TW202106682A - 作為jak激酶抑制劑之酯類及碳酸酯類嘧啶化合物 - Google Patents

作為jak激酶抑制劑之酯類及碳酸酯類嘧啶化合物 Download PDF

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TW202106682A
TW202106682A TW109113575A TW109113575A TW202106682A TW 202106682 A TW202106682 A TW 202106682A TW 109113575 A TW109113575 A TW 109113575A TW 109113575 A TW109113575 A TW 109113575A TW 202106682 A TW202106682 A TW 202106682A
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Taiwan
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
group
alkyl
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TW109113575A
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English (en)
Chinese (zh)
Inventor
菲利浦 A 格肯
建華 曹
丹尼爾 D 羅恩
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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 TW202106682A publication Critical patent/TW202106682A/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • 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
    • C07D471/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
TW109113575A 2019-04-24 2020-04-23 作為jak激酶抑制劑之酯類及碳酸酯類嘧啶化合物 TW202106682A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962837829P 2019-04-24 2019-04-24
US62/837,829 2019-04-24

Publications (1)

Publication Number Publication Date
TW202106682A true TW202106682A (zh) 2021-02-16

Family

ID=70740750

Family Applications (1)

Application Number Title Priority Date Filing Date
TW109113575A TW202106682A (zh) 2019-04-24 2020-04-23 作為jak激酶抑制劑之酯類及碳酸酯類嘧啶化合物

Country Status (11)

Country Link
US (2) US11155549B2 (https=)
EP (1) EP3958969B1 (https=)
JP (1) JP7470713B2 (https=)
AR (1) AR118768A1 (https=)
CA (1) CA3135383A1 (https=)
ES (1) ES2974577T3 (https=)
HR (1) HRP20240346T1 (https=)
HU (1) HUE066802T2 (https=)
PL (1) PL3958969T3 (https=)
TW (1) TW202106682A (https=)
WO (1) WO2020219639A1 (https=)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11202001706RA (en) 2017-10-27 2020-03-30 Theravance Biopharma R&D Ip Llc Pyrimidine compound as jak kinase inhibitor
TW202106681A (zh) * 2019-04-24 2021-02-16 美商施萬生物製藥研發Ip有限責任公司 用於治療皮膚疾病之嘧啶jak抑制劑
PL3958969T3 (pl) 2019-04-24 2024-05-20 Theravance Biopharma R&D Ip, Llc Estrowe i węglanowe związki pirymidynowe jako inhibitory kinaz
US20210212962A1 (en) * 2020-01-13 2021-07-15 Sol-Gel Technologies Ltd. Methods and compositions for the treatment of granuloma annulare or subcutaneous inflammation and non-infection granulomatous diseases
CA3216017A1 (en) * 2021-04-22 2022-10-27 Shengjian Huang Pharmaceutical composition containing jak3/jak1/tbk1 selective inhibitor and medical use thereof
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ras抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Family Cites Families (19)

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US4919934A (en) 1989-03-02 1990-04-24 Richardson-Vicks Inc. Cosmetic sticks
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002022605A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6989385B2 (en) 2000-12-21 2006-01-24 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US20070179125A1 (en) 2005-11-16 2007-08-02 Damien Fraysse Aminopyrimidines useful as kinase inhibitors
TW200817391A (en) 2006-06-30 2008-04-16 Astrazeneca Ab Novel compounds
EP2043651A2 (en) 2006-07-05 2009-04-08 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
CN104011050A (zh) 2011-12-22 2014-08-27 霍夫曼-拉罗奇有限公司 作为丝氨酸/苏氨酸激酶抑制剂的2,4-二氨基-嘧啶衍生物
WO2015094803A1 (en) 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
NO2721710T3 (https=) * 2014-08-21 2018-03-31
ES2753159T3 (es) 2015-05-28 2020-04-07 Theravance Biopharma R&D Ip Llc Compuestos de naftiridina como inhibidores de quinasa JAK
CA3020506A1 (en) 2016-04-28 2017-11-02 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as jak kinase inhibitors
SG11202001706RA (en) 2017-10-27 2020-03-30 Theravance Biopharma R&D Ip Llc Pyrimidine compound as jak kinase inhibitor
WO2020108516A1 (zh) 2018-11-27 2020-06-04 江苏豪森药业集团有限公司 含氮杂芳类衍生物调节剂、其制备方法和应用
WO2020108613A1 (zh) 2018-11-30 2020-06-04 江苏豪森药业集团有限公司 杂芳类衍生物调节剂、其制备方法和应用
PL3958969T3 (pl) 2019-04-24 2024-05-20 Theravance Biopharma R&D Ip, Llc Estrowe i węglanowe związki pirymidynowe jako inhibitory kinaz
TW202106681A (zh) 2019-04-24 2021-02-16 美商施萬生物製藥研發Ip有限責任公司 用於治療皮膚疾病之嘧啶jak抑制劑
CN113372364B (zh) 2020-03-10 2024-05-31 明慧医药(上海)有限公司 一类jak激酶抑制剂及其制备和应用
CN113372351A (zh) 2020-03-10 2021-09-10 明慧医药(杭州)有限公司 一类jak激酶抑制剂及其制备和应用

Also Published As

Publication number Publication date
US11155549B2 (en) 2021-10-26
WO2020219639A1 (en) 2020-10-29
CA3135383A1 (en) 2020-10-29
US20220009926A1 (en) 2022-01-13
PL3958969T3 (pl) 2024-05-20
HUE066802T2 (hu) 2024-09-28
EP3958969C0 (en) 2024-01-10
JP2022529370A (ja) 2022-06-21
US20200339580A1 (en) 2020-10-29
EP3958969A1 (en) 2022-03-02
AR118768A1 (es) 2021-10-27
US11845747B2 (en) 2023-12-19
HRP20240346T1 (hr) 2024-05-24
JP7470713B2 (ja) 2024-04-18
EP3958969B1 (en) 2024-01-10
ES2974577T3 (es) 2024-06-27

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