TWI681952B - 經取代之二胺基甲醯胺及二胺基甲腈嘧啶、其組合物、及以該等治療之方法 - Google Patents

經取代之二胺基甲醯胺及二胺基甲腈嘧啶、其組合物、及以該等治療之方法 Download PDF

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TWI681952B
TWI681952B TW106120278A TW106120278A TWI681952B TW I681952 B TWI681952 B TW I681952B TW 106120278 A TW106120278 A TW 106120278A TW 106120278 A TW106120278 A TW 106120278A TW I681952 B TWI681952 B TW I681952B
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Taiwan
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pyrimidine
carboxamide
alkyl
ylamino
hydroxycyclohexylamino
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TW106120278A
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Chinese (zh)
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TW201736348A (zh
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布雷登Ｌ 班奈特
簡 艾斯納
保羅 艾德曼
羅伯特 希格雷夫
勞瑞 安 勒柏恩
梅格 麥克卡瑞科
莫拉Ｆ 莫格達姆
馬克Ａ 納吉
史蒂芬 諾瑞斯
大衛Ａ 沛斯納
瑪莉安 史洛斯
威廉Ｊ 羅曼納
佐藤嘉高
傑奇瑞 提克希
尹元亨
莫塞迪斯 迪葛多
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美商標誌製藥公司
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TW106120278A 2011-04-22 2012-04-20 經取代之二胺基甲醯胺及二胺基甲腈嘧啶、其組合物、及以該等治療之方法 TWI681952B (zh)

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Application Number Priority Date Filing Date Title
US201161478076P 2011-04-22 2011-04-22
US61/478,076 2011-04-22
US201161555339P 2011-11-03 2011-11-03
US61/555,339 2011-11-03

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TW201736348A TW201736348A (zh) 2017-10-16
TWI681952B true TWI681952B (zh) 2020-01-11

