CN107709315A - 布鲁顿酪氨酸激酶的抑制剂 - Google Patents

布鲁顿酪氨酸激酶的抑制剂 Download PDF

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Publication number
CN107709315A
CN107709315A CN201680035113.2A CN201680035113A CN107709315A CN 107709315 A CN107709315 A CN 107709315A CN 201680035113 A CN201680035113 A CN 201680035113A CN 107709315 A CN107709315 A CN 107709315A
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substituted
unsubstituted
compound
piperidin
phenylamino
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Chinese (zh)
Inventor
戈尔达娜·巴比克·阿塔拉
陈伟
兆忠·J·贾
阿方索·波赞
卢卡尔·弗朗西斯科·拉韦利亚
里卡尔多·扎纳莱蒂
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Pharmacyclics LLC
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Pharmacyclics LLC
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201680035113.2A 2015-06-02 2016-06-02 布鲁顿酪氨酸激酶的抑制剂 Pending CN107709315A (zh)

Applications Claiming Priority (13)

Application Number Priority Date Filing Date Title
US201562169941P 2015-06-02 2015-06-02
US201562169945P 2015-06-02 2015-06-02
US201562169935P 2015-06-02 2015-06-02
US62/169,941 2015-06-02
US62/169,945 2015-06-02
US62/169,935 2015-06-02
US201562249336P 2015-11-01 2015-11-01
US201562249338P 2015-11-01 2015-11-01
US201562249340P 2015-11-01 2015-11-01
US62/249,340 2015-11-01
US62/249,336 2015-11-01
US62/249,338 2015-11-01
PCT/US2016/035489 WO2016196776A2 (en) 2015-06-02 2016-06-02 Inhibitors of bruton's tyrosine kinase

Publications (1)

Publication Number Publication Date
CN107709315A true CN107709315A (zh) 2018-02-16

Family

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CN201680035113.2A Pending CN107709315A (zh) 2015-06-02 2016-06-02 布鲁顿酪氨酸激酶的抑制剂

Country Status (14)

Country Link
US (2) US20180305348A1 (https=)
EP (1) EP3310776A4 (https=)
JP (1) JP2018522823A (https=)
KR (1) KR20180021740A (https=)
CN (1) CN107709315A (https=)
AU (2) AU2016270907B2 (https=)
BR (1) BR112017025986A2 (https=)
CA (1) CA2987054A1 (https=)
IL (1) IL255831A (https=)
MA (1) MA42623A (https=)
MX (1) MX2017015574A (https=)
RU (1) RU2017145650A (https=)
SG (1) SG10201911523YA (https=)
WO (1) WO2016196776A2 (https=)

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Publication number Priority date Publication date Assignee Title
WO2021244505A1 (zh) * 2020-06-01 2021-12-09 微境生物医药科技(上海)有限公司 新型吡嗪化合物
CN115557933A (zh) * 2021-07-01 2023-01-03 杭州和正医药有限公司 布鲁顿酪氨酸激酶及其突变体降解剂、组合物及应用
CN116143757A (zh) * 2021-11-22 2023-05-23 杭州和正医药有限公司 一种可降解btk激酶的多功能化合物、组合物及应用
RU2857201C2 (ru) * 2020-06-01 2026-02-27 Виген Биомедисн Текнолоджи (Шанхай) Ко., Лтд. Новое соединение пиразина

