CA2934709C - Serine/threonine kinase inhibitors - Google Patents

Serine/threonine kinase inhibitors Download PDF

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Publication number
CA2934709C
CA2934709C CA2934709A CA2934709A CA2934709C CA 2934709 C CA2934709 C CA 2934709C CA 2934709 A CA2934709 A CA 2934709A CA 2934709 A CA2934709 A CA 2934709A CA 2934709 C CA2934709 C CA 2934709C
Authority
CA
Canada
Prior art keywords
pyrazol
pyridin
triazolo
amine
methyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CA2934709A
Other languages
English (en)
French (fr)
Other versions
CA2934709A1 (en
Inventor
James F. Blake
Adam Cook
John Gaudino
Indrani W. Gunawardana
Erik James Hicken
Kevin W. Hunt
Michael Lyon
Andrew T. Metcalf
Peter J. Mohr
David A. Moreno
Brad Newhouse
Li Ren
Jacob Schwarz
Huifen Chen
Lewis Gazzard
Jane Schmidt
Steve Do
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
Array Biopharma Inc
Original Assignee
Genentech Inc
Array Biopharma Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Genentech Inc, Array Biopharma Inc filed Critical Genentech Inc
Publication of CA2934709A1 publication Critical patent/CA2934709A1/en
Application granted granted Critical
Publication of CA2934709C publication Critical patent/CA2934709C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
CA2934709A 2013-12-30 2014-12-29 Serine/threonine kinase inhibitors Active CA2934709C (en)

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
CA2934709A1 CA2934709A1 (en) 2015-07-09
CA2934709C true CA2934709C (en) 2022-08-30

Family

ID=52347479

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2934709A Active CA2934709C (en) 2013-12-30 2014-12-29 Serine/threonine kinase inhibitors

Country Status (9)

Country Link
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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DK2820009T3 (en) * 2012-03-01 2018-04-16 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
CN106029672B (zh) 2013-12-06 2019-03-29 基因泰克公司 丝氨酸/苏氨酸激酶抑制剂
BR112016015235A2 (pt) 2013-12-30 2017-08-08 Genentech Inc Composto, composição farmacêutica, método de inibição da atividade da proteína quinase erk e método de tratamento
CA3217238A1 (en) 2015-07-20 2017-01-26 Genzyme Corporation Colony stimulating factor-1 receptor (csf-1r) inhibitors
LT3374359T (lt) 2015-11-09 2020-03-25 Astrazeneca Ab Dihidroimidazopirazinono deriniai, tinkami panaudoti vėžio gydymui
KR20180134347A (ko) 2016-04-15 2018-12-18 제넨테크, 인크. 암의 진단 및 치료 방법
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
WO2017221092A1 (en) * 2016-06-20 2017-12-28 Novartis Ag Triazolopyridine compounds and uses thereof
ES2975263T3 (es) 2016-06-20 2024-07-04 Novartis Ag Formas cristalinas de un compuesto triazolopirimidínico
EP3472166A1 (en) 2016-06-20 2019-04-24 Novartis AG Imidazopyrimidine compounds useful for the treatment of cancer
JP2019534266A (ja) 2016-10-14 2019-11-28 江蘇恒瑞医薬股▲ふん▼有限公司 ５員ヘテロアリール環の架橋した環誘導体、その製造方法およびその医学的使用
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
US11937503B2 (en) * 2017-11-30 2024-03-19 Universal Display Corporation Organic electroluminescent materials and devices
EP3752200A1 (en) 2018-02-13 2020-12-23 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
PH12021553058A1 (en) 2019-06-06 2022-07-25 Hutchison Medipharma Ltd Tricyclic compounds and their use
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
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
WO2022226172A1 (en) * 2021-04-21 2022-10-27 The Regents Of The University Of California Compositions and methods for treating neurodegenerative diseases

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US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
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EP2681215B1 (en) 2011-02-28 2015-04-22 Array Biopharma, Inc. Serine/threonine kinase inhibitors
US9187462B2 (en) 2011-08-04 2015-11-17 Array Biopharma Inc. Substituted quinazolines as serine/threonine kinase inhibitors
DK2820009T3 (en) * 2012-03-01 2018-04-16 Array Biopharma Inc Serine / threonine kinase inhibitors
TW201408658A (zh) 2012-08-27 2014-03-01 Array Biopharma Inc 絲胺酸／酥胺酸激酶抑制劑
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
CN106029672B (zh) * 2013-12-06 2019-03-29 基因泰克公司 丝氨酸/苏氨酸激酶抑制剂
BR112016015235A2 (pt) 2013-12-30 2017-08-08 Genentech Inc Composto, composição farmacêutica, método de inibição da atividade da proteína quinase erk e método de tratamento

Also Published As

Publication number Publication date
CN105980387B (zh) 2019-04-19
WO2015103137A1 (en) 2015-07-09
US20160304519A1 (en) 2016-10-20
CA2934709A1 (en) 2015-07-09
US9670208B2 (en) 2017-06-06
JP6642942B2 (ja) 2020-02-12
CN105980387A (zh) 2016-09-28
BR112016015236A8 (pt) 2018-04-24
KR20160104036A (ko) 2016-09-02
JP2017502049A (ja) 2017-01-19
BR112016015236B1 (pt) 2023-11-14
MX2016008624A (es) 2017-01-06
EP3089980A1 (en) 2016-11-09
HK1225735A1 (zh) 2017-09-15
BR112016015236A2 (pt) 2018-01-23
KR102396710B1 (ko) 2022-05-10
EP3089980B1 (en) 2018-01-31
MX375902B (es) 2025-03-07

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