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1. 发明申请

US20100311945A1 HDM2-Inhibitor Complexes and Uses Thereof 有权
标题翻译： HDM2抑制剂复合物及其用途
公开(公告)号：US20100311945A1
公开(公告)日：2010-12-09
申请号：US12766139
申请日：2010-04-23
申请人： Carsten Schubert , Bruce Grasberger , Diane Maguire , Ingrid Deckman , John Spurlino
发明人： Carsten Schubert , Bruce Grasberger , Diane Maguire , Ingrid Deckman , John Spurlino
IPC分类号： C07K17/02
CPC分类号： C07K14/82 , C07K2299/00 , G01N33/6803 , G01N2500/04
摘要： The present invention includes crystallized HDM2 peptides as well as descriptions of the X-ray diffraction patterns of the crystals. The diffraction patterns allow the three dimensional structure of HDM2 to be determined at atomic resolution so that ligand binding sites on HDM2 can be identified and the interactions of ligands with HDM2 amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MDM2 and HDM2 oncoproteins.
摘要翻译：本发明包括结晶的HDM2肽以及晶体的X射线衍射图的描述。衍射图允许以原子分辨率确定HDM2的三维结构，从而可以鉴定HDM2上的配体结合位点，并且可以对配体与HDM2氨基酸残基的相互作用进行建模。使用这种图谱制备的模型允许设计可用作活性剂的配体，其包括但不限于用作MDM2和HDM2癌蛋白抑制剂的那些。

2. 发明申请

US20090088554A1 HDM2-INHIBITOR COMPLEXES AND USES THEREOF 审中-公开
标题翻译： HDM2-抑制剂复合物及其用途
公开(公告)号：US20090088554A1
公开(公告)日：2009-04-02
申请号：US11756149
申请日：2007-05-31
申请人： Carsten Schubert , Bruce Grasberger , Diane Maguire , Ingrid Deckman , John Spurlino
发明人： Carsten Schubert , Bruce Grasberger , Diane Maguire , Ingrid Deckman , John Spurlino
IPC分类号： C07K14/82 , C07K1/00
CPC分类号： C07K14/82 , C07K2299/00 , G01N33/6803 , G01N2500/04
摘要： The present invention includes crystallized HDM2 peptides as well as descriptions of the X-ray diffraction patterns of the crystals. The diffraction patterns allow the three dimensional structure of HDM2 to be determined at atomic resolution so that ligand binding sites on HDM2 can be identified and the interactions of ligands with HDM2 amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MDM2 and HDM2 oncoproteins.
摘要翻译：本发明包括结晶的HDM2肽以及晶体的X射线衍射图的描述。衍射图允许以原子分辨率确定HDM2的三维结构，从而可以鉴定HDM2上的配体结合位点，并且可以对配体与HDM2氨基酸残基的相互作用进行建模。使用这种图谱制备的模型允许设计可用作活性剂的配体，其包括但不限于用作MDM2和HDM2癌蛋白抑制剂的那些。

3. 发明授权

US06586453B2 Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1 有权
标题翻译：取代的噻唑及其作为纤溶酶原激活物抑制剂-1的抑制剂的用途
公开(公告)号：US06586453B2
公开(公告)日：2003-07-01
申请号：US09822351
申请日：2001-04-02
申请人： Dale S. Dhanoa , Declan E. Ryan , Ingrid Deckman , Anthony Sapienza
发明人： Dale S. Dhanoa , Declan E. Ryan , Ingrid Deckman , Anthony Sapienza
IPC分类号： A61K31425
CPC分类号： C07D417/04 , C07D277/38 , C07D277/42
摘要： The present invention relates to the use of aminothiazole derivatives of Formula I of as inhibitors of PAI-1, and to novel classes of aminothiazole derivatives, their synthesis and their use as inhibitors of PAI-1. It has been discovered that compounds of Formula I: or a solvate, hydrate or a pharmaceutically acceptable salt thereof, wherein Y, Ar1, Ar2, R1, R2, Z, m and n are described in the specification, inhibit plasminogen activator inhibitor-1 (PAI-1). These compounds can be used in the prophylaxis or for the treatment of thrombosis, angina pectoris, cerebral infarction, myocardial infarction, pulmonary infarction, intra-atrial thrombus in atrial fibrillation, deep venous thrombus, disseminated intravascular coagulation syndrome, diabetic complications, restenosis and stroke.
摘要翻译：本发明涉及式I的氨基噻唑衍生物作为PAI-1的抑制剂的用途，以及新类型的氨基噻唑衍生物，其合成及其作为PAI-1抑制剂的用途。已经发现，说明书中描述了式I的化合物或其溶剂化物，水合物或其药学上可接受的盐，其中Y，Ar1，Ar2，R1，R2，Z，m和n在本说明书中描述了抑制纤溶酶原激活物抑制剂-1 PAI-1）。这些化合物可用于预防或治疗血栓形成，心绞痛，脑梗塞，心肌梗死，肺梗死，心房颤动中的心房内血栓，深静脉血栓，弥散性血管内凝血综合征，糖尿病并发症，再狭窄和中风。

