CA3201793A1 - Macrocycles containing a 1,3,4-oxadiazole ring for use as modulators of cystic fibrosis transmembrane conductance regulator - Google Patents

Macrocycles containing a 1,3,4-oxadiazole ring for use as modulators of cystic fibrosis transmembrane conductance regulator

Info

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
Authority
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)
French (fr)
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/en
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/439—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/22—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
CA3201793A 2020-11-18 2021-11-17 Macrocycles containing a 1,3,4-oxadiazole ring for use as modulators of cystic fibrosis transmembrane conductance regulator Pending CA3201793A1 (en)

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 (en) 2020-11-18 2021-11-17 Macrocycles containing a 1,3,4-oxadiazole ring for use as modulators of cystic fibrosis transmembrane conductance regulator

Publications (1)

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

Family

ID=79602287

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3201793A Pending CA3201793A1 (en) 2020-11-18 2021-11-17 Macrocycles containing a 1,3,4-oxadiazole ring for use as modulators of cystic fibrosis transmembrane conductance regulator

Country Status (19)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024056791A1 (en) * 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd Combination of macrocyclic cftr modulators with cftr correctors and / or cftr potentiators

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
IL314449A (en) * 2022-02-03 2024-09-01 Vertex Pharma Methods of treatment for cystic fibrosis
WO2023154291A1 (en) * 2022-02-08 2023-08-17 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4525858A1 (en) * 2022-05-16 2025-03-26 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
CA3253977A1 (en) 2022-05-16 2023-11-23 Vertex Pharmaceuticals Incorporated SOLID FORMS OF MACROCYCLIC COMPOUNDS AS CFTR MODULATORS AND THEIR PREPARATION
WO2024054851A1 (en) * 2022-09-07 2024-03-14 Sionna Therapeutics Macrocyclic compounds, compositions and methods of using thereof
KR20250084132A (ko) 2022-09-15 2025-06-10 이도르시아 파마슈티컬스 리미티드 마크로시클릭 cftr 조절제
CA3267791A1 (en) 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd CRYSTALLINE FORM OF (3S,7S,10R,13R)-13-BENZYL-20-FLUORO-7-ISOBUTYL-N-(2-(3-METHOXY-1,2,4-OXADIAZOL-5-YL)ETHYL)-6,9-DIMETHYL-1,5,8,11-TETRAOXO-10-(2,2,2-TRIFLUOROETHYL)-1,2,3,4,5,6,7,8,9,10,11,12,13,14-TETRADECAHYDRO-[1]OXA[4,7,10,14]TETRAAZACYCLOHEPTADECINO [16,17-F]QUINOLINE-3-CARBOXAMIDE
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
WO2025186214A1 (en) 2024-03-05 2025-09-12 Idorsia Pharmaceuticals Ltd Macrocyclic cftr modulators

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013038386A1 (en) * 2011-09-16 2013-03-21 Novartis Ag Heterocyclic compounds for the treatment of cystic fibrosis
SI3519401T1 (sl) * 2016-09-30 2022-01-31 Vertex Pharmaceuticals Incorporated Modulator regulatorja transmembranske prevodnosti pri cistični fibrozi, farmacevtski sestavki, postopki zdravljenja in proces za izdelavo modulatorja
CN110267948B (zh) * 2016-12-09 2023-12-08 弗特克斯药品有限公司 囊性纤维化跨膜传导调控剂的调节剂、药物组合物、治疗方法和制备所述调节剂的方法
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
AU2019222758B2 (en) * 2018-02-15 2022-07-07 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cystic fibrosis, and process for making them
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
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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024056791A1 (en) * 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd Combination of macrocyclic cftr modulators with cftr correctors and / or cftr potentiators

Also Published As

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

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