JP2018500343A5 - - Google Patents
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- JP2018500343A5 JP2018500343A5 JP2017533772A JP2017533772A JP2018500343A5 JP 2018500343 A5 JP2018500343 A5 JP 2018500343A5 JP 2017533772 A JP2017533772 A JP 2017533772A JP 2017533772 A JP2017533772 A JP 2017533772A JP 2018500343 A5 JP2018500343 A5 JP 2018500343A5
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- JP
- Japan
- Prior art keywords
- alkyl
- group
- independently selected
- hydroxyl
- halogen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 125000000217 alkyl group Chemical group 0.000 claims 32
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000002367 halogens Chemical class 0.000 claims 18
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 17
- 125000001424 substituent group Chemical group 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- -1 NR hh Inorganic materials 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462096374P | 2014-12-23 | 2014-12-23 | |
| US62/096,374 | 2014-12-23 | ||
| US201562102244P | 2015-01-12 | 2015-01-12 | |
| US62/102,244 | 2015-01-12 | ||
| US201562196839P | 2015-07-24 | 2015-07-24 | |
| US62/196,839 | 2015-07-24 | ||
| US201562199661P | 2015-07-31 | 2015-07-31 | |
| US62/199,661 | 2015-07-31 | ||
| PCT/US2015/000212 WO2016105485A2 (en) | 2014-12-23 | 2015-12-23 | Compounds, compositions, and methods for increasing cftr activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018500343A JP2018500343A (ja) | 2018-01-11 |
| JP2018500343A5 true JP2018500343A5 (enExample) | 2019-01-31 |
| JP6700284B2 JP6700284B2 (ja) | 2020-05-27 |
Family
ID=55168337
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017533772A Active JP6700284B2 (ja) | 2014-12-23 | 2015-12-23 | Ｃｆｔｒ活性を増加するための化合物、組成物及び方法 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US10392372B2 (enExample) |
| EP (1) | EP3237411B1 (enExample) |
| JP (1) | JP6700284B2 (enExample) |
| KR (1) | KR102677444B1 (enExample) |
| CN (1) | CN107207487B (enExample) |
| AU (3) | AU2015371294B2 (enExample) |
| BR (1) | BR112017013710B1 (enExample) |
| ES (1) | ES2962673T3 (enExample) |
| IL (2) | IL252987B (enExample) |
| MA (1) | MA41253A (enExample) |
| MX (1) | MX388421B (enExample) |
| NZ (1) | NZ732701A (enExample) |
| RU (1) | RU2767460C2 (enExample) |
| SA (1) | SA517381828B1 (enExample) |
| SG (1) | SG11201704859UA (enExample) |
| WO (1) | WO2016105485A2 (enExample) |
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| LT1993360T (lt) | 2005-12-28 | 2017-06-12 | Vertex Pharmaceuticals Incorporated | N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksochinolin-3-karboksamido kieta forma |
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| 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 |
| RU2745977C2 (ru) | 2010-04-22 | 2021-04-05 | Вертекс Фармасьютикалз Инкорпорейтед | Способ получения циклоалкилкарбоксамидо-индольных соединений |
| EP3116870A1 (en) | 2014-03-13 | 2017-01-18 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| EP3116501A1 (en) | 2014-03-13 | 2017-01-18 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| SG10201913575VA (en) | 2014-04-15 | 2020-02-27 | Vertex Pharma | Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases |
| CA2952862A1 (en) | 2014-06-19 | 2015-12-23 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
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| MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| US10344023B2 (en) | 2014-12-23 | 2019-07-09 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| 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 |
| US10392378B2 (en) | 2014-12-23 | 2019-08-27 | Proteostasis Therapeutics, Inc. | Derivatives of 5-phenyl- or 5-heteroarylathiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
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| NZ741093A (en) | 2015-10-06 | 2022-12-23 | Proteostasis Therapeutics Inc | Compounds, compositions, and methods for modulating cftr |
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| EP3436446B1 (en) | 2016-03-31 | 2023-06-07 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| BR112018070747B1 (pt) | 2016-04-07 | 2024-01-09 | Proteostasis Therapeutics, Inc | Átomos de silicone contendo análogos de ivacaftor, composições farmacêuticas e usos terapêuticos |
| EP3472156B1 (en) | 2016-06-21 | 2023-06-07 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| SG10201913595YA (en) | 2016-09-30 | 2020-02-27 | Vertex Pharma | Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| KR101912153B1 (ko) * | 2016-11-24 | 2018-10-26 | 이진호 | 극지항해용 자기 부상선 |
| MA49235B1 (fr) | 2016-12-09 | 2021-02-26 | Vertex Pharma | Modulateur de régulateur de conductance transmembranaire de fibrose kystique, compositions pharmaceutiques, procédés de traitement et procédé de fabrication du modulateur |
