CA2828478C - Serine/threonine kinase inhibitors - Google Patents

Serine/threonine kinase inhibitors Download PDF

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Publication number
CA2828478C
CA2828478C CA2828478A CA2828478A CA2828478C CA 2828478 C CA2828478 C CA 2828478C CA 2828478 A CA2828478 A CA 2828478A CA 2828478 A CA2828478 A CA 2828478A CA 2828478 C CA2828478 C CA 2828478C
Authority
CA
Canada
Prior art keywords
dihydro
pyrido
pyrimidine
alkyl
carboxylic acid
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.)
Expired - Fee Related
Application number
CA2828478A
Other languages
English (en)
French (fr)
Other versions
CA2828478A1 (en
Inventor
James F. Blake
Huifen Chen
Mark Joseph Chicarelli
Jason DeMeese
Rustam Garrey
John J. Gaudino
Robert J. Kaus
Gabrielle R. Kolakowski
Allison L. Marlow
Peter J. Mohr
Li Ren
Jacob Schwarz
Christopher S. SIEDEM
Allen A. Thomas
Eli Wallace
Steven Mark Wenglowsky
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 CA2828478A1 publication Critical patent/CA2828478A1/en
Application granted granted Critical
Publication of CA2828478C publication Critical patent/CA2828478C/en
Expired - Fee Related 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2828478A 2011-02-28 2012-02-28 Serine/threonine kinase inhibitors Expired - Fee Related CA2828478C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161447587P 2011-02-28 2011-02-28
US61/447,587 2011-02-28
PCT/US2012/027009 WO2012118850A1 (en) 2011-02-28 2012-02-28 Serine/threonine kinase inhibitors

Publications (2)

Publication Number Publication Date
CA2828478A1 CA2828478A1 (en) 2012-09-07
CA2828478C true CA2828478C (en) 2019-12-31

Family

ID=45852719

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2828478A Expired - Fee Related CA2828478C (en) 2011-02-28 2012-02-28 Serine/threonine kinase inhibitors

Country Status (11)

