WO2016019237A3 - Inhibiteurs de la tyrosine kinase de bruton - Google Patents

Inhibiteurs de la tyrosine kinase de bruton Download PDF

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Publication number
WO2016019237A3
WO2016019237A3 PCT/US2015/043102 US2015043102W WO2016019237A3 WO 2016019237 A3 WO2016019237 A3 WO 2016019237A3 US 2015043102 W US2015043102 W US 2015043102W WO 2016019237 A3 WO2016019237 A3 WO 2016019237A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
bruton
tyrosine kinase
methods
btk
Prior art date
Application number
PCT/US2015/043102
Other languages
English (en)
Other versions
WO2016019237A2 (fr
Inventor
Wei Chen
Longcheng Wang
Zhaozhong J. Jia
James T. Palmer
Original Assignee
Pharmacyclics Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pharmacyclics Llc filed Critical Pharmacyclics Llc
Publication of WO2016019237A2 publication Critical patent/WO2016019237A2/fr
Publication of WO2016019237A3 publication Critical patent/WO2016019237A3/fr

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Classifications

    • 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
    • A61K9/0031Rectum, anus
    • 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
    • A61K9/0012Galenical 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • 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
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0078Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Dispersion Chemistry (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne des composés hétéroaryle contenant un groupe cyano qui sont utiles en tant qu'inhibiteurs des kinases. L'invention concerne également des procédés de synthèse de tels inhibiteurs et des méthodes d'utilisation de ces inhibiteurs dans le traitement de maladies.
PCT/US2015/043102 2014-07-31 2015-07-31 Inhibiteurs de la tyrosine kinase de bruton WO2016019237A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462031658P 2014-07-31 2014-07-31
US62/031,658 2014-07-31

Publications (2)

Publication Number Publication Date
WO2016019237A2 WO2016019237A2 (fr) 2016-02-04
WO2016019237A3 true WO2016019237A3 (fr) 2016-04-07

Family

ID=55218446

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2015/043102 WO2016019237A2 (fr) 2014-07-31 2015-07-31 Inhibiteurs de la tyrosine kinase de bruton

Country Status (1)

Country Link
WO (1) WO2016019237A2 (fr)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ736450A (en) 2015-03-30 2022-04-29 Mission Therapeutics Ltd 1-cyano-pyrrolidine compounds as usp30 inhibitors
WO2016192074A1 (fr) * 2015-06-04 2016-12-08 Merck Sharp & Dohme Corp. Inhibiteurs de la btk
EP3433246B1 (fr) * 2016-03-24 2022-05-04 Mission Therapeutics Limited Dérivés de 1-cyano-pyrrolidine comme des inhibiteurs de dbu
CN107383013B (zh) * 2016-05-16 2020-03-31 苏州信诺维医药科技有限公司 作为btk抑制剂的吡唑并嘧啶衍生物及其制备方法和药物组合物
KR102215172B1 (ko) 2016-06-30 2021-02-16 항저우 방순 파마슈티컬 컴퍼니, 리미티드 이미다조피라진아민 페닐 유도체 및 그의 용도
WO2018033091A1 (fr) 2016-08-17 2018-02-22 深圳市塔吉瑞生物医药有限公司 Composé bicyclique fusionné pour inhiber l'activité de la tyrosine kinase
GB201616511D0 (en) * 2016-09-29 2016-11-16 Mission Therapeutics Limited Novel compounds
GB201616627D0 (en) 2016-09-30 2016-11-16 Mission Therapeutics Limited Novel compounds
GB201708652D0 (en) 2017-05-31 2017-07-12 Mission Therapeutics Ltd Novel compounds and uses
EP3642196B1 (fr) 2017-06-20 2022-08-17 Mission Therapeutics Limited Cyanopyrrolidines substituées présentant une activité en tant qu'inhibiteurs de dub
KR20200067850A (ko) * 2017-10-06 2020-06-12 포르마 세라퓨틱스 인크. 유비퀴틴 특이적 펩티다제 30의 억제
RS64321B1 (sr) 2018-10-05 2023-08-31 Forma Therapeutics Inc Fuzionisani pirolini koji se ponašaju kao inhibitori ubikvitin specifične proteaze 30 (usp30)
GB201905375D0 (en) 2019-04-16 2019-05-29 Mission Therapeutics Ltd Novel compounds
GB201905371D0 (en) 2019-04-16 2019-05-29 Mission Therapeutics Ltd Novel compounds
GB201912674D0 (en) 2019-09-04 2019-10-16 Mission Therapeutics Ltd Novel compounds
CN111018865B (zh) * 2019-10-17 2021-01-15 山东大学 1-取代苄基吡唑并嘧啶衍生物及其制备方法与应用
US20230119013A1 (en) 2020-04-08 2023-04-20 Mission Therapeutics Limited N-cyanopyrrolidines with activity as usp30 inhibitors
WO2021239863A1 (fr) 2020-05-28 2021-12-02 Mission Therapeutics Limited N-(1-cyano-pyrrolidin-3-yl)-5-(3- (trifluorométhyl)phényl)oxazole-2-carboxamide et dérivés d'oxadiazole correspondants utilisés en tant qu'inhibiteurs d'usp30 pour le traitement d'un dysfonctionnement mitochondrial
CA3185654A1 (fr) 2020-06-04 2021-12-09 Mission Therapeutics Limited N-cyanopyrrolidines ayant une activite en tant qu'inhibiteurs de l'usp30
JP2023528087A (ja) 2020-06-08 2023-07-03 ミッション セラピューティクス リミティド ミトコンドリア機能不全、癌、及び線維症の治療に使用されるUSP30阻害剤としての1-(5-(2-シアノピリジン-4-イル)オキサゾール-2-カルボニル)-4-メチルヘキサヒドロピロロ[3,4-b]ピロール-5(1H)-カルボニトリル
GB202016800D0 (en) 2020-10-22 2020-12-09 Mission Therapeutics Ltd Novel compounds
CN114573586B (zh) * 2020-11-28 2023-11-03 杭州和正医药有限公司 一种抑制布鲁顿酪氨酸激酶活性的多环化合物、药物组合物及其应用
CN113968860B (zh) * 2021-11-05 2023-06-06 杭州医学院 一种可逆btk抑制剂及其合成方法和应用
WO2023099561A1 (fr) 2021-12-01 2023-06-08 Mission Therapeutics Limited N-cyanopyrrolidines substituées ayant une activité en tant qu'inhibiteurs de l'usp30

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080076921A1 (en) * 2006-09-22 2008-03-27 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US20090286768A1 (en) * 2008-05-19 2009-11-19 Osi Pharmaceuticals, Inc. Substituted imidazopyr- and imidazotri-azines
WO2014068527A1 (fr) * 2012-11-02 2014-05-08 Pfizer Inc. Inhibiteurs de la tyrosine kinase de bruton

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080076921A1 (en) * 2006-09-22 2008-03-27 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US20090286768A1 (en) * 2008-05-19 2009-11-19 Osi Pharmaceuticals, Inc. Substituted imidazopyr- and imidazotri-azines
WO2014068527A1 (fr) * 2012-11-02 2014-05-08 Pfizer Inc. Inhibiteurs de la tyrosine kinase de bruton

Also Published As

Publication number Publication date
WO2016019237A2 (fr) 2016-02-04

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