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Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA120740C2 (uk) 2011-04-22 2020-02-10 Сігнал Фармасьютікалз, Елелсі Заміщені діамінокарбоксамідні і діамінокарбонітрильні похідні піримідинів, їх композиції і способи лікування з їх допомогою
US9540333B2 (en) * 2012-11-08 2017-01-10 Bristol-Myers Squibb Company Alkyl amide-substituted pyrimidine compounds useful in the modulation of IL-12, IL-23 and/or IFNα
US9447025B2 (en) 2013-03-14 2016-09-20 Kalyra Pharmaceuticals, Inc. Bicyclic analgesic compounds
WO2015039613A1 (zh) * 2013-09-18 2015-03-26 北京韩美药品有限公司 抑制btk和/或jak3激酶活性的化合物
JP6345786B2 (ja) 2013-12-05 2018-06-20 ファーマサイクリックス エルエルシー ブルトン型チロシンキナーゼの阻害剤
CN108947867A (zh) 2013-12-12 2018-12-07 卡利拉制药公司 双环烷基化合物及合成
BR112016014412A2 (pt) * 2013-12-20 2017-08-08 Signal Pharm Llc Compostos de diaminopirimidil substituído, composições do mesmo, e métodos de tratamento com o mesmo
NZ715903A (en) * 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
EP3114107B1 (en) 2014-03-07 2020-07-22 Recurium IP Holdings, LLC Propellane derivates and synthesis
US10308609B2 (en) 2014-09-17 2019-06-04 Zeno Royalties & Milestones, LLC Bicyclic compounds
CA3210612A1 (en) * 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
JP6903577B2 (ja) * 2014-12-16 2021-07-14 シグナル ファーマシューティカルズ，エルエルシー 皮膚におけるｃ−Ｊｕｎ Ｎ末端キナーゼの阻害の測定方法
WO2016123291A1 (en) 2015-01-29 2016-08-04 Signal Pharmaceuticals, Llc Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
CA2993173C (en) 2015-07-24 2023-10-03 Celgene Corporation Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein
WO2018019244A1 (zh) * 2016-07-27 2018-02-01 广东东阳光药业有限公司 2,6-二甲基嘧啶酮衍生物的盐及其用途
WO2018029336A1 (en) 2016-08-12 2018-02-15 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for determining whether a subject was administered with an activator of the ppar beta/delta pathway.
EP3509586A4 (en) * 2016-09-12 2020-05-06 Imago Pharmaceuticals, Inc. TREATMENT OF FIBROTIC DISORDERS WITH JUN N-TERMINAL KINASE INHIBITORS
EP3551180B1 (en) 2016-12-09 2021-09-29 Cadila Healthcare Limited Treatment for primary biliary cholangitis
WO2018213140A1 (en) 2017-05-15 2018-11-22 Zeno Royalties & Milestones, LLC Analgesic compounds
KR102757890B1 (ko) 2017-08-09 2025-01-23 데날리 테라퓨틱스 인크. 화합물, 조성물 및 방법
TW201920129A (zh) 2017-09-01 2019-06-01 美商戴納立製藥公司 化合物、組合物及方法
CN107573249B (zh) * 2017-09-25 2018-12-25 上海馨远医药科技有限公司 一种反式4-烷氧基环己胺的制备方法
AR113820A1 (es) 2017-11-01 2020-06-17 Bristol Myers Squibb Co Compuestos bicíclicos en puente como moduladores del receptor farnesoide x
WO2020168011A1 (en) 2019-02-13 2020-08-20 Denali Therapeutics Inc. Compounds, compositions and methods
EP3924341A4 (en) 2019-02-13 2022-11-02 Denali Therapeutics Inc. Compounds, compositions and methods
WO2020187292A1 (zh) * 2019-03-19 2020-09-24 北京赛特明强医药科技有限公司 2-取代吡唑氨基-4-取代氨基-5-嘧啶甲酰胺类化合物、组合物及其应用
AU2020300619A1 (en) 2019-07-03 2022-01-27 Sumitomo Pharma Oncology, Inc. Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof
KR102730711B1 (ko) * 2019-08-06 2024-11-18 일라이 릴리 앤드 캄파니 피리미딘-5-카르복스아미드 화합물
CN112574123B (zh) * 2019-09-30 2024-06-11 武汉朗来科技发展有限公司 Jnk抑制剂、其药物组合物和用途
US20230131830A1 (en) * 2020-03-06 2023-04-27 National Health Research Institutes Pyrimidine compounds and their pharmaceutical uses
CN113698408B (zh) * 2020-05-22 2025-07-25 武汉朗来科技发展有限公司 Jnk抑制剂、其药物组合物和用途
WO2022048684A1 (zh) * 2020-09-07 2022-03-10 武汉朗来科技发展有限公司 Jnk抑制剂、其药物组合物和用途
US20230416225A1 (en) * 2020-11-09 2023-12-28 Merck Sharp & Dohme Llc Diaminopyrimidine carboxamide inhibitors of hpk1
WO2022178559A1 (en) * 2021-02-22 2022-08-25 The Trustees Of Princeton University 2-substituted bicyclo[1.1.1]pentanes
WO2023109954A1 (en) 2021-12-16 2023-06-22 Lynk Pharmaceuticals Co. Ltd. Tyk2 inhibitors and compositions and methods thereof
WO2023108536A1 (en) * 2021-12-16 2023-06-22 Lynk Pharmaceuticals Co. Ltd. Tyk2 inhibitors and compositions and methods thereof
CN114315738B (zh) * 2022-01-15 2023-08-18 重庆东寰科技开发有限公司 一种2,4-二氨基嘧啶-3-氧化物的制备方法
US20240165112A1 (en) 2022-11-04 2024-05-23 Bristol-Myers Squibb Company Therapy for the treatment of cancer
WO2024141066A1 (zh) * 2022-12-30 2024-07-04 杭州矩阵生物药业有限公司 具有jnk抑制活性的嘧啶类衍生物及其应用

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999031073A1 (en) * 1997-12-15 1999-06-24 Yamanouchi Pharmaceutical Co., Ltd. Novel pyrimidine-5-carboxamide derivatives
WO2003082855A1 (en) 2002-03-28 2003-10-09 Kyowa Hakko Kogyo Co., Ltd. Anti-inflammatory agent
WO2004067516A1 (en) * 2003-01-30 2004-08-12 Boehringer Ingelheim Pharmaceuticals, Inc. 2,4-diaminopyrimidine derivatives useful as inhibitors of pkc-theta
CN1665789A (zh) * 2002-06-28 2005-09-07 山之内制药株式会社 二氨基嘧啶酰胺衍生物
WO2006014482A1 (en) * 2004-07-08 2006-02-09 Boehringer Ingelheim Pharmaceuticals, Inc. Pyrimidine derivatives useful as inhibitors of pkc-theta
WO2010024430A1 (ja) * 2008-09-01 2010-03-04 アステラス製薬株式会社 2,4-ジアミノピリミジン化合物
WO2010129802A1 (en) * 2009-05-06 2010-11-11 Portola Pharmaceuticals, Inc. Inhibitors of jak
WO2010134533A1 (ja) * 2009-05-20 2010-11-25 アステラス製薬株式会社 アミノシクロヘキシルアルキル基を有する2,4-ジアミノピリミジン化合物