4. 发明授权

US08058390B2 HDM2-inhibitor complexes and uses thereof 有权
标题翻译： HDM2抑制剂复合物及其用途
公开(公告)号：US08058390B2
公开(公告)日：2011-11-15
申请号：US12766139
申请日：2010-04-23
申请人： Carsten Schubert , Bruce Grasberger , Diane Maguire , Ingrid Deckman , John Spurlino
发明人： Carsten Schubert , Bruce Grasberger , Diane Maguire , Ingrid Deckman , John Spurlino
IPC分类号： C07K14/00
CPC分类号： C07K14/82 , C07K2299/00 , G01N33/6803 , G01N2500/04
摘要： The present invention includes crystallized HDM2 peptides as well as descriptions of the X-ray diffraction patterns of the crystals. The diffraction patterns allow the three dimensional structure of HDM2 to be determined at atomic resolution so that ligand binding sites on HDM2 can be identified and the interactions of ligands with HDM2 amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MDM2 and HDM2 oncoproteins.
摘要翻译：本发明包括结晶的HDM2肽以及晶体的X射线衍射图的描述。衍射图允许以原子分辨率确定HDM2的三维结构，从而可以鉴定HDM2上的配体结合位点，并且可以对配体与HDM2氨基酸残基的相互作用进行建模。使用这种图谱制备的模型允许设计可用作活性剂的配体，其包括但不限于用作MDM2和HDM2癌蛋白抑制剂的那些。

5. 发明申请

US20060094081A1 Crystal structure of the c-fms kinase domain: applications and use of heterologous substitutions of kinase insert domains for crystallization 审中-公开
标题翻译： c-fms激酶结构域的晶体结构：应用和使用激酶插入结构域的异源取代进行结晶
公开(公告)号：US20060094081A1
公开(公告)日：2006-05-04
申请号：US11255147
申请日：2005-10-20
申请人： Carsten Schubert , Barry Springer , Ingrid Deckman , Raymond Patch , Geoffrey Struble , Hongchang Ma , Celine Schalk-Hihi , Benjamin Brandt , Ioanna Petrounia
发明人： Carsten Schubert , Barry Springer , Ingrid Deckman , Raymond Patch , Geoffrey Struble , Hongchang Ma , Celine Schalk-Hihi , Benjamin Brandt , Ioanna Petrounia
IPC分类号： G06F19/00 , C07H21/04 , C12P21/06 , C12N9/12
CPC分类号： C07K14/7153 , C07K2299/00 , C07K2319/00 , C30B7/00 , G16B15/00 , G16B20/00 , G16B50/00
摘要： The present invention includes a crystal structure of the kinase domain of c-fms and a methodology to produce diffraction quality crystals of the c-fms kinase domain by heterologous substitution of the kinase insert domain. Also included in the invention is the structure of the c-fms kinase domain in liganded form for use in the discovery of inhibitors of c-fms for the treatment of diseases caused by inappropriate activity of c-fms. The present invention includes descriptions of the X-ray diffraction patterns of the crystals. The diffraction patterns allow the three dimensional structure of c-fms to be determined at atomic resolution so that ligand binding sites on can be identified and the interactions of ligands with amino acid residues can be modeled.
摘要翻译：本发明包括c-fms的激酶结构域的晶体结构和通过激酶插入结构域的异源取代产生c-fms激酶结构域的衍射质量晶体的方法。本发明还包括配体形式的c-fms激酶结构域用于发现c-fms抑制剂用于治疗由c-fms的不适当活性引起的疾病的结构。本发明包括晶体的X射线衍射图案的描述。衍射图允许以原子分辨率确定c-fms的三维结构，从而可以鉴定配体结合位点，并且可以建模与配体与氨基酸残基的相互作用。

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