CN100567296C - 可用作蛋白激酶抑制剂的三唑并哒嗪 - Google Patents

可用作蛋白激酶抑制剂的三唑并哒嗪 Download PDF

Info

Publication number
CN100567296C
CN100567296C CNB2003801091296A CN200380109129A CN100567296C CN 100567296 C CN100567296 C CN 100567296C CN B2003801091296 A CNB2003801091296 A CN B2003801091296A CN 200380109129 A CN200380109129 A CN 200380109129A CN 100567296 C CN100567296 C CN 100567296C
Authority
CN
China
Prior art keywords
compound
disease
dmso
gsk
pim
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
CNB2003801091296A
Other languages
English (en)
Chinese (zh)
Other versions
CN1742012A (zh
Inventor
J·格林
R·小戈雷
A·C·皮尔斯
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of CN1742012A publication Critical patent/CN1742012A/zh
Application granted granted Critical
Publication of CN100567296C publication Critical patent/CN100567296C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-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
    • 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/503Pyridazines; Hydrogenated pyridazines spiro-condensed
    • 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
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/24Antidepressants
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • 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
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
CNB2003801091296A 2002-12-18 2003-12-17 可用作蛋白激酶抑制剂的三唑并哒嗪 Expired - Fee Related CN100567296C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US43512402P 2002-12-18 2002-12-18
US60/435,124 2002-12-18

Publications (2)

Publication Number Publication Date
CN1742012A CN1742012A (zh) 2006-03-01
CN100567296C true CN100567296C (zh) 2009-12-09

Family

ID=32682164

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB2003801091296A Expired - Fee Related CN100567296C (zh) 2002-12-18 2003-12-17 可用作蛋白激酶抑制剂的三唑并哒嗪

Country Status (14)

