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
alkyl
pyrido
pyrimidine
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
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 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

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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 (OSRAM)
EP (1) EP2681215B1 (OSRAM)
JP (1) JP6085866B2 (OSRAM)
KR (1) KR101961500B1 (OSRAM)
CN (1) CN103635472B (OSRAM)
BR (1) BR112013021896A2 (OSRAM)
CA (1) CA2828478C (OSRAM)
ES (1) ES2543050T3 (OSRAM)
MX (1) MX339873B (OSRAM)
RU (1) RU2013143839A (OSRAM)
WO (1) WO2012118850A1 (OSRAM)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2013143839A (ru) 2011-02-28 2015-04-10 Эррэй Биофарма Инк. Ингибиторы сериновых/треониновых киназ
EP2723718A1 (en) 2011-06-24 2014-04-30 Amgen Inc. Trpm8 antagonists and their use in treatments
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
MX340756B (es) * 2011-08-04 2016-07-25 Array Biopharma Inc Compuestos de quinazolina como inhibidores de serina/treonina quinasa.
EP2797878B1 (en) * 2011-12-27 2017-08-16 Bio-Pharm Solutions Co., Ltd. Phenyl carbamate compounds for use in preventing or treating stroke
PT2820009T (pt) 2012-03-01 2018-04-12 Array Biopharma Inc Inibidores de serina/treonina quinases
US8952009B2 (en) 2012-08-06 2015-02-10 Amgen Inc. Chroman derivatives as TRPM8 inhibitors
HK1210174A1 (en) 2012-08-27 2016-04-15 Array Biopharma, Inc. Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases
JP6186440B2 (ja) * 2012-09-19 2017-08-23 ノバルティス アーゲー キナーゼ阻害剤としてのジヒドロピロリジノピリミジン
CA2884766A1 (en) 2012-10-16 2014-04-24 Daniel Jon Burdick Serine/threonine kinase inhibitors
EP3026051A4 (en) * 2013-07-24 2017-03-08 Takeda Pharmaceutical Company Limited Heterocyclic compound
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
EA031243B1 (ru) 2013-12-06 2018-12-28 Дженентек, Инк. Ингибиторы серин/треонинкиназ
CN105980387B (zh) * 2013-12-30 2019-04-19 阵列生物制药公司 丝氨酸/苏氨酸激酶抑制剂
CA2934679C (en) 2013-12-30 2023-02-28 Genentech, Inc. Serine/threonine kinase inhibitors
CN109072311A (zh) 2016-04-15 2018-12-21 豪夫迈·罗氏有限公司 用于癌症的诊断和治疗方法
MX382339B (es) * 2016-05-18 2025-03-13 Mirati Therapeutics Inc Inhibidores g12c de kras.
WO2019051296A1 (en) 2017-09-08 2019-03-14 Genentech, Inc. DIAGNOSTIC AND THERAPEUTIC METHODS OF CANCER
JP6986565B2 (ja) 2017-09-29 2021-12-22 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
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2019158579A1 (en) 2018-02-13 2019-08-22 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
KR20210145773A (ko) 2019-03-28 2021-12-02 지앙수 헨그루이 메디슨 컴퍼니 리미티드 티에노헤테로고리형 유도체, 이의 제조 방법 및 이의 의약적 용도
US20220185818A1 (en) 2019-03-29 2022-06-16 Jiangsu Hengrui Medicine Co., Ltd. Pyrroloheterocyclic derivative, preparation method therefor, and application thereof in medicine
CN113874374B (zh) * 2019-05-24 2024-12-27 江苏恒瑞医药股份有限公司 氢化吡啶并嘧啶类衍生物、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
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
MX2023003516A (es) 2020-09-25 2023-04-19 Janssen Pharmaceutica Nv Inhibidores no covalentes de la cinasa dependiente de ciclina 7 (cdk7).
TW202221001A (zh) 2020-09-29 2022-06-01 大陸商江蘇恒瑞醫藥股份有限公司 吡咯並雜環類衍生物的晶型及其製備方法
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
EP4610256A1 (en) * 2022-10-25 2025-09-03 Tuojie Biotech (Shanghai) Co., Ltd. Piperidinopyrimidine derivative, preparation method therefor and use thereof in medicine
IT202200024963A1 (it) * 2022-12-05 2024-06-05 Angelini Pharma S P A Composti attivatori dei canali potassio Kv7.2/Kv7.3
TW202535869A (zh) * 2023-10-23 2025-09-16 大陸商上海拓界生物醫藥科技有限公司 一種含有噻唑基的哌啶并嘧啶類衍生物、其製備方法及其醫藥上的應用
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

