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1. 发明申请

US20090202541A1 COMBINATION COMPRISING N-{5-[4-(4-METHYL-PIPERAZINO-METHYL)-BENZOYLAMIDO]-2-METHYLPHENYL)-4-(3-PYRIDYL)-2PYRIMIDINE-AMINE AND A CHEMOTHERAPEUTIC AGENT 审中-公开
标题翻译：包含N- {5- [4-（4-甲基 - 哌嗪基 - 甲基） - 苯甲酰氨基] -2-甲基苯基）-4-（3-吡啶基）-2-嘧啶胺和化学代谢物的组合
公开(公告)号：US20090202541A1
公开(公告)日：2009-08-13
申请号：US12423079
申请日：2009-04-14
申请人： Christian Bruns , Elisabeth Buchdunger , Terence O'Reilly , Sandra Leta Silberman , Markus Wartmann , Gisbert Weckbecker
发明人： Christian Bruns , Elisabeth Buchdunger , Terence O'Reilly , Sandra Leta Silberman , Markus Wartmann , Gisbert Weckbecker
IPC分类号： A61K31/506 , A61K39/395 , A61K31/704 , A61P35/00
CPC分类号： A61K45/06 , A61K31/506
摘要： A method of treating a warm-blooded animal, especially a human, having a proliferative disease or acute or chronic transplant rejection comprising administering to the animal a combination which comprises (a) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and (b) a chemotherapeutic agent selected from antineoplastic agents, especially as defined herein, and agents effective in treating acute or chronic transplant rejection; a combination comprising (a) and (b) as defined above and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease.
摘要翻译：一种治疗具有增殖性疾病或急性或慢性移植排斥反应的温血动物，特别是人的方法，包括向动物施用包含（a）N- {5- [4-（4-甲基 - 哌嗪子基） - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺和（b）选自抗肿瘤剂，特别是本文所定义的化学治疗剂和有效治疗急性或慢性的药物移植排斥反应包含如上定义的（a）和（b）和任选的至少一种用于同时，分开或顺序使用的药学上可接受的载体的组合，特别是用于延缓进展或治疗增殖性疾病，特别是实体肿瘤疾病。

2. 发明申请

US20120283206A1 Combination comprising N--4-(3-pyridyl)-2pyrimidine-amine and a chemotherapeutic agent. 审中-公开
标题翻译：包含N-4-（3-吡啶基）-2嘧啶胺和化学治疗剂的组合。
公开(公告)号：US20120283206A1
公开(公告)日：2012-11-08
申请号：US13551079
申请日：2012-07-17
申请人： Christian Bruns , Elisabeth Buchdunger , Terence O'Reilly , Sandra Leta Siberman , Markus Wartmann , Gisbert Weckbecker
发明人： Christian Bruns , Elisabeth Buchdunger , Terence O'Reilly , Sandra Leta Siberman , Markus Wartmann , Gisbert Weckbecker
IPC分类号： A61K31/506 , A61K31/675 , A61P37/06 , A61K31/704 , A61P35/00
CPC分类号： A61K45/06 , A61K31/506
摘要： A method of treating a warm-blooded animal, especially a human, having a proliferative disease or acute or chronic transplant rejection comprising administering to the animal a combination which comprises (a) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and (b) a chemotherapeutic agent selected from antineoplastic agents, especially as defined herein, and agents effective in treating acute or chronic transplant rejection; a combination comprising (a) and (b) as defined above and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease.
摘要翻译：一种治疗具有增殖性疾病或急性或慢性移植排斥反应的温血动物，特别是人的方法，包括向动物施用包含（a）N- {5- [4-（4-甲基 - 哌嗪子基） - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺和（b）选自抗肿瘤剂，特别是本文所定义的化学治疗剂和有效治疗急性或慢性的药物移植排斥反应包含如上定义的（a）和（b）和任选的至少一种用于同时，分开或顺序使用的药学上可接受的载体的组合，特别是用于延缓进展或治疗增殖性疾病，特别是实体肿瘤疾病。