Country Link
US (1) US7268136B2 (https=)
EP (1) EP1575959B1 (https=)
JP (1) JP4817661B2 (https=)
KR (1) KR101075812B1 (https=)
CN (1) CN100567296C (https=)
AT (1) ATE473980T1 (https=)
AU (1) AU2003297161B8 (https=)
CA (1) CA2510534C (https=)
DE (1) DE60333387D1 (https=)
MX (1) MXPA05006478A (https=)
NO (1) NO20053470L (https=)
NZ (1) NZ541151A (https=)
RU (1) RU2005122484A (https=)
WO (1) WO2004058769A2 (https=)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040171062A1 (en) * 2002-02-28 2004-09-02 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
AU2003272548A1 (en) * 2002-09-16 2004-04-30 Plexxikon, Inc. Crystal structure of pim-1 kinase
CN100567502C (zh) * 2003-04-03 2009-12-09 株式会社康福来 药学制剂
FR2876584B1 (fr) * 2004-10-15 2007-04-13 Centre Nat Rech Scient Cnrse Utilisation de la kenpaullone pour la fabrication de medicaments pour le traitement de la mucoviscidose et de maladies liees a un defaut d'adressage des proteines dans les cellules
DE102005042742A1 (de) * 2005-09-02 2007-03-08 Schering Ag Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
WO2007044724A2 (en) * 2005-10-06 2007-04-19 Exelixis, Inc. Aminopyrimidine, aminopyridine and aniline derivatives inhibitors of pim-i and/or pim-3
HRP20170103T1 (hr) 2005-12-21 2017-03-24 Janssen Pharmaceutica N.V. Triazolopiridazini kao modulatori tirozin kinaze
CA2651979A1 (en) * 2006-05-30 2007-12-06 Pfizer Products Inc. Triazolopyridazine derivatives
EP2057164A1 (en) 2006-08-07 2009-05-13 Incyte Corporation Triazolotriazines as kinase inhibitors
JP2010519174A (ja) * 2006-09-18 2010-06-03 バーテックス ファーマシューティカルズ インコーポレイテッド c−Metの複素環阻害薬およびその使用方法
BRPI0717320A2 (pt) * 2006-10-23 2013-10-22 Sgx Pharmaceuticals Inc Triazóis bicíclicos como moduladores de proteína cinase
WO2008058126A2 (en) * 2006-11-06 2008-05-15 Supergen, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
RS54510B1 (sr) 2006-11-22 2016-06-30 Incyte Holdings Corporation Imidazotriazini i imidazopirimidini kao inhibitori kinaze
US8242129B2 (en) 2007-04-25 2012-08-14 Exelixis, Inc. 6-phenylpyrimidinones as PIM modulators
WO2009005675A1 (en) * 2007-06-28 2009-01-08 Abbott Laboratories Novel triazolopyridazines
KR20090031122A (ko) * 2007-09-21 2009-03-25 주식회사 중외제약 인다졸 골격을 함유하는 화합물, 이의 제조방법 및 상기화합물을 함유하는 약제학적 조성물
HUE025976T2 (en) 2007-09-27 2016-05-30 Fund Centro Nac De Investig Oncologicas Carlos Iii Imidazolothiadiazoles for use as protein kinase inhibitors
TWI472529B (zh) 2008-05-21 2015-02-11 Incyte Corp 2-氟-N-甲基-4-〔7-(喹啉-6-基-甲基)-咪唑并〔1,2-b〕〔1,2,4〕三-2-基〕苯甲醯胺之鹽類及其相關製備方法
US8987251B2 (en) 2008-08-19 2015-03-24 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
US8895550B2 (en) 2008-08-19 2014-11-25 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
US8557809B2 (en) 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
TWI496779B (zh) * 2008-08-19 2015-08-21 Array Biopharma Inc 作為pim激酶抑制劑之三唑吡啶化合物
FR2940284B1 (fr) * 2008-12-19 2011-02-18 Sanofi Aventis Derives de 6-cycloamino-2,3-di-pyridinyl-imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique
SG173610A1 (en) * 2009-02-13 2011-09-29 Fovea Pharmaceuticals Sa [1, 2, 4] triazolo [1, 5 -a] pyridines as kinase inhibitors
NZ595674A (en) 2009-04-02 2012-12-21 Ct Nac Investigaciones Oncologicas Cnio Imidazo[2,1-b][1,3,4]thiadiazole derivatives
PH12012501361A1 (en) * 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
MX2012008898A (es) 2010-02-03 2012-11-06 Incyte Corp Imidazo - [1, 2 - b] [1, 2, 4] triazinas como inhibidores de c - met.
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012098387A1 (en) * 2011-01-18 2012-07-26 Centro Nacional De Investigaciones Oncológicas (Cnio) 6, 7-ring-fused triazolo [4, 3 - b] pyridazine derivatives as pim inhibitors
BR112013021675A2 (pt) 2011-02-25 2016-11-01 Array Biopharma Inc compostos de triazolopiridina como inibidores de pim cinase
WO2012125667A1 (en) * 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
CA2834166A1 (en) * 2011-04-29 2012-11-01 Amgen Inc. Bicyclic pyridazine compounds as pim inhibitors
US9422292B2 (en) 2011-05-04 2016-08-23 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012174487A2 (en) 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2013001310A1 (en) * 2011-06-30 2013-01-03 Centro Nacional De Investigaciones Oncológicas (Cnio) Macrocyclic compounds and their use as cdk8 inhibitors
WO2013004984A1 (en) * 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncologicas (Cnio) Tricyclic compounds for use as kinase inhibitors
EP3812387A1 (en) 2011-07-21 2021-04-28 Sumitomo Dainippon Pharma Oncology, Inc. Heterocyclic protein kinase inhibitors
WO2013045519A1 (en) * 2011-09-27 2013-04-04 Genfit Derivatives of 6-substituted triazolopyridazines as rev-erb agonists
WO2013166276A1 (en) * 2012-05-02 2013-11-07 Southern Research Institute Triazolopyridazine compounds, use as inhibitors of the kinase lrrk2, and methods for preparation thereof
US9624244B2 (en) 2012-06-06 2017-04-18 Constellation Pharmaceuticals, Inc. Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
CN102938491B (zh) * 2012-09-28 2014-12-10 华为终端有限公司 天线、组合天线和移动终端
JP2016510039A (ja) * 2013-02-28 2016-04-04 ワシントン・ユニバーシティWashington University ブロモドメイン阻害剤によるヒトサイトメガロウイルス感染および疾患の治療方法
GB201321745D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
CA2945263A1 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
PL3157928T3 (pl) 2014-06-20 2019-07-31 Constellation Pharmaceuticals, Inc. Krystaliczne postacie 2-((4S)-6-(4-chlorofenylo)-1-metylo-4H-benzo[ c]izoksazolo-[4,5-e]azepin-4-ylo)acetamidu
CN109651253B (zh) * 2017-10-12 2022-03-25 上海医药工业研究院 苯丙烯酸酯衍生物及其作为神经保护药物的应用
CN108498512A (zh) * 2018-04-22 2018-09-07 于志国 一种治疗心力衰竭的药物组合物及其制备方法和用途
CN109045036B (zh) * 2018-07-19 2020-10-02 中山大学 [1,2,4]三唑并[4,3-b]哒嗪衍生物在制备抗肿瘤药物中的应用
KR20260008165A (ko) 2019-02-12 2026-01-15 스미토모 파마 아메리카, 인크. 헤테로시클릭 단백질 키나제 억제제를 포함하는 제제

