JP6487925B2 - セリン／トレオニンキナーゼ阻害剤 - Google Patents

セリン／トレオニンキナーゼ阻害剤 Download PDF

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Publication number
JP6487925B2
JP6487925B2 JP2016542969A JP2016542969A JP6487925B2 JP 6487925 B2 JP6487925 B2 JP 6487925B2 JP 2016542969 A JP2016542969 A JP 2016542969A JP 2016542969 A JP2016542969 A JP 2016542969A JP 6487925 B2 JP6487925 B2 JP 6487925B2
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Japan
Prior art keywords
methyl
pyrazol
benzo
triazol
pyrimidin
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JP2016542969A
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Japanese (ja)
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JP2017500364A5 (enExample
JP2017500364A (ja
Inventor
ジェイムズ エフ． ブレイク，
ジェイムズ エフ． ブレイク，
アダム クック，
アダム クック，
インドラニ ダブリュー． グナワルダナ，
インドラニ ダブリュー． グナワルダナ，
ケビン ダブリュー． ハント，
ケビン ダブリュー． ハント，
マイケル ライオン，
マイケル ライオン，
アンドリュー ティー． メトカルフ，
アンドリュー ティー． メトカルフ，
ピーター ジェイ． モール，
ピーター ジェイ． モール，
デイビッド エー． モレノ，
デイビッド エー． モレノ，
ブラッド ニューハウス，
ブラッド ニューハウス，
リ レン，
リ レン，
トニー ピー． タン，
トニー ピー． タン，
アレン エー． トーマス，
アレン エー． トーマス，
ジェイコブ シュワルツ，
ジェイコブ シュワルツ，
ジェーン シュミット，
ジェーン シュミット，
ルイス ガッザード，
ルイス ガッザード，
フイフェン チェン，
フイフェン チェン，
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Genentech Inc
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Genentech Inc
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Publication of JP2017500364A5 publication Critical patent/JP2017500364A5/ja
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
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    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P13/00—Drugs for disorders of the urinary system
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    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61P17/00—Drugs for dermatological disorders
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    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
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    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P35/02—Antineoplastic agents specific for leukemia
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    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Oncology (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)
JP2016542969A 2013-12-30 2014-12-29 セリン／トレオニンキナーゼ阻害剤 Active JP6487925B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361922045P 2013-12-30 2013-12-30
US61/922,045 2013-12-30
PCT/US2014/072547 WO2015103133A1 (en) 2013-12-30 2014-12-29 Serine/threonine kinase inhibitors

Publications (3)

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JP2017500364A JP2017500364A (ja) 2017-01-05
JP2017500364A5 JP2017500364A5 (enExample) 2019-01-24
JP6487925B2 true JP6487925B2 (ja) 2019-03-20

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US (2) US9763942B2 (enExample)
EP (1) EP3089788B1 (enExample)
JP (1) JP6487925B2 (enExample)
KR (1) KR102379517B1 (enExample)
CN (1) CN105848723B (enExample)
BR (1) BR112016015235A2 (enExample)
CA (1) CA2934679C (enExample)
MX (1) MX370906B (enExample)
WO (1) WO2015103133A1 (enExample)

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EA031243B1 (ru) 2013-12-06 2018-12-28 Дженентек, Инк. Ингибиторы серин/треонинкиназ
KR102379517B1 (ko) 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
MX375902B (es) 2013-12-30 2025-03-07 Genentech Inc Inhibidores de serina/treonina cinasa.
SMT202000152T1 (it) 2015-11-09 2020-05-08 Astrazeneca Ab Derivati di diidroimidazopirazinone utili nel trattamento di cancro
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JP7311228B2 (ja) * 2017-06-30 2023-07-19 ベイジン タイド ファーマシューティカル カンパニー リミテッド Ｒｈｏ－関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用
KR102811888B1 (ko) 2017-09-08 2025-05-27 에프. 호프만-라 로슈 아게 암의 진단 및 치료 방법
US20210008047A1 (en) 2018-02-13 2021-01-14 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
CN118286225A (zh) 2018-04-26 2024-07-05 辉瑞公司 作为细胞周期蛋白依赖性激酶抑制剂的2-氨基-吡啶或2-氨基-嘧啶衍生物
KR20210145773A (ko) 2019-03-28 2021-12-02 지앙수 헨그루이 메디슨 컴퍼니 리미티드 티에노헤테로고리형 유도체, 이의 제조 방법 및 이의 의약적 용도
WO2020200069A1 (zh) 2019-03-29 2020-10-08 江苏恒瑞医药股份有限公司 吡咯并杂环类衍生物、其制备方法及其在医药上的应用
EP3978498A1 (en) 2019-05-24 2022-04-06 Jiangsu Hengrui Medicine Co., Ltd. Substituted fused bicyclic derivative, preparation method therefor, and application thereof in medicines
CN110627775B (zh) * 2019-10-24 2026-01-30 特科罗生物科技(成都)有限公司 一种小分子化合物
US20230331731A1 (en) 2020-09-29 2023-10-19 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Crystal form of pyrrolo heterocyclic derivative and preparation method therefor

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US9133187B2 (en) 2011-02-28 2015-09-15 Array Biopharma Inc. Serine/threonine kinase inhibitors
ES2552989T3 (es) * 2011-08-04 2015-12-03 Array Biopharma, Inc. Compuestos de quinazolina como inhibidores de la cinasa de serina / treonina
PE20150666A1 (es) 2012-03-01 2015-05-06 Array Biopharma Inc Inhibidores de serina/treonina cinasa
CA2882750A1 (en) 2012-08-27 2014-03-06 Jim Blake Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases
EA031243B1 (ru) 2013-12-06 2018-12-28 Дженентек, Инк. Ингибиторы серин/треонинкиназ
KR102379517B1 (ko) 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
MX375902B (es) 2013-12-30 2025-03-07 Genentech Inc Inhibidores de serina/treonina cinasa.

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EP3089788A1 (en) 2016-11-09
HK1223877A1 (zh) 2017-08-11
CN105848723A (zh) 2016-08-10
CA2934679A1 (en) 2015-07-09
CA2934679C (en) 2023-02-28
MX2016008449A (es) 2016-10-12
JP2017500364A (ja) 2017-01-05
US20170348310A1 (en) 2017-12-07
CN105848723B (zh) 2019-08-02
WO2015103133A1 (en) 2015-07-09
US9763942B2 (en) 2017-09-19
US20160303126A1 (en) 2016-10-20
MX370906B (es) 2020-01-09
EP3089788B1 (en) 2018-10-24
US10154995B2 (en) 2018-12-18
KR102379517B1 (ko) 2022-03-25
BR112016015235A2 (pt) 2017-08-08
KR20160104003A (ko) 2016-09-02

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