CN110494433B - 布鲁顿酪氨酸激酶抑制剂 - Google Patents

布鲁顿酪氨酸激酶抑制剂 Download PDF

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Publication number
CN110494433B
CN110494433B CN201880020300.2A CN201880020300A CN110494433B CN 110494433 B CN110494433 B CN 110494433B CN 201880020300 A CN201880020300 A CN 201880020300A CN 110494433 B CN110494433 B CN 110494433B
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pyrazin
phenyl
imidazo
fluoro
pyrrolidin
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Chinese (zh)
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CN110494433A (zh
Inventor
廖细斌
李佳
吕志俭
周宇波
高安慧
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Suzhou Baijibugong Pharmaceutical Technology Co ltd
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Suzhou Baijibugong Pharmaceutical Technology Co ltd
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    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201880020300.2A 2017-03-22 2018-03-21 布鲁顿酪氨酸激酶抑制剂 Active CN110494433B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762474686P 2017-03-22 2017-03-22
US62/474,686 2017-03-22
PCT/US2018/023455 WO2018175512A1 (en) 2017-03-22 2018-03-21 Bruton's tyrosine kinase inhibitors

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CN110494433A CN110494433A (zh) 2019-11-22
CN110494433B true CN110494433B (zh) 2023-03-17

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US (3) US11554118B2 (enExample)
EP (1) EP3601264A4 (enExample)
JP (1) JP7219902B2 (enExample)
KR (1) KR102627756B1 (enExample)
CN (1) CN110494433B (enExample)
AU (1) AU2018237123B2 (enExample)
CA (1) CA3055602A1 (enExample)
EA (1) EA201992147A1 (enExample)
IL (1) IL269152B2 (enExample)
MX (1) MX2019011116A (enExample)
WO (1) WO2018175512A1 (enExample)
ZA (1) ZA201906887B (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11554118B2 (en) * 2017-03-22 2023-01-17 Xibin Liao Bruton's tyrosine kinase inhibitors
CA3126940A1 (en) * 2019-01-18 2020-07-23 Xibin Liao Bruton's tyrosine kinase inhibitors
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
JP7475370B2 (ja) * 2019-05-10 2024-04-26 河南知微生物医薬有限公司 ブルトン型チロシンキナーゼ阻害剤としての置換されている1-アミノ-1h-イミダゾール-5-カルボキサミド
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN111471048B (zh) * 2020-04-30 2021-06-15 成都海博为药业有限公司 一种具有含氮桥环、螺环或并环结构的化合物及其用途
CN115073468B (zh) * 2021-03-15 2023-12-22 药雅科技(上海)有限公司 咪唑并吡嗪类btk抑制剂的制备及用途
WO2022228302A1 (en) * 2021-04-25 2022-11-03 Bionova Pharmaceuticals (Shanghai) Limited Heteroaromatic carboxamide compounds and its use