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1026334A (en) * 1972-04-01 1978-02-14 Rudi Gall Nitroimidazolyl-triazolo-pyridazines and process for their preparation
CN1060843A (zh) * 1990-10-23 1992-05-06 罗纳-普朗农业化学公司 三唑并哒嗪类衍生物

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2153902A1 (de) * 1971-10-29 1973-05-03 Boehringer Mannheim Gmbh Antimikrobiell wirksame nitrofuranderivate und verfahren zur herstellung derselben
DE2261693A1 (de) * 1972-04-01 1974-06-20 Boehringer Mannheim Gmbh Nitroimidazolyl-triazolo-pyridazine und verfahren zu ihrer herstellung
PL91799B1 (https=) * 1972-04-01 1977-03-31
DE2261735A1 (de) * 1972-04-01 1974-06-20 Boehringer Mannheim Gmbh Nitroimidazolyl-triazolo-pyridazine und verfahren zu ihrer herstellung
DE2254783A1 (de) * 1972-04-01 1974-05-16 Boehringer Mannheim Gmbh Nitroimidazolyl-triazolo-pyridazine und verfahren zu ihrer herstellung
DE2418435A1 (de) * 1974-04-17 1975-10-30 Boehringer Mannheim Gmbh Nitroimidazolyl-triazolo-pyridazine und verfahren zu ihrer herstellung
KR20000029548A (ko) * 1996-07-25 2000-05-25 더블유. 지. 콜 가바수용체에대한리간드로서의치환된트리아졸로-피리다진유도체
GB9813576D0 (en) * 1998-06-24 1998-08-19 Merck Sharp & Dohme Therapeutic agents
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
DE10038019A1 (de) * 2000-08-04 2002-02-14 Bayer Ag Substituierte Triazolopyrid(az)ine
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
US6960584B2 (en) * 2001-04-10 2005-11-01 Merck & Co., Inc. Inhibitors of Akt activity
CN1281606C (zh) 2002-03-01 2006-10-25 安斯泰来制药有限公司 含氮杂环化合物
JP4385620B2 (ja) * 2002-03-01 2009-12-16 アステラス製薬株式会社 含窒素複素環化合物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1026334A (en) * 1972-04-01 1978-02-14 Rudi Gall Nitroimidazolyl-triazolo-pyridazines and process for their preparation
CN1060843A (zh) * 1990-10-23 1992-05-06 罗纳-普朗农业化学公司 三唑并哒嗪类衍生物

