас.% коллоидного диоксида кремния по массе композиции; и
приблизительно 1,5 мас.% стеарата магния по массе композиции.
2. Фармацевтическая композиция по п. 1, где фармацевтическая композиция представляет собой единичную дозированную форму, включающую одно или множество из гранул, пеллет, частиц или мини-таблеток, и где единичная дозированная форма содержит от приблизительно 1 мг до приблизительно 100 мг, по существу, аморфного или аморфного соединения 1.
3. Фармацевтическая композиция по п. 2, где единичная дозированная форма содержит от приблизительно 50 мг, по существу, аморфного или аморфного соединения 1.
4. Фармацевтическая композиция по п. 2, где единичная дозированная форма содержит от приблизительно 75 мг, по существу, аморфного или аморфного соединения 1.
5. Фармацевтическая композиция по п. 2, где единичная дозированная форма содержит от приблизительно 25 до приблизительно 40 гранул.
6. Фармацевтическая композиция по п. 2, где твердая дисперсия присутствует в количестве приблизительно 35 мас.% фармацевтической композиции и единичная дозированная форма содержит от приблизительно 26 гранул.
7. Фармацевтическая композиция по п. 6, где единичная дозированная форма содержит приблизительно 50 мг, по существу, аморфного или аморфного соединения 1.
8. Фармацевтическая композиция по п. 2, где твердая дисперсия присутствует в количестве приблизительно 35 мас.% фармацевтической композиции и единичная дозированная форма содержит от приблизительно 39 гранул.
9. Фармацевтическая композиция по п. 8, где единичная дозированная форма содержит от приблизительно 75 мг, по существу, аморфного или аморфного соединения 1.
10. Фармацевтическая композиция по любому из пп. 5-9, где указанная гранула имеет цилиндрическую, овальную, конусовидную, сферическую, эллиптическую, многоугольную форму или их сочетания, где указанная гранула имеет наибольший размер или длину диаметра приблизительно 2 мм.
11. Способ лечения или снижения тяжести заболевания, опосредованного CFTR, у пациента детского возраста, предусматривающий введение указанному пациенту детского возраста фармацевтической композиции по любому из пп. 1-10.
12. Способ по п. 11, где заболевание, опосредованное CFTR, выбрано из кистозного фиброза, астмы, индуцированной дымом ХОБЛ, хронического бронхита, риносинусита, констипации, панкреатита, недостаточности поджелудочной железы, мужского бесплодия, обусловленного врожденным двусторонним отсутствием семявыносящего протока (CBAVD), легочной болезни легкой степени тяжести, идиопатического панкреатита, аллергического бронхолегочного аспергиллеза (ABPA), болезни печени, наследственной эмфиземы, наследственного гемохроматоза, нарушений коагуляции-фибринолиза, таких как недостаточность белка С, наследственный ангионевротический отек типа 1, нарушений процессинга липидов, таких как семейная гиперхолестеринемия, хейломикронемия типа 1, абеталипопротеинемия, лизосомных болезней накопления, таких как болезнь клеточных включений/псевдо-Гурлера, мукополисахаридозы, болезнь Сандхоффа/Тея-Сакса, болезнь Криглера-Найяра II типа, полиэндокринопатия/гиперинсулинемия, сахарный диабет, карликовость лароновского типа, дефицит миелопероксидазы, первичный гипопаратиреоз, меланома, гликогеноз CDG 1 типа, врожденный гипертиреоз, несовершенный остеогенез, наследственная гипофибриногенемия, дефицит ACT, несахарный диабет (DI), нейрогипофизарный DI, нефрогенный DI, синдром Шарко-Мари-Тута, болезнь Пелицеуса-Мерцбахера, нейродегенеративных болезней, таких как болезнь Альцгеймера, болезнь Паркинсона, боковой амиотрофический склероз, прогрессирующий супрануклеарный паралич, болезнь Пика, некоторых неврологических расстройств, характеризующихся отложением полиглутаминсодержащих протеинов [в ядрах нейронов], таких как болезнь Хантингтона, спинально-мозжечковая атаксия I типа, спинально-бульбарная мышечная атрофия, дентаторубро-паллидолюисова атрофия и миотоническая дистрофия, а также губчатых энцефалопатий, таких как наследственная болезнь Крейцфельда-Якоба (вследствие нарушения процессинга прионного белка), болезнь Фабри, синдром Герстманна-Штраусслера-Шейнкера, COPD, болезнь сухих глаз, болезнь Шегрена, остеопороз, остеопения, болезнь Горхема, хлоридных каналопатий, таких как врожденная миотония (формы Томсона и Бекера), синдром Бартера III типа, болезнь Дента, эпилепсия, гиперэкплексия, лизосомная болезнь накопления, синдром Ангельмана и первичная цилиарная дискинезия (PCD), термин для унаследованных нарушений структуры и/или функции ресничного эпителия, включая PCD с полной инверсией внутренних органов (также известную, как синдром Картагенера), PCD без полной инверсии внутренних органов и цилиарной аплазии.
13. Способ по п. 12, где заболевание, опосредованное CFTR, представляет собой кистозный фиброз, ХОБЛ, эмфизему, болезнь сухих глаз или остеопороз.
14. Способ по п. 13, где заболевание, опосредованное CFTR, представляет собой кистозный фиброз.
15. Способ по п. 14, где пациент имеет мутацию воротного механизма CFTR.
16. Способ по п. 15, где мутация воротного механизма CFTR выбрана из G551D, G178R, G551S, G970R, G1244E, S1255P, G1349D, S549N, S549R и S1251N.
17. Способ по п. 15, где мутация воротного механизма CFTR находится по меньшей мере в одной аллели.
18. Способ по п. 15, где мутация воротного механизма CFTR находится в обеих аллелях.
19. Способ по п. 14, где пациент имеет одну или обе из следующих мутаций гена муковисцидозного трансмембранного регулятора проводимости (CFTR)человека: ∆F508 и R117H.
20. Способ по пп. 11-19, где возраст пациента составляет от 2 до 5 лет.
21. Способ по пп. 11-19, где возраст пациента составляет от 0 до 2 лет.
22. Способ по пп. 11-19, где масса тела пациента составляет приблизительно 14 кг или приблизительно более 14 кг.
23. Способ по пп. 11-19, где масса тела пациента составляет меньше 14 кг.
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Families Citing this family (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1898221A (zh) 2003-09-06 2007-01-17 沃泰克斯药物股份有限公司 Atp－结合弹夹转运蛋白的调控剂
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
HUE032540T2 (en) 2004-06-24 2017-09-28 Vertex Pharma Modulators of ATP-binding cassette transporters
ATE512145T1 (de) 2005-08-11 2011-06-15 Vertex Pharma Modulatoren des cystic fibrosis transmembrane conductance regulators
EP2395002B1 (en) 2005-11-08 2014-06-18 Vertex Pharmaceuticals Inc. Pharmaceutical composition containing a heterocyclic modulator of atp-binding cassette transporters.
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
CN101395147B (zh) 2005-12-28 2013-05-29 弗特克斯药品有限公司 作为atp-结合盒转运蛋白调节剂用于治疗囊性纤维化的1-(苯并[d][1,3]间二氧杂环戊烯-5-基)-n-(苯基)环丙烷-甲酰胺衍生物及相关化合物
PT2674428T (pt) 2006-04-07 2016-07-14 Vertex Pharma Modeladores de transportadores de cassetes de ligação de atp
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
USRE50453E1 (en) 2006-04-07 2025-06-10 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
NZ581259A (en) 2007-05-09 2012-07-27 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
HUE028426T2 (en) 2007-08-24 2016-12-28 Vertex Pharma Isothiazolopyridinones for (inter alia) treating cystic fibrosis
ES2556080T3 (es) 2007-11-16 2016-01-12 Vertex Pharmaceuticals Incorporated Moduladores de isoquinolina de transportadores de casete de unión a ATP
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
LT2639223T (lt) 2007-12-07 2017-06-26 Vertex Pharmaceuticals Incorporated Cikloalkilkarboksiamido-piridino benzenkarboksirūgščių gamybos būdas
UA102534C2 (xx) 2007-12-07 2013-07-25 Вертекс Фармасьютикалз Инкорпорейтед ТВЕРДА ФОРМА 3-(6-(1-(2,2-ДИФТОРБЕНЗО$d]$1,3]-ДІОКСОЛ-5-ІЛ)-ЦИКЛОПРОПАНКАРБОКСАМІДО)-3-МЕТИЛПІРИДИН-2-ІЛ)БЕНЗОЙНОЇ КИСЛОТИ (ВАРІАНТИ)$ТВЕРДАЯ ФОРМА 3-(6-(1-(2,2-ДИФТОРБЕНЗО$d]$1,3]-ДИОКСОЛ-5-ИЛ)-ЦИКЛОПРОПАНКАРБОКСАМИДО)-3-МЕТИЛПИРИДИН-2-ИЛ)БЕНЗОЙНОЙ КИСЛОТЫ (ВАРИАНТЫ)
NZ602030A (en) 2008-02-28 2014-02-28 Vertex Pharma Heteroaryl derivatives as cftr modulators
NZ616097A (en) 2008-03-31 2015-04-24 Vertex Pharma Pyridyl derivatives as cftr modulators
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
US12458635B2 (en) 2008-08-13 2025-11-04 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
MX2011003249A (es) 2008-09-29 2011-05-19 Vertex Pharma Unidades de dosificacion del acido 3-(6-(1-(2,2-difluorobenzo[d][1 ,3]dioxol-5-il)ciclopropancarboxamido)-3-metilpiridin-2-il)benzoi co.
