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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- 229960000502 poloxamer Drugs 0.000 description 1
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- 229940113124 polysorbate 60 Drugs 0.000 description 1
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- 229920000036 polyvinylpyrrolidone Polymers 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
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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
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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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (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
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201391615A EA028378B1 (ru) | 2011-05-18 | 2012-05-17 | Дейтерированные производные ивакафтора |
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|---|---|
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| 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) | PL2709986T3 (enExample) |
| PT (2) | PT3235812T (enExample) |
| RS (2) | RS56096B1 (enExample) |
| SI (2) | SI2709986T1 (enExample) |
| SM (2) | SMT201700302T1 (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 |
|---|---|---|---|---|
| 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 |
| US12458635B2 (en) | 2008-08-13 | 2025-11-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| DK3235812T3 (da) * | 2011-05-18 | 2019-11-25 | Vertex Pharmaceuticals Europe Ltd | Deutererede derivater af ivacaftor |
| HUE047354T2 (hu) | 2011-05-18 | 2020-04-28 | Vertex Pharmaceuticals Europe Ltd | Ivacaftor deuterizált származékai |
| JP2015511583A (ja) | 2012-02-27 | 2015-04-20 | 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 | 薬学的組成物およびその投与 |
| AU2013243857A1 (en) * | 2012-04-06 | 2014-10-16 | 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 |
| CN107250113B (zh) | 2014-10-07 | 2019-03-29 | 弗特克斯药品有限公司 | 囊性纤维化跨膜传导调节蛋白的调节剂的共晶 |
| HK1249893A1 (zh) | 2015-03-31 | 2018-11-16 | Vertex Pharmaceuticals (Europe) Limited | 氘代vx-661 |
| US10548878B2 (en) | 2015-07-24 | 2020-02-04 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods of increasing CFTR activity |
| US20180353500A1 (en) * | 2015-09-21 | 2018-12-13 | Vertex Pharmaceuticals (Europe) Limited | Administration of deuterated cftr potentiators |
| EP3352758A4 (en) * | 2015-09-25 | 2018-08-01 | Vertex Pharmaceuticals (Europe) Limited | Deuterated cftr potentiators |
| 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 |
| 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 |
| CN117924170A (zh) | 2017-12-01 | 2024-04-26 | 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 |
| 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 |
| 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 |
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| 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 |
| CR20240457A (es) | 2022-04-06 | 2024-12-11 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| CA3253026A1 (en) | 2022-05-16 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | TREATMENT METHODS 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 |
| WO2025076235A1 (en) | 2023-10-04 | 2025-04-10 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| IL327468A (en) | 2023-10-04 | 2026-05-01 | Vertex Pharmaceuticals Incorporated | Solid forms of cystic fibrosis transmembrane conductance regulator |
| WO2025166342A1 (en) | 2024-02-04 | 2025-08-07 | Vertex Pharmaceuticals Incorporated | Combination of vanzacaftor, tezacaftor, deutivacaftor for use in treating cystic fibrosis |
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| JP2005503425A (ja) | 2001-05-24 | 2005-02-03 | アレックザ モレキュラー デリヴァリー コーポレイション | 所定の吸入ルートによる薬剤エステルの送出 |
| US20060094744A1 (en) | 2004-09-29 | 2006-05-04 | Maryanoff Cynthia A | 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 |
| 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 |
| AU2007249269A1 (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 |
| 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 |
| KR20110042356A (ko) | 2008-08-13 | 2011-04-26 | 버텍스 파마슈티칼스 인코포레이티드 | 제약 조성물 및 그의 투여 |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| MX2011002033A (es) * | 2008-09-03 | 2011-05-02 | Teva Pharma | 2-oxo-1,2-dihidro-quinolinas moduladoras de la funcion inmune. |
| DK3235812T3 (da) * | 2011-05-18 | 2019-11-25 | Vertex Pharmaceuticals Europe Ltd | Deutererede derivater af ivacaftor |
-
2012
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- 2012-05-17 ME MEP-2019-325A patent/ME03652B/me unknown
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- 2012-05-17 EP EP17160386.3A patent/EP3235812B1/en active Active
- 2012-05-17 PL PL12725197T patent/PL2709986T3/pl unknown
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- 2012-05-17 DK DK12725197.3T patent/DK2709986T3/en active
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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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