JP5152922B2 - プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法 - Google Patents

プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法 Download PDF

Info

Publication number
JP5152922B2
JP5152922B2 JP2008534673A JP2008534673A JP5152922B2 JP 5152922 B2 JP5152922 B2 JP 5152922B2 JP 2008534673 A JP2008534673 A JP 2008534673A JP 2008534673 A JP2008534673 A JP 2008534673A JP 5152922 B2 JP5152922 B2 JP 5152922B2
Authority
JP
Japan
Prior art keywords
compound
cancer
alkyl
aryl
group
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
JP2008534673A
Other languages
English (en)
Japanese (ja)
Other versions
JP2009511486A (ja
Inventor
ティモシー ジェイ. グジ,
カーミル パルーシュ,
マイケル ピー. ドワイヤー,
デイビッド エー. パリー,
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.)
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme LLC
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 Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of JP2009511486A publication Critical patent/JP2009511486A/ja
Application granted granted Critical
Publication of JP5152922B2 publication Critical patent/JP5152922B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/02Local antiseptics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2008534673A 2005-10-06 2006-10-04 プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法 Active JP5152922B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US72415805P 2005-10-06 2005-10-06
US60/724,158 2005-10-06
PCT/US2006/038917 WO2007044441A2 (en) 2005-10-06 2006-10-04 Use of pyrazolo [1 , 5 -a] pyrimidine derivatives for inhibiting protein kinases methods for inhibiting protein kinases

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2012015831A Division JP5520325B2 (ja) 2005-10-06 2012-01-27 プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法

Publications (2)

Publication Number Publication Date
JP2009511486A JP2009511486A (ja) 2009-03-19
JP5152922B2 true JP5152922B2 (ja) 2013-02-27

Family

ID=37943366

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2008534673A Active JP5152922B2 (ja) 2005-10-06 2006-10-04 プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法
JP2012015831A Active JP5520325B2 (ja) 2005-10-06 2012-01-27 プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法
JP2014002164A Pending JP2014062129A (ja) 2005-10-06 2014-01-09 プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2012015831A Active JP5520325B2 (ja) 2005-10-06 2012-01-27 プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法
JP2014002164A Pending JP2014062129A (ja) 2005-10-06 2014-01-09 プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法

Country Status (11)

