TWI779016B - 稠合咪唑-哌啶jak抑制劑 - Google Patents

稠合咪唑-哌啶jak抑制劑 Download PDF

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Publication number
TWI779016B
TWI779016B TW107107936A TW107107936A TWI779016B TW I779016 B TWI779016 B TW I779016B TW 107107936 A TW107107936 A TW 107107936A TW 107107936 A TW107107936 A TW 107107936A TW I779016 B TWI779016 B TW I779016B
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Taiwan
Prior art keywords
alkyl
compound
pharmaceutically acceptable
acceptable salt
stereoisomer
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TW107107936A
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English (en)
Chinese (zh)
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TW201837037A (zh
Inventor
保羅 R 費瑟里
蓋瑞 E L 布蘭德
卡梅朗 史密斯
史蒂芬 D E 蘇利文
羅利 珍 凡歐丹
梅蘭妮 A. 克蘭斯查克
葛林 D. 卡特
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美商施萬生物製藥研發 Ip有限責任公司
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Publication of TW201837037A publication Critical patent/TW201837037A/zh
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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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pulmonology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
TW107107936A 2017-03-09 2018-03-08 稠合咪唑-哌啶jak抑制劑 TWI779016B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762469073P 2017-03-09 2017-03-09
US62/469,073 2017-03-09

Publications (2)

Publication Number Publication Date
TW201837037A TW201837037A (zh) 2018-10-16
TWI779016B true TWI779016B (zh) 2022-10-01

Family

ID=61683956

Family Applications (2)

Application Number Title Priority Date Filing Date
TW107107939A TWI754019B (zh) 2017-03-09 2018-03-08 含有4員雜環醯胺之jak抑制劑
TW107107936A TWI779016B (zh) 2017-03-09 2018-03-08 稠合咪唑-哌啶jak抑制劑

Family Applications Before (1)

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TW107107939A TWI754019B (zh) 2017-03-09 2018-03-08 含有4員雜環醯胺之jak抑制劑

Country Status (20)

Country Link
US (10) US10208040B2 (enExample)
EP (2) EP3592742B1 (enExample)
JP (2) JP6974487B2 (enExample)
KR (2) KR102533646B1 (enExample)
CN (2) CN110461839B (enExample)
AR (2) AR111241A1 (enExample)
AU (2) AU2018231032B2 (enExample)
BR (2) BR112019018649A2 (enExample)
CA (1) CA2997772A1 (enExample)
DK (1) DK3592742T3 (enExample)
EA (2) EA037748B1 (enExample)
ES (1) ES2882186T3 (enExample)
IL (2) IL268679B (enExample)
MX (2) MX388749B (enExample)
PH (2) PH12019501941A1 (enExample)
PT (1) PT3592742T (enExample)
SG (2) SG11201907840RA (enExample)
TW (2) TWI754019B (enExample)
WO (2) WO2018165395A1 (enExample)
ZA (2) ZA201905585B (enExample)

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JP6974487B2 (ja) 2017-03-09 2021-12-01 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 ４員ヘテロ環式アミドを含むｊａｋ阻害剤
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
BR112021004052A2 (pt) 2018-09-04 2021-05-25 Theravance Biopharma R&D Ip, Llc amidas de dimetil-amino azetidina como inibidores de jak
WO2020051135A1 (en) 2018-09-04 2020-03-12 Theravance Biopharma R&D Ip, Llc Process for preparing jak inhibitors and intermediates thereof
SG11202101751XA (en) * 2018-09-04 2021-03-30 Theravance Biopharma R&D Ip Llc 5 to 7 membered heterocyclic amides as jak inhibitors
MX2021004582A (es) * 2018-10-29 2021-06-15 Theravance Biopharma R&D Ip Llc Compuesto 2-azabiciclo hexano inhibidor de jak.
MX2021010242A (es) 2019-02-25 2021-09-21 Henan Medinno Pharmaceutical Tech Co Ltd Compuesto inhibidor de jak y uso del mismo.
JP2022524997A (ja) 2019-03-05 2022-05-11 インサイト・コーポレイション 慢性肺同種移植片機能不全の治療のためのｊａｋ１経路阻害剤
EP4065578A1 (en) * 2019-11-26 2022-10-05 Theravance Biopharma R&D IP, LLC Fused pyrimidine pyridinone compounds as jak inhibitors
CN113121509B (zh) * 2019-12-30 2024-04-26 河南迈英诺医药科技有限公司 Jak抑制剂化合物及其用途
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
EP3944859A1 (en) 2020-07-30 2022-02-02 Assistance Publique Hôpitaux de Paris Method for treating immune toxicities induced by immune checkpoint inhibitors
WO2022178215A1 (en) * 2021-02-19 2022-08-25 Theravance Biopharma R&D Ip, Llc Amino amide tetrahydro imidazo pyridines as jak inhibitors
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
PE20241589A1 (es) * 2021-12-17 2024-08-01 Daewoong Pharmaceutical Co Ltd Nueva sal de adicion de acido y ofrma cristalina de (2r,3s)-2-(3-(4,5-dicloro-1h-benzo[d]imidazol-1-il)propil)piperidin-3-ol
CN117658852A (zh) * 2023-11-15 2024-03-08 西北工业大学 取代苯氧乙酰肼类化合物及其制备方法和作为stat3的抗炎抑制剂的应用
WO2025157904A1 (en) * 2024-01-24 2025-07-31 Kiox Pharmaceuticals Aps Inhalable formulations of ruxolitinib, methods of manufacture and uses thereof
CN118903009B (zh) * 2024-10-11 2025-01-21 江苏长泰药业股份有限公司 一种调节呼吸道微生态的丙酮酸钠气雾剂及其制备方法和应用

