CN102791697A - 作为TBKL和/或IKKε抑制剂的氨基-嘧啶化合物 - Google Patents

作为TBKL和/或IKKε抑制剂的氨基-嘧啶化合物 Download PDF

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Publication number
CN102791697A
CN102791697A CN2010800564502A CN201080056450A CN102791697A CN 102791697 A CN102791697 A CN 102791697A CN 2010800564502 A CN2010800564502 A CN 2010800564502A CN 201080056450 A CN201080056450 A CN 201080056450A CN 102791697 A CN102791697 A CN 102791697A
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amino
phenyl
pyrimidine
base
cyanobenzene
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CN2010800564502A
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Chinese (zh)
Inventor
R·霍尔库姆
K·铃木
R·J·豪尔特
P·R·舍巴哈
D·A·麦克劳德
M·D·申杰罗维奇
K·M·亚戈
M·G·布萨维奇
A·J·韵盖
B·理查兹
P·L·巴特尔
D·A·韦特施泰因
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Myrexis Inc
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Myrexis Inc
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Publication of CN102791697A publication Critical patent/CN102791697A/zh
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Plural Heterocyclic Compounds (AREA)
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CN2010800564502A 2009-10-12 2010-10-12 作为TBKL和/或IKKε抑制剂的氨基-嘧啶化合物 Pending CN102791697A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US25084209P 2009-10-12 2009-10-12
US61/250,842 2009-10-12
US32524510P 2010-04-16 2010-04-16
US61/325,245 2010-04-16
PCT/US2010/052385 WO2011046970A1 (en) 2009-10-12 2010-10-12 Amino - pyrimidine compounds as inhibitors of tbkl and/or ikk epsilon

Publications (1)

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CN102791697A true CN102791697A (zh) 2012-11-21

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CN2010800564502A Pending CN102791697A (zh) 2009-10-12 2010-10-12 作为TBKL和/或IKKε抑制剂的氨基-嘧啶化合物

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US (2) US20120238540A1 (enExample)
EP (1) EP2488503A1 (enExample)
JP (1) JP2013507449A (enExample)
KR (1) KR20120114224A (enExample)
CN (1) CN102791697A (enExample)
AU (1) AU2010306927A1 (enExample)
BR (1) BR112012008677A2 (enExample)
CA (1) CA2777762A1 (enExample)
MX (1) MX2012004313A (enExample)
NZ (1) NZ599826A (enExample)
WO (1) WO2011046970A1 (enExample)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105503626A (zh) * 2015-12-12 2016-04-20 常州大学 一种2-氨基-4-氯-6-甲氧基苯酚的合成方法
CN106715419A (zh) * 2014-09-26 2017-05-24 吉利德科学公司 用作tank‑结合激酶抑制剂化合物的氨基三嗪衍生物
CN108349910A (zh) * 2015-06-26 2018-07-31 卡德门企业有限公司 葡萄糖摄取抑制剂
CN109912514A (zh) * 2017-12-13 2019-06-21 广东东阳光药业有限公司 (2-杂芳基胺基苯基)氮杂环衍生物及其用途
CN110330484A (zh) * 2019-07-18 2019-10-15 中国药科大学 取代类苯基嘧啶衍生物作为jak激酶抑制剂或其可药用的盐、制备方法及用途
CN111247135A (zh) * 2017-10-17 2020-06-05 默克专利股份公司 嘧啶ΤΒΚ/ΙΚΚε抑制剂化合物及其用途
CN111269215A (zh) * 2020-04-01 2020-06-12 中科利健制药(广州)有限公司 含氮杂环有机化合物及其制备方法和应用
CN112142675A (zh) * 2020-10-09 2020-12-29 嘉兴特科罗生物科技有限公司 一种作为jak激酶抑制剂的小分子化合物及其用途
CN117088851A (zh) * 2023-07-13 2023-11-21 特科罗生物科技(成都)有限公司 一种嘧啶胺类nuak抑制剂及其制备方法和用途
CN117247387A (zh) * 2022-06-16 2023-12-19 上海翊石医药科技有限公司 一种芳杂环类化合物及其制备方法

