CA3201793A1 - Macrocycles contenant un cycle 1,3,4-oxadiazole destines a etre utilises en tant que modulateurs du regulateur de la conductance transmembranaire de la fibrose kystique - Google Patents

Macrocycles contenant un cycle 1,3,4-oxadiazole destines a etre utilises en tant que modulateurs du regulateur de la conductance transmembranaire de la fibrose kystique

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Publication number
CA3201793A1
CA3201793A1 CA3201793A CA3201793A CA3201793A1 CA 3201793 A1 CA3201793 A1 CA 3201793A1 CA 3201793 A CA3201793 A CA 3201793A CA 3201793 A CA3201793 A CA 3201793A CA 3201793 A1 CA3201793 A1 CA 3201793A1
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CA
Canada
Prior art keywords
compound
independently selected
optionally substituted
pharmaceutically acceptable
therapeutic agent
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.)
Pending
Application number
CA3201793A
Other languages
English (en)
Inventor
Jeremy J. Clemens
William Schulz BECHARA
Brett C. Bookser
Thomas Cleveland
Timothy Coon
Michel Gallant
Julie LATERREUR
Mark Thomas Miller
Prasuna PARASELLI
Yeeman K. Ramtohul
Thumkunta Jagadeeswar Reddy
Claudio Sturino
Lino Valdez
Jinglan Zhou
Minson BAEK
Peter Diederik Jan Grootenhuis (Deceased)
Sara Sabina Hadida Ruah
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of CA3201793A1 publication Critical patent/CA3201793A1/fr
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/529Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La présente invention concerne des modulateurs du régulateur de la conductance transmembranaire de la fibrose kystique (CFTR), des compositions pharmaceutiques contenant au moins un tel modulateur, des méthodes de traitement de la fibrose kystique à l'aide de tels modulateurs et des compositions pharmaceutiques, et des procédés de fabrication de tels modulateurs.
CA3201793A 2020-11-18 2021-11-17 Macrocycles contenant un cycle 1,3,4-oxadiazole destines a etre utilises en tant que modulateurs du regulateur de la conductance transmembranaire de la fibrose kystique Pending CA3201793A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063115552P 2020-11-18 2020-11-18
US63/115,552 2020-11-18
PCT/US2021/072475 WO2022109573A1 (fr) 2020-11-18 2021-11-17 Macrocycles contenant un cycle 1,3,4-oxadiazole destinés à être utilisés en tant que modulateurs du régulateur de la conductance transmembranaire de la fibrose kystique

Publications (1)

Publication Number Publication Date
CA3201793A1 true CA3201793A1 (fr) 2022-05-27

Family

ID=79602287

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3201793A Pending CA3201793A1 (fr) 2020-11-18 2021-11-17 Macrocycles contenant un cycle 1,3,4-oxadiazole destines a etre utilises en tant que modulateurs du regulateur de la conductance transmembranaire de la fibrose kystique

Country Status (19)

Country Link
EP (1) EP4247817A1 (fr)
JP (1) JP2023549547A (fr)
KR (1) KR20230123522A (fr)
CN (1) CN116670140A (fr)
AR (1) AR124090A1 (fr)
AU (1) AU2021383176A1 (fr)
CA (1) CA3201793A1 (fr)
CL (1) CL2023001398A1 (fr)
CO (1) CO2023007896A2 (fr)
CR (1) CR20230260A (fr)
DO (1) DOP2023000099A (fr)
EC (1) ECSP23045439A (fr)
GE (1) GEAP202316271A (fr)
IL (1) IL302873A (fr)
JO (1) JOP20230105A1 (fr)
MX (1) MX2023005721A (fr)
PE (1) PE20231380A1 (fr)
WO (1) WO2022109573A1 (fr)
ZA (1) ZA202305296B (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024056791A1 (fr) * 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd Association de modulateurs de cftr macrocycliques avec des correcteurs de cftr et/ou des potentialisateurs de cftr

