RU2020134082A - Модуляторы регулятора трансмембранной проводимости при муковисцидозе - Google Patents
Модуляторы регулятора трансмембранной проводимости при муковисцидозе Download PDFInfo
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- RU2020134082A RU2020134082A RU2020134082A RU2020134082A RU2020134082A RU 2020134082 A RU2020134082 A RU 2020134082A RU 2020134082 A RU2020134082 A RU 2020134082A RU 2020134082 A RU2020134082 A RU 2020134082A RU 2020134082 A RU2020134082 A RU 2020134082A
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
- A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
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- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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Claims (102)
1. Соединение формулы Ia:
Ia
его фармацевтически приемлемая соль или дейтерированное производное любого из них, где независимо для каждого случая:
кольцо B представляет собой C6-C10 арильное кольцо или C3-C10 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR;
кольцо С представляет собой C6-C10 арильное кольцо, C3-C14 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой N, O или S, или C3-C10 циклоалкильное кольцо;
X представляет собой O или NR;
Y представляет собой CRR, CO, O, S, SO, SO2, S(O)NH или NR;
R1 представляет собой галоген; CN; F5S; SiR3; OH; NRR; C1-C6 алкил или фторалкил; C1-C6 алкокси или фторалкокси; C2-C6 алкенил; C2-C6 алкинил; (C1-C9 алкилен)-R4, где до четырех звеньев СН2 независимо заменены на O, CO, S, SO, SO2 или NR; C6-C10 арил; C3-C10 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; или C3-C10 циклоалкил;
R2 представляет собой галоген; OH; NRR; азид; CN; CO2R; C1-C6 алкил или фторалкил; C1-C6 алкокси или фторалкокси; C2-C6 алкенил; C2-C6 алкинил; C6-C10 арил; C3-C13 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; C3-C10 циклоалкил; или (C1-C9 алкилен)-R4, где до четырех звеньев СН2 независимо заменены на O, CO, S, SO, SO2 или NR;
или две группы R2, взятые вместе, могут образовывать группу =CH2 или =O;
R3 представляет собой галоген; CN; CO2R; C1-C6 алкил или фторалкил; C2-C6 алкенил; C2-C6 алкинил; C1-C6 алкокси или фторалкокси; или C6-C10 арил; C3-C10 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; C3-C10 циклоалкил; или (C1-C9 алкилен)-R4, где до четырех звеньев СН2 независимо заменены на O, CO, S, SO, SO2 или NR;
или две группы R3, взятые вместе, могут образовывать группу =CH2 или =O;
R4 представляет собой H; азид; CF3; CHF2; или; CCH; CO2R; OH; C6-C10 арил, C3-C10 гетероарил или гетероциклоалкил, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; C3-C10 циклоалкил; NRR, NRCOR, CONRR, CN, галоген или SO2R;
R независимо представляет собой H; OH; CO2H; CO2C1-C6 алкил; C1-C6 алкил; C2-C6 алкенил; C2-C6 алкинил; C6-C10 арил; C3-C10 гетероарил или гетероциклоалкил, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; или C3-C10 циклоалкил;
n равно 0, 1, или 2;
o равно 0, 1, 2, 3, 4 или 5;
p равно 0, 1, 2 или 3; и
q равно 0, 1, 2, 3, 4 или 5.
2. Соединение, соль или дейтерированное производное по п.1, где кольцо B представляет собой фенил, пиридил, пиридин-2(1H)-он, пиразол, индол, тиофен, дигидробензофуран, пиразин, индазол, тиазол, пиридин-4(1H)-он, пирролидинон или хинолин.
4. Соединение, соль или дейтерированное производное по любому из пп. 1-3, где кольцо C представляет собой фенил, индол, циклоалкил, пиридил, пирролидин, нафталин, пиперидин или дигидроинден.
5. Соединение, соль или дейтерированное производное по любому из пп. 1-4, где кольцо C представляет собой
6. Соединение, соль или дейтерированное производное по любому из пп. 1-5, где Y представляет собой O.
7. Соединение, соль или дейтерированное производное по любому из пп. 1-5, где Y представляет собой CH2.
8. Соединение, соль или дейтерированное производное по любому из пп. 1-5, где Y представляет собой CH(C1-C6 алифатическую группу).
9. Соединение, соль или дейтерированное производное по любому из пп. 1-5, где Y представляет собой CH(CH3).
10. Соединение, соль или дейтерированное производное по любому из пп. 1-5, где Y представляет собой CH(CH2CH3).
11. Соединение, соль или дейтерированное производное по любому из пп. 1-10, где R1 представляет собой галоген, CN, C1-C6 алифатическую группу, C1-C6 алкокси, C3-C8 циклоалкил, или фенил, пиридил, пиримидин, индол, аза-индол или тиофеновое кольцо, где все кольца могут быть заменены галогеном, C1-C6 алифатической группой, C1-C6 алкокси, C1-C6 фторалифатической группой, C1-C6 фторалкокси, OH, CH2OH, CH2OCH3, CN, CO2H, амино, амидо, C3-C10 гетероарилом, C3-C10 гетероциклоалкилом или (C1-C8 алифатическая группа)-R4, где до трех звеньев CH2 могут быть заменены на O, CO, S, SO, SO2 или NR.
13. Соединение, соль или дейтерированное производное по любому из пп. 1-12, где R2 выбран из галогена, OH, CN, азида, амино, C1-C6 алифатической группы или фторалифатической группы, C1-C6 алкокси или фторалкокси, C3-C10 моно- или бициклического гетероциклического кольца, где до 4 атомов углерода могут быть заменены на O, S, N или NR; или (C1-C8 алифатическая группа)-R4, где до трех звеньев CH2 могут быть заменены на O, CO, S, SO, SO2 или NR.
14. Соединение, соль или дейтерированное производное по любому из пп. 1-13, где R2 выбран из Cl, F, OH, CN, N3, NH2, NH(CH3), N(CH3)2, CH3, CH2OH, CH2CH3, CH(CH3)2, CHF2, OCH3, OCF3, OCHF2, OCH(CH3)2, C(O)CH3, CH2CH2OH, CH2NH2, NH(CH2)2OH, NH(CH2)2N(CH3)2, NH(CH2)2NH2, NH(CH2)3NH2, NH(CH2)2OCH3, NHCH(CH3)2, или CO2H.
15. Соединение, соль или дейтерированное производное по любому из пп. 1-14, где R3 выбран из галогена, CN, C1-C6 алифатической группы или фторалифатической группы, C1-C6 алкокси или C3-C10 моно- или бициклического гетероарила, где до 4 атомов углерода могут быть заменены на O, S, N или NR.
17. Соединение, соль или дейтерированное производное по любому из пп. 1-16, где o равно 0.
18. Соединение, соль или дейтерированное производное по любому из пп. 1-16, где o равно 1.
19. Соединение, соль или дейтерированное производное по любому из пп. 1-18, где n равно 0.
20. Соединение, соль или дейтерированное производное по любому из пп. 1-18, где n равно 1.
21. Соединение, соль или дейтерированное производное по любому из пп. 1-18, где n равно 2.
22. Соединение, соль или дейтерированное производное по любому из пп. 1-21, где p равно 0.
23. Соединение, соль или дейтерированное производное по любому из пп. 1-21, где p равно 1.
24. Соединение, соль или дейтерированное производное по любому из пп. 1-21, где p равно 2.
25. Соединение, соль или дейтерированное производное по любому из пп. 1-24, где кольцо B представляет собой фенил.
26. Соединение, соль или дейтерированное производное по любому из пп. 1-25, где кольцо B и кольцо C независимо представляют собой фенил или пиридил.
