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
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    • 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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    • A61K31/495Heterocyclic 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
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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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  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Hematology (AREA)
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  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Molecular Biology (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
US20040142864A1 (en) * 2002-09-16 2004-07-22 Plexxikon, Inc. Crystal structure of PIM-1 kinase
EP1624073A4 (en) * 2003-04-03 2006-05-17 Oncorex Inc DRUG
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
AU2006302174B2 (en) * 2005-10-06 2013-06-20 Exelixis, Inc. Pyridopyrimidinone Inhibitors of PIM-1 and/or PIM-3
AU2006331912B2 (en) 2005-12-21 2012-08-30 Janssen Pharmaceutica, N.V. Triazolopyridazines as tyrosine kinase modulators
CA2651979A1 (en) * 2006-05-30 2007-12-06 Pfizer Products Inc. Triazolopyridazine derivatives
US7683060B2 (en) 2006-08-07 2010-03-23 Incyte Corporation Triazolotriazines as kinase inhibitors
US8481538B2 (en) * 2006-09-18 2013-07-09 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of c-Met and uses thereof
PL2084162T3 (pl) * 2006-10-23 2013-01-31 Sgx Pharmaceuticals Inc Bicykliczne triazole jako modulatory kinaz białkowych
CA2667487C (en) 2006-11-06 2017-04-04 Supergen, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
GEP20125658B (en) 2006-11-22 2012-10-10 Incyte Corp Imidazotriazines and imidazo pyrimidines as kinase inhibitors
CA2685106A1 (en) 2007-04-25 2008-11-06 Exelixis, Inc. 6-phenylpyrimidinones as pim modulators
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
SI2193133T1 (sl) 2007-09-27 2015-12-31 Fundacion Centro Nacional De Investigaciones Oncologicas Carlos Iii Imidazolotiadiazoli za uporabo kot zaviralci protein-kinaze
CN103936743B (zh) 2008-05-21 2018-04-24 因西特控股公司 2-氟-N-甲基-4-[7-(喹啉-6-基甲基)咪唑并[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺的盐及与其相关的制备方法
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
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
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
JP2012517971A (ja) * 2009-02-13 2012-08-09 フォーヴィア・ファーマシューティカルズ キナーゼ阻害薬としての[1,2,4]トリアゾロ[1,5−a]ピリジン類
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
EA025304B1 (ru) 2010-02-03 2016-12-30 Инсайт Холдингс Корпорейшн ИМИДАЗО[1,2-b][1,2,4]ТРИАЗИНЫ В КАЧЕСТВЕ c-Met ИНГИБИТОРОВ
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
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
JP6039585B2 (ja) 2011-02-25 2016-12-07 アレイ バイオファーマ、インコーポレイテッド Pimキナーゼ阻害剤としてのトリアゾロピリジン化合物
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
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2721031B1 (en) 2011-06-17 2016-01-20 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
US9416132B2 (en) 2011-07-21 2016-08-16 Tolero Pharmaceuticals, Inc. Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors
US9586963B2 (en) * 2011-09-27 2017-03-07 Genfit Derivatives of 6-substituted triazolopyridazines as Rev-Erb agonists
EP2844660B1 (en) * 2012-05-02 2017-11-01 Southern Research Institute Triazolopyridazine compounds, use as inhibitors of the kinase lrrk2, and methods for preparation thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
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
WO2014134583A2 (en) * 2013-02-28 2014-09-04 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
WO2015155738A2 (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
US9969747B2 (en) 2014-06-20 2018-05-15 Constellation Pharmaceuticals, Inc. Crystalline forms of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[C]isoxazolo[4,5-e]azepin-4-yl)acetamide
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
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
PL91799B1 (enExample) * 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
DE2418435A1 (de) * 1974-04-17 1975-10-30 Boehringer Mannheim Gmbh Nitroimidazolyl-triazolo-pyridazine und verfahren zu ihrer herstellung
EP0915875B1 (en) * 1996-07-25 2003-04-09 MERCK SHARP & DOHME LTD. Substituted triazolo-pyridazine derivatives as ligands for gaba receptors
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
AU2002251266A1 (en) * 2001-04-10 2002-10-28 Merck Sharp And Dohme Limited Inhibitors of akt activity
AU2003211424A1 (en) 2002-03-01 2003-09-16 Yamanouchi Pharmaceutical Co., Ltd. Nitrogen-containing heterocyclic compound
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 *

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CA2510534A1 (en) 2004-07-15
US20040192696A1 (en) 2004-09-30
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NO20053470L (no) 2005-09-02
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