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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    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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

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Family Applications (2)

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

Family Applications After (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) US10196393B2 (https=)
EP (2) EP3592743A1 (https=)
JP (2) JP7134990B2 (https=)
KR (2) KR102533646B1 (https=)
CN (2) CN110382498B (https=)
AR (2) AR111242A1 (https=)
AU (2) AU2018231035B2 (https=)
BR (2) BR112019018648A2 (https=)
CA (1) CA2997772A1 (https=)
DK (1) DK3592742T3 (https=)
EA (2) EA037261B1 (https=)
ES (1) ES2882186T3 (https=)
IL (2) IL268679B (https=)
MX (2) MX388749B (https=)
PH (2) PH12019501941A1 (https=)
PT (1) PT3592742T (https=)
SG (2) SG11201907544VA (https=)
TW (2) TWI779016B (https=)
WO (2) WO2018165395A1 (https=)
ZA (2) ZA201905585B (https=)

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BR112019018648A2 (pt) 2017-03-09 2020-06-16 Theravance Biopharma R&D Ip, Llc Inibidores de jak contendo uma amida heterocíclica com 4 membros
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
US10406148B2 (en) 2017-05-01 2019-09-10 Theravance Biopharma R&D Ip, Llc Methods of treatment using a JAK inhibitor compound
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
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MX2021004582A (es) 2018-10-29 2021-06-15 Theravance Biopharma R&D Ip Llc Compuesto 2-azabiciclo hexano inhibidor de jak.
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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
CN114901659A (zh) * 2019-11-26 2022-08-12 施万生物制药研发Ip有限责任公司 作为jak抑制剂的稠合嘧啶吡啶酮化合物
WO2021136345A1 (zh) * 2019-12-30 2021-07-08 路良 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
JP7644873B2 (ja) * 2021-12-17 2025-03-12 デウン ファーマシューティカル カンパニー リミテッド （２Ｒ，３Ｓ）－２－（３－（４，５－ジクロロ－１Ｈ－ベンゾ［ｄ］イミダゾール－１－イル）プロピル）ピペリジン－３－オールの新規な酸付加塩および結晶形
CN117658852B (zh) * 2023-11-15 2026-03-24 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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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
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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
PT3837258T (pt) 2018-09-04 2024-06-20 Theravance Biopharma R&D Ip Llc Amidas de dimetil amino azetidina como inibidores de jak

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Also Published As

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

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