CN105980387B - 丝氨酸/苏氨酸激酶抑制剂 - Google Patents

丝氨酸/苏氨酸激酶抑制剂 Download PDF

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Publication number
CN105980387B
CN105980387B CN201480074279.6A CN201480074279A CN105980387B CN 105980387 B CN105980387 B CN 105980387B CN 201480074279 A CN201480074279 A CN 201480074279A CN 105980387 B CN105980387 B CN 105980387B
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China
Prior art keywords
base
methyl
triazol
pyrazoles
pyrimidine
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CN201480074279.6A
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English (en)
Chinese (zh)
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CN105980387A (zh
Inventor
J·F·布莱克
A·库克
J·高迪诺
I·W·古纳瓦德纳
E·J·希肯
K·W·亨特
M·里昂
A·T·梅特卡夫
P·J·莫尔
D·A·莫雷诺
B·纽豪斯
L·任
J·施瓦兹
H·陈
L·加扎尔
J·施密特
S·多
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Genentech Inc
Array Biopharma Inc
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Genentech Inc
Array Biopharma Inc
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    • 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
    • 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/444—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
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (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)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
CN201480074279.6A 2013-12-30 2014-12-29 丝氨酸/苏氨酸激酶抑制剂 Active CN105980387B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361922042P 2013-12-30 2013-12-30
US61/922,042 2013-12-30
PCT/US2014/072555 WO2015103137A1 (en) 2013-12-30 2014-12-29 Serine/threonine kinase inhibitors

Publications (2)

Publication Number Publication Date
CN105980387A CN105980387A (zh) 2016-09-28
CN105980387B true CN105980387B (zh) 2019-04-19

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Country Status (9)

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US (1) US9670208B2 (enExample)
EP (1) EP3089980B1 (enExample)
JP (1) JP6642942B2 (enExample)
KR (1) KR102396710B1 (enExample)
CN (1) CN105980387B (enExample)
BR (1) BR112016015236B1 (enExample)
CA (1) CA2934709C (enExample)
MX (1) MX375902B (enExample)
WO (1) WO2015103137A1 (enExample)

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AU2013225737B2 (en) * 2012-03-01 2018-03-01 Array Biopharma Inc. Serine/threonine kinase inhibitors
MX2015004615A (es) 2012-10-16 2015-07-17 Hoffmann La Roche Inhibidores de serina/treonina cinasa.
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
JP6449293B2 (ja) 2013-12-06 2019-01-09 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
WO2015103133A1 (en) 2013-12-30 2015-07-09 Genentech, Inc. Serine/threonine kinase inhibitors
TN2018000020A1 (en) * 2015-07-20 2019-07-08 Genzyme Corp Colony stimulating factor-1 receptor (csf-1r) inhibitors.
SI3374359T1 (sl) 2015-11-09 2020-04-30 Astrazeneca Ab Derivati dihidroimidazopirazinona uporabni pri zdravljenju raka
WO2017180581A1 (en) 2016-04-15 2017-10-19 Genentech, Inc. Diagnostic and therapeutic methods for cancer
CN107383002B (zh) * 2016-05-17 2021-07-13 中国科学院上海药物研究所 一类含氟三氮唑并吡啶类化合物及其制备方法、药物组合物和用途
CA3027246A1 (en) 2016-06-20 2017-12-28 Novartis Ag Crystalline forms of triazolopyrimidine compound
JP2019524872A (ja) 2016-06-20 2019-09-05 ノバルティス アーゲー 癌の治療に有用なイミダゾピリミジン化合物
JP2019522049A (ja) * 2016-06-20 2019-08-08 ノバルティス アーゲー トリアゾロピリジン化合物及びその使用
US10906905B2 (en) 2016-10-14 2021-02-02 Jiangsu Hengrui Medicine Co., Ltd. Five-membered heteroaryl ring bridged ring derivative, preparation method therefor and medical use thereof
ES2969536T3 (es) * 2017-06-30 2024-05-21 Beijing Tide Pharmaceutical Co Ltd Inhibidor de la proteína cinasa asociada a rho, composición farmacéutica que lo comprende, y su método de preparación y uso
EP3679159A1 (en) 2017-09-08 2020-07-15 H. Hoffnabb-La Roche Ag Diagnostic and therapeutic methods for cancer
US11937503B2 (en) * 2017-11-30 2024-03-19 Universal Display Corporation Organic electroluminescent materials and devices
WO2019158579A1 (en) 2018-02-13 2019-08-22 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
TWI879771B (zh) 2019-06-06 2025-04-11 大陸商和記黃埔醫藥（上海）有限公司 三環類化合物及其用途
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
CN112159421A (zh) * 2020-10-10 2021-01-01 珠海奥博凯生物医药技术有限公司 一种2-氟-4-甲基-3-吡啶硼酸的制备方法
JP2024500919A (ja) 2020-12-23 2024-01-10 ジェンザイム・コーポレーション 重水素化コロニー刺激因子－１受容体（ｃｓｆ－１ｒ）阻害剤
EP4326712A4 (en) * 2021-04-21 2025-03-05 The Regents of The University of California COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES

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WO2012118850A1 (en) * 2011-02-28 2012-09-07 Array Biopharma Inc. Serine/threonine kinase inhibitors
WO2013020062A1 (en) * 2011-08-04 2013-02-07 Array Biopharma Inc. Quinazoline compounds as serine/threonine kinase inhibitors
WO2013130976A1 (en) * 2012-03-01 2013-09-06 Array Biopharma Inc. Serine/threonine kinase inhibitors

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BR112015004548A2 (pt) 2012-08-27 2017-08-08 Array Biopharma Inc inibidores de serina/treonina para tratamento de doenças hiperproliferativas
US9532987B2 (en) * 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
JP6449293B2 (ja) 2013-12-06 2019-01-09 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
WO2015103133A1 (en) 2013-12-30 2015-07-09 Genentech, Inc. Serine/threonine kinase inhibitors

Patent Citations (4)

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Publication number Priority date Publication date Assignee Title
WO2003044021A2 (en) * 2001-11-16 2003-05-30 Amgen Inc. Substituted indolizine-like compounds and methods of use
WO2012118850A1 (en) * 2011-02-28 2012-09-07 Array Biopharma Inc. Serine/threonine kinase inhibitors
WO2013020062A1 (en) * 2011-08-04 2013-02-07 Array Biopharma Inc. Quinazoline compounds as serine/threonine kinase inhibitors
WO2013130976A1 (en) * 2012-03-01 2013-09-06 Array Biopharma Inc. Serine/threonine kinase inhibitors

Also Published As

Publication number Publication date
HK1225735A1 (zh) 2017-09-15
MX2016008624A (es) 2017-01-06
CA2934709C (en) 2022-08-30
BR112016015236A2 (pt) 2018-01-23
WO2015103137A1 (en) 2015-07-09
US20160304519A1 (en) 2016-10-20
KR102396710B1 (ko) 2022-05-10
BR112016015236A8 (pt) 2018-04-24
BR112016015236B1 (pt) 2023-11-14
EP3089980A1 (en) 2016-11-09
CA2934709A1 (en) 2015-07-09
CN105980387A (zh) 2016-09-28
JP2017502049A (ja) 2017-01-19
KR20160104036A (ko) 2016-09-02
US9670208B2 (en) 2017-06-06
EP3089980B1 (en) 2018-01-31
MX375902B (es) 2025-03-07
JP6642942B2 (ja) 2020-02-12

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