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 (enExample)
EP (1) EP3853229A1 (enExample)
JP (1) JP2022506111A (enExample)
KR (1) KR20210084512A (enExample)
CN (1) CN112955451A (enExample)
AU (1) AU2019373059A1 (enExample)
BR (1) BR112021007788A8 (enExample)
CA (1) CA3113667A1 (enExample)
IL (1) IL282460A (enExample)
MX (1) MX2021004582A (enExample)
SG (1) SG11202103042XA (enExample)
WO (1) WO2020092019A1 (enExample)

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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AU2010302350B2 (en) 2009-10-02 2015-06-18 Journey Medical Corporation Surfactant-free water-free foamable compositions, breakable foams and gels and their uses
US12661407B2 (en) 2010-04-08 2026-06-23 Journey Medical Corporation Compositions, gels and foams with rheology modulators and uses thereof
TWI710560B (zh) 2015-11-03 2020-11-21 美商施萬生物製藥研發Ｉｐ有限責任公司 用於治療呼吸疾病之jak激酶抑制劑化合物
MX2020012139A (es) 2016-09-08 2021-01-29 Vyne Pharmaceuticals Inc Composiciones y metodos para tratar rosacea y acne.
BR112021004063A2 (pt) 2018-09-04 2021-05-25 Theravance Biopharma R&D Ip, Llc amidas heterocíclicas com 5 a 7 membros como inibidores de jak
BR112021004087A2 (pt) 2018-09-04 2021-05-25 Theravance Biopharma R&D Ip, Llc processo para preparar inibidores de jak e seus intermediários
DK3837258T3 (da) 2018-09-04 2024-07-22 Theravance Biopharma R&D Ip Llc Dimethyl amino azetidine amides as jak inhibitors
KR20220149585A (ko) 2020-03-02 2022-11-08 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 억제제 화합물의 결정성 수화물
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
US20240325393A1 (en) * 2020-08-17 2024-10-03 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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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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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

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

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Application publication date: 20210611