TWI875911B - Ｂｒｕｔｏｎ酪胺酸激酶（ＢＴＫ）抑制劑 - Google Patents

Ｂｒｕｔｏｎ酪胺酸激酶（ＢＴＫ）抑制劑 Download PDF

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Publication number
TWI875911B
TWI875911B TW109146658A TW109146658A TWI875911B TW I875911 B TWI875911 B TW I875911B TW 109146658 A TW109146658 A TW 109146658A TW 109146658 A TW109146658 A TW 109146658A TW I875911 B TWI875911 B TW I875911B
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TW
Taiwan
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pyran
imidazo
tetrahydro
phenoxyphenyl
fluoro
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TW109146658A
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English (en)
Chinese (zh)
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TW202136267A (zh
Inventor
周全
申長茂
陳祥
劉文耕
王汝民
慶北 曾
漢忠 徐
楊振帆
小林 張
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大陸商迪哲（江蘇）醫藥股份有限公司
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/09—Geometrical isomers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
TW109146658A 2020-01-02 2020-12-29 Ｂｒｕｔｏｎ酪胺酸激酶（ＢＴＫ）抑制劑 TWI875911B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
WOPCT/CN2020/070034 2020-01-02
CN2020070034 2020-01-02
WOPCT/CN2020/134601 2020-12-08
CN2020134601 2020-12-08

Publications (2)

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TW202136267A TW202136267A (zh) 2021-10-01
TWI875911B true TWI875911B (zh) 2025-03-11

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US (1) US12624039B2 (enExample)
EP (1) EP4087845A4 (enExample)
JP (1) JP7649311B2 (enExample)
CN (2) CN114945574B (enExample)
AU (1) AU2020419422B2 (enExample)
BR (1) BR112022013227A2 (enExample)
CA (1) CA3163365A1 (enExample)
MX (1) MX2022008148A (enExample)
TW (1) TWI875911B (enExample)
WO (1) WO2021136219A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2020436612A1 (en) * 2020-03-16 2022-09-01 Flash Therapeutics, Llc Compounds for treating or inhibiting recurrence of acute myeloid leukemia
CN113943294A (zh) * 2020-07-15 2022-01-18 成都海博为药业有限公司 一种作为btk抑制剂的化合物及其制备方法与用途
CN115851606A (zh) * 2022-12-19 2023-03-28 北京爱思益普生物科技股份有限公司 Btk突变细胞株及其构建方法和应用

Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2015074138A1 (en) * 2013-11-21 2015-05-28 Pharmascience Inc. Protein kinase inhibitors
WO2016106652A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Biarylether imidazopyrazine btk inhibitors

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WO2008054827A2 (en) 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
ES2396613T3 (es) * 2008-05-19 2013-02-22 OSI Pharmaceuticals, LLC Imidazopirazinas e imidazotriazinas sustituidas
US8940725B2 (en) 2010-05-31 2015-01-27 Ono Pharmaceutical Co., Ltd. Purinone derivative
WO2012158795A1 (en) 2011-05-17 2012-11-22 Principia Biopharma Inc. Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors
WO2016020901A1 (en) * 2014-08-07 2016-02-11 Acerta Pharma B.V. Methods of treating cancers, immune and autoimmune diseases, and inflammatory diseases based on btk occupancy and btk resynthesis rate
US20180305350A1 (en) * 2015-06-24 2018-10-25 Principia Biopharma Inc. Tyrosine kinase inhibitors
CN114605327B (zh) 2015-12-16 2025-03-11 洛克索肿瘤学股份有限公司 可用作激酶抑制剂的化合物
AU2015417922B2 (en) 2015-12-23 2018-12-20 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
US10640512B2 (en) * 2016-06-30 2020-05-05 Hangzhou Sanyintai Pharmaceutical Technology Co., Ltd. Imidazopyrazinamine phenyl derivative and use thereof
AU2017315343A1 (en) 2016-08-24 2019-02-28 Arqule, Inc. Amino-pyrrolopyrimidinone compounds and methods of use thereof
CN111454268B (zh) 2019-01-18 2023-09-08 明慧医药（上海）有限公司 作为布鲁顿酪氨酸激酶抑制剂的环状分子
CA3126940A1 (en) 2019-01-18 2020-07-23 Xibin Liao Bruton's tyrosine kinase inhibitors
CN113943294A (zh) 2020-07-15 2022-01-18 成都海博为药业有限公司 一种作为btk抑制剂的化合物及其制备方法与用途

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015074138A1 (en) * 2013-11-21 2015-05-28 Pharmascience Inc. Protein kinase inhibitors
WO2016106652A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Biarylether imidazopyrazine btk inhibitors

Also Published As

Publication number Publication date
CN114945574B (zh) 2025-02-07
JP2023510212A (ja) 2023-03-13
EP4087845A1 (en) 2022-11-16
WO2021136219A1 (en) 2021-07-08
JP7649311B2 (ja) 2025-03-19
EP4087845A4 (en) 2024-01-24
US20230122807A1 (en) 2023-04-20
CN120118089A (zh) 2025-06-10
TW202136267A (zh) 2021-10-01
US12624039B2 (en) 2026-05-12
MX2022008148A (es) 2022-07-21
BR112022013227A2 (pt) 2022-09-06
AU2020419422B2 (en) 2026-08-06
CA3163365A1 (en) 2021-07-08
CN114945574A (zh) 2022-08-26
KR20220123446A (ko) 2022-09-06
AU2020419422A1 (en) 2022-06-02

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