| EP3634402B1 (en) | 2017-06-08 | 2026-01-21 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| WO2019010092A1 (en) * | 2017-07-01 | 2019-01-10 | Vertex Pharmaceuticals Incorporated | COMPOSITIONS AND METHODS FOR TREATING CYSTIC FIBROSIS |
| BR112020000941A2 (pt) | 2017-07-17 | 2020-07-21 | Vertex Pharmaceuticals Incorporated | métodos de tratamento para fibrose cística |
| TWI799435B (zh) | 2017-08-02 | 2023-04-21 | 美商維泰克斯製藥公司 | 製備化合物之製程 |
| IL273831B2 (en) | 2017-10-19 | 2024-10-01 | Vertex Pharma | Crystalline forms and compositions of cftr modulators |
| CN111757874B (zh) | 2017-12-08 | 2024-03-08 | 弗特克斯药品有限公司 | 用于制备囊性纤维化跨膜传导调节因子的调节剂的方法 |
| 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 |
| CN108440455B (zh) * | 2018-04-11 | 2019-06-14 | 上海馨远医药科技有限公司 | 一种3-氧杂环丁烷羧酸的制备方法 |
| US11414439B2 (en) | 2018-04-13 | 2022-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| CA3102077A1 (en) * | 2018-05-31 | 2019-12-05 | Sanjeev AHUJA | Method of reducing pulmonary exacerbations in respiratory disease patients |
| GB201810071D0 (en) * | 2018-06-19 | 2018-08-08 | Univ Oslo Hf | Compounds |
| WO2020006269A1 (en) | 2018-06-27 | 2020-01-02 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| CN115427050B (zh) * | 2020-02-07 | 2025-02-14 | 南佛罗里达大学 | 对tau蛋白病中的β-抑制蛋白寡聚化的抑制 |
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| US12324802B2 (en) | 2020-11-18 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| AU2022222458A1 (en) * | 2021-02-19 | 2023-08-24 | Kalvista Pharmaceuticals Limited | Factor xiia inhibitors |
| JP2025506382A (ja) | 2022-02-03 | 2025-03-11 | バーテックス ファーマシューティカルズ インコーポレイテッド | 嚢胞性線維症の治療方法 |
| KR20240155228A (ko) | 2022-02-03 | 2024-10-28 | 버텍스 파마슈티칼스 인코포레이티드 | (6a,12a)-17-아미노-12-메틸-6,15-비스(트리플루오로메틸)-13,19-디옥사-3,4,18-트리아자트리시클로[12.3.1.12,5]노나데카-1(18),2,4,14,16-펜타엔-6-올의 결정질 형태를 제조하는 방법 |
| AU2023218262A1 (en) | 2022-02-08 | 2024-08-22 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| CA3253026A1 (en) | 2022-05-16 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | TREATMENT METHODS FOR CYSTIC FIBROSIS |
| TW202425990A (zh) * | 2022-11-02 | 2024-07-01 | 南韓商日東製藥股份有限公司 | 包含ｃｆｔｒ調節劑化合物之點眼用組成物 |
| CN120136817A (zh) * | 2025-05-16 | 2025-06-13 | 安徽泽升科技股份有限公司 | 一种氧杂环丁烷-3-甲醇和氧杂环丁烷-3-甲醛的制备方法 |
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| MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| US10344023B2 (en) | 2014-12-23 | 2019-07-09 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| US20180147187A1 (en) | 2015-01-12 | 2018-05-31 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| US10548878B2 (en) | 2015-07-24 | 2020-02-04 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods of increasing CFTR activity |
| WO2017040606A1 (en) | 2015-08-31 | 2017-03-09 | Proteostasis Therapeutics, Inc. | Isoxazole derivatives for use in the treatment of pulmonary diseases and disorders |
| NZ741093A (en) | 2015-10-06 | 2022-12-23 | Proteostasis Therapeutics Inc | Compounds, compositions, and methods for modulating cftr |
| EP3393465A1 (en) | 2015-12-22 | 2018-10-31 | Proteostasis Therapeutics, Inc. | Methods of treating pulmonary diseases and disorders |
| EP3472156B1 (en) | 2016-06-21 | 2023-06-07 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
-
2015
- 2015-12-22 MA MA041253A patent/MA41253A/fr unknown
- 2015-12-23 JP JP2017533772A patent/JP6700284B2/ja active Active
- 2015-12-23 EP EP15825647.9A patent/EP3237411B1/en active Active
- 2015-12-23 WO PCT/US2015/000212 patent/WO2016105485A2/en not_active Ceased
- 2015-12-23 ES ES15825647T patent/ES2962673T3/es active Active
- 2015-12-23 BR BR112017013710-0A patent/BR112017013710B1/pt active IP Right Grant
- 2015-12-23 SG SG11201704859UA patent/SG11201704859UA/en unknown
- 2015-12-23 CN CN201580074407.1A patent/CN107207487B/zh active Active
- 2015-12-23 KR KR1020177020139A patent/KR102677444B1/ko active Active
- 2015-12-23 US US15/539,392 patent/US10392372B2/en active Active
- 2015-12-23 AU AU2015371294A patent/AU2015371294B2/en active Active
- 2015-12-23 NZ NZ732701A patent/NZ732701A/en unknown
- 2015-12-23 MX MX2017008380A patent/MX388421B/es unknown
- 2015-12-23 RU RU2017126232A patent/RU2767460C2/ru active
-
2017
- 2017-06-18 IL IL252987A patent/IL252987B/en active IP Right Grant
- 2017-06-26 SA SA517381828A patent/SA517381828B1/ar unknown
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2019
- 2019-07-12 US US16/510,406 patent/US11098035B2/en active Active
-
2020
- 2020-08-02 IL IL276426A patent/IL276426A/en unknown
- 2020-10-12 AU AU2020256305A patent/AU2020256305A1/en not_active Abandoned
-
2022
- 2022-09-06 AU AU2022228100A patent/AU2022228100A1/en not_active Abandoned
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