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201012105D0 (en) * 2010-07-19 2010-09-01 Domainex Ltd Novel pyrimidine compounds
PL2693881T3 (pl) * 2011-04-01 2020-03-31 University Of Utah Research Foundation Podstawione analogi N-fenylopirymidyno-2-aminy jako inhibitory kinazy AXL
CA2832919A1 (en) * 2011-04-12 2012-10-18 Ryan C. Holcomb Compounds, compositions, and therapeutic uses thereof
US8916557B2 (en) 2011-04-19 2014-12-23 Bayer Intellectual Property Gmbh Substituted 4-Aryl-N-phenyl-1,3,5-triazin-2-amines
TWI555737B (zh) 2011-05-24 2016-11-01 拜耳知識產權公司 含有硫醯亞胺基團之４－芳基－ｎ－苯基－１，３，５－三氮雜苯－２－胺
GB201114051D0 (en) 2011-08-15 2011-09-28 Domainex Ltd Compounds and their uses
DE102011112978A1 (de) 2011-09-09 2013-03-14 Merck Patent Gmbh Benzonitrilderivate
ES2587284T3 (es) 2011-09-16 2016-10-21 Bayer Intellectual Property Gmbh 5-Fluoro-pirimidinas 2,4-disustituidas como inhibidores selectivos de CDK9
WO2013037894A1 (en) 2011-09-16 2013-03-21 Bayer Intellectual Property Gmbh Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group
DE102011119127A1 (de) 2011-11-22 2013-05-23 Merck Patent Gmbh 3-Cyanaryl-1H-pyrrolo[2.3-b]pyridin-Derivate
HRP20161578T1 (hr) 2012-02-09 2016-12-30 Merck Patent Gmbh Derivati furo[3, 2-b]piridina kao inhibitori tbk1 i ikk
WO2013175415A1 (en) * 2012-05-23 2013-11-28 Piramal Enterprises Limited Substituted pyrimidine compounds and uses thereof
EP2904119B1 (en) * 2012-10-02 2020-06-17 The General Hospital Corporation d/b/a Massachusetts General Hospital Methods relating to dna-sensing pathway related conditions
EP2909183B1 (en) 2012-10-18 2016-08-24 Bayer Pharma Aktiengesellschaft 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfone group
ES2595222T3 (es) 2012-10-18 2016-12-28 Bayer Pharma Aktiengesellschaft Derivados de 5-fluoro-N-(piridin-2-il)piridin-2-amina que contienen un grupo sulfona
TW201418243A (zh) 2012-11-15 2014-05-16 Bayer Pharma AG 含有磺醯亞胺基團之ｎ－（吡啶－２－基）嘧啶－４－胺衍生物
WO2014106762A1 (en) * 2013-01-07 2014-07-10 Vichem Chemie Kutató Kft. 4-pyrimidinylamino-benzenesulfonamide derivatives and their use for the inhibition of polo-like kinase 1 (plk1) for the treatment of cancer and their use for the treatment of bacterial infections
GB201303109D0 (en) * 2013-02-21 2013-04-10 Domainex Ltd Novel pyrimidine compounds
US10202356B2 (en) 2013-03-14 2019-02-12 Tolero Pharmaceuticals, Inc. JAK2 and ALK2 inhibitors and methods for their use
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
JP2017531003A (ja) 2014-10-16 2017-10-19 バイエル ファーマ アクチエンゲゼルシャフト スルホン基を含有するフッ化ベンゾフラニル−ピリミジン誘導体
US20160263183A1 (en) * 2015-03-10 2016-09-15 Brown University Methods for treating lung disease
WO2016150902A1 (en) 2015-03-24 2016-09-29 Bayer Pharma Aktiengesellschaft Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating gastric cancers
WO2016150903A1 (en) 2015-03-24 2016-09-29 Bayer Pharma Aktiengesellschaft Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating lymphomas
CA2980493A1 (en) 2015-03-24 2016-09-29 Bayer Pharma Aktiengesellschaft Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating multiple myeloma
WO2016210331A1 (en) * 2015-06-26 2016-12-29 Kadmon Corporation, Llc Treatment of infectious diseases with glucose uptake inhibitors
CA2999931A1 (en) 2015-09-29 2017-04-06 Bayer Pharma Aktiengesellschaft Novel macrocyclic sulfondiimine compounds
CN108368129B (zh) 2015-10-08 2021-08-17 拜耳医药股份有限公司 改性大环化合物
WO2017060322A2 (en) 2015-10-10 2017-04-13 Bayer Pharma Aktiengesellschaft Ptefb-inhibitor-adc
JP2019500368A (ja) 2015-12-17 2019-01-10 ギリアード サイエンシーズ， インコーポレイテッド Ｔａｎｋ結合キナーゼ阻害剤化合物
US10894784B2 (en) 2015-12-18 2021-01-19 Bayer Pharma Aktiengesellschaft Heteroarylbenzimidazole compounds
