KR20180021740A - 브루톤 티로신 키나제의 억제제 - Google Patents

브루톤 티로신 키나제의 억제제 Download PDF

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KR20180021740A
KR20180021740A KR1020177037849A KR20177037849A KR20180021740A KR 20180021740 A KR20180021740 A KR 20180021740A KR 1020177037849 A KR1020177037849 A KR 1020177037849A KR 20177037849 A KR20177037849 A KR 20177037849A KR 20180021740 A KR20180021740 A KR 20180021740A
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substituted
unsubstituted
compound
carboxamide
alkyl
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Korean (ko)
Inventor
고다나 바빅 아탈라
웨이 첸
쟈오정 제이. 지아
알폰소 포잔
루칼 프란시스코 라베글리아
리카르도 자날레티
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파마싸이클릭스 엘엘씨
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    • CCHEMISTRY; METALLURGY
    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (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)
KR1020177037849A 2015-06-02 2016-06-02 브루톤 티로신 키나제의 억제제 Withdrawn KR20180021740A (ko)

Applications Claiming Priority (13)

Application Number Priority Date Filing Date Title
US201562169945P 2015-06-02 2015-06-02
US201562169941P 2015-06-02 2015-06-02
US201562169935P 2015-06-02 2015-06-02
US62/169,941 2015-06-02
US62/169,935 2015-06-02
US62/169,945 2015-06-02
US201562249336P 2015-11-01 2015-11-01
US201562249340P 2015-11-01 2015-11-01
US201562249338P 2015-11-01 2015-11-01
US62/249,338 2015-11-01
US62/249,336 2015-11-01
US62/249,340 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
KR20180021740A true KR20180021740A (ko) 2018-03-05

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Family Applications (1)

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KR1020177037849A Withdrawn KR20180021740A (ko) 2015-06-02 2016-06-02 브루톤 티로신 키나제의 억제제

Country Status (14)

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

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WO2022071772A1 (ko) * 2020-09-29 2022-04-07 (주)메디톡스 단백질 키나제 저해제 및 그의 용도

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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
JP7301958B2 (ja) 2018-05-25 2023-07-03 オンコキューブ セラピューティクス エルエルシー 新規な抗がん薬候補としての非常に強力なtacc3阻害剤
BR122023024103A2 (pt) 2018-10-15 2024-02-20 Nurix Therapeutics, Inc. Compostos bifuncionais para degradação de btk por meio da via de proteossoma de ubiquitina, composição farmacêutica compreendendo os mesmos, e seus usos
KR102850357B1 (ko) * 2018-10-22 2025-08-27 알루미스 인크. Tyk2 억제제 및 이의 용도
US20220143195A1 (en) * 2019-02-13 2022-05-12 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
MX2021012285A (es) 2019-04-09 2021-12-15 Nurix Therapeutics Inc Compuestos de piperidina 3-sustituidos para inhibicion del protooncogen-b de linfoma de linea b de casitas (cbl-b) y uso de un inhibidor de cbl-b en combinacion con una vacuna contra el cancer y/o con un virus oncolitico.
WO2020236654A1 (en) 2019-05-17 2020-11-26 Nurix Therapeutics, Inc. Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof
US11401267B2 (en) 2019-06-26 2022-08-02 Nurix Therapeutics, Inc. Substituted benzyl-triazole compounds for Cbl-b inhibition, and further uses thereof
AU2020352609A1 (en) 2019-09-24 2022-03-31 Nurix Therapeutics, Inc. Cbl inhibitors and compositions for expansion of immune cells
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
EP4570320A3 (en) 2019-12-04 2025-08-27 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
US20230167099A1 (en) * 2020-06-01 2023-06-01 Wigen Biomedicine Technology (shanghai) Co., Ltd. New pyrazine compound
WO2022217123A2 (en) 2021-04-08 2022-10-13 Nurix Therapeutics, Inc. Combination therapies with cbl-b inhibitor compounds
US20240374590A1 (en) * 2021-04-12 2024-11-14 A2A Pharmaceuticals, Inc. Compositions and methods for treating cancer
JP2024524480A (ja) * 2021-07-01 2024-07-05 ハンチョウ、ヘルズン、セラピューティクス、カンパニー、リミテッド ブルトン型チロシンキナーゼ及びその突然変異体の分解剤、組成物並びにそれらの応用
US12377106B2 (en) 2021-10-26 2025-08-05 Nurix Therapeutics, Inc. Piperidinylpyrazine-carboxamide compounds for treating and preventing cancer and for degrading BTK
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TW202400575A (zh) 2022-03-24 2024-01-01 美商A2A製藥公司 治療癌症的組合物和方法

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AU2014360446A1 (en) * 2013-12-05 2016-06-09 Pharmacyclics, Llc Inhibitors of Bruton's tyrosine kinase

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022071772A1 (ko) * 2020-09-29 2022-04-07 (주)메디톡스 단백질 키나제 저해제 및 그의 용도

Also Published As

Publication number Publication date
EP3310776A4 (en) 2019-01-16
WO2016196776A3 (en) 2017-01-05
AU2016270907B2 (en) 2020-09-17
US20180305348A1 (en) 2018-10-25
MX2017015574A (es) 2018-08-09
SG10201911523YA (en) 2020-02-27
BR112017025986A2 (pt) 2018-08-14
US20210070748A1 (en) 2021-03-11
WO2016196776A2 (en) 2016-12-08
IL255831A (en) 2018-01-31
RU2017145650A (ru) 2019-07-15
EP3310776A2 (en) 2018-04-25
CN107709315A (zh) 2018-02-16
RU2017145650A3 (OSRAM) 2019-11-22
AU2020286332A1 (en) 2021-01-21
CA2987054A1 (en) 2016-12-08
AU2016270907A1 (en) 2017-12-07
MA42623A (fr) 2018-06-20
JP2018522823A (ja) 2018-08-16

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Patent event date: 20171229

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