ES2758028T3 - Derivados deuterados de ivacaftor - Google Patents
Derivados deuterados de ivacaftor Download PDFInfo
- Publication number
- ES2758028T3 ES2758028T3 ES17160386T ES17160386T ES2758028T3 ES 2758028 T3 ES2758028 T3 ES 2758028T3 ES 17160386 T ES17160386 T ES 17160386T ES 17160386 T ES17160386 T ES 17160386T ES 2758028 T3 ES2758028 T3 ES 2758028T3
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- Prior art keywords
- compound
- pharmaceutical composition
- deuterium
- formula
- pharmaceutically acceptable
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- PURKAOJPTOLRMP-UHFFFAOYSA-N ivacaftor Chemical class C1=C(O)C(C(C)(C)C)=CC(C(C)(C)C)=C1NC(=O)C1=CNC2=CC=CC=C2C1=O PURKAOJPTOLRMP-UHFFFAOYSA-N 0.000 title description 18
- 150000001875 compounds Chemical class 0.000 claims abstract description 124
- 229910052805 deuterium Inorganic materials 0.000 claims abstract description 54
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims abstract description 47
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 35
- 150000003839 salts Chemical class 0.000 claims abstract description 25
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- 239000001257 hydrogen Substances 0.000 claims abstract description 17
- 125000004429 atom Chemical group 0.000 claims abstract description 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract description 11
- 150000001975 deuterium Chemical group 0.000 claims abstract description 8
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Classifications
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- 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
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- 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
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- 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)
- Thiazole And Isothizaole Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
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| CA2635581C (en) | 2005-12-28 | 2017-02-28 | Vertex Pharmaceuticals Incorporated | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| US12458635B2 (en) | 2008-08-13 | 2025-11-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| ES2758028T3 (es) * | 2011-05-18 | 2020-05-04 | Vertex Pharmaceuticals Europe Ltd | Derivados deuterados de ivacaftor |
| HUE047354T2 (hu) | 2011-05-18 | 2020-04-28 | Vertex Pharmaceuticals Europe Ltd | Ivacaftor deuterizált származékai |
| AU2013226076B2 (en) | 2012-02-27 | 2017-11-16 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administration thereof |
| JP6525203B2 (ja) | 2012-04-06 | 2019-06-05 | ザ ユーエイビー リサーチ ファウンデーションＴｈｅ ＵＡＢ Ｒｅｓｅａｒｃｈ Ｆｏｕｎｄａｔｉｏｎ | Ｃｆｔｒ活性を増大させるための方法 |
| 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 |
| IL313498A (en) | 2014-10-06 | 2024-08-01 | Vertex Pharma | Modulators of the cystic fibrosis transmembrane conductance regulator |
| KR20170063954A (ko) | 2014-10-07 | 2017-06-08 | 버텍스 파마슈티칼스 인코포레이티드 | 낭성 섬유증 막횡단 전도도 조절자의 조정제의 공-결정 |
| AU2016243171B2 (en) | 2015-03-31 | 2020-10-08 | Concert Pharmaceuticals, Inc. | Deuterated VX-661 |
| AU2016297886B2 (en) | 2015-07-24 | 2020-12-10 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing CFTR activity |
| MX388470B (es) * | 2015-09-21 | 2025-03-20 | Vertex Pharmaceuticals Europe Ltd | Administración de potenciadores de regulador de la conductancia transmembrana de fibrosis quística (cftr) deuterados. |
| HK1258473A1 (zh) | 2015-09-25 | 2019-11-15 | Vertex Pharmaceuticals (Europe) Limited | 氘代cftr增效剂 |
| CN109563047A (zh) * | 2016-04-07 | 2019-04-02 | 蛋白质平衡治疗股份有限公司 | 含有硅原子的依伐卡托类似物 |
| ES2954658T3 (es) | 2016-06-21 | 2023-11-23 | Proteostasis Therapeutics Inc | Compuestos, composiciones y procedimientos para aumentar la actividad de CFTR |
| MX2021013639A (es) | 2016-12-09 | 2022-09-30 | Vertex Pharma | Forma cristalina del compuesto 1, un modulador del regulador de conductancia transmembrana de fibrosis quística, procesos para su preparación, composiciones farmacéuticas del compuesto 1, y su uso en el tratamiento de fibrosis quística. |
| 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 |
| AU2018304168B2 (en) | 2017-07-17 | 2023-05-04 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| IL305169B2 (en) | 2017-12-01 | 2025-07-01 | Vertex Pharma | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
| US11465985B2 (en) | 2017-12-08 | 2022-10-11 | 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 |