WO2017207534A1 (en) 2016-06-03 2017-12-07 Bayer Pharma Aktiengesellschaft Substituted heteroarylbenzimidazole compounds
DE102016113714A1 (de) 2016-07-26 2018-02-01 Rosa Karl Transfektionsverfahren mit nicht-viralen Genliefersystemen
US10793527B2 (en) 2016-09-07 2020-10-06 National Yang-Ming University Adenosine monophosphate-activated protein kinase agonist
GB201702947D0 (en) 2017-02-23 2017-04-12 Domainex Ltd Novel compounds
EP3601253B1 (en) 2017-03-28 2021-09-15 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
EP3601236A1 (en) 2017-03-28 2020-02-05 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
DK3658552T3 (da) 2017-07-28 2023-11-20 Yuhan Corp Fremgangsmåde til fremstilling af n-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1h-pyrazol-1-yl)pyrimidin-2-yl)amino)-4-methoxy-2-morpholinophenyl)acrylamid ved reaktion af den tilsvarende amin med et 3-halogen-propionylchlorid
WO2019079375A1 (en) 2017-10-17 2019-04-25 Merck Patent Gmbh IN / ΙΚΚΕ PYRIMIDINE INHIBITOR COMPOUNDS AND USES THEREOF
CA3090843A1 (en) 2018-02-13 2019-08-22 Bayer Aktiengesellschaft Use of 5-fluoro-4-(4-fluoro-2-methoxyphenyl)-n-{4-[(s-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine for treating diffuse large b-cell lymphoma
CA3096984A1 (en) 2018-04-05 2019-10-10 Sumitomo Dainippon Pharma Oncology, Inc. Axl kinase inhibitors and use of the same
US12030857B2 (en) 2018-06-25 2024-07-09 Kadmon Corporation, Llc Glucose uptake inhibitors
MX2021000977A (es) 2018-07-26 2021-04-12 Sumitomo Pharma Oncology Inc Metodos para tratar enfermedades asociadas con expresion anormal de receptor de activina a tipo 1 (acvr1) e inhibidores de acvr1 para uso en los mismos.
CA3251183A1 (en) * 2022-02-03 2023-08-10 Nexys Therapeutics, Inc. ARYL HYDROCARBONE RECEPTOR AGONISTS AND THEIR USES
WO2025096505A1 (en) * 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008099074A1 (fr) * 2007-01-05 2008-08-21 Sanofi-Aventis Derives de phenyl- (4-phenyl-pyrimidin-2-yl) - amines comme inhibiteurs de ikk, leur preparation et leur compositions pharmaceutiques
WO2009032861A1 (en) * 2007-09-04 2009-03-12 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5149820A (en) 1987-03-11 1992-09-22 Norsk Hydro A.S. Deuterated compounds
AU693475B2 (en) * 1993-10-01 1998-07-02 Novartis Ag Pyrimidineamine derivatives and processes for the preparation thereof
US7122544B2 (en) * 2000-12-06 2006-10-17 Signal Pharmaceuticals, Llc Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
DE10162120A1 (de) 2001-12-12 2003-06-18 Berolina Drug Dev Ab Svedala Deuterierte substituierte Dihydrofuranone sowie diese Verbindungen enthaltende Arzneimittel
CA2507406A1 (en) * 2002-11-05 2004-05-21 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
EP1678147B1 (en) * 2003-09-15 2012-08-08 Lead Discovery Center GmbH Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
WO2005107760A1 (en) * 2004-04-30 2005-11-17 Irm Llc Compounds and compositions as inducers of keratinocyte differentiation
AU2005295788A1 (en) * 2004-10-13 2006-04-27 Wyeth N-benzenesulfonyl substituted anilino-pyrimidine analogs
US20080153822A1 (en) * 2006-11-30 2008-06-26 Martin Augustin Methods of treating pain
MX2009007302A (es) * 2007-01-23 2009-07-15 Palau Pharma Sa Derivados de purina.
CN101861313B (zh) * 2007-03-12 2014-06-04 Ym生物科学澳大利亚私人有限公司 苯基氨基嘧啶化合物及其用途
WO2009030890A1 (en) * 2007-09-03 2009-03-12 University Court Of The University Of Dundee Pyrimidine compounds for the treatment of cancer, septic shock and/or primary open angle glaucoma
US20090270418A1 (en) * 2008-01-09 2009-10-29 Marianne Sloss Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith
DK2283024T3 (da) * 2008-03-10 2013-08-05 Janssen Pharmaceutica Nv 4-aryl-2-anilinpyrimidiner som PLK-kinaseinhibitorer

