JP2010514689A5 - - Google Patents
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- JP2010514689A5 JP2010514689A5 JP2009543209A JP2009543209A JP2010514689A5 JP 2010514689 A5 JP2010514689 A5 JP 2010514689A5 JP 2009543209 A JP2009543209 A JP 2009543209A JP 2009543209 A JP2009543209 A JP 2009543209A JP 2010514689 A5 JP2010514689 A5 JP 2010514689A5
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Families Citing this family (115)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2152688A1 (en) * | 2007-05-04 | 2010-02-17 | Irm Llc | Compounds and compositions as c-kit and pdgfr kinase inhibitors |
| ES2535166T3 (es) * | 2007-09-04 | 2015-05-06 | The Scripps Research Institute | Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas |
| CA2738925A1 (en) * | 2008-10-01 | 2010-04-08 | The University Of North Carolina At Chapel Hill | Hematopoietic protection against chemotherapeutic compounds using selective cyclin-dependent kinase 4/6 inhibitors |
| US20110294810A1 (en) * | 2008-11-14 | 2011-12-01 | Christian Beier | Substituted (pyridyl)-azinylamine derivatives as plant protection agents |
| EP3718560A3 (en) | 2009-05-13 | 2020-12-09 | The University of North Carolina at Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
| US8415381B2 (en) * | 2009-07-30 | 2013-04-09 | Novartis Ag | Heteroaryl compounds and their uses |
| US20110130380A1 (en) * | 2009-09-04 | 2011-06-02 | Barsanti Paul A | Heteroaryl Kinase Inhibitors |
| CN102482265A (zh) * | 2009-09-04 | 2012-05-30 | 诺瓦提斯公司 | 用于治疗增殖性疾病的吡嗪基吡啶化合物 |
| AU2010338365B2 (en) * | 2009-12-31 | 2014-01-30 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
| EP2550257B1 (en) * | 2010-03-22 | 2016-12-21 | Lead Discovery Center GmbH | Pharmaceutically active disubstituted triazine derivatives |
| US9808461B2 (en) | 2010-11-17 | 2017-11-07 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from ischemia through inhibition of the proliferative kinases CDK4 and CDK6 |
| EP2640702A1 (en) * | 2010-11-17 | 2013-09-25 | Novartis AG | 3-(aminoaryl)-pyridine compounds |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| WO2012101064A1 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | N-acyl pyrimidine biaryl compounds as protein kinase inhibitors |
| WO2012101065A2 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | Pyrimidine biaryl amine compounds and their uses |
| WO2012101063A1 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | N-acyl pyridine biaryl compounds and their uses |
| WO2012101066A1 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | Pyridine biaryl amine compounds and their uses |
| JP5959537B2 (ja) * | 2011-01-28 | 2016-08-02 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換ピリジニル−ピリミジン及び医薬としてのその使用 |
| JP2014506878A (ja) * | 2011-01-28 | 2014-03-20 | ノバルティス アーゲー | Ｃｄｋ９阻害剤としての置換ビ−ヘテロアリール化合物およびそれらの使用 |
| JP6085866B2 (ja) | 2011-02-28 | 2017-03-01 | アレイ バイオファーマ、インコーポレイテッド | セリン／トレオニンキナーゼインヒビター |
| US9226929B2 (en) | 2011-03-02 | 2016-01-05 | Bayer Intellectual Property Gmbh | Pharmaceutically active disubstituted triazine derivatives |
| EP2681193B1 (en) * | 2011-03-02 | 2016-01-06 | Lead Discovery Center GmbH | Pharmaceutically active disubstituted pyridine derivatives |
| ES2613103T3 (es) | 2011-04-19 | 2017-05-22 | Bayer Intellectual Property Gmbh | 4-Aril-n-fenil-1,3,5-triacin-2-aminas sustituidas |
| EP2527332A1 (en) | 2011-05-24 | 2012-11-28 | Bayer Intellectual Property GmbH | 4-Aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group as CDK9 inhibitors |
| 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 |
| BR112014002675A2 (pt) | 2011-08-04 | 2017-02-21 | Array Biopharma Inc | "quinazolina como inibidores de serina/treonina quinase, seus usos, e composição" |
