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1. 发明授权

US09611259B2 Substituted pyridine derivatives useful as C-FMS kinase inhibitors 有权
公开(公告)号：US09611259B2
公开(公告)日：2017-04-04
申请号：US14772040
申请日：2014-03-13
申请人： Janssen Pharmaceutica NV , Jie Chen , Matthew Donahue , Heng-Keang Lim , Ronghui Lin , Rhys Salter , Jiejun Wu
发明人： Jie Chen , Matthew Donahue , Heng-Keang Lim , Ronghui Lin , Rhys Salter , Jiejun Wu , Yong Gong
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： The present invention is directed to substituted pyridine derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives in the treatment of disorders mediated by c-fms kinase. The present invention is further directed to a process for the preparation of said substituted pyridine derivatives.

2. 发明申请

US20160016942A1 SUBSTITUTED PYRIDINE DERIVATIVES USEFUL AS C-FMS KINASE INHIBITORS 有权
标题翻译：用作C-FMS激酶抑制剂的替代吡啶衍生物
公开(公告)号：US20160016942A1
公开(公告)日：2016-01-21
申请号：US14772040
申请日：2014-03-13
申请人： Jie CHEN , Matthew DONAHUE , Heng-Keang LIM , Ronghui LIN , Rhys SALTER , Jiejun WU , JANSSEN PHARMACEUTICA NV
发明人： Jie CHEN , Matthew DONAHUE , Heng-Keeng LIM , Ronghui LIN , Rhys SALTER , Jiejun WU
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： The present invention is directed to substituted pyridine derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives in the treatment of disorders mediated by c-fms kinase. The present invention is further directed to a process for the preparation of said substituted pyridine derivatives.
摘要翻译：本发明涉及取代的吡啶衍生物，含有所述衍生物的药物组合物和所述衍生物在治疗由c-fms激酶介导的病症中的用途。本发明进一步涉及制备所述取代的吡啶衍生物的方法。

3. 发明申请

US20120316338A1 Methods and Intermediates for the Preparation of Optionally Radio-Labeled Imatinib 审中-公开
标题翻译：用于制备可选择的无线电标记的伊马替尼的方法和中间体
公开(公告)号：US20120316338A1
公开(公告)日：2012-12-13
申请号：US13526115
申请日：2012-06-18
申请人： Rhys Salter , Maria Ines Rodriguez Perez , Thomas Moenius , Rolf Voges , Hendrik Andres , Kirk Bordeaux
发明人： Rhys Salter , Maria Ines Rodriguez Perez , Thomas Moenius , Rolf Voges , Hendrik Andres , Kirk Bordeaux
IPC分类号： C07D401/14
CPC分类号： C07D295/155 , C07D401/04
摘要： The invention relates to new processes for the manufacture of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine (compound of formula I, new processes for the manufacture of metabolites of N-{5[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine observed after administration of the compound to warm-blooded animals as well as to intermediates used in said processes. New starting materials as well as processes for the preparation thereof are likewise the subject of this invention. The processes described herein are especially suitable to furnish said compounds having isotopic labeling. The such obtained labeled compounds are in particular suitable to track and to investigate into the metabolism of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and its pharmaceutically acceptable salts in clinical and pre-clinical studies.
摘要翻译：本发明涉及制备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（式I化合物，用于制备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-2-甲酸的代谢物的新方法，在将化合物给予温血动物以及在所述方法中使用的中间体后观察到胺，新的原料及其制备方法同样是本发明的主题，本文所述的方法特别适用于所述具有同位素标记的化合物特别适用于追踪和研究N- {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -2- 4-（3-吡啶基）-2-嘧啶胺及其药学上可接受的盐在临床和临床前研究中。