| UY38630A (es) | 2019-04-03 | 2020-10-30 | Vertex Pharma | Agentes moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| WO2020214921A1 (en) | 2019-04-17 | 2020-10-22 | Vertex Pharmaceuticals Incorporated | Solid forms of modulators of cftr |
| 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 |
| EP4013760A1 (en) | 2019-08-14 | 2022-06-22 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
| US11584761B2 (en) | 2019-08-14 | 2023-02-21 | Vertex Pharmaceuticals Incorporated | Process of making CFTR modulators |
| MX2022001827A (es) | 2019-08-14 | 2022-06-09 | Vertex Pharma | Moduladores del regulador de conductancia transmembrana de la fibrosis quistica. |
| 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 |
| US20230303589A1 (en) | 2020-08-13 | 2023-09-28 | 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 |
| EP4225765A2 (en) | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP4225737A1 (en) | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| US20230382924A1 (en) | 2020-10-07 | 2023-11-30 | 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 |
| EP4225764A1 (en) | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| AU2021356651A1 (en) | 2020-10-07 | 2023-05-18 | 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 |
| EP4225761A1 (en) | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP4225762A1 (en) | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| US20230373935A1 (en) | 2020-10-07 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| US12324802B2 (en) | 2020-11-18 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| AU2021397294A1 (en) | 2020-12-10 | 2023-07-06 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| 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 |
| IL314449A (en) | 2022-02-03 | 2024-09-01 | Vertex Pharma | Methods of treatment 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 |
| GEAP202516620A (en) | 2022-04-06 | 2025-04-10 | Vertex Pharma | Modulators of cystic fibrosis transmembrane conductance regulator |
| CN119947720A (zh) | 2022-05-16 | 2025-05-06 | 弗特克斯药品有限公司 | 治疗囊性纤维化的方法 |
| JP2025517323A (ja) | 2022-05-16 | 2025-06-05 | 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 | Ｃｆｔｒモジュレーターとしての大環状化合物の固体形態及びその調製 |
| WO2025076235A1 (en) | 2023-10-04 | 2025-04-10 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2025076240A1 (en) | 2023-10-04 | 2025-04-10 | Vertex Pharmaceuticals Incorporated | Solid forms of modulators 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 |
| EP4648753A1 (en) | 2024-02-07 | 2025-11-19 | Vertex Pharmaceuticals Incorporated | Compositions for the treatment of cftr-mediated diseases |
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| CA2186371A1 (en) * | 1994-03-25 | 1995-10-05 | Robert T. Foster | Enhancement of the efficacy of dihydropyridines by deuteration |
| GB9925962D0 (en) | 1999-11-02 | 1999-12-29 | Novartis Ag | Organic compounds |
| BR0209325A (pt) | 2001-05-03 | 2004-07-20 | Hoffmann La Roche | Forma de dosagem farmacêutica de mesilato de nelfinavir amorfo |
| EP1392262A1 (en) | 2001-05-24 | 2004-03-03 | Alexza Molecular Delivery Corporation | Delivery of drug esters through an inhalation route |
| NZ587549A (en) * | 2004-06-24 | 2012-10-26 | Vertex Pharma | 6-Amino-indole derivatives and processes for their preparation |
| CA2581169A1 (en) | 2004-09-29 | 2006-04-13 | Cordis Corporation | Pharmaceutical dosage forms of stable amorphous rapamycin like compounds |
| EP1974212A1 (en) | 2005-12-27 | 2008-10-01 | Vertex Pharmaceuticals Incorporated | Compounds useful in cftr assays and methods therewith |
| CA2635581C (en) | 2005-12-28 | 2017-02-28 | Vertex Pharmaceuticals Incorporated | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| JP2009536969A (ja) | 2006-05-12 | 2009-10-22 | 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 | Ｎ−［２，４−ビス（１，１−ジメチルエチル）−５−ヒドロキシフェニル］−１，４−ジヒドロ−４−オキソキノリン−３−カルボキサミド組成物 |
| 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 |
| ES2660143T3 (es) | 2008-08-13 | 2018-03-21 | Vertex Pharmaceuticals Incorporated | Composición farmacéutica de N-[2,4-Bis(1,1-dimetiletilo)-5-hidroxifenilo]-1,4-dihidro-4-oxoquinolina-3carboxamida y administración de la misma |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| JP2012502038A (ja) * | 2008-09-03 | 2012-01-26 | テバ ファーマシューティカル インダストリーズ リミティド | 免疫機能の２−オキソ−１，２−ジヒドロ−キノリンモジュレーター |
| ES2758028T3 (es) * | 2011-05-18 | 2020-05-04 | Vertex Pharmaceuticals Europe Ltd | Derivados deuterados de ivacaftor |
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