| EP2562265A1 (en) | 2011-08-22 | 2013-02-27 | Lead Discovery Center GmbH | Susceptibility to selective CDK9 inhibitors |
| EP2561867A1 (en) | 2011-08-22 | 2013-02-27 | Lead Discovery Center GmbH | CDK9 inhibitors in the treatment of midline carcinoma |
| EP2755948B1 (en) | 2011-09-16 | 2016-05-25 | Bayer Intellectual Property GmbH | Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group |
| US9108926B2 (en) * | 2011-09-16 | 2015-08-18 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro-pyrimidines |
| US9498471B2 (en) | 2011-10-20 | 2016-11-22 | The Regents Of The University Of California | Use of CDK9 inhibitors to reduce cartilage degradation |
| PL2820009T3 (pl) | 2012-03-01 | 2018-09-28 | Array Biopharma, Inc. | Inhibitory kinaz serynowo/treoninowych |
| PE20190736A1 (es) | 2012-06-13 | 2019-05-23 | Incyte Holdings Corp | Compuestos triciclicos sustituidos como inhibidores del receptor del factor de crecimiento de fibroblastos (fgfr) |
| US8901305B2 (en) * | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| MX2015002310A (es) * | 2012-08-23 | 2015-06-05 | Hoffmann La Roche | Nuevas amidas de fenil-piridina/pirazina para el tratamiento de cancer. |
| CA2882750A1 (en) | 2012-08-27 | 2014-03-06 | Jim Blake | Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases |
| WO2014048065A1 (en) * | 2012-09-28 | 2014-04-03 | Merck Sharp & Dohme Corp. | Triazolyl derivatives as syk inhibitors |
| 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 |
| 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 |
| ES2616441T3 (es) | 2012-10-18 | 2017-06-13 | Bayer Pharma Aktiengesellschaft | Derivados de N-(piridin-2-il))pirimidin-4-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 |
| AU2013346939B2 (en) | 2012-11-15 | 2017-06-08 | Bayer Pharma Aktiengesellschaft | 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group |
| KR20220143164A (ko) | 2012-11-21 | 2022-10-24 | 피티씨 테라퓨틱스, 인크. | 치환된 리버스 피리미딘 ｂｍｉ-1 저해제 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| WO2014144326A1 (en) | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | Transient protection of normal cells during chemotherapy |
| CN105407723A (zh) | 2013-03-15 | 2016-03-16 | G1治疗公司 | 高效的抗赘生剂和抗增生剂 |
| KR102269032B1 (ko) | 2013-04-19 | 2021-06-24 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| ES2630115T3 (es) | 2013-07-04 | 2017-08-18 | Bayer Pharma Aktiengesellschaft | Derivados de 5-fluoro-n-(piridin-2-il)piridin-2-amina con sulfoximina sustituida y su uso como inhibidores de quinasa cdk9 |
| CA2922657C (en) | 2013-08-30 | 2022-04-12 | Ptc Therapeutics, Inc. | Substituted pyrimidine bmi-1 inhibitors |
| AR097894A1 (es) * | 2013-10-03 | 2016-04-20 | Hoffmann La Roche | Inhibidores terapéuticos de cdk8 o uso de los mismos |
| US10584115B2 (en) | 2013-11-21 | 2020-03-10 | Ptc Therapeutics, Inc. | Substituted pyridine and pyrazine BMI-1 inhibitors |
| US9949976B2 (en) | 2013-12-31 | 2018-04-24 | Xuanzhu Pharma Co., Ltd. | Kinase inhibitor and use thereof |
| HUE039504T2 (hu) * | 2013-12-31 | 2019-01-28 | Xuanzhu Pharma Co Ltd | Kináz inhibitor és alkalmazása |
| TN2016000270A1 (en) | 2014-01-14 | 2017-10-06 | Millennium Pharm Inc | Heteroaryls and uses thereof. |
| JP2017502092A (ja) | 2014-01-14 | 2017-01-19 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | ヘテロアリール及びその使用 |
| EP3116869A1 (en) | 2014-03-13 | 2017-01-18 | Bayer Pharma Aktiengesellschaft | 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group |
| CN106414412B (zh) | 2014-04-01 | 2019-06-21 | 拜耳医药股份有限公司 | 含有磺酰二亚胺基团的二取代的5-氟嘧啶衍生物 |
| CR20160471A (es) | 2014-04-11 | 2016-12-21 | Bayer Pharma AG | Compuestos novedosos macrocíclicos |
| US20150297606A1 (en) | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic Lactams for Use in the Protection of Hematopoietic Stem and Progenitor Cells Against Ionizing Radiation |
