JP2013507449A - TBK1および/またはIKKεの阻害剤としてのアミノ−ピリミジン化合物 - Google Patents

TBK1および/またはIKKεの阻害剤としてのアミノ−ピリミジン化合物 Download PDF

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JP2013507449A
JP2013507449A JP2012534299A JP2012534299A JP2013507449A JP 2013507449 A JP2013507449 A JP 2013507449A JP 2012534299 A JP2012534299 A JP 2012534299A JP 2012534299 A JP2012534299 A JP 2012534299A JP 2013507449 A JP2013507449 A JP 2013507449A
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amino
pyrimidin
phenyl
yloxy
benzonitrile
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JP2013507449A5 (enExample
Inventor
ライアン ホルコム,
和之 鈴木
ロバート ジェイ. ハルター,
ポール アール. セバハー,
ドナルド エー. マクリオド,
マーク ディー. シェンデロビッチ,
クレイグ エム. ヤイガー,
マシュー グレゴリー バーサビッチ,
アシャンタイ ジェイ. ユンガイ,
バート リチャーズ,
ポール エル. バーテル,
ダニエル エー. ウェットスタイン,
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ミレクシス, インコーポレイテッド
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Publication of JP2013507449A publication Critical patent/JP2013507449A/ja
Publication of JP2013507449A5 publication Critical patent/JP2013507449A5/ja
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    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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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    • C07—ORGANIC CHEMISTRY
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
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    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/54—Heterocyclic 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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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2012534299A 2009-10-12 2010-10-12 TBK1および/またはIKKεの阻害剤としてのアミノ−ピリミジン化合物 Pending JP2013507449A (ja)

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 (2)

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JP2013507449A true JP2013507449A (ja) 2013-03-04
JP2013507449A5 JP2013507449A5 (enExample) 2013-11-28

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JP2012534299A Pending JP2013507449A (ja) 2009-10-12 2010-10-12 TBK1および/またはIKKεの阻害剤としてのアミノ−ピリミジン化合物

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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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014509661A (ja) * 2011-04-01 2014-04-21 ユニバーシティ・オブ・ユタ・リサーチ・ファウンデイション Axlキナーゼの阻害剤としての置換n−フェニルピリミジン−2−アミン類似体
JP2017516814A (ja) * 2014-06-03 2017-06-22 ギリアード サイエンシーズ, インコーポレイテッド Tank結合キナーゼインヒビター化合物
JP2020508341A (ja) * 2017-02-23 2020-03-19 ドメイネクス リミテッド Ikke、tbk1及び/又はsik2キナーゼ阻害剤としての5−(ピリミジン−4−イル)−2−(ピロリジン−1−イル)ニコチノニトリル化合物
JP2020537671A (ja) * 2017-10-17 2020-12-24 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung ピリミジンTBK/IKKεインヒビター化合物およびそれらの使用

Families Citing this family (52)

