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
- Authority
- 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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| DK3219705T3 (da) | 2005-12-28 | 2020-04-14 | Vertex Pharma | Farmaceutiske sammensætninger af den amorfe form af n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinolin-3-carboxamid |
| 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 |
| CN105130948A (zh) | 2010-04-22 | 2015-12-09 | 弗特克斯药品有限公司 | 制备环烷基甲酰胺基-吲哚化合物的方法 |
| CA2942387A1 (en) | 2014-03-13 | 2015-09-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr actvity |
| AU2015229188A1 (en) | 2014-03-13 | 2016-09-29 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing CFTR activity |
| JP6543268B2 (ja) | 2014-04-15 | 2019-07-10 | 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調節因子が媒介する疾患を処置するための医薬組成物 |
| EP3157917B1 (en) | 2014-06-19 | 2020-03-18 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| US9855249B2 (en) | 2014-10-02 | 2018-01-02 | Flatley Discovery Lab, Llc | Isoxazole compounds and methods for the treatment of cystic fibrosis |
| RS60906B1 (sr) | 2014-10-06 | 2020-11-30 | Vertex Pharma | Modulatori regulatora transmembranske provodljivosti za cističnu fibrozu |
| MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
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| WO2016105468A1 (en) | 2014-12-23 | 2016-06-30 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| WO2016105484A1 (en) | 2014-12-23 | 2016-06-30 | 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 |
| US10548878B2 (en) * | 2015-07-24 | 2020-02-04 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods of increasing CFTR activity |
| WO2017062581A1 (en) | 2015-10-06 | 2017-04-13 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating cftr |
| AU2016379388A1 (en) * | 2015-12-22 | 2018-07-12 | Proteostasis Therapeutics, Inc. | Methods of treating pulmonary diseases and disorders |
| ES2946970T3 (es) | 2016-03-31 | 2023-07-28 | Vertex Pharma | Regulador de conductancia transmembrana de moduladores de fibrosis quística |
| US10662207B2 (en) | 2016-04-07 | 2020-05-26 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating CFTR |
| US10899751B2 (en) | 2016-06-21 | 2021-01-26 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing CFTR activity |
| LT3519401T (lt) | 2016-09-30 | 2021-11-25 | Vertex Pharmaceuticals Incorporated | Cistinės fibrozės transmembraninio laidumo reguliavimo moduliatorius, farmacinės kompozicijos, gydymo būdai ir moduliatoriaus gamybos būdas |
| KR101912153B1 (ko) * | 2016-11-24 | 2018-10-26 | 이진호 | 극지항해용 자기 부상선 |
| PT3551622T (pt) | 2016-12-09 | 2020-11-12 | Vertex Pharma | Modulador do regulador da condutância transmembrana da fibrose quística, composições farmacêuticas, métodos de tratamento e processo de fabrico do modulador |
| US11253509B2 (en) | 2017-06-08 | 2022-02-22 | 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 |
| WO2019018395A1 (en) | 2017-07-17 | 2019-01-24 | Vertex Pharmaceuticals Incorporated | METHODS OF TREATING CYSTIC FIBROSIS |
| 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 |
| US10654829B2 (en) | 2017-10-19 | 2020-05-19 | Vertex Pharmaceuticals Incorporated | Crystalline forms and compositions of CFTR modulators |
| 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 |
| 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 |
| US10898484B2 (en) | 2018-05-31 | 2021-01-26 | Celltaxis, Llc | Method of reducing pulmonary exacerbations in respiratory disease patients |
| GB201810071D0 (en) * | 2018-06-19 | 2018-08-08 | Univ Oslo Hf | Compounds |
| EP3814336A1 (en) | 2018-06-27 | 2021-05-05 | 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 |
| EP4294798A1 (en) * | 2021-02-19 | 2023-12-27 | Kalvista Pharmaceuticals Limited | Factor xiia inhibitors |
| CN117751182A (zh) * | 2021-05-18 | 2024-03-22 | 南加利福尼亚大学 | 用于扩增人粒细胞-巨噬细胞祖细胞的方法及其应用 |
| IL314691A (en) | 2022-02-03 | 2024-10-01 | Vertex Pharma | PREPARATION METHODS AND CRYSTALLINE FORMS OF (6A,12A)-17-AMINO-12-METHYL-6,15-BIS(TRIFLUOROMETHYL)-13,19-DIOXA-3,4,18-TRIAZATRICYCLO[ 12.3.112.3.1. NONADECA-1(18),2,4,14,16-PENTAEN-6-OL |
| CA3249378A1 (en) | 2022-02-03 | 2023-08-10 | Vertex Pharmaceuticals Incorporated | TREATMENT METHODS 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 |
| CA3253026A1 (en) | 2022-05-16 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | TREATMENT METHODS FOR CYSTIC FIBROSIS |
| WO2024096629A1 (ko) * | 2022-11-02 | 2024-05-10 | 일동제약 주식회사 | Cftr 조절제 화합물을 포함하는 점안용 조성물 |
| 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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| WO2016105484A1 (en) | 2014-12-23 | 2016-06-30 | 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 |
| CA2971850A1 (en) | 2014-12-23 | 2016-06-30 | Proteostasis Therapeutics, Inc. | Derivatives of 5-phenyl- or 5-heteroarylthiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| WO2016105468A1 (en) | 2014-12-23 | 2016-06-30 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| 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 |
| WO2017062581A1 (en) | 2015-10-06 | 2017-04-13 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating cftr |
| AU2016379388A1 (en) | 2015-12-22 | 2018-07-12 | Proteostasis Therapeutics, Inc. | Methods of treating pulmonary diseases and disorders |
| US10899751B2 (en) | 2016-06-21 | 2021-01-26 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing CFTR activity |
-
2015
- 2015-12-22 MA MA041253A patent/MA41253A/fr unknown
- 2015-12-23 MX MX2017008380A patent/MX388421B/es unknown
- 2015-12-23 RU RU2017126232A patent/RU2767460C2/ru active
- 2015-12-23 JP JP2017533772A patent/JP6700284B2/ja active Active
- 2015-12-23 CN CN201580074407.1A patent/CN107207487B/zh active Active
- 2015-12-23 US US15/539,392 patent/US10392372B2/en active Active
- 2015-12-23 SG SG11201704859UA patent/SG11201704859UA/en unknown
- 2015-12-23 EP EP15825647.9A patent/EP3237411B1/en active Active
- 2015-12-23 NZ NZ732701A patent/NZ732701A/en unknown
- 2015-12-23 AU AU2015371294A patent/AU2015371294B2/en active Active
- 2015-12-23 BR BR112017013710-0A patent/BR112017013710B1/pt active IP Right Grant
- 2015-12-23 ES ES15825647T patent/ES2962673T3/es active Active
- 2015-12-23 KR KR1020177020139A patent/KR102677444B1/ko active Active
- 2015-12-23 WO PCT/US2015/000212 patent/WO2016105485A2/en not_active Ceased
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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
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2020
- 2020-08-02 IL IL276426A patent/IL276426A/en unknown
- 2020-10-12 AU AU2020256305A patent/AU2020256305A1/en not_active Abandoned
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2022
- 2022-09-06 AU AU2022228100A patent/AU2022228100A1/en not_active Abandoned
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