JP2014515351A5 - - Google Patents
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- Publication number
- JP2014515351A5 JP2014515351A5 JP2014511524A JP2014511524A JP2014515351A5 JP 2014515351 A5 JP2014515351 A5 JP 2014515351A5 JP 2014511524 A JP2014511524 A JP 2014511524A JP 2014511524 A JP2014511524 A JP 2014511524A JP 2014515351 A5 JP2014515351 A5 JP 2014515351A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- deuterium
- pharmaceutically acceptable
- compound according
- same
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 33
- 229910052805 deuterium Inorganic materials 0.000 claims description 12
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 11
- 150000003839 salts Chemical class 0.000 claims description 8
- 230000000155 isotopic effect Effects 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- TVEXGJYMHHTVKP-UHFFFAOYSA-N 6-oxabicyclo[3.2.1]oct-3-en-7-one Chemical compound C1C2C(=O)OC1C=CC2 TVEXGJYMHHTVKP-UHFFFAOYSA-N 0.000 claims description 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- -1 deuterium compound Chemical class 0.000 claims 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161487497P | 2011-05-18 | 2011-05-18 | |
| US61/487,497 | 2011-05-18 | ||
| PCT/US2012/038297 WO2012158885A1 (en) | 2011-05-18 | 2012-05-17 | Deuterated derivatives of ivacaftor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016243941A Division JP2017078082A (ja) | 2011-05-18 | 2016-12-16 | 重水素化されたイバカフトルの誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014515351A JP2014515351A (ja) | 2014-06-30 |
| JP2014515351A5 true JP2014515351A5 (enExample) | 2015-07-02 |
| JP6063455B2 JP6063455B2 (ja) | 2017-01-18 |
Family
ID=46201810
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014511524A Active JP6063455B2 (ja) | 2011-05-18 | 2012-05-17 | 重水素化されたイバカフトルの誘導体 |
| JP2016243941A Pending JP2017078082A (ja) | 2011-05-18 | 2016-12-16 | 重水素化されたイバカフトルの誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016243941A Pending JP2017078082A (ja) | 2011-05-18 | 2016-12-16 | 重水素化されたイバカフトルの誘導体 |
Country Status (20)
| Country | Link |
|---|---|
| EP (2) | EP3235812B1 (enExample) |
| JP (2) | JP6063455B2 (enExample) |
| AU (5) | AU2012255711B2 (enExample) |
| BR (1) | BR112013029240B1 (enExample) |
| CA (1) | CA2834574C (enExample) |
| CY (2) | CY1119090T1 (enExample) |
| DK (2) | DK3235812T3 (enExample) |
| EA (1) | EA028378B1 (enExample) |
| ES (2) | ES2758028T3 (enExample) |
| HR (2) | HRP20170754T1 (enExample) |
| HU (1) | HUE032771T2 (enExample) |
| LT (1) | LT2709986T (enExample) |
| ME (2) | ME03652B (enExample) |
| MX (1) | MX349159B (enExample) |
| PL (2) | PL3235812T3 (enExample) |
| PT (2) | PT3235812T (enExample) |
| RS (2) | RS56096B1 (enExample) |
| SI (2) | SI3235812T1 (enExample) |
| SM (2) | SMT201900679T1 (enExample) |
| WO (1) | WO2012158885A1 (enExample) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US12458635B2 (en) | 2008-08-13 | 2025-11-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| HUE047354T2 (hu) | 2011-05-18 | 2020-04-28 | Vertex Pharmaceuticals Europe Ltd | Ivacaftor deuterizált származékai |
| ME03652B (me) * | 2011-05-18 | 2020-07-20 | Vertex Pharmaceuticals Europe Ltd | Deuterisani derivati ivakaftora |
| EP2819670B1 (en) | 2012-02-27 | 2026-05-20 | Vertex Pharmaceuticals Incorporated | Pharmaceutical Composition and Their Administration |
