KR20210084512A - Jak 억제제로서 2-아자비시클로 헥산 화합물 - Google Patents

Jak 억제제로서 2-아자비시클로 헥산 화합물 Download PDF

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Publication number
KR20210084512A
KR20210084512A KR1020217015109A KR20217015109A KR20210084512A KR 20210084512 A KR20210084512 A KR 20210084512A KR 1020217015109 A KR1020217015109 A KR 1020217015109A KR 20217015109 A KR20217015109 A KR 20217015109A KR 20210084512 A KR20210084512 A KR 20210084512A
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KR
South Korea
Prior art keywords
compound
inhibitor
disease
acid
pharmaceutically
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KR1020217015109A
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English (en)
Korean (ko)
Inventor
폴 알. 파더리
란 지앙
Original Assignee
세라밴스 바이오파마 알앤디 아이피, 엘엘씨
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Publication of KR20210084512A publication Critical patent/KR20210084512A/ko
Withdrawn legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic 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)
KR1020217015109A 2018-10-29 2019-10-18 Jak 억제제로서 2-아자비시클로 헥산 화합물 Withdrawn KR20210084512A (ko)

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
KR20210084512A true KR20210084512A (ko) 2021-07-07

Family

ID=68542755

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217015109A Withdrawn KR20210084512A (ko) 2018-10-29 2019-10-18 Jak 억제제로서 2-아자비시클로 헥산 화합물

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=)

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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
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
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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TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
JP4836788B2 (ja) 2003-07-23 2011-12-14 エグゼリクシス, インコーポレイテッド 未分化リンパ腫キナーゼ変調因子及びその使用法
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
US7884109B2 (en) 2005-04-05 2011-02-08 Wyeth Llc Purine and imidazopyridine derivatives for immunosuppression
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
JP2010111624A (ja) 2008-11-06 2010-05-20 Shionogi & Co Ltd Ttk阻害作用を有するインダゾール誘導体
EP2414340A1 (en) 2009-04-03 2012-02-08 Dainippon Sumitomo Pharma Co., Ltd. Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
EP2515655B1 (en) 2009-12-21 2015-08-05 Samumed, LLC 1h-pyrazolo[3,4-beta]pyridines and therapeutic uses thereof
US8575336B2 (en) 2011-07-27 2013-11-05 Pfizer Limited Indazoles
MX368464B (es) 2013-12-05 2019-10-02 Pfizer Acrilamidas de pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinil o y pirrolo[2,3-d]piridinilo.
CR20160525A (es) 2014-05-14 2016-12-20 Pfizer Pirazolopiridinas y pirazolopirimidinas
WO2016026078A1 (en) 2014-08-19 2016-02-25 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as erk inhibitors
KR101663277B1 (ko) 2015-03-30 2016-10-06 주식회사 녹십자 TNIK, IKKε 및 TBK1 억제제로서의 피라졸계 유도체 및 이를 포함하는 약학적 조성물
EP3712152B1 (en) * 2015-11-03 2021-01-13 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
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
US10556901B2 (en) * 2015-11-03 2020-02-11 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
BR112019018648A2 (pt) 2017-03-09 2020-06-16 Theravance Biopharma R&D Ip, Llc Inibidores de jak contendo uma amida heterocíclica com 4 membros
US10406148B2 (en) 2017-05-01 2019-09-10 Theravance Biopharma R&D Ip, Llc Methods of treatment using a JAK inhibitor compound
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
CN110603255B (zh) 2017-05-01 2023-02-10 施万生物制药研发Ip有限责任公司 Jak抑制剂化合物的结晶型式
FI3932919T3 (fi) 2019-02-25 2024-08-30 Henan Medinno Pharmaceutical Tech Co Ltd Jak-inhibiittoriyhdiste ja sen käyttö
MA55201A (fr) 2019-03-05 2022-01-12 Incyte Corp Inhibiteurs de la voie jak1 pour le traitement d'un dysfonctionnement chronique de l'allogreffe pulmonaire
CN112279848A (zh) 2019-07-25 2021-01-29 四川海思科制药有限公司 一种泛JAKs抑制剂及其用途

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
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
CN112955451A (zh) 2021-06-11

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