EP2821400B1 (en) 2009-03-20 2017-09-27 Vertex Pharmaceuticals Incorporated Process for making modulators of cystic fibrosis transmembrane conductance regulator
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
CN102917692A (zh) 2010-04-07 2013-02-06 弗特克斯药品有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]二氧杂环戊烯-5-基)环丙甲酰胺基)-3-甲基吡啶-2-基)苯甲酸的药物组合物和其给药方法
NZ602795A (en) 2010-04-07 2015-01-30 Vertex Pharma Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
CA2797118C (en) 2010-04-22 2021-03-30 Vertex Pharmaceuticals Incorporated Process of producing cycloalkylcarboxamido-indole compounds
EP2575814A1 (en) * 2010-05-20 2013-04-10 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
HUE047354T2 (hu) 2011-05-18 2020-04-28 Vertex Pharmaceuticals Europe Ltd Ivacaftor deuterizált származékai
AU2012335714B2 (en) 2011-11-08 2017-04-13 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
RU2692779C2 (ru) 2012-02-27 2019-06-27 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтическая композиция и ее введения
AU2013290444B2 (en) 2012-07-16 2018-04-26 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof
BR112016010403A2 (pt) 2013-11-12 2017-08-08 Vertex Pharma Processo de preparação de composições farmacêuticas para o tratamento de doenças mediadas por cftr
CA2944140C (en) 2014-04-15 2022-10-04 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
PL3231444T3 (pl) 2014-05-12 2020-05-18 Verona Pharma Plc Nowe leczenie
AU2015328174B2 (en) 2014-10-06 2020-05-21 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
RU2749213C2 (ru) 2014-10-07 2021-06-07 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе
US10302602B2 (en) 2014-11-18 2019-05-28 Vertex Pharmaceuticals Incorporated Process of conducting high throughput testing high performance liquid chromatography
US20170042806A1 (en) 2015-04-29 2017-02-16 Dexcel Pharma Technologies Ltd. Orally disintegrating compositions
WO2016199085A1 (en) * 2015-06-11 2016-12-15 Aizant Drug Research Solutions Private Limited Nanoparticulate ivacaftor formulations
WO2017035263A1 (en) * 2015-08-24 2017-03-02 Biocryst Pharmaceuticals, Inc. Compositions comprising a plasma kallikrein inhibitor
HK1258472A1 (zh) 2015-09-21 2019-11-15 Vertex Pharmaceuticals (Europe) Limited 氘代cftr增效剂的施用
CA2999529A1 (en) 2015-09-25 2017-03-30 Vertex Pharmaceuticals (Europe) Limited Deuterated cftr potentiators
HUP1600269A2 (hu) * 2016-04-25 2017-10-30 Druggability Tech Ip Holdco Ltd Lumacaftornak, sóinak és származékainak komplexei, eljárás azok elõállítására és azok gyógyászati készítményei
US10383865B2 (en) 2016-04-25 2019-08-20 Druggability Technologies Ip Holdco Limited Pharmaceutical combination composition comprising complex formulations of Ivacaftor and Lumacaftor and their salts and derivatives, process for their preparation thereof and pharmaceutical compositions containing them
US10206915B2 (en) 2016-04-25 2019-02-19 Druggability Technologies Ip Holdco Limited Complexes of Ivacaftor and its salts and derivatives, process for the preparation thereof and pharmaceutical compositions containing them
HUP1600270A2 (hu) * 2016-04-25 2017-10-30 Druggability Tech Ip Holdco Ltd Ivacaftornak, sóinak és származékainak komplexei, eljárás azok elõállítására és azok gyógyszerészetileg elfogadott készítményei
HUP1600271A2 (hu) 2016-04-25 2017-10-30 Druggability Tech Ip Holdco Ltd Ivacaftor és Lumacaftor sóinak és származékainak komplexei, eljárás azok elõállítására és azok gyógyszerészetileg elfogadható készítményei
US10376501B2 (en) * 2016-04-25 2019-08-13 Druggability Technologies Ip Holdco Limited Complexes of lumacaftor and its salts and derivatives, process for the preparation thereof and pharmaceutical compositions containing them
US10076494B2 (en) 2016-06-16 2018-09-18 Dexcel Pharma Technologies Ltd. Stable orally disintegrating pharmaceutical compositions
JOP20190042B1 (ar) 2016-09-30 2021-08-17 Vertex Pharma مُعدِّل‏ لمنظم موصلية التليف الكيسي عبر الغشاء، وتركيبات صيدلانية، وطرق للعلاج، وعملية لتصنيع المُعدِّل
JOP20190125B1 (ar) 2016-12-09 2022-03-14 Vertex Pharma مُعدِّل‏ لمنظم موصلية التليف الكيسي عبر الغشاء، وتركيبات صيدلانية، وطرق للعلاج، وعملية لتصنيع المُعدِّل
EP3634402A1 (en) 2017-06-08 2020-04-15 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
CA3068609A1 (en) 2017-07-01 2019-01-10 Vertex Pharmaceuticals Incorporated Compositions and methods for treatment of cystic fibrosis
AU2018304168B2 (en) 2017-07-17 2023-05-04 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
WO2019018353A1 (en) 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated METHODS OF TREATING CYSTIC FIBROSIS
US11434201B2 (en) 2017-08-02 2022-09-06 Vertex Pharmaceuticals Incorporated Processes for preparing pyrrolidine compounds
JP2020537697A (ja) * 2017-10-18 2020-12-24 ディーエフイー ファーマ ゲーエムベーハー ウント コー カーゲー ミニ錠
US10654829B2 (en) 2017-10-19 2020-05-19 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of CFTR modulators
AU2018375186B2 (en) 2017-12-01 2023-07-20 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
WO2019113089A1 (en) 2017-12-04 2019-06-13 Vertex Pharmaceuticals Incorporated Compositions for treating cystic fibrosis
CA3085006A1 (en) 2017-12-08 2019-06-13 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
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
JOP20200178A1 (ar) 2018-02-15 2022-10-30 Vertex Pharma حلقات ضخمة كمعدلات لمنظم توصيل التليف الكيسي عبر الغشاء، وتركيبات صيدلانية منها، واستخدامها في علاج التليف الكيسي، وعملية لتصنيعها
WO2019195739A1 (en) 2018-04-05 2019-10-10 Alexander Russell Abela 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
AU2019381750B2 (en) 2018-11-14 2025-08-07 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
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
WO2020214921A1 (en) 2019-04-17 2020-10-22 Vertex Pharmaceuticals Incorporated Solid forms of modulators of cftr
WO2020212898A1 (en) 2019-04-18 2020-10-22 Callidus Research Laboratories Pvt Limited Pharmaceutical oral liquid solution of ivacaftor
WO2020242935A1 (en) 2019-05-29 2020-12-03 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
CN110507640A (zh) * 2019-07-19 2019-11-29 南京市儿童医院 4-苯基丁酸钠盐在制备治疗I型Bartter综合征药物中的应用
CA3150736A1 (en) 2019-08-14 2021-02-18 Vertex Pharmaceuticals Incorporated Process of making cftr modulators
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
AU2020328568A1 (en) 2019-08-14 2022-03-03 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
KR20220064366A (ko) 2019-08-14 2022-05-18 버텍스 파마슈티칼스 인코포레이티드 Cftr 조절제의 결정질 형태
US20210069113A1 (en) * 2019-09-11 2021-03-11 Modavar Pharmaceuticals LLC Solid unit dosage form for dose individualized drug delivery
BR112022007471A2 (pt) * 2019-11-01 2022-07-12 Dare Mb Inc Dispositivo e métodos para distribuição de fármaco por microchip de dois estágios
WO2021097160A1 (en) * 2019-11-14 2021-05-20 Celgene Corporation Pediatric formulations for treatment of cancer
WO2022194399A1 (en) 2020-07-13 2022-09-22 Idorsia Pharmaceuticals Ltd Macrocycles as cftr modulators
CR20230120A (es) 2020-08-07 2023-09-01 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
EP4196221A1 (en) 2020-08-13 2023-06-21 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
US20230416275A1 (en) 2020-10-07 2023-12-28 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20230373939A1 (en) 2020-10-07 2023-11-23 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
IL301756A (en) 2020-10-07 2023-05-01 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
EP4225748A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225764A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225750A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20230382924A1 (en) 2020-10-07 2023-11-30 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022076618A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
MX2023004072A (es) 2020-10-07 2023-07-05 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica.