| WO2013151758A2 (en) | 2012-04-06 | 2013-10-10 | The Uab Research Foundation | Methods for increasing cftr activity |
| JP6146990B2 (ja) * | 2012-11-16 | 2017-06-14 | コンサート ファーマシューティカルズ インコーポレイテッド | 重水素化されたｃｆｔｒ増強物質 |
| WO2014078842A1 (en) * | 2012-11-19 | 2014-05-22 | Concert Pharmaceuticals, Inc. | Deuterated cftr potentiators |
| TW202140422A (zh) | 2014-10-06 | 2021-11-01 | 美商維泰克斯製藥公司 | 囊腫纖維化症跨膜傳導調節蛋白之調節劑 |
| CA2963945C (en) | 2014-10-07 | 2023-01-10 | Vertex Pharmaceuticals Incorporated | Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator |
| US10196384B2 (en) | 2015-03-31 | 2019-02-05 | Vertex Pharmaceuticals (Europe) Limited | Deuterated CFTR modulators |
| US10548878B2 (en) | 2015-07-24 | 2020-02-04 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods of increasing CFTR activity |
| HK1258472A1 (zh) * | 2015-09-21 | 2019-11-15 | Vertex Pharmaceuticals (Europe) Limited | 氘代cftr增效剂的施用 |
| HK1258473A1 (zh) * | 2015-09-25 | 2019-11-15 | Vertex Pharmaceuticals (Europe) Limited | 氘代cftr增效剂 |
| WO2017177124A1 (en) | 2016-04-07 | 2017-10-12 | Proteostasis Therapeutics, Inc. | Silicone atoms containing ivacaftor analogues |
| ES2954658T3 (es) | 2016-06-21 | 2023-11-23 | Proteostasis Therapeutics Inc | Compuestos, composiciones y procedimientos para aumentar la actividad de CFTR |
| EA202192783A1 (ru) | 2016-12-09 | 2022-02-24 | Вертекс Фармасьютикалз Инкорпорейтед | Модулятор регулятора трансмембранной проводимости при муковисцидозе, фармацевтические композиции, способы лечения и способ получения указанного модулятора |
| JP2017105824A (ja) * | 2017-02-10 | 2017-06-15 | コンサート ファーマシューティカルズ インコーポレイテッド | 重水素化されたｃｆｔｒ増強物質 |
| IL272032B2 (en) | 2017-07-17 | 2026-04-01 | Vertex Pharma | Combination therapy for the treatment of cystic fibrosis including N-(1,3-DIMETHYLPYRAZOL-4-YL)SULFONYL-6-[3-(3,3,3-TRIFLUORO-2,2- DIMETHYL-PROPOXY)PYRAZOL-1-YL]-2-[(4S)-2,2,4- TRIMETHYLPYRROLIDIN-1-YL]PYRIDINE-3-CARBOXAMIDE and |
| WO2019109021A1 (en) * | 2017-12-01 | 2019-06-06 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
| KR102716244B1 (ko) | 2017-12-08 | 2024-10-14 | 버텍스 파마슈티칼스 인코포레이티드 | 낭포성 섬유증 막횡단 전도 조절자의 조정제의 제조 방법 |
| JP6654223B2 (ja) * | 2018-08-13 | 2020-02-26 | バーテックス ファーマシューティカルズ （ヨーロッパ） リミテッド | 重水素化されたｃｆｔｒ増強物質 |
| MA54227B1 (fr) * | 2018-11-14 | 2023-03-31 | Vertex Pharma | Méthodes de traitement de la fibrose kystique |
| TWI848092B (zh) | 2019-04-03 | 2024-07-11 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白調節劑 |
| WO2020214921A1 (en) | 2019-04-17 | 2020-10-22 | Vertex Pharmaceuticals Incorporated | Solid forms of modulators of cftr |
| US11873300B2 (en) | 2019-08-14 | 2024-01-16 | Vertex Pharmaceuticals Incorporated | Crystalline forms of CFTR modulators |
| TWI899097B (zh) | 2019-08-14 | 2025-10-01 | 美商維泰克斯製藥公司 | 製備cftr調節劑之方法 |
| WO2021030556A1 (en) | 2019-08-14 | 2021-02-18 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| TWI867024B (zh) | 2019-08-14 | 2024-12-21 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白之調節劑 |
| LV15575A (lv) | 2019-12-20 | 2021-06-20 | Latvijas Organiskās Sintēzes Institūts | Selenofēnhromēnu deiterēti analogi, to iegūšana un izmantošana |
| CR20230120A (es) | 2020-08-07 | 2023-09-01 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| WO2022036060A1 (en) | 2020-08-13 | 2022-02-17 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
| EP3970718A1 (en) | 2020-09-18 | 2022-03-23 | Charité - Universitätsmedizin Berlin | New medical use of cystic fibrosis transmembrane conductance regulator (cftr) modulators |