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH08503971A (ja) 1993-10-01 1996-04-30 チバ−ガイギー アクチェンゲゼルシャフト ピリミジンアミン誘導体及びその調製のための方法
PT672042E (pt) 1993-10-01 2006-08-31 Novartis Ag Derivados de pirimidinoamina farmacologicamente activos e processos para a sua preparacao
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
BR9713863A (pt) 1996-12-05 2000-03-14 Amgen Inc Composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, processos de profilaxia ou tratamento, para abaixar as concentrações no plasma, para diminuir a produção de prostaglandinas, e, para diminuir a atividade de enzima ciclooxigenase
US6602872B1 (en) 1999-12-13 2003-08-05 Merck & Co., Inc. Substituted pyridazines having cytokine inhibitory activity
BR0108611A (pt) 2000-02-25 2003-05-06 Hoffmann La Roche Moduladores de receptor de adenosina
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
CA2485166A1 (en) 2002-05-21 2003-12-04 Amgen Inc. Substituted pyrimidinone and pyridinone compounds
JP4530852B2 (ja) * 2002-07-15 2010-08-25 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病治療のためのピペリジノピリミジンジペプチジルペプチダーゼ阻害剤
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
EP1742634B1 (en) 2004-04-13 2010-10-27 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
WO2006021458A2 (en) 2004-08-27 2006-03-02 Gpc Biotech Ag Pyrimidine derivatives
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
US20070078135A1 (en) 2005-04-18 2007-04-05 Neurogen Corporation 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
MX2008010635A (es) 2006-02-16 2008-10-28 Schering Corp Derivados de pirrolidina como inhibidores de cinasa regulada por señales extracelulares.
JP2009535393A (ja) 2006-05-01 2009-10-01 ファイザー・プロダクツ・インク 置換2−アミノ縮合複素環式化合物
DE102006035202A1 (de) 2006-07-29 2008-01-31 Lanxess Deutschland Gmbh Konservierungsmittel auf Basis von Carbonsäureanhydriden
ATE530540T1 (de) 2006-08-23 2011-11-15 Pfizer Prod Inc Pyrimidonverbindungen als gsk-3-inhibitoren
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
BRPI0720635A2 (pt) 2006-12-22 2014-01-07 Novartis Ag Compostos orgânicos e seus usos
US8063066B2 (en) * 2007-03-19 2011-11-22 Takeda Pharmaceutical Company Limited MAPK/ERK kinase inhibitors
WO2009011904A1 (en) * 2007-07-19 2009-01-22 Renovis, Inc. Compounds useful as faah modulators and uses thereof
EP2200436B1 (en) 2007-09-04 2015-01-21 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
JP2011503006A (ja) 2007-11-06 2011-01-27 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー 殺菌性複素環アミン
WO2009146034A2 (en) * 2008-03-31 2009-12-03 Takeda Pharmaceutical Company Limited Mapk/erk kinase inhibitors and methods of use thereof
BRPI0913966A2 (pt) 2008-06-27 2015-11-17 Novartis Ag compostos orgânicos
NZ589843A (en) 2008-06-27 2012-12-21 Avila Therapeutics Inc Pyrimidine heteroaryl compounds and uses thereof as protein kinase inhibitors
US8940891B2 (en) 2008-12-08 2015-01-27 Arena Pharmaceuticals, Inc. Modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
RU2013143839A (ru) 2011-02-28 2015-04-10 Эррэй Биофарма Инк. Ингибиторы сериновых/треониновых киназ
MX340756B (es) 2011-08-04 2016-07-25 Array Biopharma Inc Compuestos de quinazolina como inhibidores de serina/treonina quinasa.
PT2820009T (pt) 2012-03-01 2018-04-12 Array Biopharma Inc Inibidores de serina/treonina quinases
HK1210174A1 (en) 2012-08-27 2016-04-15 Array Biopharma, Inc. Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases

Also Published As

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

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