Country Link
US (2) US20070082900A1 (Direct)
EP (1) EP1942900B1 (Direct)
JP (3) JP5152922B2 (Direct)
CN (1) CN101360499B (Direct)
BR (1) BRPI0616985B1 (Direct)
CA (1) CA2627623C (Direct)
NO (1) NO20082093L (Direct)
NZ (1) NZ567151A (Direct)
TW (1) TWI421078B (Direct)
WO (1) WO2007044441A2 (Direct)
ZA (1) ZA200802998B (Direct)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7563798B2 (en) * 2002-09-04 2009-07-21 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
US7605155B2 (en) * 2002-09-04 2009-10-20 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
US7601724B2 (en) * 2002-09-04 2009-10-13 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
US8580782B2 (en) * 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7196092B2 (en) * 2002-09-04 2007-03-27 Schering Corporation N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
WO2007056468A1 (en) * 2005-11-10 2007-05-18 Schering Corporation Methods for inhibiting protein kinases
WO2007103432A2 (en) * 2006-03-08 2007-09-13 Novartis Ag Use of pyrazolo[1,5a]pyrimidin-7-yl amine derivatives in the treatment of neurological disorders
EP2027127A1 (en) * 2006-05-22 2009-02-25 Shering Corporation Pyrazolo [1, 5-a]pyrimidines as cdk inhibitors
CA2669982A1 (en) * 2006-11-17 2008-05-29 Schering Corporation Combination therapy for proliferative disorders
MX2009012054A (es) 2007-05-08 2009-11-19 Schering Corp Metodos de tratamiento que usan formulaciones intravenosas que comprenden temozolomida.
WO2008153870A1 (en) * 2007-06-07 2008-12-18 Schering Corporation Synthesis of substituted-3-aminopyrazoles
EP2217611B1 (en) * 2007-11-07 2013-07-31 Merck Sharp & Dohme Corp. Novel modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors
NZ586069A (en) 2007-12-19 2012-05-25 Amgen Inc Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
CN101959887B (zh) 2008-01-08 2013-07-31 阵列生物制药公司 作为激酶抑制剂的吡咯并吡啶
CN101965347B (zh) * 2008-01-09 2013-01-02 阵列生物制药公司 作为激酶抑制剂的吡唑并吡啶
ATE531372T1 (de) * 2008-04-07 2011-11-15 Amgen Inc Gem-disubstituierte und spirocyclische aminopyridine/pyrimidine als zellcyclus- inhibitoren
AR071717A1 (es) 2008-05-13 2010-07-07 Array Biopharma Inc Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion del cancer.
RS53350B (sr) 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
PT2725028T (pt) 2008-10-22 2016-08-31 Array Biopharma Inc Compostos de pirazolo[1,5-]pirimidina substituídos como intermediários na síntese de inibidores de cinase trk
RU2539568C2 (ru) * 2008-10-31 2015-01-20 Дженентек, Инк. Пиразолопиримидиновые соединения-ингибиторы jak и способы
CA2752105C (en) * 2009-02-13 2017-10-31 Matthias Vennemann Fused pyrimidines
US8591943B2 (en) 2009-04-09 2013-11-26 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidine derivatives as mTOR inhibitors
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011028638A1 (en) 2009-09-04 2011-03-10 Schering Corporation Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors
US20110071115A1 (en) * 2009-09-11 2011-03-24 Cylene Pharmaceuticals, Inc. Pharmaceutically useful heterocycle-substituted lactams
SG182366A1 (en) 2010-01-05 2012-08-30 Vascular Biogenics Ltd Compositions and methods for treating glioblastoma gbm
DK2521776T3 (en) * 2010-01-05 2017-02-13 Vascular Biogenics Ltd METHODS FOR USING A SPECIFIC ANTI-ANGIOGENT ADENOVIRAL AGENT
US9227971B2 (en) 2010-01-19 2016-01-05 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors
WO2011146336A1 (en) 2010-05-20 2011-11-24 Array Biopharma Inc. Macrocyclic compounds as trk kinase inhibitors
ES2620521T3 (es) 2011-03-23 2017-06-28 Amgen Inc. Inhibidores duales tricíclicos condensados de CDK 4/6 y FLT3
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8969363B2 (en) 2011-07-19 2015-03-03 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9345705B2 (en) 2011-09-15 2016-05-24 Merck Sharp & Dohme Corp. Compositions and methods for treating cancer
AU2013344716B2 (en) * 2012-11-16 2018-03-01 University Health Network Pyrazolopyrimidine compounds
SMT202100425T1 (it) 2012-12-07 2021-09-14 Vertex Pharma 2-ammino-n-(piperidin-1-il-piridin-3-il) pirazolo[1,5alpha]piirimidina-3-carbossiammide come inibitore di atr chinasi
US8969360B2 (en) 2013-03-15 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2970289A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
EA029372B1 (ru) * 2013-11-15 2018-03-30 Юниверсити Хелс Нетуорк Пиразолопиримидиновые соединения
PT3077397T (pt) 2013-12-06 2020-01-22 Vertex Pharma Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo
AU2014372638A1 (en) 2013-12-23 2016-06-16 Norgine B.V. Compounds useful as CCR9 modulators
GB201403093D0 (en) * 2014-02-21 2014-04-09 Cancer Rec Tech Ltd Therapeutic compounds and their use
SI3152212T1 (sl) 2014-06-05 2020-06-30 Vertex Pharmaceuticals Inc. Radioaktivno označeni derivati 2-amino-6-fluoro-N-(5-fluoro-piridin-3-IL)-pirazolo (1,5-A)pirimidin-3- karboksamidne spojine, koristni kot inhibitor kinaze ATR, priprava navedene spojine in njene različne trdne oblike
SG10201811175WA (en) 2014-06-17 2019-01-30 Vertex Pharma Method for treating cancer using a combination of chk1 and atr inhibitors
ES2941630T3 (es) 2014-11-16 2023-05-24 Array Biopharma Inc Forma cristalina de sulfato de hidrógeno de (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida
TW201702218A (zh) 2014-12-12 2017-01-16 美國杰克森實驗室 關於治療癌症、自體免疫疾病及神經退化性疾病之組合物及方法
GB201517263D0 (en) * 2015-09-30 2015-11-11 Ucb Biopharma Sprl And Katholieke Universiteit Leuven Therapeutic agents
HK1258570A1 (zh) 2015-09-30 2019-11-15 Vertex Pharmaceuticals Inc. 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法
TN2019000271A1 (en) 2015-10-26 2021-01-07 Univ Colorado Regents Point mutations in trk inhibitor-resistant cancer and methods relating to the same
MX386416B (es) 2016-04-04 2025-03-18 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida.
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
PE20190437A1 (es) 2016-05-18 2019-03-27 Loxo Oncology Inc Procesos para la preparacion de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
AR110252A1 (es) * 2016-11-30 2019-03-13 Gilead Sciences Inc Compuestos heterocíclicos fusionados como inhibidores de la quinasa cam
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
FI3658557T3 (fi) 2017-07-28 2024-07-30 Takeda Pharmaceuticals Co Tyk2:n estäjiä ja niiden käyttötapoja
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
EP3866789A4 (en) * 2018-10-15 2022-07-06 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND USES THEREOF
CN112996790B (zh) 2018-10-30 2023-11-03 克洛诺斯生物公司 用于调节cdk9活性的化合物、组合物和方法
TW202033526A (zh) * 2018-12-07 2020-09-16 大陸商貝達藥業股份有限公司 用作酪胺酸激酶抑制劑的化合物、包含其的藥物組合物及其用途
JP7595582B2 (ja) 2019-03-26 2024-12-06 ベンティックス バイオサイエンシーズ,インク. Tyk2偽キナーゼリガンド
US11753411B2 (en) * 2019-11-08 2023-09-12 Ventyx Biosciences, Inc. Substituted pyrazolo[1,5-a]pyrimidines as TYK2 pseudokinase ligands
JOP20220125A1 (ar) 2019-11-25 2023-01-30 Amgen Inc مركبات حلقية غير متجانسة على هيئة مثبطات دلتا-5 ديساتوراز وطرق لاستخدامها