Country Link
US (1) US9133187B2 (2)
EP (1) EP2681215B1 (2)
JP (1) JP6085866B2 (2)
KR (1) KR101961500B1 (2)
CN (1) CN103635472B (2)
BR (1) BR112013021896A2 (2)
CA (1) CA2828478C (2)
ES (1) ES2543050T3 (2)
MX (1) MX339873B (2)
RU (1) RU2013143839A (2)
WO (1) WO2012118850A1 (2)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2681215B1 (en) 2011-02-28 2015-04-22 Array Biopharma, Inc. Serine/threonine kinase inhibitors
JP2014527511A (ja) 2011-06-24 2014-10-16 アムジエン・インコーポレーテツド Ｔｒｐｍ８拮抗剤及び治療におけるそれらの使用
EP2723718A1 (en) 2011-06-24 2014-04-30 Amgen Inc. Trpm8 antagonists and their use in treatments
US9187462B2 (en) 2011-08-04 2015-11-17 Array Biopharma Inc. Substituted quinazolines as serine/threonine kinase inhibitors
EP2797880B1 (en) * 2011-12-27 2017-03-01 Bio-Pharm Solutions Co., Ltd. Phenyl carbamate compounds for use in preventing or treating epilepsy
DK2820009T3 (en) 2012-03-01 2018-04-16 Array Biopharma Inc Serine / threonine kinase inhibitors
US8952009B2 (en) 2012-08-06 2015-02-10 Amgen Inc. Chroman derivatives as TRPM8 inhibitors
TW201408658A (zh) 2012-08-27 2014-03-01 Array Biopharma Inc 絲胺酸／酥胺酸激酶抑制劑
AU2013318283A1 (en) * 2012-09-19 2015-03-05 Novartis Ag Dihydropyrrolidino-pyrimidines as kinase inhibitors
MX2015004615A (es) 2012-10-16 2015-07-17 Hoffmann La Roche Inhibidores de serina/treonina cinasa.
JPWO2015012328A1 (ja) * 2013-07-24 2017-03-02 武田薬品工業株式会社 複素環化合物
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
JP6642942B2 (ja) 2013-12-30 2020-02-12 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阻害剤
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
KR20180134347A (ko) 2016-04-15 2018-12-18 제넨테크, 인크. 암의 진단 및 치료 방법
KR102444509B1 (ko) * 2016-05-18 2022-09-19 미라티 테라퓨틱스, 인크. Kras g12c 억제제
KR102811888B1 (ko) 2017-09-08 2025-05-27 에프. 호프만-라 로슈 아게 암의 진단 및 치료 방법
WO2019065954A1 (ja) 2017-09-29 2019-04-04 田辺三菱製薬株式会社 光学活性ピロリジン化合物及びその製造方法
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3752200A1 (en) 2018-02-13 2020-12-23 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
BR112021017957A2 (pt) 2019-03-28 2021-11-23 Jiangsu Hengrui Medicine Co Derivado tienoeterocíclico, método de preparação do mesmo e uso médico do mesmo
BR112021018924A2 (pt) 2019-03-29 2022-02-01 Jiangsu Hengrui Medicine Co Derivado de heterocíclico pirrol, método de preparação do mesmo e aplicação do mesmo em medicamento
TW202110848A (zh) 2019-05-24 2021-03-16 大陸商江蘇恆瑞醫藥股份有限公司 取代的稠合雙環類衍生物、其製備方法及其在醫藥上的應用
TW202110837A (zh) * 2019-05-24 2021-03-16 大陸商江蘇恆瑞醫藥股份有限公司 氫化吡啶并嘧啶類衍生物、其製備方法及其在醫藥上的應用
CN111170929A (zh) * 2019-12-12 2020-05-19 北京达因高科儿童药物研究院有限公司 一种由末端烯烃制备β-氨基醇的方法
AU2021350161A1 (en) * 2020-09-25 2023-06-08 Janssen Pharmaceutica Nv Cyclin-dependent kinase 7 (cdk7) non-covalent inhibitors
WO2022068860A1 (zh) 2020-09-29 2022-04-07 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
CN115040522B (zh) * 2022-06-30 2024-02-06 牡丹江医学院 一种用于治疗肺癌的药物及其制备方法
CN119894886A (zh) * 2022-10-25 2025-04-25 上海拓界生物医药科技有限公司 哌啶并嘧啶类衍生物、其制备方法及其在医药上的应用
IT202200024963A1 (it) * 2022-12-05 2024-06-05 Angelini Pharma S P A Composti attivatori dei canali potassio Kv7.2/Kv7.3
WO2025087267A1 (zh) * 2023-10-23 2025-05-01 上海拓界生物医药科技有限公司 一种含有噻唑基的哌啶并嘧啶类衍生物、其制备方法及其医药上的应用
WO2025223512A1 (zh) * 2024-04-24 2025-10-30 江苏恒瑞医药股份有限公司 一种二氢吡啶并嘧啶衍生物的可药用盐、结晶形式及用途
WO2026067627A1 (zh) * 2024-09-26 2026-04-02 江苏恒瑞医药股份有限公司 一种降解剂及其用途