* 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
KR20140048873A (ko) * 2011-04-12 2014-04-24 알츠하이머즈 인스티튜트 오브 아메리카, 인크. Ikk-관련 키나제 엡실론 및 tank 결합 키나제 1 억제제의 조성물 및 치료학적 용도
AU2012244745A1 (en) 2011-04-19 2013-09-19 Bayer Intellectual Property Gmbh Substituted 4-Aryl-N-phenyl-1,3,5-triazin-2-amines
TW201636330A (zh) 2011-05-24 2016-10-16 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
CN103917527B (zh) 2011-09-16 2017-05-31 拜耳知识产权有限责任公司 二取代的5‑氟‑嘧啶
CN103930399B (zh) 2011-09-16 2016-03-16 拜耳知识产权有限责任公司 包含亚氨基亚磺酰基的二取代的5-氟嘧啶衍生物
DE102011119127A1 (de) 2011-11-22 2013-05-23 Merck Patent Gmbh 3-Cyanaryl-1H-pyrrolo[2.3-b]pyridin-Derivate
CN104093722B (zh) * 2012-02-09 2016-07-27 默克专利股份公司 作为TBK1和IKK抑制剂的呋喃并[3,2-b]-和噻吩并[3,2-b]吡啶衍生物
WO2013175415A1 (en) * 2012-05-23 2013-11-28 Piramal Enterprises Limited Substituted pyrimidine compounds and uses thereof
EP3795694A3 (en) * 2012-10-02 2021-06-23 The General Hospital Corporation d/b/a Massachusetts General Hospital Methods relating to dna-sensing pathway related conditions
HK1209414A1 (en) 2012-10-18 2016-04-01 Bayer Pharma Aktiengesellschaft 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group
CN105102434A (zh) 2012-10-18 2015-11-25 拜耳药业股份公司 含砜基团的4-(邻)-氟苯基-5-氟嘧啶-2-基胺
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
EP2941428A1 (en) * 2013-01-07 2015-11-11 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
PT2970205T (pt) 2013-03-14 2019-08-26 Tolero Pharmaceuticals Inc Inibidores da jak2 e da alk2 e métodos para a sua utilização
SG11201701724VA (en) * 2014-09-26 2017-04-27 Gilead Sciences Inc Aminotriazine derivatives useful as tank-binding kinase inhibitor compounds
CA2964683A1 (en) 2014-10-16 2016-04-21 Bayer Pharma Aktiengesellschaft Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfone group
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
JP2018509439A (ja) 2015-03-24 2018-04-05 バイエル ファーマ アクチエンゲゼルシャフト 多発性骨髄腫を治療するための4−(4−フルオロ−2−メトキシフェニル)−n−{3−[(s−メチルスルホンイミドイル)メチル]フェニル}−1,3,5−トリアジン−2−アミンの使用
JP2018509440A (ja) 2015-03-24 2018-04-05 バイエル ファーマ アクチエンゲゼルシャフト リンパ腫の治療のための4−(4−フルオロ−2−メトキシフェニル)−n−{3−[(s−メチルスルホンイミドイル)メチル]フェニル}−1,3,5−トリアジン−2−アミンの使用
US10729691B2 (en) 2015-06-26 2020-08-04 Kadmon Corporation, Llc Treatment of infectious diseases with glucose uptake inhibitors
JP2018518518A (ja) 2015-06-26 2018-07-12 カドモン コーポレイション,リミティド ライアビリティ カンパニー グルコース取り込み阻害剤
JP6847099B2 (ja) 2015-09-29 2021-03-24 バイエル ファーマ アクチエンゲゼルシャフト 新規な大環状スルホンジイミン化合物
ES2819869T3 (es) 2015-10-08 2021-04-19 Bayer Pharma AG Nuevos compuestos macrocíclicos modificados
WO2017060322A2 (en) 2015-10-10 2017-04-13 Bayer Pharma Aktiengesellschaft Ptefb-inhibitor-adc
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
BR112017002594A2 (pt) 2015-12-17 2017-12-19 Gilead Sciences Inc compostos inibidores de cinase de ligação de tank
WO2017102091A1 (en) 2015-12-18 2017-06-22 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
WO2018045969A1 (zh) * 2016-09-07 2018-03-15 法玛科技顾问股份有限公司 活化腺苷单磷酸活化蛋白激酶之化合物
CA3057891A1 (en) 2017-03-28 2018-10-04 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
EP3601253B1 (en) 2017-03-28 2021-09-15 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
ES2962961T3 (es) 2017-07-28 2024-03-22 Yuhan Corp Procedimiento de preparación de n-(5-((4-(4-(dimetilamino)metil)-3-fenil-1h-pirazol-1-il)pirimidin-2-il)amino)-4-metoxi-2-morfolinofenil)acrilamida haciendo reaccionar la amina correspondiente con un cloruro de 3-halo-propionilo
US11440899B2 (en) 2017-10-17 2022-09-13 Merck Patent Gmbh Pyrimidine TBK/IKKe inhibitor compounds and uses thereof
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
US11701347B2 (en) 2018-02-13 2023-07-18 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
BR112020020246A8 (pt) 2018-04-05 2022-10-18 Sumitomo Dainippon Pharma Oncology Inc Inibidores de cinase axl e uso dos mesmos
WO2020005935A1 (en) * 2018-06-25 2020-01-02 Kadmon Corporation, Llc Glucose uptake inhibitors
KR20210038906A (ko) 2018-07-26 2021-04-08 스미토모 다이니폰 파마 온콜로지, 인크. 비정상적 acvr1 발현과 연관된 질환을 치료하는 방법 및 그에 사용하기 위한 acvr1 억제제
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
CN111269215B (zh) * 2020-04-01 2021-10-26 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
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
CA3251183A1 (en) * 2022-02-03 2023-08-10 Nexys Therapeutics, Inc. ARYL HYDROCARBONE RECEPTOR AGONISTS AND THEIR USES
CN117247387B (zh) * 2022-06-16 2026-07-28 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
KR20260109851A (ko) * 2023-10-31 2026-07-13 브리스톨-마이어스 스큅 컴퍼니 유비퀴틴 특이적 프로세싱 프로테아제 1 (usp1) 화합물
WO2025245367A1 (en) * 2024-05-22 2025-11-27 Psy Therapeutics, Inc. Inhibiting catechol-o-methyltransferase (comt)

Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH08503971A (ja) * 1993-10-01 1996-04-30 チバ−ガイギー アクチェンゲゼルシャフト ピリミジンアミン誘導体及びその調製のための方法
JP2004523497A (ja) * 2000-12-06 2004-08-05 シグナル ファーマシューティカルズ, インコーポレイテッド Ikk阻害剤としてのアニリノピリミジン誘導体ならびにそれに関する組成物および方法
WO2005026129A1 (en) * 2003-09-15 2005-03-24 Gpc Biotech Ag 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
JP2006508107A (ja) * 2002-11-05 2006-03-09 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 Jakおよび他のプロテインキナーゼのインヒビターとして有用な化合物
JP2008515986A (ja) * 2004-10-13 2008-05-15 ワイス N−ベンゼンスルホニル置換アニリノ−ピリミジン類似物
WO2008065155A1 (en) * 2006-11-30 2008-06-05 Ingenium Pharmaceuticals Gmbh Cdk inhibitors for treating pain
WO2008090181A1 (en) * 2007-01-23 2008-07-31 Palau Pharma, S. A. Purine derivatives
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
WO2008109943A1 (en) * 2007-03-12 2008-09-18 Cytopia Research Pty Ltd Phenyl amino pyrimidine compounds and uses thereof
WO2009032861A1 (en) * 2007-09-04 2009-03-12 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
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
WO2009089042A1 (en) * 2008-01-09 2009-07-16 Signal Pharmaceuticals, Llc Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith
WO2009112439A1 (en) * 2008-03-10 2009-09-17 Janssen Pharmaceutica Nv 4-aryl-2-anilino-pyrimidines as plk kinase inhibitors

Family Cites Families (3)

* 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
DE10162120A1 (de) 2001-12-12 2003-06-18 Berolina Drug Dev Ab Svedala Deuterierte substituierte Dihydrofuranone sowie diese Verbindungen enthaltende Arzneimittel

Patent Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH08503971A (ja) * 1993-10-01 1996-04-30 チバ−ガイギー アクチェンゲゼルシャフト ピリミジンアミン誘導体及びその調製のための方法
JP2004523497A (ja) * 2000-12-06 2004-08-05 シグナル ファーマシューティカルズ, インコーポレイテッド Ikk阻害剤としてのアニリノピリミジン誘導体ならびにそれに関する組成物および方法
JP2006508107A (ja) * 2002-11-05 2006-03-09 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 Jakおよび他のプロテインキナーゼのインヒビターとして有用な化合物
WO2005026129A1 (en) * 2003-09-15 2005-03-24 Gpc Biotech Ag 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
JP2008515986A (ja) * 2004-10-13 2008-05-15 ワイス N−ベンゼンスルホニル置換アニリノ−ピリミジン類似物
WO2008065155A1 (en) * 2006-11-30 2008-06-05 Ingenium Pharmaceuticals Gmbh Cdk inhibitors for treating pain
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
WO2008090181A1 (en) * 2007-01-23 2008-07-31 Palau Pharma, S. A. Purine derivatives
WO2008109943A1 (en) * 2007-03-12 2008-09-18 Cytopia Research Pty Ltd Phenyl amino pyrimidine compounds and uses thereof
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
WO2009032861A1 (en) * 2007-09-04 2009-03-12 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
WO2009089042A1 (en) * 2008-01-09 2009-07-16 Signal Pharmaceuticals, Llc Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith
WO2009112439A1 (en) * 2008-03-10 2009-09-17 Janssen Pharmaceutica Nv 4-aryl-2-anilino-pyrimidines as plk kinase inhibitors

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014509661A (ja) * 2011-04-01 2014-04-21 ユニバーシティ・オブ・ユタ・リサーチ・ファウンデイション Axlキナーゼの阻害剤としての置換n−フェニルピリミジン−2−アミン類似体
JP2017516814A (ja) * 2014-06-03 2017-06-22 ギリアード サイエンシーズ, インコーポレイテッド Tank結合キナーゼインヒビター化合物
JP2020508341A (ja) * 2017-02-23 2020-03-19 ドメイネクス リミテッド Ikke、tbk1及び/又はsik2キナーゼ阻害剤としての5−(ピリミジン−4−イル)−2−(ピロリジン−1−イル)ニコチノニトリル化合物
JP7136793B2 (ja) 2017-02-23 2022-09-13 ドメイネクス リミテッド Ikke、tbk1及び/又はsik2キナーゼ阻害剤としての5-(ピリミジン-4-イル)-2-(ピロリジン-1-イル)ニコチノニトリル化合物
JP2020537671A (ja) * 2017-10-17 2020-12-24 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung ピリミジンTBK/IKKεインヒビター化合物およびそれらの使用
JP7266592B2 (ja) 2017-10-17 2023-04-28 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング ピリミジンTBK/IKKεインヒビター化合物およびそれらの使用

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