27. Соединение формулы Ic:
Ic
его фармацевтически приемлемая соль или дейтерированное производное любого из них, где независимо для каждого случая:
кольцо B представляет собой C6-C10 арильное кольцо или C3-C10 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR;
кольцо С представляет собой C6-C10 арильное кольцо, C3-C14гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой N, O или S, или C3-C10 циклоалкильное кольцо;
Y представляет собой CRR, CO, O, S, SO, SO2, S(O)NH или NR;
R1 представляет собой галоген; CN; F5S; SiR3; OH; NRR; C1-C6 алкил или фторалкил; C1-C6 алкокси или фторалкокси; C2-C6 алкенил; C2-C6 алкинил; (C1-C9 алкилен)-R4, где до четырех звеньев СН2 независимо заменены на O, CO, S, SO, SO2 или NR; C6-C10 арил; C3-C10 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; или C3-C10 циклоалкил;
R2 представляет собой галоген; OH; NRR; азид; CN; CO2R; C1-C6 алкил или фторалкил; C1-C6 алкокси или фторалкокси; C2-C6 алкенил; C2-C6 алкинил; C6-C10 арил; C3-C13 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; C3-C10 циклоалкил; или (C1-C9 алкилен)-R4, где до четырех звеньев СН2 независимо заменены на O, CO, S, SO, SO2 или NR;
или две группы R2, взятые вместе, могут образовывать группу =CH2 или =O;
R3 представляет собой галоген; CN; CO2R; C1-C6 алкил или фторалкил; C2-C6 алкенил; C2-C6 алкинил; C1-C6 алкокси или фторалкокси; или C6-C10 арил; C3-C10 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; C3-C10 циклоалкил; или (C1-C9 алкилен)-R4, где до четырех звеньев СН2 независимо заменены на O, CO, S, SO, SO2 или NR;
или две группы R3, взятые вместе, могут образовывать группу =CH2 или =O;
R4 представляет собой H; азид; CF3; CHF2; или; CCH; CO2R; OH; C6-C10 арил, C3-C10 гетероарил или гетероциклоалкил, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; C3-C10 циклоалкил; NRR, NRCOR, CONRR, CN, галоген или SO2R;
R независимо представляет собой H; OH; CO2H; CO2C1-C6 алкил; C1-C6 алкил; C2-C6 алкенил; C2-C6 алкинил; C6-C10 арил; C3-C10 гетероарил или гетероциклоалкил, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; или C3-C10 циклоалкил;
n равно 0, 1, 2 или 3;
o равно 0, 1, 2, 3, 4 или 5;
p равно 0, 1, 2 или 3; и
q равно 0, 1, 2, 3, 4 или 5.
28. Соединение формулы Id:
Id
его фармацевтически приемлемая соль или дейтерированное производное любого из них, где независимо для каждого случая:
кольцо B представляет собой C6-C10 арильное кольцо или C3-C10 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой O, S, N или NR;
кольцо С представляет собой C6-C10 арильное кольцо, C3-C14 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой N, O или S, или C3-C10 циклоалкильное кольцо;
Y представляет собой CRR, CO, O, S, SO, SO2, S(O)NH или NR;
R1 представляет собой галоген; CN; F5S; SiR3; OH; NRR; C1-C6 алкил или фторалкил; C1-C6 алкокси или фторалкокси; C2-C6 алкенил; C2-C6 алкинил; (C1-C9 алкилен)-R4, где до четырех звеньев СН2 независимо заменены на O, CO, S, SO, SO2 или NR; C6-C10 арил; C3-C10 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; или C3-C10 циклоалкил;
R2 представляет собой галоген; OH; NRR; азид; CN; CO2R; C1-C6 алкил или фторалкил; C1-C6 алкокси или фторалкокси; C2-C6 алкенил; C2-C6 алкинил; C6-C10 арил; C3-C13 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; C3-C10 циклоалкил; или (C1-C9 алкилен)-R4, где до четырех звеньев СН2 независимо заменены на O, CO, S, SO, SO2 или NR;
или две группы R2, взятые вместе, могут образовывать группу =CH2 или =O;
R3 представляет собой галоген; CN; CO2R; C1-C6 алкил или фторалкил; C2-C6 алкенил; C2-C6 алкинил; C1-C6 алкокси или фторалкокси; или C6-C10 арил; C3-C10 гетероарильное или гетероциклическое кольцо, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; C3-C10 циклоалкил; или (C1-C9 алкилен)-R4, где до четырех звеньев СН2 независимо заменены на O, CO, S, SO, SO2 или NR;
или две группы R3, взятые вместе, могут образовывать группу =CH2 или =O;
R4 представляет собой H; азид; CF3; CHF2; или; CCH; CO2R; OH; C6-C10 арил, C3-C10 гетероарил или гетероциклоалкил, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; C3-C10 циклоалкил; NRR, NRCOR, CONRR, CN, галоген или SO2R;
R независимо представляет собой H; OH; CO2H; CO2C1-C6 алкил; C1-C6 алкил; C2-C6 алкенил; C2-C6 алкинил; C6-C10 арил; C3-C10 гетероарил или гетероциклоалкил, где любые из от 1 до 4 кольцевых атомов независимо представляют собой О, S, N или NR; или C3-C10 циклоалкил;
n равно 0, 1, 2 или 3;
o равно 0, 1, 2, 3, 4 или 5;
p равно 0, 1, 2 или 3; и
q равно 0, 1, 2, 3, 4 или 5.
29. Соединение, соль или дейтерированное производное любого из них по любому из пп. 1-28, выбранное из таблицы 1.
30. Фармацевтическая композиция, содержащая соединение, соль или дейтерированное производное по любому из пп. 1-29 и фармацевтически приемлемый носитель.
31. Фармацевтическая композиция по п.30, дополнительно содержащая один или несколько дополнительных терапевтических агентов.
32. Фармацевтическая композиция по п.31, где один или несколько дополнительных терапевтических агентов включают модулятор CFTR.
33. Фармацевтическая композиция по п.32, где один или несколько дополнительных терапевтических агентов включают
или его фармацевтически приемлемую соль.
34. Фармацевтическая композиция по п.32, где один или несколько дополнительных терапевтических агентов включают
или его фармацевтически приемлемую соль.
35. Способ лечения кистозного фиброза у пациента, включающий введение пациенту эффективного количества соединения по любому из пп. 1-29 или фармацевтической композиции по любому из пп. 30-34.
36. Способ по п.35, дополнительно включающий введение пациенту одного или нескольких дополнительных терапевтических агентов до, одновременно с или после введения соединения по любому из пп. 1-29 или фармацевтической композиции по любому из пп. 30-34.
37. Способ по п.36, где одного или несколько дополнительных терапевтических агентов включают модулятор CFTR.
38. Способ по п.37, где один или несколько дополнительных терапевтических агентов включают
или его фармацевтически приемлемую соль.
39. Способ по п.37, где один или несколько дополнительных терапевтических агентов включают
или его фармацевтически приемлемую соль.
40. Способ по п.35, где пациент является гомозиготным по F508del мутации.
41. Способ по п.35, где пациент является гетерозиготным по F508del мутации.