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0438730Y2 (Direct) * 1986-03-26 1992-09-10
JP3039751U (ja) * 1996-12-09 1997-07-31 尚子 小園 鞄類用補助具
JP2002295682A (ja) * 2001-03-28 2002-10-09 Yazaki Corp 防水構造およびこの防水構造に用いられる座金部材
ATE389656T1 (de) * 2002-06-04 2008-04-15 Neogenesis Pharmaceuticals Inc Pyrazolo(1,5-a)pyrimidin-verbindungen als antivirale agentien
US7605155B2 (en) * 2002-09-04 2009-10-20 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
US7196092B2 (en) * 2002-09-04 2007-03-27 Schering Corporation N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7196078B2 (en) * 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
WO2004022559A1 (en) * 2002-09-04 2004-03-18 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7601724B2 (en) * 2002-09-04 2009-10-13 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
US7119200B2 (en) * 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
EP1537116B1 (en) * 2002-09-04 2010-06-02 Schering Corporation Pyrazolopyrimidines suitable for the treatment of cancer diseases
CA2516824A1 (en) * 2003-02-28 2004-09-10 Teijin Pharma Limited Pyrazolo[1,5-a]pyrimidine derivatives
EP1608652A1 (en) * 2003-03-31 2005-12-28 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
JP3940700B2 (ja) * 2003-05-22 2007-07-04 茂 相馬 楽器用ケース
AR049769A1 (es) * 2004-01-22 2006-09-06 Novartis Ag Derivados de pirazolo(1,5-a)pirimidin 7-il-amina para utilizarse en el tratamiento de enfermedades dependientes de la quinasa de proteina
JP3104094U (ja) * 2004-03-18 2004-09-02 チャン ホアン−リン 両用スーツケース
KR20080063806A (ko) * 2005-10-06 2008-07-07 쉐링 코포레이션 단백질 키나제 억제제로서의 피라졸로피리미딘
AR055206A1 (es) * 2005-10-06 2007-08-08 Schering Corp Pirazolo[1, 5 - a]pirimidinas como inhibidoras de proteina quinasa, composiciones farmaceuticas y combinaciones con agentes citostaticos que las comprenden y su uso en la fabricacion de un medicamento para el tratamiento del cancer.
JP3174645U (ja) * 2012-01-19 2012-03-29 株式会社セイバン ランドセル

