JP6063455B2 - 重水素化されたイバカフトルの誘導体 - Google Patents

重水素化されたイバカフトルの誘導体 Download PDF

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Publication number
JP6063455B2
JP6063455B2 JP2014511524A JP2014511524A JP6063455B2 JP 6063455 B2 JP6063455 B2 JP 6063455B2 JP 2014511524 A JP2014511524 A JP 2014511524A JP 2014511524 A JP2014511524 A JP 2014511524A JP 6063455 B2 JP6063455 B2 JP 6063455B2
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compound
pharmaceutically acceptable
deuterium
acceptable salt
acid
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JP2014515351A5 (enExample
JP2014515351A (ja
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アダム ジェイ． モーガン
アダム ジェイ． モーガン
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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
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
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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
    • 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

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  • 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)
JP2014511524A 2011-05-18 2012-05-17 重水素化されたイバカフトルの誘導体 Active JP6063455B2 (ja)

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 JP2014515351A5 (enExample) 2015-07-02
JP6063455B2 true JP6063455B2 (ja) 2017-01-18

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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)

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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

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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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017078082A (ja) * 2011-05-18 2017-04-27 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 重水素化されたイバカフトルの誘導体

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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
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
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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
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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
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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
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Publication number Priority date Publication date Assignee Title
JP2017078082A (ja) * 2011-05-18 2017-04-27 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 重水素化されたイバカフトルの誘導体

Also Published As

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AU2019222862B2 (en) 2021-03-11
RS59744B1 (sr) 2020-02-28
DK2709986T3 (en) 2017-05-08
ES2628465T3 (es) 2017-08-02
EP3235812B1 (en) 2019-09-04
MX2013013450A (es) 2014-02-27
SI2709986T1 (sl) 2017-07-31
EP2709986A1 (en) 2014-03-26
ES2758028T3 (es) 2020-05-04
AU2012255711B2 (en) 2017-05-04
HUE032771T2 (en) 2017-10-30
CY1122498T1 (el) 2021-01-27
BR112013029240B1 (pt) 2023-05-16
AU2019222862A1 (en) 2019-09-19
CA2834574C (en) 2019-09-17
PL2709986T3 (pl) 2017-09-29
JP2017078082A (ja) 2017-04-27
CY1119090T1 (el) 2018-01-10
ME03652B (me) 2020-07-20
SMT201700302T1 (it) 2017-07-18
HRP20192114T1 (hr) 2020-02-21
WO2012158885A1 (en) 2012-11-22
BR112013029240A2 (pt) 2017-01-31
HRP20170754T1 (hr) 2017-07-28
DK3235812T3 (da) 2019-11-25
AU2021200970A1 (en) 2021-03-11
HK1244183A1 (en) 2018-08-03
CA2834574A1 (en) 2012-11-22
EP2709986B1 (en) 2017-03-22
EA028378B1 (ru) 2017-11-30
SMT201900679T1 (it) 2020-01-14
PT2709986T (pt) 2017-06-26
SI3235812T1 (sl) 2020-02-28
AU2021200970B2 (en) 2022-07-14
MX349159B (es) 2017-07-14
JP2014515351A (ja) 2014-06-30
AU2021203786B2 (en) 2023-03-16
PL3235812T3 (pl) 2020-04-30
AU2017208313A1 (en) 2017-08-17
AU2021203786A1 (en) 2021-07-08
EA201391615A1 (ru) 2014-03-31
ME02749B (me) 2018-01-20
PT3235812T (pt) 2019-12-09
LT2709986T (lt) 2017-05-25
RS56096B1 (sr) 2017-10-31
EP3235812A1 (en) 2017-10-25

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