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Families Citing this family (79)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
EP1912983B1 (en) | 2005-08-11 | 2011-06-08 | Vertex Pharmaceuticals, Inc. | Modulators of cystic fibrosis transmembrane conductance regulator |
RS60205B1 (sr) | 2005-12-28 | 2020-06-30 | Vertex Pharma | Farmaceutske kompozicije amorfnog oblika n-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksohinolin-3-karboksamida |
HUE055205T2 (hu) | 2006-04-07 | 2021-11-29 | Vertex Pharma | ATP-kötõ kazetta transzporterek modulátorainak elõállítása |
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 |
US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
US8969386B2 (en) | 2007-05-09 | 2015-03-03 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
US8507524B2 (en) | 2007-11-16 | 2013-08-13 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette-transporters |
US8507534B2 (en) | 2007-12-07 | 2013-08-13 | 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 |
CN101910134B (zh) | 2007-12-07 | 2014-03-19 | 沃泰克斯药物股份有限公司 | 环烷基甲酰氨基-吡啶苯甲酸类的生产方法 |
CN103382201B (zh) | 2008-02-28 | 2016-12-28 | 沃泰克斯药物股份有限公司 | 作为cftr调节剂的杂芳基衍生物 |
LT2821400T (lt) | 2009-03-20 | 2018-02-12 | Vertex Pharmaceuticals Incorporated | Cistinės fibrozės transmembraninio laidumo reguliatoriaus moduliatorių gamybos būdas |
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 |
JP2013523833A (ja) | 2010-04-07 | 2013-06-17 | 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)安息香酸の医薬組成物およびその投与 |
CA2797118C (en) | 2010-04-22 | 2021-03-30 | Vertex Pharmaceuticals Incorporated | Process of producing cycloalkylcarboxamido-indole compounds |
CN109966264A (zh) | 2012-02-27 | 2019-07-05 | 沃泰克斯药物股份有限公司 | 药物组合物及其施用 |
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 |
WO2015073231A1 (en) | 2013-11-12 | 2015-05-21 | Vertex Pharmaceuticals Incorporated | Process of preparing pharmaceutical compositions for the treatment of cftr mediated diseases |
KR102447581B1 (ko) | 2014-04-15 | 2022-09-28 | 버텍스 파마슈티칼스 인코포레이티드 | 낭포성 섬유증 막전도 조절자 매개 질환 치료용 약제학적 조성물 |
PL3203840T3 (pl) * | 2014-10-06 | 2021-01-11 | Vertex Pharmaceuticals Incorporated | Modulatory mukowiscydozowego przezbłonowego regulatora przewodnictwa |
KR20170063954A (ko) | 2014-10-07 | 2017-06-08 | 버텍스 파마슈티칼스 인코포레이티드 | 낭성 섬유증 막횡단 전도도 조절자의 조정제의 공-결정 |
SI3221692T1 (sl) | 2014-11-18 | 2021-11-30 | Vertex Pharmaceuticals Inc. | Postopek za izvajanje testov visoke prepustnosti z visoko zmogljivostno tekočinsko kromatografijo |
US9840513B2 (en) | 2015-07-16 | 2017-12-12 | Abbvie S.Á.R.L. | Substituted tricyclics and method of use |
TW201735769A (zh) | 2015-10-09 | 2017-10-16 | 盧森堡商艾伯維公司 | 經取代之吡唑并[3,4-b]吡啶-6-羧酸及使用方法 |
US10738030B2 (en) | 2016-03-31 | 2020-08-11 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
TW201811766A (zh) | 2016-08-29 | 2018-04-01 | 瑞士商諾華公司 | N-(吡啶-2-基)吡啶-磺醯胺衍生物及其用於疾病治療之用途 |
WO2018064632A1 (en) * | 2016-09-30 | 2018-04-05 | Vertex Pharmaceuticals Incorporated | Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
WO2018107100A1 (en) * | 2016-12-09 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
BR112019025801A2 (pt) | 2017-06-08 | 2020-07-07 | Vertex Pharmaceuticals Incorporated | métodos de tratamento para fibrose cística |
WO2019010092A1 (en) | 2017-07-01 | 2019-01-10 | Vertex Pharmaceuticals Incorporated | COMPOSITIONS AND METHODS FOR TREATING CYSTIC FIBROSIS |
CA3069225A1 (en) | 2017-07-17 | 2019-01-24 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
AU2018304168B2 (en) * | 2017-07-17 | 2023-05-04 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
WO2019028228A1 (en) * | 2017-08-02 | 2019-02-07 | Vertex Pharmaceuticals Incorporated | PROCESSES FOR THE PREPARATION OF PYRROLIDINE COMPOUNDS |
US10988454B2 (en) * | 2017-09-14 | 2021-04-27 | Abbvie Overseas S.À.R.L. | Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
WO2019079760A1 (en) * | 2017-10-19 | 2019-04-25 | Vertex Pharmaceuticals Incorporated | CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS |
US20210228489A1 (en) * | 2017-12-04 | 2021-07-29 | Vertex Pharmaceuticals Incorporated | Compositions for treating cystic fibrosis |
AU2018380426B2 (en) * | 2017-12-08 | 2023-05-18 | 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 |
PT3752510T (pt) * | 2018-02-15 | 2023-03-15 | Vertex Pharma | Macrociclos como moduladores do regulador de condutância de transmembrana da fibrose cística, suas composições farmacêuticas, seu uso no tratamento da fibrose cística e processos para produzi-los |
WO2019191620A1 (en) | 2018-03-30 | 2019-10-03 | Vertex Pharmaceuticals Incorporated | Crystalline forms of modulators of cftr |
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 |
CA3104913A1 (en) * | 2018-08-31 | 2020-03-05 | Xenon Pharmaceuticals Inc. | Heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors |
GB201817038D0 (en) * | 2018-10-19 | 2018-12-05 | Inflazome Ltd | Novel processes |
PT3880197T (pt) | 2018-11-14 | 2023-05-09 | Vertex Pharma | Métodos de tratamento para a fibrose quística |
CN113226464A (zh) * | 2018-12-18 | 2021-08-06 | 诺华股份有限公司 | N-(吡啶-2-基磺酰基)环丙烷甲酰胺衍生物及其在治疗cftr介导的疾病中的用途 |
CN109608415B (zh) * | 2019-01-21 | 2020-12-01 | 暨南大学 | 噻唑甲酰胺类化合物及其合成和应用 |
UY38630A (es) * | 2019-04-03 | 2020-10-30 | Vertex Pharma | Agentes moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
WO2020214921A1 (en) | 2019-04-17 | 2020-10-22 | Vertex Pharmaceuticals Incorporated | Solid forms of modulators of cftr |
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 |
TW202120517A (zh) | 2019-08-14 | 2021-06-01 | 美商維泰克斯製藥公司 | 製備cftr調節劑之方法 |
WO2021030552A1 (en) | 2019-08-14 | 2021-02-18 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
CN110776616B (zh) * | 2019-10-26 | 2021-06-22 | 福建华夏蓝新材料科技有限公司 | 一种高效润湿水性异氰酸酯固化剂 |
CA3157798A1 (en) | 2019-11-12 | 2021-05-20 | Zhongli Gao | 6-membered heteroarylaminosulfonamides for treating diseases and conditions mediated by deficient cftr activity |
WO2021113806A1 (en) | 2019-12-05 | 2021-06-10 | Genzyme Corporation | Arylamides and methods of use thereof |
WO2021113809A1 (en) | 2019-12-05 | 2021-06-10 | Genzyme Corporation | Arylamides and methods of use thereof |
EP4082614A4 (en) * | 2019-12-27 | 2024-01-24 | Japan Tobacco Inc | ACYLSULFAMIDE COMPOUND AND PHARMACEUTICAL USE THEREOF |
CR20230120A (es) | 2020-08-07 | 2023-09-01 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
AU2021325923A1 (en) | 2020-08-13 | 2023-04-06 | Vertex Pharmaceuticals Incorporated | Crystalline forms of CFTR modulators |
JP2023538125A (ja) | 2020-08-20 | 2023-09-06 | ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティー | 粘液過剰分泌を特徴とする呼吸器疾患を処置するための方法 |
EP4225765A2 (en) * | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
CN113402499B (zh) * | 2021-06-21 | 2022-05-13 | 上海勋和医药科技有限公司 | 一种亚磺酰亚胺取代的吲唑类irak4激酶抑制剂、制备方法及用途 |
WO2023023376A2 (en) * | 2021-08-19 | 2023-02-23 | University Of Virginia Patent Foundation | Sulfonyl-triazoles useful as covalent kinase ligands |
WO2023034946A1 (en) | 2021-09-03 | 2023-03-09 | Genzyme Corporation | Indole compounds and uses thereof in the treatement of cystic fibrosis |