3. 发明授权

US07723339B2 Combination comprising a signal transduction inhibitor and an epothilone derivative 失效
标题翻译：包含信号转导抑制剂和埃坡霉素衍生物的组合
公开(公告)号：US07723339B2
公开(公告)日：2010-05-25
申请号：US10469367
申请日：2002-02-26
申请人： Ralf Brandt , Elisabeth Buchdunger , Carl-Henrik Heldin , Arne Östman , Kristian Pietras , Terence O'Reilly , John D Rothermel , Peter Traxler , Markus Wartmann
发明人： Ralf Brandt , Elisabeth Buchdunger , Carl-Henrik Heldin , Arne Östman , Kristian Pietras , Terence O'Reilly , John D Rothermel , Peter Traxler , Markus Wartmann
IPC分类号： A61K31/497 , A61K31/425 , A01N43/78 , A01N43/54 , C07D239/42 , C07D401/04 , A61K31/435 , A01N43/40 , A61K31/505
CPC分类号： A61K31/505 , A61K31/425 , A61K45/06 , A61K31/435 , A61K2300/00
摘要： The present invention relates to a combination comprising N-{5-[4-(4-methyl-piperazino-methyl) -benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and an epothiione derivative; pharmaceutical composition comprising said combination; method of treatment comprising said combination; and commercial packages comprising said combination.
摘要翻译：本发明涉及包含N- {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺和环硫代衍生物; 包含所述组合的药物组合物; 包括所述组合的处理方法; 以及包括所述组合的商业包装。

4. 发明授权

US06958335B2 Treatment of gastrointestinal stromal tumors 有权
标题翻译：治疗胃肠道间质瘤
公开(公告)号：US06958335B2
公开(公告)日：2005-10-25
申请号：US10415015
申请日：2001-10-26
申请人： Elisabeth Buchdunger , Renaud Capdeville , George Daniel Demetri , Sasa Dimitrijevic , Brian Jay Druker , Jonathan A. Fletcher , Michael C. Heinrich , Heikki Joensuu , Sandra Leta Silberman , David Tuveson
发明人： Elisabeth Buchdunger , Renaud Capdeville , George Daniel Demetri , Sasa Dimitrijevic , Brian Jay Druker , Jonathan A. Fletcher , Michael C. Heinrich , Heikki Joensuu , Sandra Leta Silberman , David Tuveson
IPC分类号： A61K31/506 , A61P35/00 , C07D401/04 , A61K31/497
CPC分类号： C07D401/04 , A61K31/506
摘要： 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of the formula I or a pharmaceutically acceptable salt thereof can be used in the treatment of gastrointestinal stromal tumours.
摘要翻译： 4-（4-甲基哌嗪-1-基甲基）-N- [4-甲基-3-（4-吡啶-3-基）嘧啶-2-基氨基）苯基] - 苯甲酰胺或其药学上可接受的盐可用于治疗胃肠道间质瘤。

5. 发明授权

US08017621B2 Inhibitors of the mutant form of kit 有权
标题翻译：试剂盒突变形式的抑制剂
公开(公告)号：US08017621B2
公开(公告)日：2011-09-13
申请号：US10579586
申请日：2004-11-17
申请人： Elisabeth Buchdunger , Doriano Fabbro
发明人： Elisabeth Buchdunger , Doriano Fabbro
IPC分类号： A61K31/506 , C07D401/14 , C07D213/38
CPC分类号： A61K31/553 , A61K31/502 , A61K31/506 , G01N2800/44
摘要： The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT selected form midostaurin, vatalanib and compound A is administered.
摘要翻译：本发明涉及KIT依赖性疾病的治疗，其特征在于突变体形式的KIT，由此鉴定突变型KIT，并且施用选自Midostaurin，瓦他拉尼和化合物A的突变型KIT的合适的抑制剂。

6. 发明授权

US08124611B2 Inhibitors of the mutant form of kit 有权
标题翻译：试剂盒突变形式的抑制剂
公开(公告)号：US08124611B2
公开(公告)日：2012-02-28
申请号：US12700106
申请日：2010-02-04
申请人： Elisabeth Buchdunger , Doriano Fabbro
发明人： Elisabeth Buchdunger , Doriano Fabbro
IPC分类号： A61K31/506 , C07D401/14 , C07D213/38
CPC分类号： A61K31/553 , A61K31/502 , A61K31/506 , G01N2800/44
摘要： The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT is administered.
摘要翻译：本发明涉及以突变体形式的KIT为特征的KIT依赖性疾病的治疗，由此鉴定突变型KIT并施用适当的突变型KIT抑制剂。