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH549339A (de) 1971-05-12 1974-05-31 Ciba Geigy Ag Herbizides mittel.
US4301281A (en) * 1979-04-18 1981-11-17 American Home Products Corporation 7,8-Dihydro-2,5,8-trisubstituted-7-oxo-pyrido[2,3-d]-pyrimidine-6-carboxylic acid amides
DE3338859A1 (de) * 1983-10-26 1985-05-09 Bayer Ag, 5090 Leverkusen Substituierte pyrimidine
DE69839338T2 (de) * 1997-02-05 2008-07-10 Warner-Lambert Company Llc Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation
SK17532000A3 (sk) 1998-05-26 2002-08-06 Warner-Lambert Company Prípadne substituované 3,4-dihydrogenované pyrimidíny, ich použitie a farmaceutické formulácie na ich báze
ATE342892T1 (de) 1998-08-29 2006-11-15 Astrazeneca Ab Pyrimidine verbindungen
JP4622047B2 (ja) 1999-06-09 2011-02-02 アステラス製薬株式会社 新規なヘテロ環カルボキサミド誘導体
DE60017898T2 (de) * 1999-06-09 2006-01-12 Yamanouchi Pharmaceutical Co., Ltd. Neuartige heterocyclische carboxamidderivate
AU5108000A (en) 1999-06-10 2001-01-02 Yamanouchi Pharmaceutical Co., Ltd. Novel nitrogen-contaiing heterocyclic derivatives or salts thereof
ATE253915T1 (de) 1999-06-30 2003-11-15 Merck & Co Inc Src-kinase hemmende verbindungen
GB0016877D0 (en) * 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
JP4329290B2 (ja) * 2000-10-06 2009-09-09 田辺三菱製薬株式会社 脂肪族含窒素五員環化合物
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
KR20050008849A (ko) 2002-06-25 2005-01-21 교와 핫꼬 고교 가부시끼가이샤 2 환성 복소환 화합물
IL166241A0 (en) * 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
KR20050065670A (ko) * 2002-11-01 2005-06-29 아보트 러보러터리즈 항감염제
US7902203B2 (en) 2002-11-01 2011-03-08 Abbott Laboratories, Inc. Anti-infective agents
JPWO2004054617A1 (ja) 2002-12-13 2006-04-20 協和醗酵工業株式会社 中枢疾患の予防および／または治療剤
MXPA05007503A (es) 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
KR100864393B1 (ko) * 2003-04-10 2008-10-20 에프. 호프만-라 로슈 아게 피리미도 화합물
EP1518655A1 (en) * 2003-07-24 2005-03-30 John Palmer Corp. Apparatus for and process of gas-assisted injection molding of plastics material
PL2287156T3 (pl) 2003-08-15 2013-11-29 Novartis Ag 2,4-Di(fenyloamino)-pirymidyny stosowane w leczeniu chorób nowotworowych, chorób zapalnych i zaburzeń układu immunologicznego
RU2006107578A (ru) 2003-09-24 2007-10-27 Вайет Холдингз Корпорейшн (Us) 6-арилпиримидин, применяемый в качестве противоракового агента
US7253204B2 (en) * 2004-03-26 2007-08-07 Methylgene Inc. Inhibitors of histone deacetylase
EP1749827A4 (en) 2004-03-30 2010-04-21 Kyowa Hakko Kirin Co Ltd ANTITUMOR AGENTS
JP2008512429A (ja) 2004-09-10 2008-04-24 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング ロフルミラストとｓｙｋインヒビターとの組合せ物並びにその使用方法
EP1796679A1 (en) 2004-09-10 2007-06-20 Altana Pharma AG Ciclesonide and syk inhibitor combination and methods of use thereof
JP2006124387A (ja) 2004-09-30 2006-05-18 Taisho Pharmaceut Co Ltd 新規なキノリン、テトラヒドロキナゾリン、及びピリミジン誘導体と、これらを使用することに関連した治療方法
WO2006035069A1 (en) 2004-09-30 2006-04-06 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 5-substituted pyrimidines
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
US20110098301A1 (en) 2005-03-10 2011-04-28 Bayer Healthcare Llc Pyrimidine Derivatives for Treatment of Hyperproliferative Disorders