| TW202233635A (zh) | 2020-10-07 | 2022-09-01 | 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 |
| WO2022076627A1 (en) | 2020-10-07 | 2022-04-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| US12612416B2 (en) | 2020-10-07 | 2026-04-28 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| US20230373974A1 (en) | 2020-10-07 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2022076620A1 (en) | 2020-10-07 | 2022-04-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2022076626A1 (en) | 2020-10-07 | 2022-04-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2022076628A1 (en) | 2020-10-07 | 2022-04-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| BR112023006470A2 (pt) | 2020-10-07 | 2023-09-26 | Vertex Pharma | Moduladores de regulador de condutância transmembrana de fibrose cística |
| US20230382924A1 (en) | 2020-10-07 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| MX2023004072A (es) | 2020-10-07 | 2023-07-05 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica. |
| US12324802B2 (en) | 2020-11-18 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| MX2023006770A (es) | 2020-12-10 | 2023-08-14 | Vertex Pharma | Metodos de tratamiento para fibrosis quistica. |
| US20250320226A1 (en) | 2022-02-03 | 2025-10-16 | 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 |
| CN119095597A (zh) | 2022-02-03 | 2024-12-06 | 弗特克斯药品有限公司 | 治疗囊性纤维化的方法 |
| CA3251045A1 (en) | 2022-02-08 | 2023-08-17 | Vertex Pharmaceuticals Incorporated | MODULATORS OF THE TRANSMEMBRANE CONDUCTANCE REGULATOR IN CYSTIC FIBROSIS |
| PE20250606A1 (es) | 2022-04-06 | 2025-02-26 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica |
| AU2023273614A1 (en) | 2022-05-16 | 2024-11-07 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| US20250340568A1 (en) | 2022-05-16 | 2025-11-06 | Vertex Pharmaceuticals Incorporated | Solid forms of a macrocyclic compounds as cftr modulators and their preparation |
| IL327468A (en) | 2023-10-04 | 2026-05-01 | Vertex Pharma | Solid forms of cystic fibrosis transmembrane conductance regulator |
| CN122374316A (zh) | 2023-10-04 | 2026-07-10 | 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 |
| WO2025166342A1 (en) | 2024-02-04 | 2025-08-07 | Vertex Pharmaceuticals Incorporated | Combination of vanzacaftor, tezacaftor, deutivacaftor for use in treating cystic fibrosis |
| ES3069804T3 (en) | 2024-02-07 | 2026-06-10 | Vertex Pharma | Compositions for the treatment of cftr-mediated diseases |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100477070B1 (ko) * | 1994-03-25 | 2006-04-21 | 이소테크니카 인코포레이티드 | 중수소화작용에의한의약품의효능강화법 |
| GB9925962D0 (en) | 1999-11-02 | 1999-12-29 | Novartis Ag | Organic compounds |
| CZ20033211A3 (cs) | 2001-05-03 | 2004-09-15 | F. Hoffmann-La Roche Ag | Farmaceutická léková forma amorfního nelfinavir mesylátu |
| CA2446904A1 (en) | 2001-05-24 | 2003-04-03 | Alexza Pharmaceuticals, Inc. | Delivery of drug esters through an inhalation route |
| CA2881078C (en) * | 2004-06-24 | 2018-10-02 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| WO2006039237A1 (en) | 2004-09-29 | 2006-04-13 | Cordis Corporation | Pharmaceutical dosage forms of stable amorphous rapamycin like compounds |
| AU2006331565A1 (en) | 2005-12-27 | 2007-07-05 | Vertex Pharmaceuticals Incorporated | Compounds useful in CFTR assays and methods therewith |