US12186512B2 (en) * 2020-10-26 2025-01-07 Christopher Green Treatment for dry eyes
US12324802B2 (en) 2020-11-18 2025-06-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
IL303519A (en) 2020-12-10 2023-08-01 Vertex Pharma Cystic fibrosis treatment methods
EP4472635A1 (en) 2022-02-03 2024-12-11 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
CN118974059A (zh) 2022-02-08 2024-11-15 弗特克斯药品有限公司 囊性纤维化跨膜传导调控因子的调节剂
WO2023196429A1 (en) 2022-04-06 2023-10-12 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
CN119947720A (zh) 2022-05-16 2025-05-06 弗特克斯药品有限公司 治疗囊性纤维化的方法
MA71698A (fr) 2022-08-04 2025-05-30 Vertex Pharmaceuticals Incorporated Compositions pour le traitement de maladies médiées par cftr
JP2025529476A (ja) 2022-09-15 2025-09-04 イドルシア・ファーマシューティカルズ・リミテッド （３Ｓ，７Ｓ，１０Ｒ，１３Ｒ）－１３－ベンジル－２０－フルオロ－７－イソブチル－Ｎ－（２－（３－メトキシ－１，２，４－オキサジアゾール－５－イル）エチル）－６，９－ジメチル－１，５，８，１１－テトラオキソ－１０－（２，２，２－トリフルオロエチル）－１，２，３，４，５，６，７，８，９，１０，１１，１２，１３，１４－テトラデカヒドロ－［１］オキサ［４，７，１０，１４］テトラアザシクロヘプタデシノ［１６，１７－ｆ］キノリン－３－カルボキサミドの結晶形
JP2025531206A (ja) 2022-09-15 2025-09-19 イドルシア・ファーマシューティカルズ・リミテッド 大環状ｃｆｔｒ調節剤
JP2025530377A (ja) 2022-09-15 2025-09-11 イドルシア・ファーマシューティカルズ・リミテッド 大環状ｃｆｔｒ調節剤とｃｆｔｒコレクター及び／又はｃｆｔｒポテンシエーターとの合剤
CN115590831A (zh) * 2022-10-26 2023-01-13 力品药业（厦门）股份有限公司（Cn） 一种富马酸二甲酯缓释微片及其制备方法
WO2025076240A1 (en) 2023-10-04 2025-04-10 Vertex Pharmaceuticals Incorporated Solid forms of modulators of cystic fibrosis transmembrane conductance regulator
WO2025076235A1 (en) 2023-10-04 2025-04-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20250248981A1 (en) * 2024-02-07 2025-08-07 Vertex Pharmaceuticals Incorporated Compositions for the treatment of cftr-mediated diseases
WO2025186214A1 (en) 2024-03-05 2025-09-12 Idorsia Pharmaceuticals Ltd Macrocyclic cftr modulators

Family Cites Families (323)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR960299A (ru) 1950-04-15
DE279887C (ru)
US3830797A (en) 1964-11-05 1974-08-20 Pennwalt Corp Tertiary-aliphatic-alpha-(peracyl)azo compounds
US5874424A (en) 1995-12-20 1999-02-23 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US3524858A (en) 1967-05-18 1970-08-18 Warner Lambert Pharmaceutical 1,4 - dihydro-1-substituted alkyl-6,7-methylenedioxy - 4 - oxoquinoline-3-carboxylic acid
US3751406A (en) 1967-07-24 1973-08-07 Polaroid Corp Azo compounds useful in photographic processes
DE1908548A1 (de) 1968-02-29 1970-11-05 Warner Lambert Co Chinolinderivate
BE757639A (fr) 1969-10-17 1971-04-16 Roussel Uclaf Nouveaux derives de la cephalosporine et procede de preparation
AT308173B (de) 1970-02-03 1973-06-25 Maurer Friedrich Soehne Überbrückungsvorrichtung für Dehnungsfugen in Brücken od. dgl.
US4110355A (en) 1972-12-26 1978-08-29 Polaroid Corporation Anthraquinone compounds useful in photographic processes
US3931145A (en) 1972-12-27 1976-01-06 Gaf Corporation Keto-amido containing phenylazophenyl dyestuffs
GB1433774A (en) 1973-02-26 1976-04-28 Allen & Hanburys Ltd Heterocyclic compounds apparatus for conveying articles
GB1433151A (en) 1973-04-05 1976-04-22 Allen & Hanburys Ltd Benzo-ij-quinolizines
FR2281761A1 (fr) 1974-08-13 1976-03-12 Roussel Uclaf Nouveaux derives de l'acide 3-quinoleine carboxylique, leur procede de preparation et leur application comme medicament
FR2324304A2 (fr) 1975-09-22 1977-04-15 Roussel Uclaf Nouveaux derives de l'acide 3-quinoleine carboxylique, leur procede de preparation et leur application comme medicament
FR2340092A2 (fr) 1976-02-09 1977-09-02 Roussel Uclaf Nouveaux derives de l'acide 3-quinoleine carboxylique, leur procede de preparation et leur application comme medicament
FR2340735A1 (fr) 1976-02-11 1977-09-09 Roussel Uclaf Nouveaux derives de l'acide 3-quinoleine carboxylique, leur procede de preparation et leur application comme medicament
DE2861226D1 (en) 1977-06-28 1981-12-10 Univ Strathclyde A pharmaceutical composition for tropical diseases
DE2808070A1 (de) 1978-02-24 1979-08-30 Bayer Ag Verfahren zur herstellung von 4-pyridon-3-carbonsaeuren und/oder deren derivaten
FR2443467A1 (fr) 1978-12-08 1980-07-04 Roussel Uclaf Nouveaux derives de l'acide 3-quinoleine carboxylique, leur procede de preparation et leur application comme medicament
US4312870A (en) 1979-06-21 1982-01-26 Ciba-Geigy Corporation Pyrazoloquinolines
JPS56110612A (en) 1980-02-08 1981-09-01 Yamanouchi Pharmaceut Co Ltd Readily disintegrable and absorbable compression molded article of slightly soluble drug
US4390541A (en) 1980-12-19 1983-06-28 Lilly Industries Limited Quinolone derivatives and their use in a method of controlling an immediate hypersensitivity disease
HU190796B (en) 1981-06-12 1986-11-28 Roussel Uclaf,Fr Process for producing n-dihydrothiazolyl-3-quinoline-carboxamide derivatives
FR2509728A1 (fr) 1981-07-17 1983-01-21 Roussel Uclaf Nouveaux derives de la quinoleine, leurs sels, procede de preparation, application a titre de medicaments et compositions les renfermant
US4638067A (en) 1982-09-09 1987-01-20 Warner-Lambert Co. Antibacterial agents
US5281612A (en) 1982-09-09 1994-01-25 Warner-Lambert Company Naphthyridine antibacterial agents
FR2537140B1 (fr) 1982-12-07 1986-07-18 Roussel Uclaf Nouveaux derives de la 4-hydroxy-3-quinoleine carboxamide, leur sels, procede de preparation, application a titre de medicaments, et compositions les renfermant
SU1360584A3 (ru) 1983-08-12 1987-12-15 Варнер-Ламберт Компани (Фирма) Способ получени нафтиридинхинолин-или бензоксазинкарбоновых кислот или их фармацевтически допустимых солей присоединени кислоты
US4845105A (en) 1984-10-30 1989-07-04 Roussel Uclaf 4-OH-quinoline carboxylic acid amides having analgesic and anti-inflammatory activity
EP0180548B1 (de) 1984-11-01 1989-06-28 Ciba-Geigy Ag Gegen Lichteinwirkung stabilisierte Ueberzugsmittel
DE3702393A1 (de) 1987-01-28 1988-08-11 Bayer Ag 8-cyano-1-cyclopropyl-1,4-dihydro-4-oxo- 3-chinolincarbonsaeuren, verfahren zu ihrer herstellung und diese enthaltende antibakterielle mittel
US4777252A (en) 1987-08-13 1988-10-11 E. R. Squibb & Sons, Inc. 2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines
DE3827253A1 (de) 1987-08-20 1989-03-02 Sandoz Ag Ester und amide von cyclischen carbonsaeuren und cyclischen alkoholen und aminen sowie verfahren zu deren herstellung und sie enthaltende therapeutische zusammensetzungen
DE3731516A1 (de) 1987-09-18 1989-03-30 Bayer Ag N-aryl-stickstoffheterocyclen