| WO2016040858A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| CA3000633C (en) | 2014-10-14 | 2023-10-03 | The Regents Of The University Of California | Use of cdk9 and brd4 inhibitors to inhibit inflammation |
| CA2964696C (en) | 2014-10-16 | 2022-09-06 | Bayer Pharma Aktiengesellschaft | Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfoximine group |
| CA2964683A1 (en) | 2014-10-16 | 2016-04-21 | Bayer Pharma Aktiengesellschaft | Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfone group |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CN105085489B (zh) | 2014-11-05 | 2019-03-01 | 益方生物科技（上海）有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| ES2895769T3 (es) | 2015-02-20 | 2022-02-22 | Incyte Corp | Heterociclos bicíclicos como inhibidores de FGFR |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| EP3274338A1 (en) | 2015-03-24 | 2018-01-31 | 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 |
| 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 |
| CN106188029B (zh) * | 2015-05-05 | 2018-09-18 | 山东轩竹医药科技有限公司 | 二并环类间变性淋巴瘤激酶抑制剂 |
| CN106699785A (zh) * | 2015-07-13 | 2017-05-24 | 南开大学 | 作为CDK4/6抑制剂的2-(N-氧化吡啶-2基氨基)-吡啶并[2,3-d]嘧啶-7-酮类化合物 |
| CA2999931A1 (en) | 2015-09-29 | 2017-04-06 | Bayer Pharma Aktiengesellschaft | Novel macrocyclic sulfondiimine compounds |
| JP6888000B2 (ja) | 2015-10-08 | 2021-06-16 | バイエル ファーマ アクチエンゲゼルシャフト | 新規な修飾された大環状化合物 |
| WO2017060322A2 (en) | 2015-10-10 | 2017-04-13 | Bayer Pharma Aktiengesellschaft | Ptefb-inhibitor-adc |
| WO2018106729A1 (en) | 2016-12-05 | 2018-06-14 | G1 Therapeutics, Inc. | Preservation of immune response during chemotherapy regimens |
| EP3601236A1 (en) | 2017-03-28 | 2020-02-05 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| ES2900199T3 (es) | 2017-03-28 | 2022-03-16 | Bayer Ag | Novedosos compuestos macrocíclicos inhibidores de PTEFB |
| GB201705263D0 (en) * | 2017-03-31 | 2017-05-17 | Probiodrug Ag | Novel inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CN109985241B (zh) * | 2017-12-29 | 2024-10-18 | 广州威溶特医药科技有限公司 | Cdk抑制剂和溶瘤病毒在制备抗肿瘤药物的应用 |
| WO2019136451A1 (en) | 2018-01-08 | 2019-07-11 | G1 Therapeutics, Inc. | G1t38 superior dosage regimes |
| CN110041253B (zh) * | 2018-01-17 | 2022-03-29 | 上海翰森生物医药科技有限公司 | 吡啶类n-氧化衍生物及其制备方法和应用 |
| 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 |
| SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
| SI3788047T1 (sl) | 2018-05-04 | 2024-11-29 | Incyte Corporation | Trdne oblike inhibitorja fgfr in postopki priprave le-teh |
| BR112021002630A2 (pt) | 2018-08-17 | 2021-05-11 | Ptc Therapeutics, Inc. | método para tratar câncer pancreático |
| TWI831829B (zh) | 2018-09-12 | 2024-02-11 | 美商建南德克公司 | 苯氧基-吡啶基-嘧啶化合物及使用方法 |
| JP7098826B2 (ja) * | 2018-09-12 | 2022-07-11 | ジェネンテック， インコーポレイテッド | ピリミジニル－ヘテロアリールオキシ－ナフチル化合物および使用方法 |
| WO2020125513A1 (zh) | 2018-12-19 | 2020-06-25 | 凯复制药有限公司 | 作为cdk抑制剂的大环化合物、其制备方法及其在医药上的应用 |
| WO2020142612A1 (en) | 2019-01-03 | 2020-07-09 | Genentech, Inc. | Pyrido-pyrimidinone and pteridinone compounds as inhibitors of endoribonuclease inositol requiring enzyme i (ire i alpha) for the treatment of cancer diseases. |
| CN109678962B (zh) * | 2019-01-22 | 2020-05-08 | 山西农业大学 | 一种Cdk5纳米抗体和筛选方法 |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| CN109836385B (zh) * | 2019-04-04 | 2021-12-17 | 上海翰森生物医药科技有限公司 | 四氢喹啉类n-氧化衍生物及其制备方法和应用 |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CN110511211B (zh) * | 2019-08-30 | 2020-10-16 | 武汉工程大学 | 一种吲唑哌啶嘧啶类化合物的应用 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11607416B2 (en) | 2019-10-14 | 2023-03-21 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CN111349624A (zh) * | 2020-03-20 | 2020-06-30 | 深圳大学 | 核酸、多肽偶联组合物、多肽组合物及其制备方法和应用 |