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20230120A (es) 2020-08-07 2023-09-01 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
US12324802B2 (en) 2020-11-18 2025-06-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
JP2025506382A (ja) * 2022-02-03 2025-03-11 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 嚢胞性線維症の治療方法
JP2025505643A (ja) * 2022-02-08 2025-02-28 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 嚢胞性線維症膜コンダクタンス制御因子の調節因子
WO2023224931A1 (fr) * 2022-05-16 2023-11-23 Vertex Pharmaceuticals Incorporated Méthodes de traitement de la fibrose kystique
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
WO2024054851A1 (fr) * 2022-09-07 2024-03-14 Sionna Therapeutics Composés macrocycliques, compositions et méthodes d'utilisation associées
CN119998297A (zh) 2022-09-15 2025-05-13 爱杜西亚药品有限公司 (3S,7S,10R,13R)-13-苄基-20-氟-7-异丁基-N-(2-(3-甲氧基-1,2,4-噁二唑-5-基)乙基)-6,9-二甲基-1,5,8,11-四氧代-10-(2,2,2-三氟乙基)-1,2,3,4,5,6,7,8,9,10,11,12,13,14-十四氢-[1]氧杂[4,7,10,14]四氮杂环十七烷并[16,17-f]喹啉-3-甲酰胺的晶型
WO2024056798A1 (fr) 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd Modulateurs du cftr macrocycliques
WO2025076235A1 (fr) 2023-10-04 2025-04-10 Vertex Pharmaceuticals Incorporated Modulateurs du régulateur de la conductance transmembranaire de la fibrose kystique
WO2025076240A1 (fr) 2023-10-04 2025-04-10 Vertex Pharmaceuticals Incorporated Formes solides de modulateurs du régulateur de la perméabilité transmembranaire de la fibrose kystique
WO2025186214A1 (fr) 2024-03-05 2025-09-12 Idorsia Pharmaceuticals Ltd Modulateurs de cftr macrocycliques

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103946221B (zh) * 2011-09-16 2016-08-03 诺华股份有限公司 用于治疗囊性纤维化的杂环化合物
CN109803962B (zh) * 2016-09-30 2022-04-29 弗特克斯药品有限公司 囊性纤维化跨膜传导调控蛋白的调节剂、以及药物组合物
MD3551622T2 (ro) * 2016-12-09 2021-03-31 Vertex Pharma Modulator al regulatorului conductanței transmembranare în fibroză chistică, compoziții farmaceutice, metode de tratament și procedeu pentru fabricarea modulatorului
TWI810243B (zh) * 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
JP7214743B2 (ja) * 2018-02-15 2023-01-30 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 嚢胞性線維症膜コンダクタンス制御因子のモジュレーターとしての大環状分子、それらの医薬組成物、嚢胞性線維症の治療におけるそれらの使用、及びそれらの製造方法
CN109134431B (zh) * 2018-10-10 2021-06-04 成都理工大学 作为囊性纤维化跨膜传导调节因子抑制剂的氨基咪唑偶联吡啶酮衍生物
UY38630A (es) * 2019-04-03 2020-10-30 Vertex Pharma Agentes moduladores del regulador de la conductancia transmembrana de la fibrosis quística

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024056791A1 (fr) * 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd Association de modulateurs de cftr macrocycliques avec des correcteurs de cftr et/ou des potentialisateurs de cftr

Also Published As

Publication number Publication date
CL2023001398A1 (es) 2023-11-24
EP4247817A1 (fr) 2023-09-27
CO2023007896A2 (es) 2023-09-18
ECSP23045439A (es) 2023-08-31
IL302873A (en) 2023-07-01
AR124090A1 (es) 2023-02-15
JP2023549547A (ja) 2023-11-27
MX2023005721A (es) 2023-07-25
DOP2023000099A (es) 2023-08-15
ZA202305296B (en) 2025-09-25
PE20231380A1 (es) 2023-09-07
JOP20230105A1 (ar) 2023-05-11
KR20230123522A (ko) 2023-08-23
GEAP202316271A (en) 2023-10-25
CN116670140A (zh) 2023-08-29
AU2021383176A1 (en) 2023-06-22
WO2022109573A1 (fr) 2022-05-27
CR20230260A (es) 2023-10-05

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