DE3811341A1 (de) 1987-10-09 1989-04-27 Bayer Ag In 7-stellung c-verknuepfte chinolon- und 1,8-naphthyridin-4-on-carbonsaeure und ein verfahren zu ihrer herstellung
US4786644A (en) 1987-11-27 1988-11-22 Hoechst-Roussel Pharmaceuticals Inc. 1-aryl-3-quinolinecarboxamide
DE3808118A1 (de) 1988-03-11 1989-09-21 Bayer Ag Verfahren zur herstellung von 1-cyclopropyl-chinoloncarbonsaeuren und deren derivaten
DE3808117A1 (de) 1988-03-11 1989-09-21 Bayer Ag N-cyclopropylaniline und deren verwendung in verfahren zur herstellung von 1-cyclopropyl-chinoloncarbonsaeuren und deren derivaten
DE3816119A1 (de) 1988-05-11 1989-11-23 Bayer Ag 7-substituierte chinolon- und naphthyridoncarbonsaeure-derivate
JPH01287066A (ja) 1988-05-13 1989-11-17 Fujimoto Seiyaku Kk 新規なアントラニル酸誘導体
DK273689A (da) 1988-06-06 1989-12-07 Sanofi Sa 4-amino-3-carboxyquinoliner og -naphthyridiner, fremgangsmaade til deres fremstilling og anvendelse deraf i laegemidler
DE3827221A1 (de) 1988-08-11 1990-02-15 Bayer Ag Substituierte n-phenyl-stickstoff- bzw. stickstoff-schwefel-heterocyclen, verfahren sowie entsprechende heterocyclische phenolderivate, phenyliso(thio)cyanate und -carbamate als zwischenprodukte zu ihrer herstellung, ihre verwendung in herbiziden und pflanzenwuchsregulierenden mitteln
US5491139A (en) 1988-10-24 1996-02-13 The Procter & Gamble Company Antimicrobial quinolonyl lactams
DE3903799A1 (de) 1989-02-09 1990-08-16 Bayer Ag N-aryl-stickstoffheterocyclen
JPH0334977A (ja) 1989-06-29 1991-02-14 Yoshitomi Pharmaceut Ind Ltd イミダゾリルベンゾラクタム化合物
DE3924052A1 (de) 1989-07-21 1991-01-24 Bayer Ag N- (indol-6-yl)-heterocyclen
EP0418596A3 (en) 1989-09-21 1991-10-23 American Cyanamid Company Controlled release pharmaceutical compositions from spherical granules in tabletted oral dosage unit form
GB2236751B (en) 1989-10-14 1993-04-28 Wyeth John & Brother Ltd Heterocyclic compounds
LU87611A1 (fr) 1989-10-20 1991-05-07 Oreal Composition tinctoriale pour fibres keratiniques contenant des precurseurs de colorants par oxydation et des coupleurs amino indoliques,procedes de teinture mettant en oeuvre ces compositions et composes nouveaux
US5254135A (en) 1989-10-20 1993-10-19 L'oreal Methods for dyeing keratinous fibres with aminoindoles, compositions and devices for use
FR2659552B2 (fr) 1989-10-20 1994-11-04 Oreal Procede de teinture des fibres keratiniques avec des aminoindoles, composition et dispositif de mise en óoeuvre.
FR2662713B1 (fr) 1990-05-29 1994-04-08 Oreal Procede de teinture de fibres keratiniques avec un aminoindole associe a un derive quinonique.
US5409503A (en) 1990-05-31 1995-04-25 Wella Aktiengesellschaft Oxidation hair dye with a content of 5-aminophenyl derivatives, process for oxidative dyeing of hair and new 5-aminophenol derivatives
DE4017516A1 (de) 1990-05-31 1991-12-05 Wella Ag Oxidationshaarfaerbemittel mit einem gehalt an 3-aminophenol-derivaten, verfahren zum oxidativen faerben von haaren sowie neue 3-aminophenol-derivate
DE4026530A1 (de) 1990-08-22 1992-02-27 Basf Ag Synergistische mittel zur regulierung des pflanzenwachstums
CA2091172C (en) 1990-09-07 1997-05-20 Adriano Afonso Antiviral compounds and antihypertensive compounds
US5175151A (en) 1990-09-07 1992-12-29 Schering Corporation Antiviral compounds and antihypertensive compounds
CA2091173A1 (en) 1990-09-07 1992-03-08 Adriano Afonso Antiviral compounds and antihypertensive compounds
IL100917A0 (en) 1991-02-16 1992-11-15 Fisons Plc Pyridinone and pyrimidinone derivatives,their preparation and pharmaceutical compositions containing them
CA2065106A1 (en) 1991-04-04 1992-10-05 Junichi Fukawa Silver halide photographic light-sensitive material and photographic product for film-making process
US5938792A (en) 1991-04-18 1999-08-17 L'oreal Process for dyeing keratinous fibers with aminoindoles and oxidation dye precursors at basic Ph's and dyeing agents
FR2675380A1 (fr) 1991-04-18 1992-10-23 Oreal Procede de teinture des fibres keratiniques avec des aminoindoles, a ph basique, compositions mises en óoeuvre et nouveaux composes.
GB9108547D0 (en) 1991-04-22 1991-06-05 Fujisawa Pharmaceutical Co Quinoline derivatives
SK117793A3 (en) 1991-04-29 1994-05-11 Merck & Co Inc Optimized tablet formulation
CA2075154A1 (en) 1991-08-06 1993-02-07 Neelakantan Balasubramanian Peptide aldehydes as antithrombotic agents
JPH05345780A (ja) 1991-12-24 1993-12-27 Kumiai Chem Ind Co Ltd ピリミジンまたはトリアジン誘導体及び除草剤
AU668181B2 (en) 1992-05-20 1996-04-26 Merck & Co., Inc. Ester derivatives of 4-aza-steroids
AU668180B2 (en) 1992-05-20 1996-04-26 Merck & Co., Inc. 17-ethers and thioethers of 4-aza-steroids
JPH0672979A (ja) 1992-06-08 1994-03-15 Hiroyoshi Hidaka アミノベンジル誘導体
RU2047614C1 (ru) 1992-06-15 1995-11-10 Джон Вайс энд Бразер Лимитед Гетероциклические соединения, или их фармацевтически приемлемые аддитивные соли кислоты, или n-оксид гетероциклического соединения, или его аддитивная соль кислоты
US5352690A (en) 1992-07-01 1994-10-04 Eli Lilly And Company 1,2,4-trioxygenated benzene derivatives useful as leukotriene antagonists
DK0649410T3 (da) 1992-07-10 1997-09-15 Glaxo Lab Sa Anilidderivater.
US5322847A (en) 1992-11-05 1994-06-21 Pfizer Inc. Azabenzimidazoles in the treatment of asthma, arthritis and related diseases
WO1994014797A1 (en) 1992-12-23 1994-07-07 Smithkline Beecham Corporation Quinoline compounds and the treatment of leucotriene related diseases therewith
US5750754A (en) 1993-03-29 1998-05-12 Zeneca Limited Heterocyclic compounds
JP3760474B2 (ja) 1993-04-22 2006-03-29 ダイキン工業株式会社 電気エネルギーを発生させる方法、装置およびそれに用いるｎ−ｆ結合を有する化合物
JPH0733729A (ja) 1993-07-26 1995-02-03 Kirin Brewery Co Ltd Ｎ−シアノ−ｎ′−置換−アリールカルボキシイミダミド化合物の製造法
JPH0782498A (ja) 1993-09-17 1995-03-28 Fuji Photo Film Co Ltd ビスアゾ化合物
IL111266A (en) 1993-10-22 2002-03-10 Zeneca Ltd 2-HETEROARYL OR 2-ARYLPYRIDAZINO [4,5-b] QUINOLINE - 1, 10 - DIONES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
JPH07179407A (ja) 1993-11-12 1995-07-18 Green Cross Corp:The 新規縮合環系化合物またはその塩、およびその医薬用途
US5728691A (en) 1994-02-25 1998-03-17 Laboratorios Aranda S.A. De C.V. Quinolonylcarboxamidocephalosporin derivatives and pharmaceutical compositions containing them
FR2720397B1 (fr) 1994-05-24 1996-08-23 Laphal Laboratoires Sa Nouveaux oxathiolanes, leur procédé de préparation et les compositions pharmaceutiques qui en renferment.
