CN113227087A - 大环化合物及其在治疗疾病中的用途 - Google Patents

大环化合物及其在治疗疾病中的用途 Download PDF

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Publication number
CN113227087A
CN113227087A CN201980083703.6A CN201980083703A CN113227087A CN 113227087 A CN113227087 A CN 113227087A CN 201980083703 A CN201980083703 A CN 201980083703A CN 113227087 A CN113227087 A CN 113227087A
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CN
China
Prior art keywords
thia
trifluoromethyl
diaza
dioxide
bipyridine
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Pending
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CN201980083703.6A
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English (en)
Chinese (zh)
Inventor
M·阿奇米奥拉
B·布尔苏拉亚
蒋松春
C·J·N·马蒂松
V·I·尼库林
T·N·源
B·奥克拉姆
S·帕特尔
D·P·菲利普斯
L·怀特黑德
吴报根
晏珊珊
朱雪峰
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Novartis AG
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Novartis AG
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Publication of CN113227087A publication Critical patent/CN113227087A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three 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
    • A61K31/435—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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D513/12—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 three hetero rings
    • C07D513/18—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, 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 three hetero rings
    • C07D515/18—Bridged systems

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  • 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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201980083703.6A 2018-12-21 2019-12-18 大环化合物及其在治疗疾病中的用途 Pending CN113227087A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862783270P 2018-12-21 2018-12-21
US62/783,270 2018-12-21
PCT/IB2019/061054 WO2020128925A1 (en) 2018-12-21 2019-12-18 Macrocyclic compounds and their use in the treatment of disease

Publications (1)

Publication Number Publication Date
CN113227087A true CN113227087A (zh) 2021-08-06

Family

ID=69165443

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980083703.6A Pending CN113227087A (zh) 2018-12-21 2019-12-18 大环化合物及其在治疗疾病中的用途

Country Status (10)

Country Link
US (1) US20220071971A1 (https=)
EP (1) EP3898621A1 (https=)
JP (1) JP2022513959A (https=)
KR (1) KR20210107046A (https=)
CN (1) CN113227087A (https=)
AU (1) AU2019404934B2 (https=)
BR (1) BR112021011643A2 (https=)
CA (1) CA3119656A1 (https=)
MX (1) MX2021007592A (https=)
WO (1) WO2020128925A1 (https=)

Families Citing this family (21)

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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
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
CA3150162A1 (en) 2019-08-14 2021-02-18 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
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
WO2022194399A1 (en) 2020-07-13 2022-09-22 Idorsia Pharmaceuticals Ltd Macrocycles as cftr modulators
CR20230120A (es) * 2020-08-07 2023-09-01 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
IL300413A (en) 2020-08-13 2023-04-01 Vertex Pharma Crystal forms of CFTR modulators
EP4225762A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225765A2 (en) * 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225447A1 (en) * 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
MX2023004074A (es) * 2020-10-07 2023-07-05 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica.
AU2021397294A1 (en) 2020-12-10 2023-07-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
EP4308575A1 (en) * 2021-03-16 2024-01-24 Idorsia Pharmaceuticals Ltd Macrocycles as cftr modulators
TWI904194B (zh) * 2021-07-12 2025-11-11 瑞士商愛杜西亞製藥有限公司 作為cftr調節劑之巨環
IL315715A (en) * 2022-04-06 2024-11-01 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulation
TW202421102A (zh) 2022-09-15 2024-06-01 瑞士商愛杜西亞製藥有限公司 巨環cftr調節劑與cftr校正子及/或cftr增效劑之組合
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
KR20250084132A (ko) 2022-09-15 2025-06-10 이도르시아 파마슈티컬스 리미티드 마크로시클릭 cftr 조절제
CN115498160B (zh) * 2022-09-29 2025-09-30 郑州大学 一种锂-有机硫电池正极材料及其制备方法和应用
WO2025186214A1 (en) 2024-03-05 2025-09-12 Idorsia Pharmaceuticals Ltd Macrocyclic cftr modulators

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015138934A1 (en) * 2014-03-13 2015-09-17 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
US20170101395A1 (en) * 2015-10-07 2017-04-13 NuBridge BioSciences Pyrimidine derivatives as cftr modulators
WO2018042316A1 (en) * 2016-08-29 2018-03-08 Novartis Ag N-(pyridin-2-yl)pyridine-sulfonamide derivatives and their use in the treatment of disease
WO2018148204A1 (en) * 2017-02-07 2018-08-16 Biogen Ma Inc. Ask1 inhibiting agents

Family Cites Families (2)

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US9617282B2 (en) * 2013-03-15 2017-04-11 Biogen Ma Inc. Macrocyclic compounds as IRAK4 inhibitors for the treatment of inflammatory diseases
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015138934A1 (en) * 2014-03-13 2015-09-17 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
US20170101395A1 (en) * 2015-10-07 2017-04-13 NuBridge BioSciences Pyrimidine derivatives as cftr modulators
WO2018042316A1 (en) * 2016-08-29 2018-03-08 Novartis Ag N-(pyridin-2-yl)pyridine-sulfonamide derivatives and their use in the treatment of disease
WO2018148204A1 (en) * 2017-02-07 2018-08-16 Biogen Ma Inc. Ask1 inhibiting agents

Non-Patent Citations (1)

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Title
PUAY-WAH PHUAN等: "Synergy-Based Small-Molecule Screen Using a Human Lung Epithelial Cell Line Yields DF508-CFTR Correctors That Augment VX-809 Maximal Efficacy", MOL PHARMACOL, vol. 88, 31 July 2014 (2014-07-31), pages 42 - 51 *

Also Published As

Publication number Publication date
AU2019404934A1 (en) 2021-06-03
BR112021011643A2 (pt) 2021-09-08
EP3898621A1 (en) 2021-10-27
WO2020128925A1 (en) 2020-06-25
JP2022513959A (ja) 2022-02-09
KR20210107046A (ko) 2021-08-31
US20220071971A1 (en) 2022-03-10
CA3119656A1 (en) 2020-06-25
AU2019404934B2 (en) 2022-04-21
MX2021007592A (es) 2021-08-11

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