4. 发明授权

US07655686B2 Certain substituted spirocyclic lactams and use thereof as pharmaceuticals 失效
标题翻译：某些取代的螺环内酰胺及其作为药物的用途
公开(公告)号：US07655686B2
公开(公告)日：2010-02-02
申请号：US11823311
申请日：2007-06-26
申请人： Yves Auberson , Ralf Glatthar , Rhys Salter , Oliver Simic , Marina Tintelnot-Blomley
发明人： Yves Auberson , Ralf Glatthar , Rhys Salter , Oliver Simic , Marina Tintelnot-Blomley
IPC分类号： A61K31/407 , C07D487/10
CPC分类号： C07D487/10
摘要： The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4.4]non-7-yl)-propionamides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及下式的新的2-（6-氧代-1,7-二氮杂 - 螺[4.4]壬-7-基） - 丙酰胺其中R1，R2，R3，R4，R5，R6，m和p 在本说明书中对其制备，其用作药物和含有它们的药物组合物的用途。

5. 发明申请

US20070265328A1 Certain substituted spirocyclic lactams and use thereof as pharmaceuticals 失效
标题翻译：某些取代的螺环内酰胺及其作为药物的用途
公开(公告)号：US20070265328A1
公开(公告)日：2007-11-15
申请号：US11823311
申请日：2007-06-26
申请人： Yves Auberson , Ralf Glatthar , Rhys Salter , Oliver Simic , Marina Tintelnot-Blomley
发明人： Yves Auberson , Ralf Glatthar , Rhys Salter , Oliver Simic , Marina Tintelnot-Blomley
IPC分类号： A61K31/40 , A61P25/00 , A61P9/00 , C07D491/00
CPC分类号： C07D487/10
摘要： The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4.4]non-7-yl)-propionamides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及下式的新的2-（6-氧代-1,7-二氮杂 - 螺[4.4]壬-7-基） - 丙酰胺其中R 1，R 2 R 3，R 3，R 4，R 5，R 6，m和p分别为在本说明书中定义，它们的制备，用作药物和含有它们的药物组合物。

6. 发明申请

US20090299064A1 METHODS AND INTERMEDIATES FOR THE PREPARATION OF OPTIONALLY RADIO-LABELED IMATINIB 审中-公开
标题翻译：用于准备无线电标签图像的方法和中间件
公开(公告)号：US20090299064A1
公开(公告)日：2009-12-03
申请号：US11917353
申请日：2006-06-13
申请人： Rhys Salter , Maria Ines Rodriguez Perez , Thomas Moenius , Rolf Voges , Hendrik Andres , Kirk Bordeaux
发明人： Rhys Salter , Maria Ines Rodriguez Perez , Thomas Moenius , Rolf Voges , Hendrik Andres , Kirk Bordeaux
IPC分类号： C07D401/14 , C07D401/04 , C07D241/04
CPC分类号： C07D295/155 , C07D401/04
摘要： The invention relates to new processes for the manufacture of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}4-(3-pyridyl)-2-pyrimidine-amine (compound of formula I, new processes for the manufacture of metabolites of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine observed after administration of the compound to warm-blooded animals as well as to intermediates used in said processes. New starting materials as well as processes for the preparation thereof are likewise the subject of this invention. The processes described herein are especially suitable to furnish said compounds having isotopic labeling. The such obtained labeled compounds are in particular suitable to track and to investigate into the metabolism of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}4-(3-pyridyl)-2-pyrimidine-amine and its pharmaceutically acceptable salts in clinical and pre-clinical studies.
摘要翻译：本发明涉及制备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（化合物的式I的制备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-4-甲酸的代谢物的新方法，在将化合物给予温血动物以及在所述方法中使用的中间体后观察到胺，新的原料及其制备方法同样是本发明的主题，本文所述的方法特别适用于所述具有同位素标记的化合物特别适用于追踪和研究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-嘧啶胺及其药学上可接受的盐在临床和临床前研究中。

7. 发明申请

US20070015781A1 Certain substituted spirocyclic lactams and use thereof as pharmaceuticals 审中-公开
公开(公告)号：US20070015781A1
公开(公告)日：2007-01-18
申请号：US10574536
申请日：2004-10-04
申请人： Yves Auberson , Ralf Glatthar , Rhys Salter , Oliver Simic , Marina Tintelnot-Blomley
发明人： Yves Auberson , Ralf Glatthar , Rhys Salter , Oliver Simic , Marina Tintelnot-Blomley
IPC分类号： A61K31/4747 , A61K31/407 , C07D471/10
CPC分类号： C07D487/10
摘要： The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4.4]non-7-yl)-propionamides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.

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