ITMI941099A1 (it) 1994-05-27 1995-11-27 Smithkline Beecham Farma Derivati chinolinici
DE69533408T2 (de) 1994-05-27 2005-09-08 Glaxosmithkline S.P.A. Chinolinderivate als Tachykinin NK3 Rezeptor Antagonisten
EP0705835A1 (de) 1994-09-01 1996-04-10 Ciba-Geigy Ag Oxa- oder thiaaliphatisch überbrückte Chinoxalin-2,3-dione
WO1996015099A1 (en) 1994-11-09 1996-05-23 Novo Nordisk A/S Heterocyclic compounds, their preparation and use
WO1996019239A1 (en) 1994-12-21 1996-06-27 Yamanouchi Pharmaceutical Co., Ltd. Solid composition with improved solubility and absorbability
GB9501567D0 (en) 1995-01-26 1995-03-15 Pharmacia Spa Hydrosoluble 3-arylidene-2-oxindole derivatives as tyrosine kinase inhibitors
JPH08301849A (ja) 1995-05-01 1996-11-19 Takeda Chem Ind Ltd ヘテロ環化合物およびその製造法
JPH0971534A (ja) 1995-06-26 1997-03-18 Tanabe Seiyaku Co Ltd 医薬組成物
DE19601142A1 (de) 1995-07-13 1997-01-16 Agfa Gevaert Ag Verfahren zur Erzeugung eines farbigen Bildes
ES2211965T3 (es) 1995-08-02 2004-07-16 Darwin Discovery Limited Quinolonas y su utilizacion terapeutica.
WO1997004779A1 (en) 1995-08-02 1997-02-13 Chiroscience Limited Quinolones and their therapeutic use
DE19532235A1 (de) 1995-08-31 1997-03-06 Keppler Bernhard K Priv Doz Dr An Phosphonsäuren gekoppelte antibakteriell wirksame Verbindungen zur Therapie von Infektionen im Bereich des Knochens
AU7333496A (en) 1995-10-19 1997-05-07 Takeda Chemical Industries Ltd. Quinoline derivatives as gnrh antagonists
JPH09143100A (ja) * 1995-11-20 1997-06-03 Sumitomo Pharmaceut Co Ltd 服用感の改善された固形製剤
GB9526546D0 (en) 1995-12-23 1996-02-28 Pfizer Ltd Compounds useful in therapy
CA2242598A1 (en) 1996-02-21 1997-08-28 John Gary Montana Quinolones and their therapeutic use
US6215016B1 (en) 1996-03-27 2001-04-10 Toray Industries, Inc. Ketone derivatives and medical application thereof
DE19615262A1 (de) 1996-04-18 1997-10-23 Bayer Ag Heteroverknüpfte Phenylglycinolamide
ATE406163T1 (de) 1996-05-20 2008-09-15 Darwin Discovery Ltd Chinolincarboxamide als tnf-inhibitoren und als pde-iv inhibitoren
BR9709105A (pt) 1996-05-20 1999-08-03 Darwin Discovery Ltd Sulfonamidas de quinolina como inibidoras de tnf e como inobidoras de pde-iv
KR20000022040A (ko) 1996-06-20 2000-04-25 보오드 오브 리젠츠, 더 유니버시티 오브 텍사스 시스템 약학적 활성 제제를 제공하기 위한 화합물, 방법 및 그의 용도
PT918761E (pt) 1996-07-23 2003-09-30 Neurogen Corp Algumas amidas e aminas substituidas com derivados de benzilamina uma nova classe de ligandos especificos do neuropeptido y1
GB9717576D0 (en) 1997-08-19 1997-10-22 Xenova Ltd Pharmaceutical compounds
US6069151A (en) 1996-11-06 2000-05-30 Darwin Discovery, Ltd. Quinolines and their therapeutic use
DE19651099A1 (de) 1996-12-09 1998-06-10 Consortium Elektrochem Ind Mehrkomponentensystem zum Verändern, Abbau oder Bleichen von Lignin, ligninhaltigen Materialien oder ähnlichen Stoffen sowie Verfahren zu seiner Anwendung
WO1998031226A1 (de) 1997-01-15 1998-07-23 Novartis Ag Herbizides mittel
US5948814A (en) 1997-02-20 1999-09-07 The Curators Of The University Of Missouri Genistein for the treatment of cystic fibrosis
JP3591801B2 (ja) * 1997-06-19 2004-11-24 田辺製薬株式会社 口腔内速崩壊性製剤の製法
ZA986594B (en) 1997-07-25 1999-01-27 Abbott Lab Urokinase inhibitors
US6258822B1 (en) 1997-08-06 2001-07-10 Abbott Laboratories Urokinase inhibitors
ATE364374T1 (de) 1997-08-11 2007-07-15 Pfizer Prod Inc Feste pharmazeutische dispersionen mit erhöhter bioverfügbarkeit
SK283803B6 (sk) 1997-08-26 2004-02-03 Aventis Pharmaceuticals Inc. Farmaceutický prostriedok vo forme dvojvrstvovej tabletky na kombinovanie piperidinoalkanolu s dekongestantom
US6429207B1 (en) 1997-11-21 2002-08-06 Nps Pharmaceuticals, Inc. Metabotropic glutamate receptor antagonists and their use for treating central nervous system diseases
CN1213022C (zh) 1997-12-22 2005-08-03 拜尔有限公司 用对称和不对称的取代二苯脲抑制raf激酶
EP1080068A1 (en) 1998-03-12 2001-03-07 Novo Nordisk A/S Modulators of protein tyrosine phosphatases
WO1999046267A1 (en) 1998-03-12 1999-09-16 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (ptpases)
DE19818614A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Amide, deren Herstellung und Anwendung
JP2000016982A (ja) 1998-06-30 2000-01-18 Kumiai Chem Ind Co Ltd キノリン誘導体及びこれを有効成分とする除草剤
US6133285A (en) 1998-07-15 2000-10-17 Active Biotech Ab Quinoline derivatives
US6444617B1 (en) 1998-07-28 2002-09-03 Nihon Nohyaku Co., Ltd. Fused-heterocycle dicarboxylic acid diamide derivatives or salts thereof, herbicide and usage thereof
KR100624239B1 (ko) 1998-08-03 2006-09-13 어플라이드 리서치 시스템스 에이알에스 홀딩 엔.브이. (1ｈ)-벤조〔ｃ〕퀴놀리진-3-온 유도체의 합성방법
US7001770B1 (en) 1998-10-15 2006-02-21 Canji, Inc. Calpain inhibitors and their applications
FR2786483B1 (fr) 1998-12-01 2001-02-16 Rhodia Chimie Sa Procede de preparation de 4-hydroxyquinoleines et/ou formes tautomeres
US6248739B1 (en) 1999-01-08 2001-06-19 Pharmacia & Upjohn Company Quinolinecarboxamides as antiviral agents
US6248736B1 (en) 1999-01-08 2001-06-19 Pharmacia & Upjohn Company 4-oxo-1,4-dihydro-3-quinolinecarboxamides as antiviral agents
JP2000273039A (ja) * 1999-01-20 2000-10-03 Taisho Pharmaceut Co Ltd 口腔内崩壊性組成物
DE60018225T2 (de) 1999-03-01 2005-12-29 Pfizer Products Inc., Groton Oxamsäuren mit einer Cyanogruppe als Liganden für den Thyroidrezeptor
JP2000256358A (ja) 1999-03-10 2000-09-19 Yamanouchi Pharmaceut Co Ltd ピラゾール誘導体
ATE289593T1 (de) 1999-05-06 2005-03-15 Neurogen Corp Substituierte 4-oxo-chinolin-3-carboxamide als gaba gehirnrezeptorliganden