| US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
| CN115843296B (zh) * | 2020-08-07 | 2024-03-08 | 南京迈晟科技有限责任公司 | Cdk9抑制剂及其用途 |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| KR102693170B1 (ko) * | 2021-04-27 | 2024-08-08 | 재단법인 아산사회복지재단 | 사이클린 의존성 키나아제 억제용 조성물 및 이의 의학적 용도 |
| US12097261B2 (en) | 2021-05-07 | 2024-09-24 | Kymera Therapeutics, Inc. | CDK2 degraders and uses thereof |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CN117384135A (zh) * | 2022-07-04 | 2024-01-12 | 浙江同源康医药股份有限公司 | 用作cdk7激酶抑制剂的化合物及其应用 |
| CN119841771A (zh) * | 2025-01-08 | 2025-04-18 | 华中农业大学 | 一种猪链球菌丝氨酸蛋白激酶抑制剂的筛选方法及其应用 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2087056T3 (es) * | 1986-01-13 | 1996-07-16 | American Cyanamid Co | 2-pirimidinaminas sustituidas en las posiciones 4, 5 y 6. |
| US4788195A (en) * | 1986-01-13 | 1988-11-29 | American Cyanamid Company | 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines |
| US5521184A (en) * | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| GB9523675D0 (en) * | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| US5744460A (en) * | 1996-03-07 | 1998-04-28 | Novartis Corporation | Combination for treatment of proliferative diseases |
| JP2001507349A (ja) * | 1996-12-23 | 2001-06-05 | セルテック セラピューティックス リミテッド | 縮合多環式２−アミノピリミジン誘導体、それらの製造およびたんぱく質チロシンキナーゼ抑制因子としてのそれらの使用 |
| WO2000040243A1 (en) * | 1999-01-08 | 2000-07-13 | Smithkline Beecham Corporation | Novel compounds |
| US7122544B2 (en) * | 2000-12-06 | 2006-10-17 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto |
| CA2441733A1 (en) * | 2001-03-29 | 2002-10-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| RU2315043C2 (ru) * | 2002-06-28 | 2008-01-20 | Ниппон Синяку Ко., Лтд. | Амидное производное, фармацевтическая композиция и терапевтические средства на его основе |
| GB0226724D0 (en) * | 2002-11-15 | 2002-12-24 | Merck Sharp & Dohme | Therapeutic agents |
| SE0203654D0 (sv) * | 2002-12-09 | 2002-12-09 | Astrazeneca Ab | New compounds |
| US7151096B2 (en) * | 2003-03-05 | 2006-12-19 | Irm Llc | Cyclic compounds and compositions as protein kinase inhibitors |
| GB0307268D0 (en) * | 2003-03-28 | 2003-05-07 | Syngenta Ltd | Organic compounds |
| WO2005065074A2 (en) * | 2003-09-09 | 2005-07-21 | Temple University Of The Commonwealth System Of Higher Education | Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors |
| JPWO2005063709A1 (ja) * | 2003-12-25 | 2007-07-19 | 日本新薬株式会社 | アミド誘導体及び医薬 |
| EP1751136B1 (en) * | 2004-05-07 | 2014-07-02 | Amgen Inc. | Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer |
| CA2578122A1 (en) * | 2004-08-27 | 2006-03-02 | Gpc Biotech Ag | Pyrimidine derivatives |
| US8268809B2 (en) * | 2006-09-05 | 2012-09-18 | Emory University | Kinase inhibitors for preventing or treating pathogen infection and method of use thereof |
-
2007
- 2007-12-20 WO PCT/US2007/088292 patent/WO2008079933A2/en not_active Ceased
- 2007-12-20 AU AU2007336933A patent/AU2007336933A1/en not_active Abandoned
- 2007-12-20 JP JP2009543209A patent/JP2010514689A/ja active Pending
- 2007-12-20 US US12/520,755 patent/US20100048597A1/en not_active Abandoned
- 2007-12-20 KR KR1020097012787A patent/KR20090091306A/ko not_active Withdrawn
- 2007-12-20 BR BRPI0720635-6A patent/BRPI0720635A2/pt not_active Application Discontinuation
- 2007-12-20 MX MX2009006536A patent/MX2009006536A/es not_active Application Discontinuation
- 2007-12-20 EA EA200900799A patent/EA200900799A1/ru unknown
- 2007-12-20 CA CA002672518A patent/CA2672518A1/en not_active Abandoned
- 2007-12-20 CN CNA2007800476340A patent/CN101568529A/zh active Pending
- 2007-12-20 EP EP07869607A patent/EP2094682A2/en not_active Withdrawn
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