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
"2H-pyran-2-ones as synthons for(E)-alpha,beta-didehydroamino acid derivatives". VRANICAR ET AL.:.TETRAHEDRON,Vol.55 . 1999 *
"2H-pyran-2-ones as synthons for(E)-alpha,beta-didehydroamino acid derivatives". VRANICAR ET AL.:.TETRAHEDRON,Vol.55. 1999 *
"Derivati della 3-idrazinopiridazina". PARRAVICINI ET AL.IL FARMACO,,Vol.34 No.4. 1979 *
"Derivati della 3-idrazinopiridazina". PARRAVICINI ET AL.IL FARMACO,Vol.34 No.4. 1979 *
"Transformation of4-(1-dimethylaminoethylidene)-2-phenyl-5(4 H)-oxazolone intomethyl 2-benzoylamino-3-oxobutanoate. The synthesis of1-substituted 4-benzoylamino-3-methyl-5(2H)-pyrazolones". BRATUSEK ET AL.J. HET. CHEM.,,Vol.35 . 1998 *

Also Published As

Publication number Publication date
NO20053470L (no) 2005-09-02
CN1742012A (zh) 2006-03-01
AU2003297161B2 (en) 2011-03-10
EP1575959B1 (en) 2010-07-14
AU2003297161A1 (en) 2004-07-22
JP4817661B2 (ja) 2011-11-16
MXPA05006478A (es) 2005-09-08
CA2510534A1 (en) 2004-07-15
WO2004058769A2 (en) 2004-07-15
WO2004058769A3 (en) 2004-09-30
RU2005122484A (ru) 2006-01-20
NZ541151A (en) 2008-09-26
JP2006513208A (ja) 2006-04-20
DE60333387D1 (de) 2010-08-26
ATE473980T1 (de) 2010-07-15
CA2510534C (en) 2011-09-20
US20040192696A1 (en) 2004-09-30
EP1575959A2 (en) 2005-09-21
US7268136B2 (en) 2007-09-11
HK1087700A1 (zh) 2006-10-20
KR101075812B1 (ko) 2011-10-25
KR20050084428A (ko) 2005-08-26
AU2003297161B8 (en) 2011-03-31

Similar Documents

Publication Publication Date Title
CN100567296C (zh) 可用作蛋白激酶抑制剂的三唑并哒嗪
CN101039933B (zh) 可用作蛋白激酶抑制剂的二氨基三唑化合物
US7122552B2 (en) Inhibitors of JAK and CDK2 protein kinases
DE60223790T4 (de) Hemmer von c-jun-terminal kinase (jnk) und andere protein kinase
CN100436427C (zh) 用作糖原合酶激酶3β抑制剂的氨基苯甲酰胺衍生物
CN101547924B (zh) 抑制有丝分裂的化合物
CN101801971A (zh) 可用作janus激酶抑制剂的脱氮嘌呤
CN102532133A (zh) 适用作詹纳斯激酶抑制剂的吖吲哚类
CN1934113B (zh) 可用作蛋白激酶抑制剂的组合物
CN101848909A (zh) 可用作蛋白激酶抑制剂的吡咯并[3,2-c]吡啶
TW201609705A (zh) 做為週期素依賴型激酶(cdk)抑制劑之2-h-吲唑衍生物及其醫療用途
KR20050006237A (ko) 티아디아졸 또는 옥사디아졸 및 jak 단백질 키나제억제제로서의 이들의 용도
CN101824043A (zh) 可用作蛋白激酶抑制剂的组合物
CN104788427A (zh) 3-(2-嘧啶氨基)苯基丙烯酰胺类化合物及其应用
AU2012342891A1 (en) 3-Cyanoaryl-1H-pyrrolo[2.3-b]pyridine derivatives
CN101495474A (zh) 可用作蛋白激酶抑制剂的噻吩-甲酰胺类
AU2004288728A1 (en) Use of thienopyrimidines
CN104130265A (zh) 一种含有螺环或桥环的嘧啶类化合物
US20040186119A1 (en) 4-Substituted-5-cyano-1H-pyrimidin-6-(thi) ones as GSK-3 inhibitors
HK1087700B (en) Triazolopyridazines as protein kinases inhibitors
EP2243781A1 (en) Pyrazolopyridine derivatives as inhibitors of JAK and CDK2 protein kinases
CN101573365A (zh) 可用作蛋白激酶抑制剂的化合物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1087700

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1087700

Country of ref document: HK

C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20091209

Termination date: 20121217