CO5200844A1 (es) 1999-09-17 2002-09-27 Novartis Ag Una combinacion que comprende nateglinida y cuando por menos otro compuesto antidiabetico usada para el tratamiento de desordenes metabolicos, especialmente diabetes, o de una enfermedad o condicion asociada con dibetes
SE0002320D0 (sv) 1999-10-25 2000-06-21 Active Biotech Ab Malignant tumors
US6395750B1 (en) 1999-10-25 2002-05-28 Active Biotech Ab Drugs for the treatment of malignant tumors
AU7961100A (en) 1999-10-28 2001-05-08 Daiichi Pharmaceutical Co., Ltd. Drug discharge pump inhibitors
AU1302301A (en) 1999-11-08 2001-06-06 Sankyo Company Limited Nitrogenous heterocycle derivatives
JP2001199965A (ja) 1999-11-08 2001-07-24 Sankyo Co Ltd 含窒素複素環誘導体
UA75055C2 (ru) 1999-11-30 2006-03-15 Пфайзер Продактс Інк. Производные бензоимидазола, которые применяются как антипролиферативное средство, фармацевтическая композиция на их основании
CO5261615A1 (es) 1999-12-01 2003-03-31 Agouron Pharma Compuestos, composiciones y metodos para estimular el crecimiento y elongacion de neuronas
US20030181449A1 (en) 1999-12-23 2003-09-25 Urbanek Rebecca Ann Methods and compositions for the treatment of pain
JP2001233859A (ja) 2000-02-23 2001-08-28 Yamanouchi Pharmaceut Co Ltd 抗ヘリコバクター・ヒ゜ロリ化合物の新規製造法及びその中間体
GB0011409D0 (en) 2000-05-11 2000-06-28 Smithkline Beecham Plc Novel compounds
KR100795712B1 (ko) 2000-05-17 2008-01-21 신젠타 파티서페이션즈 아게 아닐린 화합물의 제조방법
US6800297B2 (en) 2000-06-15 2004-10-05 Acusphere, Inc. Porous COX-2 inhibitor matrices and methods of manufacture thereof
WO2002003938A1 (en) 2000-06-29 2002-01-17 Clairol Incorporated Iodo-containing organic couplers for use in oxidative hair dyeing
CA2429008A1 (en) 2000-07-13 2003-01-09 Takeda Chemical Industries, Ltd. Lipid-rich plaque regressing agents
AU2001277731A1 (en) 2000-08-09 2002-02-18 Welfide Corporation Fused bicyclic amide compounds and medicinal use thereof
AU2002212102A1 (en) 2000-11-08 2002-05-21 Aeromatic-Fielder Ag A process for production of particles for pharmaceutical compositions having increased bioavailability
JP2002212179A (ja) 2001-01-15 2002-07-31 Wakunaga Pharmaceut Co Ltd 新規アニリド誘導体又はその塩及びこれを含有する医薬
GB2372986A (en) 2001-01-17 2002-09-11 Xenova Ltd 2-oxo, 4-hydroxy pyrroles and quinolines
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
TWI243164B (en) 2001-02-13 2005-11-11 Aventis Pharma Gmbh Acylated indanyl amines and their use as pharmaceuticals
DE10108271A1 (de) 2001-02-21 2002-08-22 Schering Ag Chinolin-, Isochinolin- und Phthalazinderivate als Antagonisten des Gonadotropin freisetzenden Hormons
US6515001B2 (en) 2001-03-05 2003-02-04 Chemokine Therapeutic Corporation IL-8 receptor ligands-drugs for inflammatory and autoimmune diseases
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
DK1859798T3 (en) 2001-03-29 2016-03-21 Lilly Co Eli N- (2-arylethyl) -BENZYLAMINER as antagonists of 5-HT6 receptor
US6878713B2 (en) 2001-04-25 2005-04-12 Wockhardt Limited Generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, their preparation, compositions and use as medicaments
JP2002322054A (ja) 2001-04-26 2002-11-08 Dai Ichi Seiyaku Co Ltd 薬剤排出ポンプ阻害薬
JP2002322154A (ja) 2001-04-27 2002-11-08 Dai Ichi Seiyaku Co Ltd 抗真菌化合物
JP2002326935A (ja) 2001-05-07 2002-11-15 Sankyo Co Ltd 含窒素複素環誘導体を含有する医薬
CN1511151A (zh) 2001-05-24 2004-07-07 ֮����ҩ��ʽ���� 3-喹啉-2(1h)-亚基二氢吲哚-2-酮衍生物
JP2003012667A (ja) 2001-06-26 2003-01-15 Rrf Kenkyusho:Kk キノリンカルボキサミド骨格を有する抗菌剤
AU2002349882A1 (en) 2001-09-21 2003-04-01 Case Western Reserve University Q4n2neg2 enhances cftr activity
EP1434585A1 (en) 2001-10-12 2004-07-07 Warner-Lambert Company LLC Alkyne matrix metalloproteinase inhibitors
PL374442A1 (en) 2001-11-14 2005-10-17 Teva Pharmaceutical Industries Ltd. Amorphous and crystalline forms of losartan potassium and process for their preparation
TW200300349A (en) 2001-11-19 2003-06-01 Sankyo Co A 4-oxoqinoline derivative
AU2002352878B2 (en) 2001-11-27 2007-11-22 Merck Sharp & Dohme Corp. 2-Aminoquinoline compounds
MXPA04005427A (es) 2001-12-10 2005-04-19 Amgen Inc Ligandos de receptor vainilloide y su uso en tratamientos.
EP1469830A2 (en) 2002-02-01 2004-10-27 Pfizer Products Inc. Method for making homogeneous spray-dried solid amorphous drug dispersions using pressure nozzles
JP2003238413A (ja) 2002-02-14 2003-08-27 Kyowa Hakko Kogyo Co Ltd ステロイドスルファターゼ阻害剤
DE20221945U1 (de) 2002-03-15 2009-10-15 Wella Aktiengesellschaft Chinolinium-Salze enthaltende Färbemittel
US6930131B2 (en) 2002-04-10 2005-08-16 Wyeth Aryl substituted 3-ethoxy phenyl trifluoromethane sulfonamides for the treatment of non-insulin dependent diabetes mellitus (NIDDM)
US7718663B2 (en) 2002-04-26 2010-05-18 Nippon Shinyaku Co., Ltd. Quinazoline derivatives and medicaments
US7037913B2 (en) 2002-05-01 2006-05-02 Bristol-Myers Squibb Company Bicyclo 4.4.0 antiviral derivatives
EP1506188B1 (en) 2002-05-14 2009-02-25 Xenova Limited Process for the preparation of a hydrate of an anthranilic acid derivative
EP1503759B1 (en) 2002-05-14 2008-12-17 The Regents Of The University Of California Substituted quinolone carboxylic acids, their derivatives, site of action, and uses thereof
SE0201669D0 (sv) 2002-06-03 2002-06-03 Pharmacia Ab New formulation and use thereof
KR20050029209A (ko) 2002-07-15 2005-03-24 미리어드 제네틱스, 인크. 화합물, 조성물 및 이의 사용방법
US20040033959A1 (en) 2002-07-19 2004-02-19 Boehringer Ingelheim Pharmaceuticals, Inc. Pharmaceutical compositions for hepatitis C viral protease inhibitors
MXPA05001642A (es) 2002-08-13 2005-04-25 Warner Lambert Co Derivados de naftaleno como inhibidores de metaloproteinasas de matriz.