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JP6974487B2 (ja) * 2017-03-09 2021-12-01 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 ４員ヘテロ環式アミドを含むｊａｋ阻害剤
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TWI808083B (zh) 2017-05-01 2023-07-11 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型式
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
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WO2020051135A1 (en) 2018-09-04 2020-03-12 Theravance Biopharma R&D Ip, Llc Process for preparing jak inhibitors and intermediates thereof
BR112021004052A2 (pt) 2018-09-04 2021-05-25 Theravance Biopharma R&D Ip, Llc amidas de dimetil-amino azetidina como inibidores de jak

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US20200181141A1 (en) 2020-06-11
KR20190127798A (ko) 2019-11-13
US10954237B2 (en) 2021-03-23
AU2018231032A1 (en) 2019-09-05
IL268689B2 (en) 2023-02-01
DK3592742T3 (da) 2021-08-09
ZA201905585B (en) 2020-05-27
MX2019010539A (es) 2019-10-21
ZA201905618B (en) 2021-05-26
IL268689A (en) 2019-10-31
US11453668B2 (en) 2022-09-27
BR112019018648A2 (pt) 2020-06-16
US20200216447A1 (en) 2020-07-09
KR102526764B1 (ko) 2023-04-27
AU2018231032A8 (en) 2019-10-17
MX2019010541A (es) 2019-10-21
WO2018165392A1 (en) 2018-09-13
BR112019018649A2 (pt) 2020-04-07
NZ756823A (en) 2021-04-30
WO2018165395A1 (en) 2018-09-13
US10519153B2 (en) 2019-12-31
US10208040B2 (en) 2019-02-19
AU2018231032B2 (en) 2021-08-19
US10550118B2 (en) 2020-02-04
EA201992128A1 (ru) 2020-01-29
US20190119275A1 (en) 2019-04-25
ES2882186T3 (es) 2021-12-01
CA2997772A1 (en) 2018-09-09
TWI754019B (zh) 2022-02-01
CN110461839B (zh) 2022-08-23
KR102533646B1 (ko) 2023-05-17
JP7134990B2 (ja) 2022-09-12
PH12019501941A1 (en) 2020-07-06
US20190337945A1 (en) 2019-11-07
KR20190127796A (ko) 2019-11-13
JP2020510010A (ja) 2020-04-02
US10196393B2 (en) 2019-02-05
TW201840560A (zh) 2018-11-16
AU2018231035A1 (en) 2019-09-05
EA037261B1 (ru) 2021-03-01
MX388749B (es) 2025-03-11
AR111242A1 (es) 2019-06-19
US20210269436A1 (en) 2021-09-02
IL268689B (en) 2022-10-01
EP3592743A1 (en) 2020-01-15
IL268679A (en) 2019-10-31
PH12019501985A1 (en) 2020-10-05
SG11201907544VA (en) 2019-09-27
EP3592742B1 (en) 2021-05-19
US10392386B2 (en) 2019-08-27
PT3592742T (pt) 2021-07-30
EP3592742A1 (en) 2020-01-15
SG11201907840RA (en) 2019-09-27
US11667637B2 (en) 2023-06-06
US11254669B2 (en) 2022-02-22
US20180258088A1 (en) 2018-09-13
TW201837037A (zh) 2018-10-16
AU2018231035B2 (en) 2021-09-09
US20220289737A1 (en) 2022-09-15
JP6974487B2 (ja) 2021-12-01
US20230063643A1 (en) 2023-03-02
JP2020510015A (ja) 2020-04-02
IL268679B (en) 2021-10-31
CN110382498A (zh) 2019-10-25
MX388750B (es) 2025-03-20
US20180258087A1 (en) 2018-09-13
AR111241A1 (es) 2019-06-19
US20190127371A1 (en) 2019-05-02
CN110382498B (zh) 2022-07-12
EA037748B1 (ru) 2021-05-18
CN110461839A (zh) 2019-11-15
EA201992126A1 (ru) 2020-02-05
US11878977B2 (en) 2024-01-23

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