TWI672294B - 布魯頓氏酪胺酸激酶之抑制劑 - Google Patents

布魯頓氏酪胺酸激酶之抑制劑 Download PDF

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TWI672294B
TWI672294B TW103142505A TW103142505A TWI672294B TW I672294 B TWI672294 B TW I672294B TW 103142505 A TW103142505 A TW 103142505A TW 103142505 A TW103142505 A TW 103142505A TW I672294 B TWI672294 B TW I672294B
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substituted
unsubstituted
amino
formula
compound
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TW201607937A (zh
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照中 賈
陳偉
威廉Ｄ 湯瑪斯
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美商製藥公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P19/00—Drugs for skeletal disorders
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • 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
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
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    • C07D403/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • C07D417/14—Heterocyclic 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
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    • 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

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  • Chemical & Material Sciences (AREA)
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  • 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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW103142505A 2013-12-05 2014-12-05 布魯頓氏酪胺酸激酶之抑制劑 TWI672294B (zh)

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US201361912483P 2013-12-05 2013-12-05
US61/912,483 2013-12-05

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TWI672294B true TWI672294B (zh) 2019-09-21

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US (5) US9382246B2 (OSRAM)
EP (1) EP3077388A1 (OSRAM)
JP (3) JP6345786B2 (OSRAM)
KR (1) KR20160093675A (OSRAM)
CN (1) CN105960404B (OSRAM)
AR (1) AR099367A1 (OSRAM)
AU (3) AU2014360446A1 (OSRAM)
BR (1) BR112016012728A2 (OSRAM)
CA (1) CA2932609A1 (OSRAM)
MX (2) MX375752B (OSRAM)
TW (2) TWI672294B (OSRAM)
WO (1) WO2015084998A1 (OSRAM)

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JP2018522823A (ja) * 2015-06-02 2018-08-16 ファーマサイクリックス エルエルシー ブルトン型チロシンキナーゼの阻害剤
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CN107445981B (zh) * 2017-08-25 2018-06-22 牡丹江医学院 一种用于防治宫颈炎的活性化合物
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KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
WO2020210508A1 (en) 2019-04-09 2020-10-15 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
CN114206855B (zh) 2019-05-17 2024-11-26 紐力克斯治疗公司 用于Cbl-b抑制的氰基环丁基类化合物及其用途
EP3972963A1 (en) 2019-05-21 2022-03-30 Bayer Aktiengesellschaft Identification and use of kras inhibitors
CN110066259A (zh) * 2019-05-22 2019-07-30 南京合巨药业有限公司 一种n-环戊基-1,1-二氧代-4-硫代吗啉甲酰胺的合成方法
BR112021026241A2 (pt) 2019-06-26 2022-06-07 Nurix Therapeutics Inc Compostos de benzil-triazol substituído para inibição de cbl-b e outros usos dos mesmos
AU2020353015A1 (en) 2019-09-24 2022-03-31 Nurix Therapeutics, Inc. CBL inhibitors and compositions for use in adoptive cell therapy
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
JP2023504147A (ja) * 2019-12-04 2023-02-01 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たｂｔｋの分解のための二官能性化合物
CN111018842B (zh) * 2019-12-04 2021-02-12 宜春市人民医院 一种唑代嘧啶衍生物、其药物组合物和在抗肿瘤中的应用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2022032484A1 (zh) * 2020-08-11 2022-02-17 北京诺诚健华医药科技有限公司 哒嗪-3-甲酰胺类化合物、其制备方法及其在医药学上的应用
WO2022071772A1 (ko) * 2020-09-29 2022-04-07 (주)메디톡스 단백질 키나제 저해제 및 그의 용도
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KR20240029070A (ko) * 2021-07-01 2024-03-05 항저우 힐젠 테라퓨틱스 컴퍼니 리미티드 브루톤 티로신 키나아제, 이의 돌연변이체 분해제, 조성물 및 응용
JP2024542984A (ja) 2021-10-26 2024-11-19 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 がんを治療および予防するためのピペリジニルピラジン－カルボキサミド化合物、およびｂｔｋを分解するためのピペリジニルピラジン－カルボキサミド化合物
CN118598858A (zh) * 2021-11-22 2024-09-06 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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CN115417827B (zh) * 2022-09-30 2023-05-26 中国药科大学 6-氨基-1,3,5-三嗪类化合物及其合成方法和应用
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