CN112135826A - 氨基降茨烷衍生物及其制备方法与应用 - Google Patents

氨基降茨烷衍生物及其制备方法与应用 Download PDF

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CN112135826A
CN112135826A CN201980029247.7A CN201980029247A CN112135826A CN 112135826 A CN112135826 A CN 112135826A CN 201980029247 A CN201980029247 A CN 201980029247A CN 112135826 A CN112135826 A CN 112135826A
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CN112135826B (zh
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陈荣耀
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Yaojie Ankang (Nanjing) Technology Co.,Ltd.
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Nanjing Transthera Biosciences Co Ltd
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    • 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
    • A61K31/535—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
    • 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
    • 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
    • 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

Abstract

本发明涉及式I结构的化合物或其药学上可接受的盐、溶剂化物、活性代谢物、多晶型物、酯、光学异构体或前药，包含式I结构的化合物的药物组合物及其作为BTK(C481S)突变体高选择性的布鲁顿酪氨酸激酶抑制剂用于制备预防或治疗异种免疫性疾病、自身免疫性疾病或癌症的药物的用途。
Figure DDA0002750974940000011

Description

PCT国内申请，说明书已公开。

Claims (22)

  1. PCT国内申请，权利要求书已公开。
CN201980029247.7A 2018-09-29 2019-07-05 氨基降茨烷衍生物及其制备方法与应用 Active CN112135826B (zh)

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CN2018111531233 2018-09-29
CN201811153123.3A CN110964016B (zh) 2018-09-29 2018-09-29 氨基降茨烷衍生物及其制备方法与应用
PCT/CN2019/094864 WO2020063012A1 (zh) 2018-09-29 2019-07-05 氨基降茨烷衍生物及其制备方法与应用

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US20230145305A1 (en) * 2020-03-12 2023-05-11 Fochon Biosciences, Ltd. Compounds useful as kinase inhibitors
CN114075190A (zh) * 2020-08-20 2022-02-22 北京诺诚健华医药科技有限公司 杂环类btk抑制剂
CN114634512B (zh) * 2020-12-16 2023-11-14 江苏恒瑞医药股份有限公司 作为布鲁顿酪氨酸激酶抑制剂的化合物、其制备方法和医药应用
CN115417789B (zh) * 2022-09-03 2023-08-04 郑州大学 一种治疗帕金森氏病的化合物、其制备方法以及复方药物组合物和应用
WO2024088311A1 (zh) * 2022-10-26 2024-05-02 药捷安康(南京)科技股份有限公司 咪唑并吡嗪衍生物的晶型及其制备方法和应用

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WO2017161002A1 (en) * 2016-03-16 2017-09-21 Kura Oncology, Inc. Bridged bicyclic inhibitors of menin-mll and methods of use
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US7514444B2 (en) * 2006-09-22 2009-04-07 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US7718662B1 (en) * 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
EP2548877A1 (en) * 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
US8501724B1 (en) 2012-01-31 2013-08-06 Pharmacyclics, Inc. Purinone compounds as kinase inhibitors
KR102181915B1 (ko) 2012-11-13 2020-11-23 어레이 바이오파마 인크. Trka 키나아제 억제제로서 n-피롤리디닐, n'-피라졸릴-우레아, 티오우레아, 구아니딘 및 시아노구아니딘 화합물
US9624224B2 (en) * 2013-09-30 2017-04-18 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
EP3174539A4 (en) 2014-08-01 2017-12-13 Pharmacyclics, LLC Inhibitors of bruton's tyrosine kinase
US10611766B2 (en) 2015-09-16 2020-04-07 Loxo Oncology Inc. Pyrazolopyrimidine derivatives as BTK inhibitors for the treatment of cancer
CN107459521B (zh) * 2016-06-03 2021-04-16 合肥中科普瑞昇生物医药科技有限公司 Flt3激酶的新型抑制剂及其用途

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WO2016109222A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Tertiary alcohol imidazopyrazine btk inhibitors
WO2016109223A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Benzamide imidazopyrazine btk inhibitors
WO2017161002A1 (en) * 2016-03-16 2017-09-21 Kura Oncology, Inc. Bridged bicyclic inhibitors of menin-mll and methods of use
CN106831789A (zh) * 2016-12-21 2017-06-13 南京亘泰医药技术有限公司 布鲁顿酪氨酸激酶抑制剂
CN107602564A (zh) * 2017-09-20 2018-01-19 南京亘泰医药技术有限公司 布鲁顿酪氨酸激酶抑制剂

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EP3858833A4 (en) 2022-06-22
EP3858833A1 (en) 2021-08-04
MX2021003662A (es) 2021-05-28
CN110964016A (zh) 2020-04-07
CN110964016B (zh) 2021-05-28
US20220144843A1 (en) 2022-05-12
JP2022501403A (ja) 2022-01-06
JP7370617B2 (ja) 2023-10-30
US11420975B2 (en) 2022-08-23
AU2019348752B2 (en) 2024-03-28
BR112021005960A2 (pt) 2021-07-13
CA3114259A1 (en) 2020-04-02
CN112135826B (zh) 2021-05-28
KR20210070304A (ko) 2021-06-14
AU2019348752A1 (en) 2021-05-06
WO2020063012A1 (zh) 2020-04-02

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