7. 发明申请

US20120157441A1 INHIBITORS OF THE MUTANT FORM OF KIT 审中-公开
标题翻译：工具箱的突变形式的抑制剂
公开(公告)号：US20120157441A1
公开(公告)日：2012-06-21
申请号：US13357972
申请日：2012-01-25
申请人： Elisabeth Buchdunger , Doriano Fabbro
发明人： Elisabeth Buchdunger , Doriano Fabbro
IPC分类号： A61K31/553 , A61P35/02 , A61P35/00 , A61K31/502
CPC分类号： A61K31/553 , A61K31/502 , A61K31/506 , G01N2800/44
摘要： The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT selected form midostaurin, vatalanib and compound A is administered.
摘要翻译：本发明涉及KIT依赖性疾病的治疗，其特征在于突变体形式的KIT，由此鉴定突变型KIT，并且施用选自Midostaurin，瓦他拉尼和化合物A的突变型KIT的合适的抑制剂。

8. 发明申请

US20100179179A1 INHIBITORS OF THE MUTANT FORM OF KIT 有权
标题翻译：工具箱的突变形式的抑制剂
公开(公告)号：US20100179179A1
公开(公告)日：2010-07-15
申请号：US12700106
申请日：2010-02-04
申请人： Elisabeth Buchdunger , Doriano Fabbro
发明人： Elisabeth Buchdunger , Doriano Fabbro
IPC分类号： A61K31/506
CPC分类号： A61K31/553 , A61K31/502 , A61K31/506 , G01N2800/44
摘要： The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT is administered.
摘要翻译：本发明涉及以突变体形式的KIT为特征的KIT依赖性疾病的治疗，由此鉴定突变型KIT并施用适当的突变型KIT抑制剂。

9. 发明申请

US20070213317A1 Inhibitors of the Mutant Form of Kit 有权
标题翻译：试剂盒突变体形式的抑制剂
公开(公告)号：US20070213317A1
公开(公告)日：2007-09-13
申请号：US10579586
申请日：2004-11-17
申请人： Elisabeth Buchdunger , Doriano Fabbro
发明人： Elisabeth Buchdunger , Doriano Fabbro
IPC分类号： A61K31/506 , A61K31/553
CPC分类号： A61K31/553 , A61K31/502 , A61K31/506 , G01N2800/44
摘要： The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT selected form midostaurin, vatalanib and compound A is administered.
摘要翻译：本发明涉及KIT依赖性疾病的治疗，其特征在于突变体形式的KIT，由此鉴定突变型KIT，并且施用选自Midostaurin，瓦他拉尼和化合物A的突变型KIT的合适的抑制剂。

10. 发明申请

US20110124670A1 Use of Pyrimidylaminobenzamide Derivatives for the Treatment of Fibrosis 审中-公开
标题翻译：使用嘧啶基氨基苯甲酰胺衍生物治疗纤维化
公开(公告)号：US20110124670A1
公开(公告)日：2011-05-26
申请号：US13054011
申请日：2009-07-14
申请人： Elisabeth Buchdunger , Paul W. Manley
发明人： Elisabeth Buchdunger , Paul W. Manley
IPC分类号： A61K31/506 , A61P11/00 , A61P1/16
CPC分类号： A61K31/506 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K45/06 , A61K2300/00
摘要： The invention relates to the use of a pyrimidylaminobenzamides of formula I wherein the radicals have the meanings as defined herein, or of a pharmaceutically acceptable salt thereof for the manufacture of pharmaceutical compositions for use in the treatment of fibrosis, to the use of a pyrimidylaminobenzamides of formula I or pharmaceutically acceptable salt thereof in the treatment of fibrosis, to a method of treating warm-blooded animals including humans suffering from fibrosis by administering to a said animal in need of such treatment an effective dose of a pyrimidylaminobenzamide of formula I or a pharmaceutically acceptable salt thereof, and to combinations comprising (a) at least one pyrimidylaminobenzamides of formula I as and (b) at least one compound selected form AT1-receptor antagonists and ACE inhibitors and the use of such combinations in the treatment of fibrosis, in particular hepatic fibrosis.
摘要翻译：本发明涉及式I的嘧啶基氨基苯甲酰胺的用途，其中基团具有如本文所定义的含义或其药学上可接受的盐在制备用于治疗纤维化的药物组合物中的用途，使用嘧啶基氨基苯甲酰胺式I或其药学上可接受的盐在治疗纤维化中的用途，涉及一种通过向需要这种治疗的所述动物施用有效剂量的式I的嘧啶基氨基苯甲酰胺或其药学上可接受的方法来治疗包括患有纤维化的人的温血动物和（a）至少一种式I的嘧啶基氨基苯甲酰胺和（b）至少一种选自AT1受体拮抗剂和ACE抑制剂的化合物，以及这些组合在治疗纤维化中的用途，特别是肝纤维化。

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