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

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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
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compound
disease
dmso
gsk
pim
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Chinese (zh)
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CN1742012A (zh
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J·格林
R·小戈雷
A·C·皮尔斯
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (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

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

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
JP5238506B2 (ja) * 2005-10-06 2013-07-17 エグゼリクシス, インコーポレイテッド Pim−1および/またはpim−3のピリドピリミジノンインヒビター
DK1966214T3 (en) * 2005-12-21 2017-02-13 Janssen Pharmaceutica Nv TRIAZOLPYRIDAZINES AS TYROSINKINASA MODULATORS
CA2651979A1 (en) * 2006-05-30 2007-12-06 Pfizer Products Inc. Triazolopyridazine derivatives
CA2660836A1 (en) 2006-08-07 2008-02-21 Incyte Corporation Triazolotriazines as kinase inhibitors
WO2008036272A1 (en) * 2006-09-18 2008-03-27 Vertex Pharmaceuticals Incorporated HETEROCYCLIC INHIBITORS OF c-MET AND USES THEREOF
KR20090071612A (ko) * 2006-10-23 2009-07-01 에스지엑스 파마슈티컬스, 인코포레이티드 단백질 키나제 조정제로서의 바이시클릭 트리아졸
MX2009004700A (es) 2006-11-06 2009-05-15 Supergen Inc Derivados de imidazo[1,2-b]piridazin y pirazolo[1,5-a] pirimidina y su uso como inhibidores de proteina cinasa.
MX2009005144A (es) 2006-11-22 2009-05-27 Incyte Corp Imidazotriazinas e imidazopirimidinas como inhibidores de cinasa.
JP2010525062A (ja) * 2007-04-25 2010-07-22 エグゼリクシス, インコーポレイテッド Pimモジュレーターとしてのピリミジノン類
EP2170337A4 (en) * 2007-06-28 2013-12-18 Abbvie Inc NEW TRIAZOLOPYRIDAZINE
KR20090031122A (ko) * 2007-09-21 2009-03-25 주식회사 중외제약 인다졸 골격을 함유하는 화합물, 이의 제조방법 및 상기화합물을 함유하는 약제학적 조성물
PL2193133T3 (pl) 2007-09-27 2016-01-29 Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii Imidazolotiadiazole do stosowania jako inhibitory kinazy białkowej
NZ602791A (en) 2008-05-21 2014-04-30 Incyte Corp Salts of 2-fluoro-n-methyl-4-[7-(quinolin-6-yl-methyl)- imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same
US8895550B2 (en) 2008-08-19 2014-11-25 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
WO2010022081A1 (en) * 2008-08-19 2010-02-25 Array Biopharma Inc. Triazolopyridine compounds as pim kinase inhibitors
US8987251B2 (en) 2008-08-19 2015-03-24 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
EA201101188A1 (ru) * 2009-02-13 2012-04-30 Фовеа Фармасьютикалз [1,2,4]триазоло[1,5-а]пиридины в качестве ингибиторов киназы
PL2414369T3 (pl) 2009-04-02 2016-04-29 Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii Pochodne imidazo[2,1-b][1,3,4]tiadiazolu
PH12012501361A1 (en) 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
AU2011269788B2 (en) 2010-02-03 2015-12-10 Incyte Holdings Corporation Imidazo[1,2-b][1,2,4]triazines as c-Met inhibitors
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. 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
RS54586B1 (sr) 2011-02-25 2016-08-31 Array Biopharma Inc. Jedinjenja triazolopiridina kao inhibitori pim kinaze
WO2012125667A1 (en) * 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
EP2702063A1 (en) * 2011-04-29 2014-03-05 Amgen Inc. Bicyclic pyridazine compounds as pim inhibitors
EP2705039B1 (en) 2011-05-04 2017-07-26 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
EP3409278B8 (en) 2011-07-21 2020-11-04 Sumitomo Dainippon Pharma Oncology, Inc. Heterocyclic protein kinase inhibitors
MX356683B (es) * 2011-09-27 2018-06-08 Genfit Derivados de triazolpiridazinas 6-sustituidas como agonistas rev-erb.
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
AU2014223990A1 (en) * 2013-02-28 2015-09-10 Washington University Methods of treatment of human cytomegalovirus infection and diseases with bromodomain inhibitors
GB201321745D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
US20170165230A1 (en) 2014-04-09 2017-06-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
LT3157928T (lt) 2014-06-20 2019-05-27 Constellation Pharmaceuticals, Inc. 2-((4s)-6-(4-chlorfenil)-1-metil-4h-benzo[c]iizoksazolo[4,5-e]azepin-4-il)acetamido kristalinės formos
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
CA3127502A1 (en) 2019-02-12 2020-08-20 Sumitomo Dainippon Pharma Oncology, Inc. Formulations comprising heterocyclic protein kinase inhibitors

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
PL91799B1 (enExample) * 1972-04-01 1977-03-31
DE2254783A1 (de) 1972-04-01 1974-05-16 Boehringer Mannheim Gmbh Nitroimidazolyl-triazolo-pyridazine und verfahren zu ihrer herstellung
DE2261693A1 (de) 1972-04-01 1974-06-20 Boehringer Mannheim Gmbh Nitroimidazolyl-triazolo-pyridazine und verfahren zu ihrer herstellung
DE2261735A1 (de) 1972-04-01 1974-06-20 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
YU2899A (sh) * 1996-07-25 2000-03-21 Merck Sharp & Dohme Limited Supstituisani triazolo-piridazin derivati kao ligandi za gaba receptore
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
WO2002083675A2 (en) * 2001-04-10 2002-10-24 Merck Sharp & Dohme Limited Inhibitors of akt activity
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
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

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 *

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AU2003297161A1 (en) 2004-07-22
CA2510534C (en) 2011-09-20
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ATE473980T1 (de) 2010-07-15
US7268136B2 (en) 2007-09-11
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