EA028378B1 - Дейтерированные производные ивакафтора - Google Patents
Дейтерированные производные ивакафтора Download PDFInfo
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- EA028378B1 EA028378B1 EA201391615A EA201391615A EA028378B1 EA 028378 B1 EA028378 B1 EA 028378B1 EA 201391615 A EA201391615 A EA 201391615A EA 201391615 A EA201391615 A EA 201391615A EA 028378 B1 EA028378 B1 EA 028378B1
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- Eurasian Patent Office
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- 229950009215 phenylbutanoic acid Drugs 0.000 description 1
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- 231100000614 poison Toxicity 0.000 description 1
- 229960000502 poloxamer Drugs 0.000 description 1
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- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
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- 229920001155 polypropylene Polymers 0.000 description 1
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- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000004302 potassium sorbate Substances 0.000 description 1
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- 229940069338 potassium sorbate Drugs 0.000 description 1
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- 239000003755 preservative agent Substances 0.000 description 1
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- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- KCXFHTAICRTXLI-UHFFFAOYSA-N propane-1-sulfonic acid Chemical compound CCCS(O)(=O)=O KCXFHTAICRTXLI-UHFFFAOYSA-N 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 229950008679 protamine sulfate Drugs 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
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- 229960004889 salicylic acid Drugs 0.000 description 1
- 229940116351 sebacate Drugs 0.000 description 1
- CXMXRPHRNRROMY-UHFFFAOYSA-L sebacate(2-) Chemical compound [O-]C(=O)CCCCCCCCC([O-])=O CXMXRPHRNRROMY-UHFFFAOYSA-L 0.000 description 1
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- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 230000003381 solubilizing effect Effects 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
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- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
- C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/12—Mucolytics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Quinoline Compounds (AREA)
- Saccharide Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161487497P | 2011-05-18 | 2011-05-18 | |
| PCT/US2012/038297 WO2012158885A1 (en) | 2011-05-18 | 2012-05-17 | Deuterated derivatives of ivacaftor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201391615A1 EA201391615A1 (ru) | 2014-03-31 |
| EA028378B1 true EA028378B1 (ru) | 2017-11-30 |
Family
ID=46201810
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201391615A EA028378B1 (ru) | 2011-05-18 | 2012-05-17 | Дейтерированные производные ивакафтора |
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) |
Cited By (4)
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|---|---|---|---|---|
| US12168009B2 (en) | 2014-10-06 | 2024-12-17 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| US12350262B2 (en) | 2017-07-17 | 2025-07-08 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| US12384762B2 (en) | 2016-12-09 | 2025-08-12 | Vertex Pharmaceuticals Incorporated | Modulator of the Cystic Fibrosis Transmembrane Conductance Regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| US12415798B2 (en) | 2017-12-08 | 2025-09-16 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
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| 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 |
| 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 |
| 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 |
| WO2019109021A1 (en) * | 2017-12-01 | 2019-06-06 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
| 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 |
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| US12612416B2 (en) | 2020-10-07 | 2026-04-28 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
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| 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 |
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| 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 |
| 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
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12168009B2 (en) | 2014-10-06 | 2024-12-17 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| US12384762B2 (en) | 2016-12-09 | 2025-08-12 | Vertex Pharmaceuticals Incorporated | Modulator of the Cystic Fibrosis Transmembrane Conductance Regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| US12350262B2 (en) | 2017-07-17 | 2025-07-08 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| US12415798B2 (en) | 2017-12-08 | 2025-09-16 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
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