JP2018522823A - ブルトン型チロシンキナーゼの阻害剤 - Google Patents

ブルトン型チロシンキナーゼの阻害剤 Download PDF

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Publication number
JP2018522823A
JP2018522823A JP2017560655A JP2017560655A JP2018522823A JP 2018522823 A JP2018522823 A JP 2018522823A JP 2017560655 A JP2017560655 A JP 2017560655A JP 2017560655 A JP2017560655 A JP 2017560655A JP 2018522823 A JP2018522823 A JP 2018522823A
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substituted
unsubstituted
carboxamide
compound
piperidin
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Japanese (ja)
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JP2018522823A5 (enExample
Inventor
アタッラー，ゴルダナ，バビチ
チェン，ウェイ
ジア，チャオチョン，ジェイ．
ポザン，アルフォンソ
ラヴェグリア，ルカル，フランチェスコ
ゼナレッティ，リカルド
Original Assignee
ファーマサイクリックス エルエルシー
ファーマサイクリックス エルエルシー
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Publication of JP2018522823A publication Critical patent/JP2018522823A/ja
Publication of JP2018522823A5 publication Critical patent/JP2018522823A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • 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
    • 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
    • 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
    • A61K31/53—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • 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
    • C07D401/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • 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
    • 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
    • C07D471/08—Bridged 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)
  • Pain & Pain Management (AREA)
  • Epidemiology (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)
JP2017560655A 2015-06-02 2016-06-02 ブルトン型チロシンキナーゼの阻害剤 Pending JP2018522823A (ja)

Applications Claiming Priority (13)

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

Publications (2)

Publication Number Publication Date
JP2018522823A true JP2018522823A (ja) 2018-08-16
JP2018522823A5 JP2018522823A5 (enExample) 2019-07-04

Family

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Family Applications (1)

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JP2017560655A Pending JP2018522823A (ja) 2015-06-02 2016-06-02 ブルトン型チロシンキナーゼの阻害剤

Country Status (14)

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

Cited By (1)

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JP2022505987A (ja) * 2018-10-22 2022-01-14 エスカー セラピューティクス，インコーポレイテッド Ｔｙｋ２阻害剤およびその使用

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US10858364B2 (en) * 2016-12-21 2020-12-08 Acerta Pharma B.V. Imidazopyrazine inhibitors of Bruton's tyrosine kinase
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
EP3867242A1 (en) 2018-10-15 2021-08-25 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
WO2020167518A1 (en) * 2019-02-13 2020-08-20 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
US11464802B2 (en) 2019-04-09 2022-10-11 Nurix Therapeutics, Inc. 3-substituted piperidine compounds for Cbl-b inhibition, and use thereof
AU2020278592B2 (en) 2019-05-17 2024-10-10 Nurix Therapeutics, Inc. Cyano cyclobutyl compounds for Cbl-b inhibition and uses thereof
CN114364670B (zh) 2019-06-26 2025-06-13 纽力克斯治疗公司 用于Cbl-b抑制的取代苄基-三唑类化合物及其进一步用途
JP2022549303A (ja) 2019-09-24 2022-11-24 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 免疫細胞を拡大増殖するためのｃｂｌ阻害剤および組成物
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
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
BR112022022220A2 (pt) * 2020-06-01 2022-12-13 Wigen Biomedicine Tech Shanghai Co Ltd Composto, composição farmacêutica, uso do composto, e método para tratar, regular e/ou prevenir uma doença relacionada a uma proteína mutante de egfr
WO2022071772A1 (ko) * 2020-09-29 2022-04-07 (주)메디톡스 단백질 키나제 저해제 및 그의 용도
AU2022254104A1 (en) 2021-04-08 2023-10-26 Nurix Therapeutics, Inc. Combination therapies with cbl-b inhibitor compounds
EP4323351A4 (en) * 2021-04-12 2025-07-30 A2A Pharmaceuticals Inc COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER
US20240360146A1 (en) * 2021-07-01 2024-10-31 Hangzhou Healzen Therapeutics Co., Ltd. Bruton's tyrosine kinase and mutant degrader, composition and application thereof
KR20240090898A (ko) 2021-10-26 2024-06-21 누릭스 테라퓨틱스 인코포레이티드 암을 치료 및 예방하고 btk를 분해하기 위한 피페리디닐피라진-카복스아미드 화합물
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
WO2023183520A1 (en) 2022-03-24 2023-09-28 A2A Pharmaceuticals, Inc. Compositions and methods for treating cancer

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US20130345191A1 (en) * 2012-06-22 2013-12-26 Portola Pharmaceuticals, Inc. 1,2,4-triazine-6-carboxamide kinase inhibitors
WO2014135473A1 (en) * 2013-03-05 2014-09-12 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
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JP2001055378A (ja) * 1999-06-09 2001-02-27 Yamanouchi Pharmaceut Co Ltd 新規なヘテロ環カルボキサミド誘導体
WO2012053606A1 (ja) * 2010-10-22 2012-04-26 アステラス製薬株式会社 アリールアミノヘテロ環カルボキサミド化合物
WO2013047813A1 (ja) * 2011-09-30 2013-04-04 大鵬薬品工業株式会社 １，２，４－トリアジン－６－カルボキサミド誘導体
WO2013052394A1 (en) * 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
JP2014533731A (ja) * 2011-11-23 2014-12-15 ポートラ ファーマシューティカルズ， インコーポレイテッド ピラジンキナーゼ阻害剤
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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022505987A (ja) * 2018-10-22 2022-01-14 エスカー セラピューティクス，インコーポレイテッド Ｔｙｋ２阻害剤およびその使用
JP7631193B2 (ja) 2018-10-22 2025-02-18 アルミス インコーポレイテッド Ｔｙｋ２阻害剤およびその使用
US12351572B2 (en) 2018-10-22 2025-07-08 Alumis Inc. Substituted 1,2,4-triazoles as TYK2 inhibitors

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US20180305348A1 (en) 2018-10-25
EP3310776A4 (en) 2019-01-16
WO2016196776A2 (en) 2016-12-08
AU2020286332A1 (en) 2021-01-21
SG10201911523YA (en) 2020-02-27
WO2016196776A3 (en) 2017-01-05
IL255831A (en) 2018-01-31
MA42623A (fr) 2018-06-20
CA2987054A1 (en) 2016-12-08
RU2017145650A3 (enExample) 2019-11-22
KR20180021740A (ko) 2018-03-05
RU2017145650A (ru) 2019-07-15
AU2016270907A1 (en) 2017-12-07
BR112017025986A2 (pt) 2018-08-14
US20210070748A1 (en) 2021-03-11
CN107709315A (zh) 2018-02-16
AU2016270907B2 (en) 2020-09-17
EP3310776A2 (en) 2018-04-25
MX2017015574A (es) 2018-08-09

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