CN116670140A - 用作囊性纤维化跨膜转导调节因子的调节剂的含有1,3,4-噁二唑环的大环 - Google Patents

用作囊性纤维化跨膜转导调节因子的调节剂的含有1,3,4-噁二唑环的大环 Download PDF

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Publication number
CN116670140A
CN116670140A CN202180090910.1A CN202180090910A CN116670140A CN 116670140 A CN116670140 A CN 116670140A CN 202180090910 A CN202180090910 A CN 202180090910A CN 116670140 A CN116670140 A CN 116670140A
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compound
group
independently selected
therapeutic agents
pharmaceutically acceptable
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Chinese (zh)
Inventor
J·J·克莱门斯
W·S·贝查拉
B·C·布克赛尔
T·克里夫兰
T·库恩
M·加兰特
P·D·J·格罗滕豪斯
S·S·哈迪达鲁阿
J·拉特鲁尔
M·T·米勒
P·帕拉赛利
Y·K·拉姆托胡尔
T·J·雷迪
C·斯图里诺
L·瓦尔德兹
J·周
M·拜克
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication of CN116670140A publication Critical patent/CN116670140A/zh
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (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)
CN202180090910.1A 2020-11-18 2021-11-17 用作囊性纤维化跨膜转导调节因子的调节剂的含有1,3,4-噁二唑环的大环 Pending CN116670140A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063115552P 2020-11-18 2020-11-18
US63/115552 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
CN116670140A true CN116670140A (zh) 2023-08-29

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CN202180090910.1A Pending CN116670140A (zh) 2020-11-18 2021-11-17 用作囊性纤维化跨膜转导调节因子的调节剂的含有1,3,4-噁二唑环的大环

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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)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021113808A1 (en) 2019-12-05 2021-06-10 Genzyme Corporation Cftr-modulating arylamides
WO2021113806A1 (en) 2019-12-05 2021-06-10 Genzyme Corporation Arylamides and methods of use thereof
WO2021113809A1 (en) 2019-12-05 2021-06-10 Genzyme Corporation Arylamides and methods of use thereof
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
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
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
WO2024054851A1 (en) * 2022-09-07 2024-03-14 Sionna Therapeutics Macrocyclic compounds, compositions and methods of using thereof
IL319374A (en) 2022-09-07 2025-05-01 Sionna Therapeutics Inc Macrocyclic compounds, compositions and methods of using them
WO2024056798A1 (en) 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd Macrocyclic cftr modulators
CN119907667A (zh) * 2022-09-15 2025-04-29 爱杜西亚药品有限公司 大环cftr调节剂与cftr校正剂和/或cftr增效剂的组合
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
IL327468A (en) 2023-10-04 2026-05-01 Vertex Pharma Solid forms of cystic fibrosis transmembrane conductance regulator
CN122374316A (zh) 2023-10-04 2026-07-10 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
WO2025186214A1 (en) 2024-03-05 2025-09-12 Idorsia Pharmaceuticals Ltd Macrocyclic cftr modulators

Citations (5)

* 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
CN109134431A (zh) * 2018-10-10 2019-01-04 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
WO2019161078A1 (en) * 2018-02-15 2019-08-22 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cycstic fibrosis, and process for making them
CN110267948A (zh) * 2016-12-09 2019-09-20 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
CN111818918A (zh) * 2018-02-05 2020-10-23 弗特克斯药品有限公司 用于治疗囊性纤维化的药物组合物

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GEP20217329B (en) * 2016-09-30 2021-12-10 Vertex Pharma Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
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

Patent Citations (5)

* 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
CN110267948A (zh) * 2016-12-09 2019-09-20 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
CN111818918A (zh) * 2018-02-05 2020-10-23 弗特克斯药品有限公司 用于治疗囊性纤维化的药物组合物
WO2019161078A1 (en) * 2018-02-15 2019-08-22 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cycstic fibrosis, and process for making them
CN109134431A (zh) * 2018-10-10 2019-01-04 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

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CR20230260A (es) 2023-10-05
JP2023549547A (ja) 2023-11-27
ECSP23045439A (es) 2023-08-31
GEAP202316271A (en) 2023-10-25
JOP20230105A1 (ar) 2023-05-11
ZA202305296B (en) 2025-09-25
CL2023001398A1 (es) 2023-11-24
MX2023005721A (es) 2023-07-25
PE20231380A1 (es) 2023-09-07
EP4247817A1 (en) 2023-09-27
DOP2023000099A (es) 2023-08-15
IL302873A (en) 2023-07-01
AU2021383176A1 (en) 2023-06-22
CA3201793A1 (en) 2022-05-27
WO2022109573A1 (en) 2022-05-27
AR124090A1 (es) 2023-02-15
KR20230123522A (ko) 2023-08-23
CO2023007896A2 (es) 2023-09-18

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