TWI314041B (en) 2002-10-21 2009-09-01 Sankyo Agro Co Ltd Quinolyl-3-carboxamide compound
PE20040844A1 (es) 2002-11-26 2004-12-30 Novartis Ag Acidos fenilaceticos y derivados como inhibidores de la cox-2
JP2004189738A (ja) 2002-11-29 2004-07-08 Nippon Nohyaku Co Ltd 置換アニリド誘導体、その中間体及び農園芸用薬剤並びにその使用方法
EP1601657A1 (en) 2003-03-12 2005-12-07 Vertex Pharmaceuticals Incorporated Pyrazole modulators of atp-binding cassette transporters
WO2004105779A2 (en) 2003-05-27 2004-12-09 Cesare Montecucco Green tea and oplyphenol inhibitors of bacterial proteases
ATE440825T1 (de) 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
US7488739B2 (en) 2003-07-24 2009-02-10 Astellas Pharma Inc. Quinolone derivative or salt thereof
CN1191252C (zh) 2003-08-11 2005-03-02 中国药科大学 3－位取代的喹诺酮衍生物及其在药学上的应用
CN1898221A (zh) 2003-09-06 2007-01-17 沃泰克斯药物股份有限公司 Atp－结合弹夹转运蛋白的调控剂
US20050059035A1 (en) 2003-09-09 2005-03-17 Quest Diagnostics Incorporated Methods and compositions for the amplification of mutations in the diagnosis of cystic fibrosis
HUE044822T2 (hu) 2003-09-12 2019-11-28 Amgen Inc Cinakalcet HCl gyors feloldódású készítménye
US7223759B2 (en) 2003-09-15 2007-05-29 Anadys Pharmaceuticals, Inc. Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds
CA2540978A1 (en) 2003-10-08 2005-04-21 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters containing cycloalkyl or pyranyl groups
US7407976B2 (en) 2003-11-14 2008-08-05 Vertex Pharmaceuticals Incorporated Thiazoles and oxazoles useful as modulators of ATP-Binding Cassette transporters
DK1683524T3 (da) 2003-11-14 2011-03-14 Ajinomoto Kk Dispergering på fast form eller medicinsk præparat på fast form af phenyalaninderivat
US20050208095A1 (en) 2003-11-20 2005-09-22 Angiotech International Ag Polymer compositions and methods for their use
CA2548281C (en) 2003-12-09 2013-11-12 Medcrystalforms, Llc Method of preparation of mixed phase co-crystals with active agents
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
WO2005074913A2 (en) 2004-01-30 2005-08-18 Angiotech International Ag Compositions and methods for treating contracture
SE0400235D0 (sv) 2004-02-06 2004-02-06 Active Biotech Ab New composition containing quinoline compounds
WO2005094805A1 (ja) 2004-04-01 2005-10-13 Institute Of Medicinal Molecular Design. Inc. イミン誘導体及びアミド誘導体
JP2006206612A (ja) 2004-05-27 2006-08-10 Ono Pharmaceut Co Ltd 固形製剤用組成物
US7939558B2 (en) 2004-06-04 2011-05-10 The Regents Of The University Of California Compounds having activity in increasing ion transport by mutant-CFTR and uses thereof
AR049297A1 (es) 2004-06-08 2006-07-12 Vertex Pharma Una composicion farmaceutica y dispersiones solidas de vx-950 (inhibidor de la proteasa de hcv ns3/4a) y proceso de obtencion
US20140343098A1 (en) 2004-06-24 2014-11-20 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US8354427B2 (en) 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
HUE032540T2 (en) 2004-06-24 2017-09-28 Vertex Pharma Modulators of ATP-binding cassette transporters
AU2005269981A1 (en) 2004-07-02 2006-02-09 Bonck, John A Tablet for pulsed delivery
JP5323354B2 (ja) 2004-09-21 2013-10-23 トーマス ジョセフ ラリー， 多目的生体材料組成物
EP1865949B1 (en) 2005-03-11 2012-11-14 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
RU2007138584A (ru) 2005-03-18 2009-04-27 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния (Us) Соединения, обладающие активностью для коррекции процессинга мутантного cftr, и их применение
EP1875911A4 (en) * 2005-04-28 2010-03-03 Eisai R&D Man Co Ltd STABILIZED COMPOSITION
CA2609392A1 (en) 2005-05-24 2006-11-30 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
ATE512145T1 (de) 2005-08-11 2011-06-15 Vertex Pharma Modulatoren des cystic fibrosis transmembrane conductance regulators
ES2367844T3 (es) 2005-08-11 2011-11-10 Vertex Pharmaceuticals, Inc. Moduladores del regulador de la conductancia transmembrana de la fibrosis quística.
AU2006302371A1 (en) 2005-10-06 2007-04-19 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding cassette transporters
US20120232059A1 (en) 2005-11-08 2012-09-13 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette Transporters
EP2395002B1 (en) 2005-11-08 2014-06-18 Vertex Pharmaceuticals Inc. Pharmaceutical composition containing a heterocyclic modulator of atp-binding cassette transporters.
US20080057047A1 (en) 2005-11-29 2008-03-06 Benedikt Sas Use of bacillus amyloliquefaciens PB6 for the prophylaxis or treatment of gastrointestinal and immuno-related diseases
US7989430B2 (en) 2005-12-06 2011-08-02 Regents Of The University Of Minnesota Antibacterial agents
US20090105272A1 (en) 2005-12-24 2009-04-23 Grootenhuis Peter D J Prodrugs of modulators of ABC transporters
WO2007074472A2 (en) 2005-12-27 2007-07-05 Jubilant Organosys Limited Mouth dissolving pharmaceutical composition and process for preparing the same using a high amount of silicon dioxide
AU2006331565A1 (en) 2005-12-27 2007-07-05 Vertex Pharmaceuticals Incorporated Compounds useful in CFTR assays and methods therewith
CN101395147B (zh) 2005-12-28 2013-05-29 弗特克斯药品有限公司 作为atp-结合盒转运蛋白调节剂用于治疗囊性纤维化的1-(苯并[d][1,3]间二氧杂环戊烯-5-基)-n-(苯基)环丙烷-甲酰胺衍生物及相关化合物
US7671221B2 (en) 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
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
CN101443314B (zh) 2006-03-13 2014-04-09 杏林制药株式会社 作为gsk-3抑制剂的氨基喹诺酮类
WO2007106957A1 (en) 2006-03-21 2007-09-27 Laboratoires Smb S.A. Multiple units controlled-release floating dosage forms
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
PT2674428T (pt) 2006-04-07 2016-07-14 Vertex Pharma Modeladores de transportadores de cassetes de ligação de atp
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
AU2007240439B2 (en) 2006-04-20 2012-10-11 Janssen Pharmaceutica N.V. Inhibitors of c-fms kinase
CN101478964B (zh) 2006-05-12 2012-02-29 沃泰克斯药物股份有限公司 N-[2,4-双(1,1-二甲基乙基)-5-羟苯基]-1,4-二氢-4-氧代喹啉-3-羧酰胺的组合物
TW200824723A (en) 2006-09-12 2008-06-16 Glaxo Group Ltd Pharmaceutical composition
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
RU2009120976A (ru) 2006-11-03 2010-12-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Производные азаиндола в качестве модуляторов cftr
US7754739B2 (en) 2007-05-09 2010-07-13 Vertex Pharmaceuticals Incorporated Modulators of CFTR
MX2009006806A (es) 2006-12-22 2009-08-27 Vertex Pharma Secado por rocio fluidizado.
WO2008083130A2 (en) 2006-12-26 2008-07-10 Dr. Reddy's Laboratories Limited Amorphous and crystalline form a of carvedilol phosphate
NZ581259A (en) 2007-05-09 2012-07-27 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
ES2548292T3 (es) 2007-05-25 2015-10-15 Vertex Pharmaceuticals Incorporated Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
WO2009023509A2 (en) 2007-08-09 2009-02-19 Vertex Pharmaceuticals Incorporated Therapeutic combinations useful in treating cftr related diseases
HUE028426T2 (en) 2007-08-24 2016-12-28 Vertex Pharma Isothiazolopyridinones for (inter alia) treating cystic fibrosis
AU2008298545B2 (en) 2007-09-14 2013-12-12 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP2222304A2 (en) 2007-09-14 2010-09-01 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
ES2556080T3 (es) 2007-11-16 2016-01-12 Vertex Pharmaceuticals Incorporated Moduladores de isoquinolina de transportadores de casete de unión a ATP
UA95199C2 (en) 2007-12-07 2011-07-11 Вертекс Фармасьютикалз Инкорпорейтед Aqueous formulation 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
UA102534C2 (xx) 2007-12-07 2013-07-25 Вертекс Фармасьютикалз Инкорпорейтед ТВЕРДА ФОРМА 3-(6-(1-(2,2-ДИФТОРБЕНЗО$d]$1,3]-ДІОКСОЛ-5-ІЛ)-ЦИКЛОПРОПАНКАРБОКСАМІДО)-3-МЕТИЛПІРИДИН-2-ІЛ)БЕНЗОЙНОЇ КИСЛОТИ (ВАРІАНТИ)$ТВЕРДАЯ ФОРМА 3-(6-(1-(2,2-ДИФТОРБЕНЗО$d]$1,3]-ДИОКСОЛ-5-ИЛ)-ЦИКЛОПРОПАНКАРБОКСАМИДО)-3-МЕТИЛПИРИДИН-2-ИЛ)БЕНЗОЙНОЙ КИСЛОТЫ (ВАРИАНТЫ)
LT2639223T (lt) 2007-12-07 2017-06-26 Vertex Pharmaceuticals Incorporated Cikloalkilkarboksiamido-piridino benzenkarboksirūgščių gamybos būdas
CN101925603B (zh) 2007-12-13 2013-12-04 沃泰克斯药物股份有限公司 囊性纤维化跨膜通道调节因子的调节剂
NZ602030A (en) 2008-02-28 2014-02-28 Vertex Pharma Heteroaryl derivatives as cftr modulators
NZ616097A (en) 2008-03-31 2015-04-24 Vertex Pharma Pyridyl derivatives as cftr modulators
US20100074949A1 (en) * 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
US12458635B2 (en) 2008-08-13 2025-11-04 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
CN102231990B (zh) * 2008-08-13 2013-09-25 沃泰克斯药物股份有限公司 N-[2，4-双(1，1-二甲基乙基)-5-羟基苯基]-1，4-二氢-4-氧代喹啉-3-甲酰胺的药物组合物和其给药
US20100256184A1 (en) 2008-08-13 2010-10-07 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
WO2010025126A1 (en) 2008-08-26 2010-03-04 Cystic Fibrosis Foundation Therapeutics, Inc. Rapidly disintegrating tablets comprising lipase, amylase, and protease
MX2011003249A (es) 2008-09-29 2011-05-19 Vertex Pharma Unidades de dosificacion del acido 3-(6-(1-(2,2-difluorobenzo[d][1 ,3]dioxol-5-il)ciclopropancarboxamido)-3-metilpiridin-2-il)benzoi co.
