CN112955451A - 作为jak抑制剂的2-氮杂双环已烷化合物 - Google Patents

作为jak抑制剂的2-氮杂双环已烷化合物 Download PDF

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Publication number
CN112955451A
CN112955451A CN201980070126.7A CN201980070126A CN112955451A CN 112955451 A CN112955451 A CN 112955451A CN 201980070126 A CN201980070126 A CN 201980070126A CN 112955451 A CN112955451 A CN 112955451A
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CN
China
Prior art keywords
compound
pharmaceutically acceptable
inhibitors
eye
disease
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Pending
Application number
CN201980070126.7A
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English (en)
Chinese (zh)
Inventor
P·R·法特里
姜岚
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.)
Theravance Biopharma R&D IP LLC
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Theravance Biopharma R&D IP LLC
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Application filed by Theravance Biopharma R&D IP LLC filed Critical Theravance Biopharma R&D IP LLC
Publication of CN112955451A publication Critical patent/CN112955451A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
CN201980070126.7A 2018-10-29 2019-10-18 作为jak抑制剂的2-氮杂双环已烷化合物 Pending CN112955451A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862751967P 2018-10-29 2018-10-29
US62/751,967 2018-10-29
PCT/US2019/056947 WO2020092019A1 (en) 2018-10-29 2019-10-18 2-azabicyclo hexane compound as jak inhibitor

Publications (1)

Publication Number Publication Date
CN112955451A true CN112955451A (zh) 2021-06-11

Family

ID=68542755

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980070126.7A Pending CN112955451A (zh) 2018-10-29 2019-10-18 作为jak抑制剂的2-氮杂双环已烷化合物

Country Status (12)

Country Link
US (2) US10968222B2 (https=)
EP (1) EP3853229A1 (https=)
JP (1) JP2022506111A (https=)
KR (1) KR20210084512A (https=)
CN (1) CN112955451A (https=)
AU (1) AU2019373059A1 (https=)
BR (1) BR112021007788A8 (https=)
CA (1) CA3113667A1 (https=)
IL (1) IL282460A (https=)
MX (1) MX2021004582A (https=)
SG (1) SG11202103042XA (https=)
WO (1) WO2020092019A1 (https=)

Cited By (1)

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CN114181055A (zh) * 2021-12-21 2022-03-15 苏州楚凯药业有限公司 1-苄氧基-4-溴-5-乙基-2-氟苯的制备方法

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US10029013B2 (en) 2009-10-02 2018-07-24 Foamix Pharmaceuticals Ltd. Surfactant-free, water-free formable composition and breakable foams and their uses
HK1252685A1 (zh) 2015-11-03 2019-05-31 Theravance Biopharma R&D Ip, Llc 用於治疗呼吸疾病的jak激酶抑制剂化合物
MX377365B (es) 2016-09-08 2025-03-10 Journey Medical Corp Composiciones y métodos para tratar rosácea y acné.
PT3837258T (pt) 2018-09-04 2024-06-20 Theravance Biopharma R&D Ip Llc Amidas de dimetil amino azetidina como inibidores de jak
WO2020051139A1 (en) 2018-09-04 2020-03-12 Theravance Biopharma R&D Ip, Llc 5 to 7 membered heterocyclic amides as jak inhibitors
CA3108848A1 (en) 2018-09-04 2020-03-12 Theravance Biopharma R&D Ip, Llc Process for preparing jak inhibitors and intermediates thereof
TW202144343A (zh) 2020-03-02 2021-12-01 美商施萬生物製藥研發 Ip有限責任公司 Jak抑制劑化合物之結晶水合物
CN111620868B (zh) * 2020-05-28 2021-08-31 爱斯特（成都）生物制药股份有限公司 一种1H-吡唑并[3,4-b]吡啶-3-甲醛的制备方法
CN111973599A (zh) * 2020-08-07 2020-11-24 杭州邦顺制药有限公司 用于眼部疾病治疗的化合物
EP4196477A4 (en) * 2020-08-17 2024-10-09 Vyne Therapeutics Inc. TOFACITINIB-CONTAINING ANHYDROUS ELASTOMER-BASED GEL FORMULATIONS
TW202317550A (zh) 2021-06-25 2023-05-01 美商施萬生物製藥研發 Ip有限責任公司 作為jak抑制劑之咪唑吲唑化合物
CN115969796B (zh) * 2022-12-06 2024-07-09 苏州大学 一种jak抑制剂长效微球及其制备方法与应用

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WO2017077283A1 (en) * 2015-11-03 2017-05-11 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
WO2017077288A1 (en) * 2015-11-03 2017-05-11 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
CN108349972A (zh) * 2015-11-03 2018-07-31 施万生物制药研发Ip有限责任公司 用于治疗呼吸疾病的jak激酶抑制剂化合物
WO2018165395A1 (en) * 2017-03-09 2018-09-13 Theravance Biopharma R&D Ip, Llc Fused imidazo-piperidine jak inhibitors

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US20050090529A1 (en) 2003-07-31 2005-04-28 Pfizer Inc 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
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KR101663277B1 (ko) 2015-03-30 2016-10-06 주식회사 녹십자 TNIK, IKKε 및 TBK1 억제제로서의 피라졸계 유도체 및 이를 포함하는 약학적 조성물
US10406148B2 (en) 2017-05-01 2019-09-10 Theravance Biopharma R&D Ip, Llc Methods of treatment using a JAK inhibitor compound
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FI3932919T3 (fi) 2019-02-25 2024-08-30 Henan Medinno Pharmaceutical Tech Co Ltd Jak-inhibiittoriyhdiste ja sen käyttö
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Patent Citations (5)

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Publication number Priority date Publication date Assignee Title
CN103717599A (zh) * 2011-07-27 2014-04-09 辉瑞有限公司 吲唑
WO2017077283A1 (en) * 2015-11-03 2017-05-11 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
WO2017077288A1 (en) * 2015-11-03 2017-05-11 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
CN108349972A (zh) * 2015-11-03 2018-07-31 施万生物制药研发Ip有限责任公司 用于治疗呼吸疾病的jak激酶抑制剂化合物
WO2018165395A1 (en) * 2017-03-09 2018-09-13 Theravance Biopharma R&D Ip, Llc Fused imidazo-piperidine jak inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114181055A (zh) * 2021-12-21 2022-03-15 苏州楚凯药业有限公司 1-苄氧基-4-溴-5-乙基-2-氟苯的制备方法

Also Published As

Publication number Publication date
EP3853229A1 (en) 2021-07-28
JP2022506111A (ja) 2022-01-17
US10968222B2 (en) 2021-04-06
MX2021004582A (es) 2021-06-15
WO2020092019A1 (en) 2020-05-07
KR20210084512A (ko) 2021-07-07
BR112021007788A8 (pt) 2022-04-26
SG11202103042XA (en) 2021-04-29
CA3113667A1 (en) 2020-05-07
AU2019373059A1 (en) 2021-05-06
US20210206764A1 (en) 2021-07-08
BR112021007788A2 (pt) 2021-07-27
IL282460A (en) 2021-06-30
US20200131178A1 (en) 2020-04-30

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Application publication date: 20210611