Citations (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103889987A (zh) * 2011-07-19 2014-06-25 默沙东有限责任公司 作为btk-抑制剂的4-咪唑并哒嗪-1-基-苯甲酰胺类和4-咪唑并三嗪-1-基-苯甲酰胺类
CN103917545A (zh) * 2011-07-19 2014-07-09 默沙东公司 Btk抑制剂
CN104080789A (zh) * 2012-01-31 2014-10-01 南京奥昭生物科技有限公司 作为布鲁顿酪氨酸激酶抑制剂的环状分子
WO2015057992A1 (en) * 2013-10-16 2015-04-23 Izumi Raquel Btk inhibitors for hematopoietic mobilization
WO2016109219A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Biarylether imidazopyrazine btk inhibitors
WO2016106626A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Imidazopyrazine analogs with 3-tertiary carbon substitutions as btk inhibitors
WO2016109223A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Benzamide imidazopyrazine btk inhibitors
WO2016210165A1 (en) * 2015-06-24 2016-12-29 Principia Biopharma Inc. Tyrosine kinase inhibitors
CN106459045A (zh) * 2014-04-17 2017-02-22 艾伯维公司 杂环激酶抑制剂
WO2017033113A1 (en) * 2015-08-21 2017-03-02 Acerta Pharma B.V. Therapeutic combinations of a mek inhibitor and a btk inhibitor
CN106478633A (zh) * 2015-08-27 2017-03-08 正大天晴药业集团股份有限公司 一类布鲁顿酪氨酸激酶抑制剂
WO2017077507A1 (en) * 2015-11-06 2017-05-11 Acerta Pharma B.V. Imidazopyrazine inhibitors of bruton's tyrosine kinase
WO2017156495A1 (en) * 2016-03-11 2017-09-14 Corvus Pharmaceuticals, Inc. Compounds and methods for modulating bruton's tyrosine kinase
CN107556317A (zh) * 2016-06-30 2018-01-09 杭州华东医药集团新药研究院有限公司 一种咪唑吡啶胺苯基衍生物及其用途
WO2018033091A1 (zh) * 2016-08-17 2018-02-22 深圳市塔吉瑞生物医药有限公司 用于抑制酪氨酸激酶活性的稠合双环类化合物

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003290333A1 (en) * 2002-12-24 2004-07-22 Biofocus Plc Compound libraries of imidazo(1,5-a)pyridin-3-yl derivatives and related heterobicycles for targetting compounds capable of binding to g-protein coupled receptors
WO2005021545A1 (en) 2003-09-03 2005-03-10 Galapagos Nv IMIDAZO[1,5-a]PYRIDINE OR IMIDAZO[1,5-a]PIPERIDINE DERIVATIVES AND THEIR USE FOR THE PREPARATION OF MEDICAMENT AGAINST 5-HT2A RECEPTOR-RELATED DISORDERS
WO2008022060A2 (en) * 2006-08-14 2008-02-21 Novartis Ag Imidazo-pyridine derivatives for modulating protein kinase activity
EP2529621B1 (en) * 2006-09-22 2016-10-05 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
EP2139487B1 (en) 2007-03-28 2015-11-11 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
ES2396613T3 (es) 2008-05-19 2013-02-22 OSI Pharmaceuticals, LLC Imidazopirazinas e imidazotriazinas sustituidas
US8658794B2 (en) 2010-02-08 2014-02-25 Merck Sharp & Dohme B.V. 8-methyl-1-phenyl-imidazol[1,5-a]pyrazine compounds as Lck inhibitors and uses thereof
JP2014509616A (ja) 2011-03-31 2014-04-21 エーエムベーエルエーエム テクノロジー トランスファー ゲーエムベーハー 治療用イミダゾ[1,2−a]ピリジン化合物
GB2513821A (en) * 2011-06-28 2014-11-12 Andrew Levine Speech-to-text conversion
WO2013010869A1 (en) * 2011-07-19 2013-01-24 Msd Oss B.V. 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides btk-inhibitors
FR2985185B1 (fr) * 2012-01-04 2013-12-27 Sanofi Sa Utilisation en therapeutique de derives d'imidazopyridine
US9481682B2 (en) * 2013-01-23 2016-11-01 Merck Sharp & Dohme Corp. Substituted benzamides and substituted pyridinecarboxamides as Btk inhibitors
WO2014113942A1 (en) 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
JP2016533385A (ja) * 2013-08-22 2016-10-27 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft アルキニルアルコール及び使用方法
CN105017256A (zh) 2014-04-29 2015-11-04 浙江导明医药科技有限公司 多氟化合物作为布鲁顿酪氨酸激酶抑制剂
MA41614A (fr) * 2015-02-25 2018-01-02 Alios Biopharma Inc Composés antiviraux
US20170071962A1 (en) 2015-09-11 2017-03-16 Acerta Pharma B.V. Therapeutic Combinations of a Proteasome Inhibitor and a BTK Inhibitor
US20170035881A1 (en) * 2015-10-19 2017-02-09 Acerta Pharma B.V. Therapeutic Combinations of an IRAK4 Inhibitor and a BTK Inhibitor
US11554118B2 (en) * 2017-03-22 2023-01-17 Xibin Liao Bruton's tyrosine kinase inhibitors