JP2009506006A (ja) * 2005-08-25 2009-02-12 エフ．ホフマン−ラ ロシュ アーゲー ｐ３８ＭＡＰキナーゼ阻害剤およびその使用方法
WO2007032445A1 (ja) 2005-09-16 2007-03-22 Kyowa Hakko Kogyo Co., Ltd. タンパク質キナーゼ阻害剤
US20090221600A1 (en) * 2005-09-28 2009-09-03 Ashwani Kumar Verma Pyrido-pyridimidine derivatives useful as antiinflammatory agents
WO2007076247A1 (en) * 2005-12-21 2007-07-05 Boehringer Ingelheim International Gmbh Pyrimidine derivatives useful as inhibitors of pkc-theta
JP2009544592A (ja) * 2006-07-21 2009-12-17 ノバルティス アクチエンゲゼルシャフト Ｊａｋキナーゼ阻害剤としての２，４−ジ（アリールアミノ）−ピリミジン−５−カルボキサミド化合物
US8188113B2 (en) 2006-09-14 2012-05-29 Deciphera Pharmaceuticals, Inc. Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
US20080139531A1 (en) 2006-12-04 2008-06-12 Alcon Manufacturing Ltd. Use of connective tissue mast cell stabilizers to facilitate ocular surface re-epithelization and wound repair
JP4782239B2 (ja) 2007-04-18 2011-09-28 ファイザー・プロダクツ・インク 異常細胞増殖治療のためのスルホニルアミド誘導体
US20090036440A1 (en) 2007-04-27 2009-02-05 Astrazeneca Ab Novel pyrimidine derivatives - 816
CN101796046A (zh) 2007-07-16 2010-08-04 阿斯利康(瑞典)有限公司 嘧啶衍生物934
WO2009012421A1 (en) 2007-07-17 2009-01-22 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
US8063058B2 (en) * 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
CN102066340B (zh) * 2008-04-16 2014-05-14 波托拉医药品公司 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物
KR20100132550A (ko) * 2008-04-16 2010-12-17 포톨라 파마슈티컬스, 인코포레이티드 ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드
CA2719936A1 (en) 2008-04-22 2009-10-29 Astrazeneca Ab Substituted pyrimidin-5-carboxamides 281
JP2011518219A (ja) 2008-04-22 2011-06-23 ポートラ ファーマシューティカルズ， インコーポレイテッド タンパク質キナーゼの阻害剤
CA2719868A1 (en) * 2008-04-29 2009-11-05 F. Hoffmann-La Roche Ag Pyrimidinyl pyridone inhibitors of jnk.
AU2009248923B2 (en) 2008-05-21 2015-01-29 Takeda Pharmaceutical Company Limited Phosphorous derivatives as kinase inhibitors
PE20100087A1 (es) 2008-06-25 2010-02-08 Irm Llc Compuestos y composiciones como inhibidores de cinasa
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
NZ589843A (en) 2008-06-27 2012-12-21 Avila Therapeutics Inc Pyrimidine heteroaryl compounds and uses thereof as protein kinase inhibitors
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶，其組合物及使用其之治療方法
KR20110060894A (ko) 2008-09-18 2011-06-08 아스테라스 세이야쿠 가부시키가이샤 복소환 카르복사미드 화합물
WO2010038081A2 (en) 2008-10-03 2010-04-08 Astrazeneca Ab Heterocyclic derivatives and methods of use thereof
JP2012505927A (ja) * 2008-10-22 2012-03-08 エフ．ホフマン−ラ ロシュ アーゲー Ｊｎｋのピリミジニルピリドン阻害剤
EP2346988B1 (en) 2008-10-31 2017-05-31 Janssen Biotech, Inc. Differentiation of human embryonic stem cells to the pancreatic endocrine lineage
AU2009325398A1 (en) * 2008-12-12 2010-06-17 Msd K.K. Dihydropyrimidopyrimidine derivative
US8809538B2 (en) 2009-01-12 2014-08-19 Array Biopharma Inc. Piperidine-containing compounds and use thereof
WO2010097248A1 (en) 2009-01-13 2010-09-02 Glaxo Group Limited Pyrimidinecarboxamide derivatives as inhibitors of syk kinase
JP5781943B2 (ja) * 2009-01-21 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 炎症性疾患、自己免疫疾患または増殖性疾患の治療に有用なｎ２−（３−ピリジルまたはフェニル）−ｎ４−（４−ピペリジル）−２，４−ピリミジンジアミン誘導体