WO2023034992A1 (en) | 2021-09-03 | 2023-03-09 | Genzyme Corporation | Indole compounds and methods of use |
TW202333699A (zh) | 2022-02-03 | 2023-09-01 | 美商維泰克斯製藥公司 | 囊腫纖維化之治療方法 |
WO2023150236A1 (en) | 2022-02-03 | 2023-08-10 | Vertex Pharmaceuticals Incorporated | Methods of preparing and crystalline forms of (6a,12a)-17-amino-12-methyl-6,15-bis(trifluoromethyl)-13,19-dioxa-3,4,18-triazatricyclo[ 12.3.1.12,5]nonadeca-1(18),2,4,14,16-pentaen-6-ol |
WO2023154291A1 (en) | 2022-02-08 | 2023-08-17 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
WO2023211990A1 (en) * | 2022-04-25 | 2023-11-02 | Siteone Therapeutics, Inc. | Bicyclic heterocyclic amide inhibitors of na v1.8 for the treatment of pain |
CN115611693B (zh) * | 2022-05-12 | 2023-11-28 | 常州大学 | 一种催化合成异色满-1-酮类或芳香酮类化合物的方法 |
WO2023224931A1 (en) | 2022-05-16 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
WO2023224924A1 (en) | 2022-05-16 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | Solid forms of a macrocyclic compounds as cftr modulators and their preparation |
WO2024054851A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocyclic compounds, compositions and methods of using thereof |
WO2024054845A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocycic compounds, compositions, and methods of using thereof |
WO2024054840A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocyclic compounds, compositions, and methods of using thereof |
WO2024056791A1 (en) | 2022-09-15 | 2024-03-21 | Idorsia Pharmaceuticals Ltd | Combination of macrocyclic cftr modulators with cftr correctors and / or cftr potentiators |
WO2024056798A1 (en) | 2022-09-15 | 2024-03-21 | Idorsia Pharmaceuticals Ltd | Macrocyclic cftr modulators |
Family Cites Families (265)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0194599A3 (en) | 1985-03-14 | 1988-01-20 | Nissan Chemical Industries Ltd. | Benzamide derivatives, process for producing the same, and soil fungicides containing the same |
GB9122590D0 (en) | 1991-10-24 | 1991-12-04 | Lilly Industries Ltd | Pharmaceutical compounds |
DE4410453A1 (de) | 1994-03-25 | 1995-09-28 | Hoechst Ag | Substituierte heterocyclische Carbonsäureamidester, ihre Herstellung und ihre Verwendung als Arzneimittel |
GB9514160D0 (en) | 1994-07-25 | 1995-09-13 | Zeneca Ltd | Aromatic compounds |
EP0804077A1 (en) | 1995-01-19 | 1997-11-05 | Novartis AG | Herbicidal composition |
EA001418B1 (ru) | 1995-11-23 | 2001-02-26 | Новартис Аг | Гербицидная композиция |
EP0873311A1 (en) | 1995-12-15 | 1998-10-28 | Merck Frosst Canada Inc. | Tri-aryl ethane derivatives as pde iv inhibitors |
AU717430B2 (en) | 1996-08-26 | 2000-03-23 | Genetics Institute, Llc | Inhibitors of phospholipase enzymes |
JPH10114654A (ja) | 1996-10-09 | 1998-05-06 | Fujisawa Pharmaceut Co Ltd | 新規用途 |
AU6209098A (en) | 1997-01-15 | 1998-08-07 | Novartis Ag | Herbicidal agent |
GB9716657D0 (en) * | 1997-08-07 | 1997-10-15 | Zeneca Ltd | Chemical compounds |
DE19742951A1 (de) | 1997-09-29 | 1999-04-15 | Hoechst Schering Agrevo Gmbh | Acylsulfamoylbenzoesäureamide, diese enthaltende nutzpflanzenschützende Mittel und Verfahren zu ihrer Herstellung |
US5972995A (en) | 1997-10-16 | 1999-10-26 | Children's Hospital Medical Center Of Northern California | Compositions and methods for cystic fibrosis therapy |
DE19802697A1 (de) | 1998-01-24 | 1999-07-29 | Bayer Ag | Selektive Herbizide auf Basis von N-Aryl-triazolin(thi)onen und N-Arylsulfonylamino(thio)carbonyltriazolin(thi)onen |
WO1999041238A1 (fr) | 1998-02-13 | 1999-08-19 | Kureha Kagaku Kogyo K.K. | Derives de n-(pnenylsulfonyle) picolinamide, procede de production de ces derniers et herbicide |
BR9909440A (pt) | 1998-04-06 | 2000-12-26 | Fujisawa Pharmaceutical Co | Derivados de indol |
DZ3262A1 (fr) | 1999-06-10 | 2000-12-12 | Warner Lambert Co | Procede d'inhibition d'agregation de proteines amyloides et d'imagerie de depots amyloides au moyen de derives d'isoindoline |
DE19936438A1 (de) | 1999-08-03 | 2001-02-08 | Aventis Cropscience Gmbh | Kombinationen von Herbiziden und Safenern |
DE19940860A1 (de) | 1999-08-27 | 2001-03-01 | Bayer Ag | Selektive Herbizide auf Basis eines substituierten Phenylsulfonyl aminocarbonyltriazolinons und Safenern II |
DE19958381A1 (de) | 1999-12-03 | 2001-06-07 | Bayer Ag | Herbizide auf Basis von N-Aryl-uracilen |
AU2001229501A1 (en) | 2000-01-24 | 2001-07-31 | Isis Pharmaceuticals, Inc. | Antisense modulation of inducible nitric oxide synthase expression |
WO2002015902A1 (en) | 2000-08-23 | 2002-02-28 | Merck & Co., Inc. | Method of treating or preventing urinary incontinence using prostanoid ep1 receptor antagonists |
US6720338B2 (en) | 2000-09-20 | 2004-04-13 | Abbott Laboratories | N-acylsulfonamide apoptosis promoters |
US20020055631A1 (en) | 2000-09-20 | 2002-05-09 | Augeri David J. | N-acylsulfonamide apoptosis promoters |
UY26942A1 (es) | 2000-09-20 | 2002-04-26 | Abbott Lab | N-acilsulfonamidas promotoras de la apoptosis |
KR20030036917A (ko) * | 2000-10-10 | 2003-05-09 | 스미스클라인 비참 코포레이션 | 치환된 인돌, 이를 함유하는 약제학적 조성물, 및 이의PPAR-γ결합제로서의 용도 |
US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
DE10119721A1 (de) | 2001-04-21 | 2002-10-31 | Bayer Cropscience Gmbh | Herbizide Mittel enthaltend Benzoylcyclohexandione und Safener |
DE60222409T2 (de) | 2001-05-31 | 2008-09-25 | Vicore Pharma Ab | Trizyklische verbindungen, nützlich als angiotensin ii agonisten |
SI1404653T1 (sl) | 2001-06-28 | 2008-12-31 | Pfizer Prod Inc | S triamidom substituirani indoli, benzofurani in benzotiofeni kot zaviralci mikrosomske prenašalnebeljakovine za trigliceride (MTP) in/ali izločanja apolipoproteina B (APO B) |
DE10145019A1 (de) | 2001-09-13 | 2003-04-03 | Bayer Cropscience Gmbh | Kombinationen aus Herbiziden und Safenern |
DE10146873A1 (de) | 2001-09-24 | 2003-04-17 | Bayer Cropscience Gmbh | Heterocyclische Amide und -Iminderivate, Verfahren zu ihrer Herstellung, sie enthaltende Mittel und ihre Verwendung als Schädlingsbekämpfungsmittel |
CA2672549A1 (en) | 2001-11-14 | 2003-06-12 | Ben-Zion Dolitzky | Amorphous and crystalline forms of losartan potassium and process for their preparation |
AU2002354056A1 (en) | 2001-11-19 | 2003-06-10 | Ono Pharmaceutical Co., Ltd. | Remedies for urinary frequency |
DE10157545A1 (de) | 2001-11-23 | 2003-06-12 | Bayer Cropscience Gmbh | Herbizide Mittel enthaltend Benzoylpyrazole und Safener |
US7247748B2 (en) | 2002-03-27 | 2007-07-24 | Smithkline Corporation | Amide compounds and methods of using the same |
GB0212785D0 (en) | 2002-05-31 | 2002-07-10 | Glaxo Group Ltd | Compounds |
RS51816B (en) | 2002-06-08 | 2011-12-31 | Bayer Cropscience Ag. | COMBINATION OF HERBICIDIC AROMATIC CARBONIC ACIDS AND PROTECTANTS |
DE10237461A1 (de) | 2002-08-16 | 2004-02-26 | Bayer Cropscience Gmbh | Herbizide Mittel enthaltend Benzoylpyrazole und Safener |
EP1536794A2 (en) | 2002-09-06 | 2005-06-08 | Merck & Co., Inc. | Treatment of rheumatoid arthritis by inhibition of pde4 |
