CN114450289A - 作为选择性btk激酶抑制剂的吡唑并吡啶类化合物 - Google Patents

作为选择性btk激酶抑制剂的吡唑并吡啶类化合物 Download PDF

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CN114450289A
CN114450289A CN202080068213.1A CN202080068213A CN114450289A CN 114450289 A CN114450289 A CN 114450289A CN 202080068213 A CN202080068213 A CN 202080068213A CN 114450289 A CN114450289 A CN 114450289A
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compound
pharmaceutically acceptable
acceptable salt
isomer
compounds
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CN114450289B (zh
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沈春莉
魏霞蔚
吴成德
胡国平
姜宁
郑维
黎健
陈曙辉
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Chengdu Jiabao Pharmaceutical Silver Pharmaceutical Technology Co ltd
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Chengdu Jiabao Pharmaceutical Silver Pharmaceutical Technology Co ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

公开了一类具有高活性、高选择性的BTK激酶抑制剂类化合物，及其在制备治疗BTK靶标相关疾病的药物中的应用。具体公开了式(I)所示化合物、其异构体及其药学上可接受的盐。

Description

PCT国内申请，说明书已公开。

Claims (19)

  1. PCT国内申请，权利要求书已公开。
CN202080068213.1A 2019-09-26 2020-09-25 作为选择性btk激酶抑制剂的吡唑并吡啶类化合物 Active CN114450289B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2019109191806 2019-09-26
CN201910919180 2019-09-26
CN202010330226 2020-04-24
CN2020103302263 2020-04-24
PCT/CN2020/117690 WO2021057893A1 (zh) 2019-09-26 2020-09-25 作为选择性btk激酶抑制剂的吡唑并吡啶类化合物

Publications (2)

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CN114450289A true CN114450289A (zh) 2022-05-06
CN114450289B CN114450289B (zh) 2024-01-02

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US (1) US11739090B2 (zh)
EP (1) EP4036095B1 (zh)
JP (1) JP7213604B2 (zh)
KR (1) KR102500569B1 (zh)
CN (1) CN114450289B (zh)
AU (1) AU2020355845B2 (zh)
BR (1) BR112022005729A2 (zh)
CA (1) CA3152587C (zh)
DK (1) DK4036095T3 (zh)
FI (1) FI4036095T3 (zh)
HR (1) HRP20240283T1 (zh)
LT (1) LT4036095T (zh)
MX (1) MX2022003707A (zh)
PL (1) PL4036095T3 (zh)
PT (1) PT4036095T (zh)
RS (1) RS65239B1 (zh)
SI (1) SI4036095T1 (zh)
WO (1) WO2021057893A1 (zh)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024511614A (ja) * 2021-03-23 2024-03-14 成都嘉葆薬銀医薬科技有限公司 フッ素置換ピリドピラゾール系化合物の結晶形及びその製造方法
WO2024022234A1 (zh) * 2022-07-28 2024-02-01 成都嘉葆药银医药科技有限公司 吡唑并吡啶类化合物在制备治疗包括中枢神经系统疾病的btk相关疾病的药物中的用途

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WO2014116504A1 (en) * 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
WO2014199171A1 (en) * 2013-06-12 2014-12-18 Proximagen Limited New therapeutic uses of enzyme inhibitors
US20150152115A1 (en) * 2007-12-27 2015-06-04 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
WO2015095099A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Btk inhibitors
WO2015095102A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Btk inhibitors
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
WO2015169233A1 (zh) * 2014-05-07 2015-11-12 北京赛林泰医药技术有限公司 布鲁顿酪氨酸激酶抑制剂
CN105399756A (zh) * 2014-09-05 2016-03-16 广东东阳光药业有限公司 Btk抑制剂及其用途
WO2016106652A1 (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
WO2017041536A1 (zh) * 2015-09-11 2017-03-16 东莞市真兴贝特医药技术有限公司 氧代二氢咪唑并吡啶类化合物及其应用
CN106588937A (zh) * 2017-01-16 2017-04-26 东莞市真兴贝特医药技术有限公司 咪唑并吡嗪类化合物及其制备方法和应用
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

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WO2016106627A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
MX2018008815A (es) 2016-01-21 2019-03-28 Zibo Biopolar Changsheng Pharmaceutical Co Ltd Inhibidores de tirosina quinasa de bruton.
CN115746000A (zh) * 2016-03-11 2023-03-07 嘉兴和剂药业有限公司 用于调节布鲁顿酪氨酸激酶的化合物及方法
JOP20190113A1 (ar) 2016-11-18 2019-05-15 Biocad Joint Stock Co مثبطات بروتون تيروزين كيناز
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WO2008121742A2 (en) * 2007-03-28 2008-10-09 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US20150152115A1 (en) * 2007-12-27 2015-06-04 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
WO2014082598A1 (en) * 2012-11-30 2014-06-05 Centaurus Biopharma Co., Ltd. Inhibitors of bruton's tyrosine kinase
WO2014116504A1 (en) * 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
WO2014199171A1 (en) * 2013-06-12 2014-12-18 Proximagen Limited New therapeutic uses of enzyme inhibitors
WO2015095102A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Btk inhibitors
WO2015095099A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Btk inhibitors
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
WO2015169233A1 (zh) * 2014-05-07 2015-11-12 北京赛林泰医药技术有限公司 布鲁顿酪氨酸激酶抑制剂
CN105399756A (zh) * 2014-09-05 2016-03-16 广东东阳光药业有限公司 Btk抑制剂及其用途
WO2016106652A1 (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
WO2017041536A1 (zh) * 2015-09-11 2017-03-16 东莞市真兴贝特医药技术有限公司 氧代二氢咪唑并吡啶类化合物及其应用
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
CN106588937A (zh) * 2017-01-16 2017-04-26 东莞市真兴贝特医药技术有限公司 咪唑并吡嗪类化合物及其制备方法和应用

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PT4036095T (pt) 2024-02-19
KR102500569B1 (ko) 2023-02-16
FI4036095T3 (fi) 2024-02-14
EP4036095A4 (en) 2022-12-07
EP4036095A1 (en) 2022-08-03
US11739090B2 (en) 2023-08-29
US20220324864A1 (en) 2022-10-13
KR20220061262A (ko) 2022-05-12
SI4036095T1 (sl) 2024-04-30
WO2021057893A1 (zh) 2021-04-01
RS65239B1 (sr) 2024-03-29
CA3152587C (en) 2023-05-23
LT4036095T (lt) 2024-03-25
AU2020355845A1 (en) 2022-05-19
JP7213604B2 (ja) 2023-01-27
CN114450289B (zh) 2024-01-02
BR112022005729A2 (pt) 2022-06-21
JP2022542196A (ja) 2022-09-29
EP4036095B1 (en) 2024-01-31
PL4036095T3 (pl) 2024-04-15
AU2020355845B2 (en) 2023-04-06
CA3152587A1 (en) 2021-04-01
HRP20240283T1 (hr) 2024-05-10
MX2022003707A (es) 2022-06-23
DK4036095T3 (da) 2024-03-04

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