Patent Citations (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103889987A (zh) * 2011-07-19 2014-06-25 默沙东有限责任公司 作为btk-抑制剂的4-咪唑并哒嗪-1-基-苯甲酰胺类和4-咪唑并三嗪-1-基-苯甲酰胺类
CN103917545A (zh) * 2011-07-19 2014-07-09 默沙东公司 Btk抑制剂
CN104080789A (zh) * 2012-01-31 2014-10-01 南京奥昭生物科技有限公司 作为布鲁顿酪氨酸激酶抑制剂的环状分子
WO2015057992A1 (en) * 2013-10-16 2015-04-23 Izumi Raquel Btk inhibitors for hematopoietic mobilization
CN106459045A (zh) * 2014-04-17 2017-02-22 艾伯维公司 杂环激酶抑制剂
WO2016109223A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Benzamide imidazopyrazine btk inhibitors
WO2016106626A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Imidazopyrazine analogs with 3-tertiary carbon substitutions as btk inhibitors
WO2016109219A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Biarylether imidazopyrazine btk inhibitors
WO2016210165A1 (en) * 2015-06-24 2016-12-29 Principia Biopharma Inc. Tyrosine kinase inhibitors
WO2017033113A1 (en) * 2015-08-21 2017-03-02 Acerta Pharma B.V. Therapeutic combinations of a mek inhibitor and a btk inhibitor
CN106478633A (zh) * 2015-08-27 2017-03-08 正大天晴药业集团股份有限公司 一类布鲁顿酪氨酸激酶抑制剂
WO2017077507A1 (en) * 2015-11-06 2017-05-11 Acerta Pharma B.V. Imidazopyrazine inhibitors of bruton's tyrosine kinase
WO2017156495A1 (en) * 2016-03-11 2017-09-14 Corvus Pharmaceuticals, Inc. Compounds and methods for modulating bruton's tyrosine kinase
CN107556317A (zh) * 2016-06-30 2018-01-09 杭州华东医药集团新药研究院有限公司 一种咪唑吡啶胺苯基衍生物及其用途
WO2018033091A1 (zh) * 2016-08-17 2018-02-22 深圳市塔吉瑞生物医药有限公司 用于抑制酪氨酸激酶活性的稠合双环类化合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Discovery of novel BTK inhibitors with carboxylic acids;Gao, Xiaolei等;《Bioorganic & Medicinal Chemistry Letters》;20161125;第27卷(第6期);第1471-1477页 *

Also Published As

Publication number Publication date
EP3601264A1 (en) 2020-02-05
BR112019019588A2 (pt) 2020-04-22
CA3055602A1 (en) 2018-09-27
US20190275037A1 (en) 2019-09-12
ZA201906887B (en) 2022-03-30
US20210121458A1 (en) 2021-04-29
MX2019011116A (es) 2020-02-05
JP7219902B2 (ja) 2023-02-09
IL269152A (en) 2019-11-28
IL269152B2 (en) 2023-11-01
EA201992147A1 (ru) 2020-02-20
US20210107903A1 (en) 2021-04-15
US11974999B2 (en) 2024-05-07
CN110494433A (zh) 2019-11-22
WO2018175512A1 (en) 2018-09-27
KR102627756B1 (ko) 2024-01-23
US10933063B2 (en) 2021-03-02
EP3601264A4 (en) 2021-03-24
US11554118B2 (en) 2023-01-17
AU2018237123A1 (en) 2019-10-10
JP2020511547A (ja) 2020-04-16
AU2018237123B2 (en) 2022-08-04
KR20190133199A (ko) 2019-12-02
IL269152B1 (en) 2023-07-01

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