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008099074A1 (fr) * 2007-01-05 2008-08-21 Sanofi-Aventis Derives de phenyl- (4-phenyl-pyrimidin-2-yl) - amines comme inhibiteurs de ikk, leur preparation et leur compositions pharmaceutiques
WO2009032861A1 (en) * 2007-09-04 2009-03-12 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors

Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106715419A (zh) * 2014-09-26 2017-05-24 吉利德科学公司 用作tank‑结合激酶抑制剂化合物的氨基三嗪衍生物
CN108349910A (zh) * 2015-06-26 2018-07-31 卡德门企业有限公司 葡萄糖摄取抑制剂
CN105503626A (zh) * 2015-12-12 2016-04-20 常州大学 一种2-氨基-4-氯-6-甲氧基苯酚的合成方法
CN111247135A (zh) * 2017-10-17 2020-06-05 默克专利股份公司 嘧啶ΤΒΚ/ΙΚΚε抑制剂化合物及其用途
CN109912514A (zh) * 2017-12-13 2019-06-21 广东东阳光药业有限公司 (2-杂芳基胺基苯基)氮杂环衍生物及其用途
CN109912514B (zh) * 2017-12-13 2022-11-18 广东东阳光药业有限公司 (2-杂芳基胺基苯基)氮杂环衍生物及其用途
CN110330484B (zh) * 2019-07-18 2022-08-26 中国药科大学 取代类苯基嘧啶衍生物作为jak激酶抑制剂或其可药用的盐、制备方法及用途
CN110330484A (zh) * 2019-07-18 2019-10-15 中国药科大学 取代类苯基嘧啶衍生物作为jak激酶抑制剂或其可药用的盐、制备方法及用途
CN111269215A (zh) * 2020-04-01 2020-06-12 中科利健制药(广州)有限公司 含氮杂环有机化合物及其制备方法和应用
WO2022073424A1 (zh) * 2020-10-09 2022-04-14 嘉兴特科罗生物科技有限公司 一种作为jak激酶抑制剂的小分子化合物及其用途
CN112142675B (zh) * 2020-10-09 2021-11-30 嘉兴特科罗生物科技有限公司 一种作为jak激酶抑制剂的小分子化合物及其用途
CN112142675A (zh) * 2020-10-09 2020-12-29 嘉兴特科罗生物科技有限公司 一种作为jak激酶抑制剂的小分子化合物及其用途
CN117247387A (zh) * 2022-06-16 2023-12-19 上海翊石医药科技有限公司 一种芳杂环类化合物及其制备方法
CN117088851A (zh) * 2023-07-13 2023-11-21 特科罗生物科技(成都)有限公司 一种嘧啶胺类nuak抑制剂及其制备方法和用途
WO2025011445A1 (zh) * 2023-07-13 2025-01-16 特科罗生物科技(成都)有限公司 一种嘧啶胺类nuak抑制剂及其制备方法和用途

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