AU2003277162C1 (en) | 2002-09-30 | 2009-12-24 | The Regents Of The University Of California | Cystic fibrosis transmembrane conductance regulator protein inhibitors and uses thereof |
EP1562914A1 (en) | 2002-10-22 | 2005-08-17 | Merck Frosst Canada & Co. | Nitric oxide releasing selective cyclooxygenase-2 inhibitors |
GB0225548D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Compounds |
AU2003302106A1 (en) | 2002-11-21 | 2004-06-15 | Vicore Pharma Ab | New tricyclic angiotensin ii agonists |
AU2003286347A1 (en) | 2002-12-20 | 2004-07-14 | Pfizer Products Inc. | Microsomal triglyceride transfer protein inhibitors |
CA2505604A1 (en) | 2002-12-20 | 2004-07-08 | Pfizer Products Inc. | Microsomal triglyceride transfer protein inhibitors |
WO2004078114A2 (en) | 2003-02-28 | 2004-09-16 | Encysive Pharmaceuticals Inc. | Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-ii receptor antagonists. |
WO2004080972A1 (en) | 2003-03-12 | 2004-09-23 | Vertex Pharmaceuticals Incorporated | Pirazole modulators of atp-binding cassette transporters |
AU2003219291A1 (en) | 2003-03-24 | 2004-10-18 | Vicore Pharma Ab | Bicyclic compounds useful as angiotensin ii agonists |
HUE059464T2 (hu) | 2003-04-11 | 2022-11-28 | Ptc Therapeutics Inc | 1,2,4-Oxadiazolbenzoesav-vegyületek és ezek alkalmazása nonsense szuppresszióhoz és betegségek kezelésére |
US7696244B2 (en) | 2003-05-16 | 2010-04-13 | The Regents Of The University Of California | Compounds having activity in increasing ion transport by mutant-CFTR and uses thereof |
WO2004111014A1 (en) | 2003-06-06 | 2004-12-23 | Vertex Pharmaceuticals Incorporated | Pyrimidine derivatives as modulators of atp-binding cassette transporters |
CN1886393A (zh) | 2003-10-08 | 2006-12-27 | 沃泰克斯药物股份有限公司 | 含有环烷基或吡喃基基团的atp-结合弹夹转运蛋白的调控剂 |
WO2005049593A2 (en) * | 2003-11-13 | 2005-06-02 | Abbott Laboratories | N-acylsulfonamide apoptosis promoters |
CA2545719A1 (en) | 2003-11-14 | 2005-06-02 | Vertex Pharmaceuticals Incorporated | Thiazoles and oxazoles useful as modulators of atp-binding cassette transporters |
GB0328024D0 (en) | 2003-12-03 | 2004-01-07 | Glaxo Group Ltd | Compounds |
AU2005207037A1 (en) | 2004-01-22 | 2005-08-04 | Nitromed, Inc. | Nitrosated and/or nitrosylated compounds, compositions and methods of use |
AU2005210474B2 (en) | 2004-01-30 | 2011-07-07 | 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 |
CA2555133A1 (en) | 2004-02-04 | 2005-09-01 | Pfizer Products Inc. | Substituted quinoline compounds |
US20050197376A1 (en) | 2004-03-02 | 2005-09-08 | Fujisawa Pharmaceutical Co. Ltd. | Concomitant drugs |
WO2005085216A1 (ja) | 2004-03-05 | 2005-09-15 | Nissan Chemical Industries, Ltd. | イソキサゾリン置換ベンズアミド化合物及び有害生物防除剤 |
WO2005099705A2 (en) | 2004-03-24 | 2005-10-27 | Bayer Pharmaceuticals Corporation | Preparation of imidazole derivatives and methods of use |
US7414037B2 (en) | 2004-03-30 | 2008-08-19 | The Regents Of The University Of California | Hydrazide-containing CFTR inhibitor compounds and uses thereof |
GB0410121D0 (en) | 2004-05-06 | 2004-06-09 | Glaxo Group Ltd | Compounds |
EP1765347A4 (en) | 2004-06-04 | 2008-10-01 | Univ California | COMPOUNDS WITH ION TRANSPORTER HEALING EFFECT BY MUTANT CFTR AND ITS USE |
US8354427B2 (en) | 2004-06-24 | 2013-01-15 | Vertex Pharmaceutical Incorporated | Modulators of ATP-binding cassette transporters |
LT2489659T (lt) | 2004-06-24 | 2018-03-26 | Vertex Pharmaceuticals Incorporated | Atp rišančios kasetės transporterių moduliatoriai |
US7550463B2 (en) | 2004-09-15 | 2009-06-23 | Shionogi & Co., Ltd. | Carbamoylpyridone derivatives having inhibitory activity against HIV integrase |
NZ554211A (en) | 2004-09-29 | 2010-10-29 | Portola Pharm Inc | Substituted 2H-1,3-Benzoxazin-4(3H)-ones |
BRPI0516110A (pt) | 2004-10-13 | 2008-08-26 | Ptc Therapeutics Inc | compostos para supressão sem sentido e métodos para seu uso |
US20080287399A1 (en) | 2004-12-14 | 2008-11-20 | Astrazeneca Ab | Substituted Aminopyridines and Uses Thereof |
RU2423351C2 (ru) * | 2004-12-16 | 2011-07-10 | Вертекс Фармасьютикалз Инкорпорейтед | Пирид-2-оны, применимые как ингибиторы протеинкиназ семейства тес для лечения воспалительных, пролиферативных и иммунологически-опосредованных заболеваний |
GB0428173D0 (en) * | 2004-12-23 | 2005-01-26 | Astrazeneca Ab | Compounds |
US20100137378A1 (en) | 2004-12-23 | 2010-06-03 | Glaxo Group Limited | Pyridine Compounds For The Treatment Of Prostaglandin Mediated Diseases |
EP1865949B1 (en) | 2005-03-11 | 2012-11-14 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
CA2600869A1 (en) | 2005-03-18 | 2006-09-28 | The Regents Of The University Of California | Compounds having activity in correcting mutant-cftr processing and uses thereof |
ES2390804T3 (es) | 2005-04-08 | 2012-11-16 | Ptc Therapeutics, Inc. | Composiciones de un 1,2,4-oxadiazol oralmente activo para terapia de supresión de la mutación sin sentido |
EP1891018B1 (en) | 2005-05-24 | 2011-11-16 | Vertex Pharmaceuticals, Inc. | Modulators of atp-binding cassette transporters |
WO2007019397A2 (en) | 2005-08-05 | 2007-02-15 | Genelabs Technologies, Inc. | 6-membered aryl and heteroaryl derivatives for the treatment of hepatitis c virus |
EP1912983B1 (en) | 2005-08-11 | 2011-06-08 | Vertex Pharmaceuticals, Inc. | Modulators of cystic fibrosis transmembrane conductance regulator |
US8314256B2 (en) | 2005-10-06 | 2012-11-20 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
WO2007053641A2 (en) | 2005-11-01 | 2007-05-10 | Mars, Incorporated | A-type procyanidins and inflammation |
WO2007075946A1 (en) | 2005-12-27 | 2007-07-05 | Vertex Pharmaceuticals Incorporated | Compounds useful in cftr assays and methods therewith |
RS60205B1 (sr) | 2005-12-28 | 2020-06-30 | Vertex Pharma | Farmaceutske kompozicije amorfnog oblika n-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksohinolin-3-karboksamida |
US7671221B2 (en) | 2005-12-28 | 2010-03-02 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
US7691902B2 (en) | 2005-12-28 | 2010-04-06 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
JP2009532437A (ja) | 2006-04-05 | 2009-09-10 | バイエル・クロツプサイエンス・エス・アー | 殺菌剤n−シクロプロピル−スルホニルアミド誘導体 |
HUE055205T2 (hu) | 2006-04-07 | 2021-11-29 | Vertex Pharma | ATP-kötõ kazetta transzporterek modulátorainak elõállítása |
CA2652072A1 (en) | 2006-05-12 | 2007-11-22 | Vertex Pharmaceuticals Incorporated | Compositions of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
WO2008005457A2 (en) | 2006-06-30 | 2008-01-10 | Sunesis Pharmaceuticals | Pyridinonyl pdk1 inhibitors |
MX2009004702A (es) | 2006-11-03 | 2009-06-19 | Vertex Pharma | Derivados de azaindol como moduladores del regulador de conductancia de transmembrana de fibrosis quistica. |
US7754739B2 (en) | 2007-05-09 | 2010-07-13 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
US20090047246A1 (en) | 2007-02-12 | 2009-02-19 | Intermune, Inc. | Novel inhibitors of hepatitis c virus replication |
WO2008141385A1 (en) | 2007-05-21 | 2008-11-27 | Biota Scientific Management Pty Ltd | Viral polymerase inhibitors |
US8058299B2 (en) | 2007-05-22 | 2011-11-15 | Via Pharmaceuticals, Inc. | Diacylglycerol acyltransferase inhibitors |