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995009847A1 (en) 1993-10-01 1995-04-13 Ciba-Geigy Ag Pyrimidineamine derivatives and processes for the preparation thereof
WO1995009851A1 (en) 1993-10-01 1995-04-13 Ciba-Geigy Ag Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
EP0948496A2 (en) 1996-12-05 1999-10-13 Amgen inc. Substituted pyrimidinone and pyridone compounds and methods of use
US6602872B1 (en) 1999-12-13 2003-08-05 Merck & Co., Inc. Substituted pyridazines having cytokine inhibitory activity
WO2001062233A2 (en) 2000-02-25 2001-08-30 F. Hoffmann La Roche Ag Adenosine receptor modulators
WO2002088079A2 (en) * 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
JP4606161B2 (ja) 2002-05-21 2011-01-05 アムジエン・インコーポレーテツド 置換複素環式化合物および使用方法
US7208498B2 (en) 2002-07-15 2007-04-24 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
US7419978B2 (en) * 2003-10-22 2008-09-02 Bristol-Myers Squibb Company Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors
TW200533357A (en) 2004-01-08 2005-10-16 Millennium Pharm Inc 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases
CA2561895A1 (en) 2004-04-13 2005-10-27 Icagen, Inc. Polycyclic pyrimidines as potassium ion channel modulators
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
JP2008510766A (ja) 2004-08-27 2008-04-10 ゲーペーツェー ビオテック アーゲー ピリミジン誘導体
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
GB0428514D0 (en) 2004-12-31 2005-02-09 Prosidion Ltd Compounds
TW200716594A (en) 2005-04-18 2007-05-01 Neurogen Corp Substituted heteroaryl CB1 antagonists
US20100022531A1 (en) * 2005-09-01 2010-01-28 Renovis, Inc. Novel compounds as p2x7 modulators and uses thereof
US7572809B2 (en) 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
JP2009528280A (ja) 2006-02-16 2009-08-06 シェーリング コーポレイション Ｅｒｋインヒビターとしてのピロリジン誘導体
CA2651072A1 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
DE102006035202A1 (de) 2006-07-29 2008-01-31 Lanxess Deutschland Gmbh Konservierungsmittel auf Basis von Carbonsäureanhydriden
CN101528729A (zh) 2006-08-23 2009-09-09 辉瑞产品公司 作为gsk-3抑制剂的嘧啶酮化合物
US7897762B2 (en) * 2006-09-14 2011-03-01 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of proliferative diseases
WO2008039882A1 (en) 2006-09-30 2008-04-03 Sanofi-Aventis U.S. Llc A combination of niacin and a prostaglandin d2 receptor antagonist
CN101568529A (zh) 2006-12-22 2009-10-28 诺瓦提斯公司 作为cdk抑制剂、用于治疗癌症、炎症和病毒感染的杂芳基-杂芳基化合物
JP5363350B2 (ja) * 2007-03-19 2013-12-11 武田薬品工業株式会社 Ｍａｐｋ／ｅｒｋキナーゼ阻害剤
WO2009011904A1 (en) * 2007-07-19 2009-01-22 Renovis, Inc. Compounds useful as faah modulators and uses thereof
JP5611826B2 (ja) 2007-09-04 2014-10-22 ザ スクリプス リサーチ インスティテュート タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン
AU2008324833A1 (en) 2007-11-06 2009-05-14 E. I. Du Pont De Nemours And Company Fungicidal heterocyclic amines
WO2009146034A2 (en) * 2008-03-31 2009-12-03 Takeda Pharmaceutical Company Limited Mapk/erk kinase inhibitors and methods of use thereof
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US9187426B2 (en) 2008-06-27 2015-11-17 Novartis Ag Organic compounds
ES2548882T3 (es) 2008-12-08 2015-10-21 Arena Pharmaceuticals, Inc. Moduladores del receptor de prostaciclina (PGl2) útiles para el tratamiento de trastornos relacionados con los mismos
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

Also Published As

Publication number Publication date
MX339873B (es) 2016-06-15
US20130338140A1 (en) 2013-12-19
JP6085866B2 (ja) 2017-03-01
CA2828478A1 (en) 2012-09-07
US9133187B2 (en) 2015-09-15
EP2681215A1 (en) 2014-01-08
JP2014506930A (ja) 2014-03-20
CN103635472B (zh) 2018-01-12
MX2013009877A (es) 2014-02-11
CN103635472A (zh) 2014-03-12
BR112013021896A2 (pt) 2016-11-08
KR20140014190A (ko) 2014-02-05
EP2681215B1 (en) 2015-04-22
ES2543050T3 (es) 2015-08-14
WO2012118850A1 (en) 2012-09-07
KR101961500B1 (ko) 2019-03-22
RU2013143839A (ru) 2015-04-10

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