CN102292333B - 蛋白激酶c抑制剂及其用途 - Google Patents

蛋白激酶c抑制剂及其用途 Download PDF

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Publication number
CN102292333B
CN102292333B CN201080005581.8A CN201080005581A CN102292333B CN 102292333 B CN102292333 B CN 102292333B CN 201080005581 A CN201080005581 A CN 201080005581A CN 102292333 B CN102292333 B CN 102292333B
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fluoro
benzo
pyrimidine
alkyl
diamine
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Chinese (zh)
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CN102292333A (zh
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赵浩然
R·克鲁瑞
C·巴尔德斯
K·曹
R·辛格
J·拉姆菲尔
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Rigel Pharmaceuticals Inc
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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
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CN201080005581.8A 2009-01-15 2010-01-13 蛋白激酶c抑制剂及其用途 Expired - Fee Related CN102292333B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US14502109P 2009-01-15 2009-01-15
US61/145,021 2009-01-15
US14735309P 2009-01-26 2009-01-26
US61/147,353 2009-01-26
PCT/US2010/020888 WO2010083207A2 (en) 2009-01-15 2010-01-13 Protein kinase c inhibitors and uses thereof

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CN102292333A CN102292333A (zh) 2011-12-21
CN102292333B true CN102292333B (zh) 2015-05-13

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US (3) US8394951B2 (https=)
EP (1) EP2387572B1 (https=)
JP (1) JP5603881B2 (https=)
CN (1) CN102292333B (https=)
CA (1) CA2749195C (https=)
ES (1) ES2555982T3 (https=)
WO (1) WO2010083207A2 (https=)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6035238B2 (ja) 2010-07-21 2016-11-30 ライジェル ファーマシューティカルズ, インコーポレイテッド プロテインキナーゼc阻害剤およびその使用
CN104169272A (zh) 2011-12-23 2014-11-26 赛尔佐姆有限公司 作为激酶抑制剂的嘧啶-2,4-二胺衍生物
ES2658395T3 (es) 2012-04-04 2018-03-09 Rigel Pharmaceuticals, Inc. Inhibidores de proteína cinasa C y usos de los mismos
EP2928891B1 (en) 2012-12-04 2019-02-20 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
CA2904610A1 (en) 2013-03-14 2014-09-25 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
ES2851724T3 (es) 2013-09-18 2021-09-08 Epiaxis Therapeutics Pty Ltd Modulación de células madre
CA2958704A1 (en) 2014-08-25 2016-03-03 University Of Canberra Compositions for modulating cancer stem cells and uses therefor
WO2017038552A1 (ja) * 2015-09-04 2017-03-09 Dic株式会社 安定剤化合物、液晶組成物および表示素子
US10633590B2 (en) 2015-09-04 2020-04-28 Dic Corporation Liquid crystal composition and liquid crystal display device including the same
CN108913655B (zh) * 2018-07-16 2022-07-15 浙江大学 基于多能干细胞技术建立“人源性”心肌肥大模型的方法
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
CA3150681A1 (en) 2019-08-14 2021-02-18 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
US11851426B2 (en) 2019-10-11 2023-12-26 Incyte Corporation Bicyclic amines as CDK2 inhibitors
CN117015543A (zh) * 2020-09-14 2023-11-07 高德美控股有限公司 新型jak抑制剂化合物、其合成方法及其用途
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1704404A (zh) * 1999-12-29 2005-12-07 惠氏公司 三环蛋白激酶抑制剂
CN1798748A (zh) * 2003-04-07 2006-07-05 Gpc生物科技公司 依赖细胞周期蛋白的激酶抑制剂及其组合物和相关用途
WO2006129100A1 (en) * 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
CN101072556A (zh) * 2004-10-21 2007-11-14 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的三唑
WO2008024634A1 (en) * 2006-08-25 2008-02-28 Smithkline Beecham Corporation Pyrimdine compounds useful as kinase inhibitors
US20080287410A1 (en) * 2004-07-08 2008-11-20 Barbosa Antonio J M Pyrimidine derivatives useful as inhibitors of pkc-theta
US20080306099A1 (en) * 2005-06-08 2008-12-11 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
WO2003095448A1 (en) * 2002-05-06 2003-11-20 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
WO2005012294A1 (en) * 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
ATE506953T1 (de) * 2003-08-07 2011-05-15 Rigel Pharmaceuticals Inc 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
CN1998221A (zh) 2004-08-03 2007-07-11 诺基亚公司 移动通信和/或游戏终端
US8227455B2 (en) * 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
WO2007002847A2 (en) 2005-06-28 2007-01-04 Community Power Corporation Method and apparatus for a self-cleaning filter
WO2007028445A1 (en) * 2005-07-15 2007-03-15 Glaxo Group Limited 6-indolyl-4-yl-amino-5-halogeno-2-pyrimidinyl-amino derivatives
RU2008152195A (ru) * 2006-06-15 2010-07-20 БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) 2-анилино-4-(гетероциклил)аминопиримидины, как ингибиторы протеинкиназы с-альфа
US20100269694A1 (en) 2006-06-28 2010-10-28 The Governors Of The University Of Alberta Silicate Materials, Method For Their Manufacture, And Method For Using Such Silicate Materials For Adsorptive Fluid Separations
ITVI20070184A1 (it) 2007-06-27 2008-12-28 Simec Spa Puleggia per macchine utensili multifilo.
CN101903357A (zh) * 2007-07-17 2010-12-01 里格尔药品股份有限公司 作为pkc抑制剂的环状胺取代的嘧啶二胺
JP5781942B2 (ja) * 2009-01-14 2015-09-24 ライジェル ファーマシューティカルズ, インコーポレイテッド 2,4−ピリミジンジアミン化合物を用いた炎症性障害の治療法

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1704404A (zh) * 1999-12-29 2005-12-07 惠氏公司 三环蛋白激酶抑制剂
CN1798748A (zh) * 2003-04-07 2006-07-05 Gpc生物科技公司 依赖细胞周期蛋白的激酶抑制剂及其组合物和相关用途
US20080287410A1 (en) * 2004-07-08 2008-11-20 Barbosa Antonio J M Pyrimidine derivatives useful as inhibitors of pkc-theta
CN101072556A (zh) * 2004-10-21 2007-11-14 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的三唑
WO2006129100A1 (en) * 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
US20080306099A1 (en) * 2005-06-08 2008-12-11 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2008024634A1 (en) * 2006-08-25 2008-02-28 Smithkline Beecham Corporation Pyrimdine compounds useful as kinase inhibitors

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
Discovery of potent and selective PKC-θ inhibitors;Charles L. Cywin,等;《Bioorganic & Medicinal Chemistry Letters》;20061019;第17卷(第1期);第225-230页 *
Jürg Zimmermann,等.PHENYLAMINO-PYRIMIDINE (PAP)- DERIVATIVES: A NEW CLASS OF POTENT AND HIGHLY SELECTIVE PDGF-RECEPTOR AUTOPHOSPHORYLATION INHIBITORS.《Bioorganic & Medicinal Chemistry Letters》.1996,第6卷(第11期),第1221-1226页. *
吲哚马来酰亚胺类蛋白激酶C抑制剂的研究进展;赵圣印,等;《有机化学》;20081231;第28卷(第10期);第1676-1684页 *
蛋白激酶C的抑制剂;刘世英,等;《科学通报》;20050331;第50卷(第5期);第405-415页 *

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