EP2167471B1 (en) | 2007-05-25 | 2013-10-16 | Amgen Inc. | Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use |
GB0716532D0 (en) | 2007-08-24 | 2007-10-03 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
BRPI0816116A2 (pt) * | 2007-08-29 | 2015-03-03 | Schering Corp | Derivados de indol 2,3-substituídos para o tratamento de infecções virais. |
JP2010540417A (ja) | 2007-09-14 | 2010-12-24 | 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 | N−[2,4−ビス(1,1−ジメチルエチル)−5−ヒドロキシフェニル]−1,4−ジヒドロ−4−オキソキノリン−3−カルボキサミドの固体形態 |
AU2013231151B2 (en) | 2007-11-16 | 2015-06-25 | Vertex Pharmaceuticals Incorporated | Isoquinoline modulators of ATP-Binding Cassette transporters |
JP5249344B2 (ja) * | 2007-11-16 | 2013-07-31 | メルク・シャープ・アンド・ドーム・コーポレーション | ヘテロ環の3位が置換されたインドール誘導体およびその使用 |
GB0723794D0 (en) | 2007-12-05 | 2008-01-16 | Lectus Therapeutics Ltd | Potassium ion channel modulators and uses thereof |
US8507534B2 (en) | 2007-12-07 | 2013-08-13 | 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 |
CN101910134B (zh) | 2007-12-07 | 2014-03-19 | 沃泰克斯药物股份有限公司 | 环烷基甲酰氨基-吡啶苯甲酸类的生产方法 |
AU2013270464B2 (en) | 2008-03-31 | 2016-05-26 | Vertex Pharmaceuticals Incorporated | Pyridyl derivatives as CFTR modulators |
JP2011520785A (ja) * | 2008-04-16 | 2011-07-21 | バイオリポックス エービー | 薬剤としての使用のためのビスアリール化合物 |
US20110112193A1 (en) | 2008-05-14 | 2011-05-12 | Peter Nilsson | Bis-aryl compounds for use as medicaments |
US8888400B2 (en) * | 2010-10-07 | 2014-11-18 | Mcgard Llc | Corrosion-resistant self-locking manhole cover |
EP2145537A1 (en) | 2008-07-09 | 2010-01-20 | Bayer CropScience AG | Plant growth regulator |
UY31982A (es) | 2008-07-16 | 2010-02-26 | Boehringer Ingelheim Int | Derivados de 1,2-dihidropiridin-3-carboxamidas n-sustituidas |
ES2857152T3 (es) | 2008-08-13 | 2021-09-28 | Vertex Pharma | Composición farmacéutica y administraciones de la misma |
WO2010022307A2 (en) | 2008-08-21 | 2010-02-25 | Smithkline Beecham Corporation | Prolyl hydroxylase inhibitors |
MX2011002149A (es) | 2008-08-27 | 2011-04-05 | Calcimedica Inc | Compuestos que modulan el calcio intracelular. |
US9333235B2 (en) | 2008-10-22 | 2016-05-10 | Trustees Of Dartmouth College | Combination therapy and kit for the prevention and treatment of cystic fibrosis |
AR074060A1 (es) | 2008-10-23 | 2010-12-22 | Vertex Pharma | Moduladores del regulador de conductancia transmembrana de la fibrosis quistica |
EP2940016A1 (en) | 2008-11-06 | 2015-11-04 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
UA104876C2 (ru) | 2008-11-06 | 2014-03-25 | Вертекс Фармасьютікалз Інкорпорейтед | Модуляторы атф-связывающих кассетных транспортеров |
UA108193C2 (uk) | 2008-12-04 | 2015-04-10 | Апоптозіндукуючий засіб для лікування раку і імунних і аутоімунних захворювань | |
US20100160322A1 (en) | 2008-12-04 | 2010-06-24 | Abbott Laboratories | Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases |
US8367660B2 (en) | 2008-12-30 | 2013-02-05 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
DK2511264T3 (da) | 2009-01-19 | 2015-06-22 | Abbvie Inc | Apoptose-inducerende midler til behandling af cancer og immunsygdomme og autoimmune sygdomme |
BRPI1008949B1 (pt) | 2009-03-11 | 2018-07-10 | Bayer Intellectual Property Gmbh | Cetoenóis haloalquilmetilenóxi-fenil-substituídos e seu uso, composição, seu uso e seu método de produção, métodos para combate de pestes animais e/ou crescimento de plantas indesejadas |
LT2821400T (lt) | 2009-03-20 | 2018-02-12 | Vertex Pharmaceuticals Incorporated | Cistinės fibrozės transmembraninio laidumo reguliatoriaus moduliatorių gamybos būdas |
RU2518897C2 (ru) | 2009-03-20 | 2014-06-10 | Вертекс Фармасьютикалз Инкорпорейтед | Производные 3-карбоксамида-4-оксохинолина, полезные в качестве модуляторов регулятора трансмембранной проводимости кистозного фиброза |
WO2010110231A1 (ja) | 2009-03-26 | 2010-09-30 | 塩野義製薬株式会社 | 置換された3-ヒドロキシ-4-ピリドン誘導体 |
CN102458122A (zh) * | 2009-04-20 | 2012-05-16 | 人类健康研究所 | 含有哒嗪磺胺衍生物的化合物、组合物和方法 |
PE20120345A1 (es) | 2009-05-26 | 2012-05-17 | Abbvie Bahamas Ltd | Derivados de 2-(1h-pirrolo[2,3-b]piridin-5-iloxi)-n-fenilsulfonilbenzamida como inhibidores de proteinas anti-apoptoticas |
WO2011102514A1 (ja) | 2010-02-22 | 2011-08-25 | 武田薬品工業株式会社 | 芳香環化合物 |
AU2011227021A1 (en) | 2010-03-19 | 2012-10-18 | Vertex Pharmaceuticals Incorporated | Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
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 |
AR081069A1 (es) | 2010-04-07 | 2012-06-06 | Vertex Pharma | Formas solidas del acido 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioxol-5-il)ciclopropancarboxamido)-3-metilpiridin-2-il)benzoico |
JP2013523833A (ja) | 2010-04-07 | 2013-06-17 | 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)安息香酸の医薬組成物およびその投与 |
US8344137B2 (en) | 2010-04-14 | 2013-01-01 | Hoffman-La Roche Inc. | 3,3-dimethyl tetrahydroquinoline derivatives |
CA2796642A1 (en) | 2010-04-22 | 2011-10-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
CA2797118C (en) | 2010-04-22 | 2021-03-30 | Vertex Pharmaceuticals Incorporated | Process of producing cycloalkylcarboxamido-indole compounds |
TWI520960B (zh) | 2010-05-26 | 2016-02-11 | 艾伯維有限公司 | 用於治療癌症及免疫及自體免疫疾病之細胞凋亡誘導劑 |
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 |
US20120046330A1 (en) | 2010-08-23 | 2012-02-23 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions 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 and administration thereof |
RU2013113627A (ru) | 2010-08-27 | 2014-10-10 | Вертекс Фармасьютикалз Инкорпорейтед | Фармацевтическая композиция и ее введения |
US9394290B2 (en) | 2010-10-21 | 2016-07-19 | Universitaet Des Saarlandes Campus Saarbruecken | Selective CYP11B1 inhibitors for the treatment of cortisol dependent diseases |
WO2012078902A2 (en) | 2010-12-08 | 2012-06-14 | Proteostasis Therapeutics, Inc. | Proteostasis regulators |
WO2012078909A1 (en) | 2010-12-08 | 2012-06-14 | Proteostasis Therapeutics, Inc. | Thiazolpyrimidine proteostasis regulators |
WO2012087938A1 (en) | 2010-12-20 | 2012-06-28 | Glaxosmithkline Llc | Quinazolinone derivatives as antiviral agents |
EP2471363A1 (de) | 2010-12-30 | 2012-07-04 | Bayer CropScience AG | Verwendung von Aryl-, Heteroaryl- und Benzylsulfonamidocarbonsäuren, -carbonsäureestern, -carbonsäureamiden und -carbonitrilen oder deren Salze zur Steigerung der Stresstoleranz in Pflanzen |
JPWO2012102297A1 (ja) | 2011-01-26 | 2014-06-30 | 杏林製薬株式会社 | ピラゾロピリジン誘導体、またはその薬理学的に許容される塩 |
US9000026B2 (en) | 2011-02-17 | 2015-04-07 | Bayer Intellectual Property Gmbh | Substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones for therapy |
KR101789527B1 (ko) | 2011-03-01 | 2017-10-25 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 2-아실옥시피롤린-4-온 |
AR085585A1 (es) | 2011-04-15 | 2013-10-09 | Bayer Cropscience Ag | Vinil- y alquinilciclohexanoles sustituidos como principios activos contra estres abiotico de plantas |
WO2012154888A1 (en) | 2011-05-09 | 2012-11-15 | Proteostasis Therapeutics, Inc. | Compounds for treating protein folding disorders |