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ES2856248T3 (es) * 2016-12-21 2021-09-27 Acerta Pharma Bv Inhibidores de imidazopirazina de la tirosina quinasa de Bruton
KR101956815B1 (ko) * 2017-02-14 2019-03-12 한국화학연구원 트리아졸로피리다진 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 브루톤티로신 키나제 활성 관련 질환의 예방 또는 치료용 약학적 조성물
CN109384774B (zh) * 2017-08-11 2023-02-17 中国科学院上海药物研究所 一类多取代的吡嗪/三嗪酰胺类化合物及其制备方法和应用
CN108530450B (zh) * 2018-05-03 2021-03-30 赖建智 具有egfr抑制活性的化合物、制备方法及其在疾病治疗中的应用
KR102797697B1 (ko) 2018-05-25 2025-04-22 에이2에이 파마수티칼스, 잉크. 신종 항암제 후보로서, 매우 강력한 tacc3 억제제
JP7600123B2 (ja) 2018-10-15 2024-12-16 ニューリックス セラピューティクス,インコーポレイテッド ユビキチンプロテオソーム経路を介してbtkを分解するための二官能性化合物
AU2019364336B2 (en) 2018-10-22 2023-11-16 Alumis Inc. TYK2 inhibitors and uses thereof
WO2020167518A1 (en) * 2019-02-13 2020-08-20 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP3953346A1 (en) 2019-04-09 2022-02-16 Nurix Therapeutics, Inc. 3-substituted piperidine compounds for cbl-b inhibition, and use of a cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus
EP3969447A1 (en) 2019-05-17 2022-03-23 Nurix Therapeutics, Inc. Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof
MX2021015675A (es) 2019-06-26 2022-02-03 Nurix Therapeutics Inc Compuestos de bencil-triazol sustituidos para la inhibicion de cbl-b y otros usos de los mismos.
EP4034141A1 (en) 2019-09-24 2022-08-03 Nurix Therapeutics, Inc. Cbl inhibitors and compositions for expansion of immune cells
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
US11820781B2 (en) 2019-12-04 2023-11-21 Nurix Therapeutics, Inc. Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2022071772A1 (ko) * 2020-09-29 2022-04-07 (주)메디톡스 단백질 키나제 저해제 및 그의 용도
US12016860B2 (en) 2021-04-08 2024-06-25 Nurix Therapeutics, Inc. Combination therapies with Cbl-b inhibitor compounds
KR20240005751A (ko) * 2021-04-12 2024-01-12 에이2에이 파마수티칼스, 잉크. 암 치료를 위한 조성물 및 방법
AU2022379494A1 (en) 2021-10-26 2024-05-30 Nurix Therapeutics, Inc. Piperidinylpyrazine-carboxamide compounds for treating and preventing cancer and for degrading btk
EP4499625A4 (en) 2022-03-24 2026-03-18 A2A Pharmaceuticals Inc CANCER COMPOSITIONS AND TREATMENT METHODS

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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021244505A1 (zh) * 2020-06-01 2021-12-09 微境生物医药科技(上海)有限公司 新型吡嗪化合物
CN115698000A (zh) * 2020-06-01 2023-02-03 微境生物医药科技(上海)有限公司 新型吡嗪化合物
RU2857201C2 (ru) * 2020-06-01 2026-02-27 Виген Биомедисн Текнолоджи (Шанхай) Ко., Лтд. Новое соединение пиразина
US12600714B2 (en) 2020-06-01 2026-04-14 Wigen Biomedicine Technology (shanghai) Co., Ltd. Substituted pyrazinecarboxamide compounds for treating diseases related to EGFR mutation
CN115557933A (zh) * 2021-07-01 2023-01-03 杭州和正医药有限公司 布鲁顿酪氨酸激酶及其突变体降解剂、组合物及应用
CN115557933B (zh) * 2021-07-01 2024-08-16 杭州和正医药有限公司 布鲁顿酪氨酸激酶及其突变体降解剂、组合物及应用
CN116143757A (zh) * 2021-11-22 2023-05-23 杭州和正医药有限公司 一种可降解btk激酶的多功能化合物、组合物及应用

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EP3310776A2 (en) 2018-04-25
JP2018522823A (ja) 2018-08-16
AU2020286332A1 (en) 2021-01-21
RU2017145650A (ru) 2019-07-15
KR20180021740A (ko) 2018-03-05
IL255831A (en) 2018-01-31
EP3310776A4 (en) 2019-01-16
AU2016270907A1 (en) 2017-12-07
MA42623A (fr) 2018-06-20
WO2016196776A2 (en) 2016-12-08
RU2017145650A3 (https=) 2019-11-22
BR112017025986A2 (pt) 2018-08-14
AU2016270907B2 (en) 2020-09-17
CA2987054A1 (en) 2016-12-08
WO2016196776A3 (en) 2017-01-05
SG10201911523YA (en) 2020-02-27
MX2017015574A (es) 2018-08-09
US20180305348A1 (en) 2018-10-25
US20210070748A1 (en) 2021-03-11

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