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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JP2017500364A (ja
JP2017500364A5 (OSRAM
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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—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
    • A—HUMAN NECESSITIES
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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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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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    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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    • A61P13/00—Drugs for disorders of the urinary system
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
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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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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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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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    • C07D401/14—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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    • 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)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (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

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

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

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CR20160309A (es) 2013-12-06 2016-08-25 Genentech Inc Inhibidores de serina/treonina cinasa
JP6487925B2 (ja) 2013-12-30 2019-03-20 ジェネンテック， インコーポレイテッド セリン／トレオニンキナーゼ阻害剤
WO2015103137A1 (en) 2013-12-30 2015-07-09 Array Biopharma Inc. Serine/threonine kinase inhibitors
TWI730012B (zh) 2015-11-09 2021-06-11 瑞典商阿斯特捷利康公司 化學化合物
MX2018012471A (es) 2016-04-15 2019-02-21 Genentech Inc Metodos de diagnostico y terapeuticos para el cancer.
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TW202428305A (zh) 2017-09-08 2024-07-16 美商建南德克公司 癌症之診斷及治療方法
US20210008047A1 (en) 2018-02-13 2021-01-14 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
GEP20227433B (en) 2018-04-26 2022-10-25 Pfizer 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors
WO2020192750A1 (zh) 2019-03-28 2020-10-01 江苏恒瑞医药股份有限公司 噻吩并杂环类衍生物、其制备方法及其在医药上的应用
MX2021011823A (es) 2019-03-29 2021-10-22 Jiangsu Hengrui Medicine Co Derivado pirroloheterociclico, metodo de preparacion del mismo y su aplicacion en medicina.
JP2022534224A (ja) 2019-05-24 2022-07-28 江蘇恒瑞医薬股▲ふん▼有限公司 置換縮合二環式誘導体、その調製方法、および医薬におけるその適用
CN110627775A (zh) * 2019-10-24 2019-12-31 嘉兴特科罗生物科技有限公司 一种小分子化合物
CN116437915B (zh) 2020-09-29 2025-03-18 江苏恒瑞医药股份有限公司 一种吡咯并杂环类衍生物的晶型及其制备方法

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JP6085866B2 (ja) 2011-02-28 2017-03-01 アレイ バイオファーマ、インコーポレイテッド セリン／トレオニンキナーゼインヒビター
BR112014002675A2 (pt) * 2011-08-04 2017-02-21 Array Biopharma Inc "quinazolina como inibidores de serina/treonina quinase, seus usos, e composição"
PL2820009T3 (pl) 2012-03-01 2018-09-28 Array Biopharma, Inc. Inhibitory kinaz serynowo/treoninowych
CA2882750A1 (en) 2012-08-27 2014-03-06 Jim Blake Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases
CR20160309A (es) 2013-12-06 2016-08-25 Genentech Inc Inhibidores de serina/treonina cinasa
JP6487925B2 (ja) 2013-12-30 2019-03-20 ジェネンテック， インコーポレイテッド セリン／トレオニンキナーゼ阻害剤
WO2015103137A1 (en) 2013-12-30 2015-07-09 Array Biopharma Inc. Serine/threonine kinase inhibitors

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

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