WO2012154880A1 (en) | 2011-05-09 | 2012-11-15 | Proteostasis Therapeutics, Inc. | Proteostasis regulators for treating cystic fibrosis and other protein misfolding diseases |
CN103635230B (zh) | 2011-05-12 | 2017-10-31 | 普罗蒂斯特斯治疗公司 | 蛋白内稳态调节剂 |
HUE047354T2 (hu) | 2011-05-18 | 2020-04-28 | Vertex Pharmaceuticals Europe Ltd | Ivacaftor deuterizált származékai |
PL3235812T3 (pl) | 2011-05-18 | 2020-04-30 | Vertex Pharmaceuticals (Europe) Limited | Deuterowane pochodne iwakaftoru |
US9260416B2 (en) | 2011-05-27 | 2016-02-16 | Amira Pharmaceuticals, Inc. | Heterocyclic autotaxin inhibitors and uses thereof |
EP2751086A4 (en) | 2011-08-30 | 2015-09-16 | Chdi Foundation Inc | KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHOD OF USE THEREOF |
WO2013038381A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine/pyrazine amide derivatives |
WO2013038373A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine amide derivatives |
WO2013038378A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine amide derivatives |
CA2848620C (en) | 2011-09-16 | 2020-03-10 | Bayer Intellectual Property Gmbh | Use of cyprosulfamide for inducing a growth regulating response in useful plants and increasing the yield of harvested plant organs therefrom |
WO2013038390A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | N-substituted heterocyclyl carboxamides |
WO2013038386A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Heterocyclic compounds for the treatment of cystic fibrosis |
US9226505B2 (en) | 2011-09-23 | 2016-01-05 | Bayer Intellectual Property Gmbh | 4-substituted 1-phenylpyrazole-3-carboxylic acid derivatives as agents against abiotic plant stress |
GB201118704D0 (en) | 2011-10-28 | 2011-12-14 | Univ Oxford | Cystic fibrosis treatment |
EP2776427B1 (en) | 2011-11-08 | 2017-02-01 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
US8426450B1 (en) | 2011-11-29 | 2013-04-23 | Helsinn Healthcare Sa | Substituted 4-phenyl pyridines having anti-emetic effect |
AU2013202368B2 (en) | 2012-01-25 | 2016-06-16 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating compounds |
CA3128556A1 (en) | 2012-01-25 | 2013-08-01 | Vertex Pharmaceuticals Incorporated | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
AU2013202373B2 (en) | 2012-01-25 | 2016-04-14 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
JP2015083542A (ja) | 2012-02-08 | 2015-04-30 | 大日本住友製薬株式会社 | 3位置換プロリン誘導体 |
CN109966264A (zh) | 2012-02-27 | 2019-07-05 | 沃泰克斯药物股份有限公司 | 药物组合物及其施用 |
US8889730B2 (en) | 2012-04-10 | 2014-11-18 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
WO2013158121A1 (en) | 2012-04-20 | 2013-10-24 | Vertex Pharmaceuticals Incorporated | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
MX2014014234A (es) | 2012-05-22 | 2015-05-07 | Genentech Inc | Benzamidas n-sustituidas y su uso en el tratamiento del dolor. |
EP2858645A1 (en) | 2012-06-08 | 2015-04-15 | Vertex Pharmaceuticals Incorporated | Pharmaceuticl compositions for the treatment of cftr -mediated disorders |
WO2013185202A1 (en) | 2012-06-14 | 2013-12-19 | Beta Pharma Canada Inc | Apoptosis inducers |
CA2878478A1 (en) | 2012-07-06 | 2014-01-09 | Genentech, Inc. | N-substituted benzamides and methods of use thereof |
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 |
JP2015178458A (ja) | 2012-07-25 | 2015-10-08 | 杏林製薬株式会社 | ベンゼン環縮合含窒素5員複素環式化合物、またはその薬理学的に許容される塩 |
EP2882439B1 (en) | 2012-08-13 | 2018-04-11 | AbbVie Inc. | Apoptosis-inducing agents |
EP2888251B1 (en) | 2012-08-21 | 2019-04-24 | Peter MacCallum Cancer Institute | Perforin inhibiting benzenesulfonamide compounds, preparation and uses thereof |
JP6318156B2 (ja) | 2012-09-06 | 2018-04-25 | プレキシコン インコーポレーテッドPlexxikon Inc. | キナーゼをモジュレートするための化合物および方法、ならびにその指標 |
WO2014047427A2 (en) * | 2012-09-21 | 2014-03-27 | Vanderbilt University | Substituted benzofuran, benzothiophene and indole mcl-1 inhibitors |
SG10201703452PA (en) | 2012-11-02 | 2017-06-29 | Vertex Pharma | Pharmaceutical compositions for the treatment of cftr mediated diseases |
US9567301B2 (en) * | 2012-11-02 | 2017-02-14 | Dana-Farber Cancer Institute, Inc. | Pyrrol-1-yl benzoic acid derivatives useful as myc inhibitors |
CA2890018A1 (en) | 2012-11-05 | 2014-05-08 | Nant Holdings Ip, Llc | Substituted indol-5-ol derivatives and their therapeutical applications |
WO2014078842A1 (en) | 2012-11-19 | 2014-05-22 | Concert Pharmaceuticals, Inc. | Deuterated cftr potentiators |
AU2013348018A1 (en) | 2012-11-20 | 2015-06-04 | Discoverybiomed, Inc. | Small molecule CFTR correctors |
ITMI20122065A1 (it) | 2012-12-03 | 2014-06-04 | Univ Padova | Uso dei correttori del cftr nel trattamento delle patologie del muscolo striato |
JP2016504300A (ja) | 2012-12-05 | 2016-02-12 | バイエル・クロップサイエンス・アクチェンゲゼルシャフト | 置換された1−(アリールエチニル)−、1−(ヘテロアリールエチニル)−、1−(複素環エチニル)−および1−(シクロアルケニルエチニル)ビシクロアルカノールの非生物的植物ストレスに対する活性薬剤としての使用 |
EP2928296A1 (de) | 2012-12-05 | 2015-10-14 | Bayer CropScience AG | Verwendung substituierter 1-(arylethinyl)-, 1-(heteroarylethinyl)-, 1-(heterocyclylethinyl)- und 1-(cyloalkenylethinyl)-cyclohexanole als wirkstoffe gegen abiotischen pflanzenstress |
UA115576C2 (uk) | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
RU2018138195A (ru) | 2012-12-17 | 2018-12-18 | Пэрион Сайенсиз, Инк. | Соединения 3,5-диамино-6-хлор-n-(n-(4- фенилбутил)карбамимидоил)пиразин-2-карбоксамида |
GB201223265D0 (en) | 2012-12-21 | 2013-02-06 | Selvita Sa | Novel benzimidazole derivatives as kinase inhibitors |
US20140199728A1 (en) | 2013-01-14 | 2014-07-17 | Amgen Inc. | Methods of using cell-cycle inhibitors to modulate one or more properties of a cell culture |
JP6545148B2 (ja) | 2013-03-13 | 2019-07-17 | フラットリー ディスカバリー ラブ,エルエルシー | ピリダジノン化合物及び嚢胞性線維症の治療のための方法 |
EP2968304B1 (en) | 2013-03-14 | 2018-10-10 | The Trustees of Columbia University in the City of New York | 4-phenylpiperidines, their preparation and use |
EP2968303B1 (en) | 2013-03-14 | 2018-07-04 | The Trustees of Columbia University in the City of New York | Octahydrocyclopentapyrroles, their preparation and use |
AU2014240026B2 (en) | 2013-03-15 | 2018-06-14 | Discoverybiomed, Inc. | Coumarin derivatives and methods of use in treating cystic fibrosis, chronic obstructive pulmonary disease, and misfolded protein disorders |
RS63108B1 (sr) | 2013-03-15 | 2022-04-29 | Cyclerion Therapeutics Inc | Sgc stimulatori |
WO2014160810A1 (en) | 2013-03-29 | 2014-10-02 | Takeda Pharmaceutical Company Limited | 6-(5-hydroxy-1h-pyrazol-1-yl)nicotinamide derivatives and their use as phd inhibitors |
MX368263B (es) | 2013-05-07 | 2019-09-26 | Galapagos Nv | Compuestos novedosos y composiciones farmaceuticas de los mismos para el tratamiento de fibrosis quistica. |
WO2014181287A1 (en) | 2013-05-09 | 2014-11-13 | Piramal Enterprises Limited | Heterocyclyl compounds and uses thereof |
CA2911326A1 (en) | 2013-05-24 | 2014-11-27 | The California Institute For Biomedical Research | Compounds for treatment of drug resistant and persistent tuberculosis |
US20160151335A1 (en) | 2013-06-26 | 2016-06-02 | Proteostasis Therapeutics, Inc. | Methods of modulating cftr activity |