JP5645834B2 (ja) 2008-10-23 2014-12-24 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修飾因子
US20110257223A1 (en) 2008-10-23 2011-10-20 Vertex Pharmaceuticals Incorporated Modulators of Cystic Fibrosis Transmembrane Conductance Regulator
AR074060A1 (es) 2008-10-23 2010-12-22 Vertex Pharma Moduladores del regulador de conductancia transmembrana de la fibrosis quistica
NZ592504A (en) 2008-10-23 2013-04-26 Vertex Pharma Solid forms of n-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide
UA104876C2 (ru) 2008-11-06 2014-03-25 Вертекс Фармасьютікалз Інкорпорейтед Модуляторы атф-связывающих кассетных транспортеров
ES2532753T3 (es) 2008-11-06 2015-03-31 Vertex Pharmaceuticals Incorporated Moduladores de transportadores del casete de unión a ATP
US8367660B2 (en) 2008-12-30 2013-02-05 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
CN102361856A (zh) 2009-03-20 2012-02-22 沃泰克斯药物股份有限公司 囊性纤维化跨膜传导调节因子的调节剂
EP2821400B1 (en) 2009-03-20 2017-09-27 Vertex Pharmaceuticals Incorporated Process for making modulators of cystic fibrosis transmembrane conductance regulator
KR20120083416A (ko) 2009-09-17 2012-07-25 버텍스 파마슈티칼스 인코포레이티드 아자비시클릭 화합물의 제조 방법
EP2490687A1 (en) 2009-10-22 2012-08-29 Vertex Pharmaceuticals Incorporated Compositions for treatment of cystic fibrosis and other chronic diseases
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
US8389727B2 (en) 2009-10-23 2013-03-05 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
EP2547658A1 (en) 2010-03-19 2013-01-23 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
RU2711481C2 (ru) 2010-03-25 2020-01-17 Вертекс Фармасьютикалз Инкорпорейтед ТВЕРДЫЕ ФОРМЫ (R)-1-(2, 2-ДИФТОРБЕНЗО[d][1, 3]ДИОКСОЛ-5-ИЛ)-N-(1-(2, 3-ДИГИДРОКСИПРОПИЛ)-6-ФТОР-2-(1-ГИДРОКСИ-2-МЕТИЛПРОПАН-2-ИЛ)-1H-ИНДОЛ-5-ИЛ)ЦИКЛОПРОПАНКАРБОКСАМИДА
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
CN102917692A (zh) 2010-04-07 2013-02-06 弗特克斯药品有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]二氧杂环戊烯-5-基)环丙甲酰胺基)-3-甲基吡啶-2-基)苯甲酸的药物组合物和其给药方法
NZ602795A (en) 2010-04-07 2015-01-30 Vertex Pharma Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
EP2560650A1 (en) 2010-04-22 2013-02-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
NZ603042A (en) 2010-04-22 2015-02-27 Vertex Pharma Pharmaceutical compositions comprising cftr modulators and administrations thereof
NZ603044A (en) 2010-04-22 2015-08-28 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
US8404849B2 (en) 2010-05-20 2013-03-26 Vertex Pharmaceuticals Processes for producing modulators of cystic fibrosis transmembrane conductance regulator
EP2575814A1 (en) 2010-05-20 2013-04-10 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
ES2894936T3 (es) * 2010-06-24 2022-02-16 Viropharma Biologics Llc Métodos de tratamiento para la inflamación del esófago
WO2012027247A2 (en) 2010-08-23 2012-03-01 Vertex Pharmaceuticals Incorporated Pharmaceutical composition of (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxy propyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide and administration therof
NZ607494A (en) * 2010-08-27 2015-04-24 Vertex Pharma Pharmaceutical composition and administrations thereof
US8802700B2 (en) 2010-12-10 2014-08-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
SI3235812T1 (sl) 2011-05-18 2020-02-28 Vertex Pharmaceuticals (Europe) Limited Devterirani derivati ivakaftorja
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
AU2012332225A1 (en) 2011-11-02 2014-05-15 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
AU2012335714B2 (en) 2011-11-08 2017-04-13 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US20140127901A1 (en) 2012-11-08 2014-05-08 Taiwan Semiconductor Manufacturing Company, Ltd. Low-k damage free integration scheme for copper interconnects
US20130186801A1 (en) 2012-01-25 2013-07-25 Vertex Pharmaceuticals Incorporated Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
RU2692779C2 (ru) 2012-02-27 2019-06-27 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтическая композиция и ее введения
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
EP2858645A1 (en) 2012-06-08 2015-04-15 Vertex Pharmaceuticals Incorporated Pharmaceuticl compositions for the treatment of cftr -mediated disorders
AU2013290444B2 (en) 2012-07-16 2018-04-26 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof
PL2914248T5 (pl) 2012-11-02 2024-01-15 Vertex Pharmaceuticals Incorporated Kompozycje farmaceutyczne do leczenia chorób w których pośredniczy CFTR
MY178621A (en) 2012-11-19 2020-10-19 Vertex Pharmaceuticals Europe Ltd Deuterated cftr potentiators
US20140221424A1 (en) 2013-01-30 2014-08-07 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for use in the treatment of cystic fibrosis
BR112016010403A2 (pt) 2013-11-12 2017-08-08 Vertex Pharma Processo de preparação de composições farmacêuticas para o tratamento de doenças mediadas por cftr
CA2944140C (en) 2014-04-15 2022-10-04 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
AU2015328174B2 (en) 2014-10-06 2020-05-21 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
RU2749213C2 (ru) 2014-10-07 2021-06-07 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе
US10302602B2 (en) 2014-11-18 2019-05-28 Vertex Pharmaceuticals Incorporated Process of conducting high throughput testing high performance liquid chromatography
MA41031A (fr) 2014-11-26 2017-10-03 Catabasis Pharmaceuticals Inc Conjugués cystéamine-acide gras et leur utilisation comme activateurs de l'autophagie
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
CA2969587A1 (en) 2014-12-05 2016-06-09 Centre National De La Recherche Scientifique (Cnrs) Compounds for treating cystic fibrosis
US9957234B2 (en) 2014-12-09 2018-05-01 Laurus Labs Limited Polymorphs of Ivacaftor, process for its preparation and pharmaceutical composition thereof
US10196384B2 (en) 2015-03-31 2019-02-05 Vertex Pharmaceuticals (Europe) Limited Deuterated CFTR modulators
GB201507926D0 (en) 2015-05-08 2015-06-24 Proqr Therapeutics N V Improved treatments using oligonucleotides
US10336703B2 (en) 2015-05-12 2019-07-02 Council Of Scientific And Industrial Research Process for the synthesis of ivacaftor and related compounds
UY36680A (es) 2015-05-19 2016-12-30 Glaxosmithkline Ip Dev Ltd Amidas heterocíclicas como inhibidores de quinasa
WO2016199085A1 (en) 2015-06-11 2016-12-15 Aizant Drug Research Solutions Private Limited Nanoparticulate ivacaftor formulations
HK1258472A1 (zh) 2015-09-21 2019-11-15 Vertex Pharmaceuticals (Europe) Limited 氘代cftr增效剂的施用
CA2999529A1 (en) 2015-09-25 2017-03-30 Vertex Pharmaceuticals (Europe) Limited Deuterated cftr potentiators
CN105884628B (zh) 2016-06-06 2018-06-29 上海工程技术大学 2,4-二叔丁基-5-氨基酚的制备方法
WO2018080591A1 (en) 2016-10-27 2018-05-03 Vertex Pharmaceuticals (Europe) Limited Methods of treatment with deuterated cftr potentiators
US20180280349A1 (en) 2017-03-28 2018-10-04 Vertex Pharmaceuticals Incorporated Methods of treating cystic fibrosis in patients with residual function mutations
AU2018375186B2 (en) 2017-12-01 2023-07-20 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator

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