| 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 |
| ATE534383T1 (de) | 2006-05-12 | 2011-12-15 | Vertex Pharma | Zusammensetzungen aus n-ä2,4-bis(1,1- dimethylethyl)-5-hydroxyphenylü-1,4-dihydro-4- oxochinolin-3-carboxamid |
| JP5647519B2 (ja) * | 2007-09-13 | 2014-12-24 | コンサート ファーマシューティカルズ インコーポレイテッド | 重水素化カテコールおよびベンゾ［ｄ］［１，３］ジオキソールおよびその誘導体の合成 |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| RS56894B1 (sr) | 2008-08-13 | 2018-04-30 | Vertex Pharma | Farmaceutska kompozicija n-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksohinolin-3-karboksamida i njeno ordiniranje |
| AU2009288108B2 (en) * | 2008-09-03 | 2013-10-17 | Teva Pharmaceutical Industries, Ltd. | 2-oxo-1,2-dihydro-quinoline modulators of immune function |
| ME03652B (me) * | 2011-05-18 | 2020-07-20 | Vertex Pharmaceuticals Europe Ltd | Deuterisani derivati ivakaftora |
-
2012
- 2012-05-17 ME MEP-2019-325A patent/ME03652B/me unknown
- 2012-05-17 LT LTEP12725197.3T patent/LT2709986T/lt unknown
- 2012-05-17 SM SM20190679T patent/SMT201900679T1/it unknown
- 2012-05-17 PT PT171603863T patent/PT3235812T/pt unknown
- 2012-05-17 SM SM20170302T patent/SMT201700302T1/it unknown
- 2012-05-17 SI SI201231694T patent/SI3235812T1/sl unknown
- 2012-05-17 MX MX2013013450A patent/MX349159B/es active IP Right Grant
- 2012-05-17 EP EP17160386.3A patent/EP3235812B1/en active Active
- 2012-05-17 ME MEP-2017-112A patent/ME02749B/me unknown
- 2012-05-17 BR BR112013029240-7A patent/BR112013029240B1/pt active IP Right Grant
- 2012-05-17 EA EA201391615A patent/EA028378B1/ru unknown
- 2012-05-17 SI SI201230988A patent/SI2709986T1/sl unknown
- 2012-05-17 PT PT127251973T patent/PT2709986T/pt unknown
- 2012-05-17 HR HRP20170754TT patent/HRP20170754T1/hr unknown
- 2012-05-17 AU AU2012255711A patent/AU2012255711B2/en active Active
- 2012-05-17 PL PL17160386T patent/PL3235812T3/pl unknown
- 2012-05-17 WO PCT/US2012/038297 patent/WO2012158885A1/en not_active Ceased
- 2012-05-17 HU HUE12725197A patent/HUE032771T2/en unknown
- 2012-05-17 RS RS20170601A patent/RS56096B1/sr unknown
- 2012-05-17 JP JP2014511524A patent/JP6063455B2/ja active Active
- 2012-05-17 EP EP12725197.3A patent/EP2709986B1/en active Active
- 2012-05-17 RS RS20191494A patent/RS59744B1/sr unknown
- 2012-05-17 PL PL12725197T patent/PL2709986T3/pl unknown
- 2012-05-17 CA CA2834574A patent/CA2834574C/en active Active
- 2012-05-17 ES ES17160386T patent/ES2758028T3/es active Active
- 2012-05-17 DK DK17160386T patent/DK3235812T3/da active
- 2012-05-17 ES ES12725197.3T patent/ES2628465T3/es active Active
- 2012-05-17 DK DK12725197.3T patent/DK2709986T3/en active
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2016
- 2016-12-16 JP JP2016243941A patent/JP2017078082A/ja active Pending
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2017
- 2017-06-02 CY CY20171100584T patent/CY1119090T1/el unknown
- 2017-07-27 AU AU2017208313A patent/AU2017208313A1/en not_active Abandoned
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2019
- 2019-08-28 AU AU2019222862A patent/AU2019222862B2/en active Active
- 2019-11-25 HR HRP20192114TT patent/HRP20192114T1/hr unknown
- 2019-12-04 CY CY20191101275T patent/CY1122498T1/el unknown
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2021
- 2021-02-15 AU AU2021200970A patent/AU2021200970B2/en active Active
- 2021-06-08 AU AU2021203786A patent/AU2021203786B2/en active Active