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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (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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WO2011064631A1 (en) 2009-10-02 2011-06-03 Foamix Ltd. Surfactant-free, water-free, foamable compositions and breakable foams and their uses
UA123633C2 (uk) 2015-11-03 2021-05-05 Тереванс Байофарма Ар Енд Ді Айпі, Елелсі Сполуки інгібітору jak-кінази для лікування респіраторного захворювання
US10398641B2 (en) 2016-09-08 2019-09-03 Foamix Pharmaceuticals Ltd. Compositions and methods for treating rosacea and acne
FI3837258T3 (fi) 2018-09-04 2024-05-27 Theravance Biopharma R&D Ip Llc Dimetyyliaminoatsetidiiniamideja jak-estäjinä
JP2021535176A (ja) 2018-09-04 2021-12-16 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー Ｊａｋ阻害剤およびその中間体を調製するためのプロセス
UA127328C2 (uk) 2018-09-04 2023-07-19 Тереванс Байофарма Ар Енд Ді Айпі, Елелсі 5-7-членні гетероциклічні аміди як інгібітори jak
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
EP4359402B1 (en) * 2021-06-25 2026-03-11 Theravance Biopharma R&D IP, LLC Imidazolo indazole compounds as jak inhibitors
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
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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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
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
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
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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US10968222B2 (en) 2021-04-06
BR112021007788A2 (pt) 2021-07-27
JP2022506111A (ja) 2022-01-17
US20210206764A1 (en) 2021-07-08
MX2021004582A (es) 2021-06-15
AU2019373059A1 (en) 2021-05-06
KR20210084512A (ko) 2021-07-07
BR112021007788A8 (pt) 2022-04-26
IL282460A (en) 2021-06-30
SG11202103042XA (en) 2021-04-29
EP3853229A1 (en) 2021-07-28
CA3113667A1 (en) 2020-05-07
US20200131178A1 (en) 2020-04-30
WO2020092019A1 (en) 2020-05-07

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Application publication date: 20210611