CA2915633A1 (en) | 2013-07-02 | 2015-01-08 | The California Institute For Biomedical Research | Compounds for treatment of cystic fibrosis |
WO2015007516A1 (en) | 2013-07-15 | 2015-01-22 | Boehringer Ingelheim International Gmbh | Novel 5-substituted benzimidazolium compounds |
JP6461133B2 (ja) | 2013-07-15 | 2019-01-30 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規4置換及び5置換ベンゾイミダゾリウム化合物 |
EP3022196B1 (en) | 2013-07-15 | 2017-09-06 | Boehringer Ingelheim International GmbH | Novel benzimidazolium compounds |
WO2015010832A1 (en) | 2013-07-22 | 2015-01-29 | Syngenta Participations Ag | Microbiocidal heterocyclic derivatives |
CA2922341C (en) | 2013-08-28 | 2022-06-07 | Vanderbilt University | Substituted indole mcl-1 inhibitors |
US9663508B2 (en) | 2013-10-01 | 2017-05-30 | Amgen Inc. | Biaryl acyl-sulfonamide compounds as sodium channel inhibitors |
WO2015069287A1 (en) | 2013-11-08 | 2015-05-14 | Allergan, Inc. | Compounds as tyrosine kinase modulators |
WO2015073231A1 (en) | 2013-11-12 | 2015-05-21 | Vertex Pharmaceuticals Incorporated | Process of preparing pharmaceutical compositions for the treatment of cftr mediated diseases |
KR102447581B1 (ko) | 2014-04-15 | 2022-09-28 | 버텍스 파마슈티칼스 인코포레이티드 | 낭포성 섬유증 막전도 조절자 매개 질환 치료용 약제학적 조성물 |
PL3203840T3 (pl) * | 2014-10-06 | 2021-01-11 | Vertex Pharmaceuticals Incorporated | Modulatory mukowiscydozowego przezbłonowego regulatora przewodnictwa |
KR20170063954A (ko) | 2014-10-07 | 2017-06-08 | 버텍스 파마슈티칼스 인코포레이티드 | 낭성 섬유증 막횡단 전도도 조절자의 조정제의 공-결정 |
SI3221692T1 (sl) | 2014-11-18 | 2021-11-30 | Vertex Pharmaceuticals Inc. | Postopek za izvajanje testov visoke prepustnosti z visoko zmogljivostno tekočinsko kromatografijo |
MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
US10738011B2 (en) | 2014-12-23 | 2020-08-11 | Proteostasis Therapeutics, Inc. | Derivatives of 5-(hetero)arylpyrazol-3-carboxylic amide or 1-(hetero)aryltriazol-4-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
AU2016217851A1 (en) | 2015-02-15 | 2017-08-03 | F. Hoffmann-La Roche Ag | 1-(het)arylsulfonyl-(pyrrolidine or piperidine)-2-carboxamide derivatives and their use as TRPA1 antagonists |
WO2016160945A1 (en) | 2015-03-31 | 2016-10-06 | Concert Pharmaceuticals, Inc. | Deuterated vx-661 |
BR112018005454A2 (pt) | 2015-09-21 | 2018-10-09 | Vertex Pharmaceuticals Europe Ltd | administração de potencializadores de cftr deuterados |
EP3854782A1 (en) | 2016-03-30 | 2021-07-28 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
US10738030B2 (en) | 2016-03-31 | 2020-08-11 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
MX2018012331A (es) | 2016-04-07 | 2019-05-23 | Proteostasis Therapeutics Inc | Atomos de silicona que contienen analogos de ivacaftor. |
AU2017256172A1 (en) | 2016-04-26 | 2018-09-06 | AbbVie S.à.r.l. | Modulators of cystic fibrosis transmembrane conductance regulator protein |
US10138227B2 (en) | 2016-06-03 | 2018-11-27 | Abbvie S.Á.R.L. | Heteroaryl substituted pyridines and methods of use |
AU2017280206A1 (en) | 2016-06-21 | 2019-01-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing CFTR activity |
WO2018064632A1 (en) | 2016-09-30 | 2018-04-05 | Vertex Pharmaceuticals Incorporated | Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
US10399940B2 (en) | 2016-10-07 | 2019-09-03 | Abbvie S.Á.R.L. | Substituted pyrrolidines and methods of use |
US9981910B2 (en) | 2016-10-07 | 2018-05-29 | Abbvie S.Á.R.L. | Substituted pyrrolidines and methods of use |
WO2018081381A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc | Pyridazine derivatives, compositions and methods for modulating cftr |
AU2017348183A1 (en) | 2016-10-26 | 2019-05-16 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating CFTR |
US20190256474A1 (en) | 2016-10-26 | 2019-08-22 | Proteostasis Therapeutics, Inc. | N-phenyl-2-(3-phenyl-6-oxo-1,6-dihydropyridazin-1-yl)acetamide derivatives for treating cystic fibrosis |
SG10202106949XA (en) | 2016-11-18 | 2021-07-29 | Cystic Fibrosis Found | Pyrrolopyrimidines as cftr potentiators |
WO2018107100A1 (en) | 2016-12-09 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
JP7150721B2 (ja) | 2016-12-16 | 2022-10-11 | システィック・ファイブロシス・ファンデーション | Cftr増強物質としての二環式ヘテロアリール誘導体 |
WO2018116185A1 (en) | 2016-12-20 | 2018-06-28 | AbbVie S.à.r.l. | Deuterated cftr modulators and methods of use |
CN110177788B (zh) | 2017-01-07 | 2023-03-24 | 重庆复创医药研究有限公司 | 作为bcl-2选择性凋亡诱导剂的化合物 |
TW201831471A (zh) | 2017-02-24 | 2018-09-01 | 盧森堡商艾伯維公司 | 囊腫纖化症跨膜傳導調節蛋白的調節劑及其使用方法 |
US20180280349A1 (en) | 2017-03-28 | 2018-10-04 | Vertex Pharmaceuticals Incorporated | Methods of treating cystic fibrosis in patients with residual function mutations |
US20200055844A1 (en) | 2017-04-28 | 2020-02-20 | Proteostasis Therapeutics, Inc. | 4-sulfonylaminocarbonylquinoline derivatives for increasing cftr activity |
BR112019025801A2 (pt) | 2017-06-08 | 2020-07-07 | Vertex Pharmaceuticals Incorporated | métodos de tratamento para fibrose cística |
WO2019010092A1 (en) | 2017-07-01 | 2019-01-10 | Vertex Pharmaceuticals Incorporated | COMPOSITIONS AND METHODS FOR TREATING CYSTIC FIBROSIS |
AU2018304168B2 (en) | 2017-07-17 | 2023-05-04 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
CA3069225A1 (en) | 2017-07-17 | 2019-01-24 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
US11427858B2 (en) | 2017-07-31 | 2022-08-30 | Technion Research & Development Foundation Limited | Methods of detecting modified and unmodified DNA |
WO2019028228A1 (en) | 2017-08-02 | 2019-02-07 | Vertex Pharmaceuticals Incorporated | PROCESSES FOR THE PREPARATION OF PYRROLIDINE COMPOUNDS |
US10988454B2 (en) | 2017-09-14 | 2021-04-27 | Abbvie Overseas S.À.R.L. | Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
EP3691638A1 (en) | 2017-10-06 | 2020-08-12 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods for increasing cftr activity |
WO2019079760A1 (en) | 2017-10-19 | 2019-04-25 | Vertex Pharmaceuticals Incorporated | CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS |
US20210228489A1 (en) | 2017-12-04 | 2021-07-29 | Vertex Pharmaceuticals Incorporated | Compositions for treating cystic fibrosis |
AU2018380426B2 (en) | 2017-12-08 | 2023-05-18 | 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 |
WO2019191620A1 (en) | 2018-03-30 | 2019-10-03 | Vertex Pharmaceuticals Incorporated | Crystalline forms of modulators of cftr |
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 |
WO2020214921A1 (en) | 2019-04-17 | 2020-10-22 | Vertex Pharmaceuticals Incorporated | Solid forms of modulators of cftr |
WO2020242935A1 (en) | 2019-05-29 | 2020-12-03 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
WO2021030552A1 (en) | 2019-08-14 | 2021-02-18 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
TW202120517A (zh) | 2019-08-14 | 2021-06-01 | 美商維泰克斯製藥公司 | 製備cftr調節劑之方法 |
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 |
EP4013759A1 (en) | 2019-08-14 | 2022-06-22 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
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