Also Published As

Publication number Publication date
US20070082900A1 (en) 2007-04-12
WO2007044441A3 (en) 2007-07-26
EP1942900B1 (en) 2015-06-03
CA2627623C (en) 2014-04-22
ZA200802998B (en) 2009-10-28
JP2012082234A (ja) 2012-04-26
JP2014062129A (ja) 2014-04-10
EP1942900A2 (en) 2008-07-16
JP5520325B2 (ja) 2014-06-11
WO2007044441A2 (en) 2007-04-19
NO20082093L (no) 2008-07-03
US20100125068A1 (en) 2010-05-20
CN101360499B (zh) 2015-10-07
JP2009511486A (ja) 2009-03-19
AU2006302435A1 (en) 2007-04-19
CA2627623A1 (en) 2007-04-19
NZ567151A (en) 2012-03-30
TWI421078B (zh) 2014-01-01
BRPI0616985A2 (pt) 2009-08-04
CN101360499A (zh) 2009-02-04
BRPI0616985B1 (pt) 2021-10-26
TW200800218A (en) 2008-01-01
US8211854B2 (en) 2012-07-03

Similar Documents

Publication Publication Date Title
JP5152922B2 (ja) プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法
JP5052518B2 (ja) プロテインキナーゼインヒビターとしてのピラゾロピリミジン
JP5031760B2 (ja) プロテインキナーゼインヒビターとしてのイミダゾピラジン
CN101801958B (zh) 作为蛋白质激酶抑制剂的杂环酰胺化合物
JP5109109B2 (ja) サイクリン依存性キナーゼ阻害剤としての新規イミダゾピラジン
US20070105864A1 (en) Methods for inhibiting protein kinases
CN101316847A (zh) 用作蛋白激酶抑制剂的吡唑并(1,5a)嘧啶化合物
WO2008156614A2 (en) Imidazopyrazines as protein kinase inhibitors
CN101589045A (zh) 作为蛋白质激酶抑制剂的咪唑并吡嗪
JP2010505839A (ja) サイクリン依存性キナーゼインヒビターのピラゾロピリミジン
JP2009511484A (ja) プロテインキナーゼインヒビターとしてのピラゾロピリミジン
AU2006302435B2 (en) Use of pyrazolo [1 , 5 -a] pyrimidine derivatives for inhibiting protein kinases methods for inhibiting protein kinases
MX2008004668A (en) Use of pyrazolo [1 , 5 -a]pyrimidine derivatives for inhibiting protein kinases methods for inhibiting protein kinases
AU2013200310A1 (en) Pyrazolopyrimidines as Protein Kinase Inhibitors

Legal Events

Date Code Title Description
A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20110928

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20111227

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20120110

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120127

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20120402

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120620

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20120705

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20120828

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120830

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20121112

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20121121

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20121129

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20121130

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20151214

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

Ref document number: 5152922

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313111

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250