US8419772B2 (en) * 2009-06-08 2013-04-16 Reduction Technologies, Inc. Systems, methods and devices for correcting spinal deformities
EP2440548A1 (en) * 2009-06-10 2012-04-18 Abbott Laboratories 2- ( lh-pyrazol-4 -ylamino ) -pyrimidine as kinase inhibitors
JP2012197231A (ja) 2009-08-06 2012-10-18 Oncotherapy Science Ltd Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体
WO2011065800A2 (ko) * 2009-11-30 2011-06-03 주식회사 오스코텍 피리미딘 유도체, 이의 제조방법 및 이를 함유하는 약학적 조성물
JP5802677B2 (ja) 2009-12-01 2015-10-28 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
JP2011173853A (ja) * 2010-02-26 2011-09-08 Astellas Pharma Inc 置換アミノアダマンチルアルキル基を有する２，４−ジアミノピリミジン化合物
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
WO2012045020A1 (en) 2010-09-30 2012-04-05 Portola Pharmaceuticals, Inc. Combinations of 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide and fludarabine
WO2012044936A1 (en) 2010-09-30 2012-04-05 Portola Pharmaceuticals, Inc. Combination therapy with 4-(3-(2h-1,2,3-triazol-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide
UA120740C2 (uk) * 2011-04-22 2020-02-10 Сігнал Фармасьютікалз, Елелсі Заміщені діамінокарбоксамідні і діамінокарбонітрильні похідні піримідинів, їх композиції і способи лікування з їх допомогою
BR112016014412A2 (pt) * 2013-12-20 2017-08-08 Signal Pharm Llc Compostos de diaminopirimidil substituído, composições do mesmo, e métodos de tratamento com o mesmo
NZ715903A (en) * 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
JP6903577B2 (ja) * 2014-12-16 2021-07-14 シグナル ファーマシューティカルズ，エルエルシー 皮膚におけるｃ−Ｊｕｎ Ｎ末端キナーゼの阻害の測定方法
CA3210612A1 (en) * 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999031073A1 (en) * 1997-12-15 1999-06-24 Yamanouchi Pharmaceutical Co., Ltd. Novel pyrimidine-5-carboxamide derivatives
WO2003082855A1 (en) 2002-03-28 2003-10-09 Kyowa Hakko Kogyo Co., Ltd. Anti-inflammatory agent
CN1665789A (zh) * 2002-06-28 2005-09-07 山之内制药株式会社 二氨基嘧啶酰胺衍生物
WO2004067516A1 (en) * 2003-01-30 2004-08-12 Boehringer Ingelheim Pharmaceuticals, Inc. 2,4-diaminopyrimidine derivatives useful as inhibitors of pkc-theta
WO2006014482A1 (en) * 2004-07-08 2006-02-09 Boehringer Ingelheim Pharmaceuticals, Inc. Pyrimidine derivatives useful as inhibitors of pkc-theta
WO2010024430A1 (ja) * 2008-09-01 2010-03-04 アステラス製薬株式会社 2,4-ジアミノピリミジン化合物
WO2010129802A1 (en) * 2009-05-06 2010-11-11 Portola Pharmaceuticals, Inc. Inhibitors of jak
WO2010134533A1 (ja) * 2009-05-20 2010-11-25 アステラス製薬株式会社 アミノシクロヘキシルアルキル基を有する2,4-ジアミノピリミジン化合物

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Nagashima S et al., Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine-5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors, Bioorg Med Chem., vol.16, 2008, pp.6509-6521
Nagashima S et al., Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors, Bioorg Med Chem., vol.15, 2007, pp.1044-1055
Nagashima S et al., Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors, Bioorg Med Chem., vol.15, 2007, pp.1044-1055 Nagashima S et al., Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine-5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors, Bioorg Med Chem., vol.16, 2008, pp.6509-6521 *

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