公开(公告)号：US06686390B2

公开(公告)日：2004-02-03

申请号：US09861903

申请日：2001-05-21

申请人： Manojit Pal ,  Koteswar Rao Yeleswarapu ,  Rajagopalan Ramanujam ,  Parimal Misra ,  Prem Kumar Mamnoor ,  Seshagiri Rao Casturi

发明人： Manojit Pal ,  Koteswar Rao Yeleswarapu ,  Rajagopalan Ramanujam ,  Parimal Misra ,  Prem Kumar Mamnoor ,  Seshagiri Rao Casturi

IPC分类号： A61K3134

CPC分类号： C07D207/444 ,  C07D207/38 ,  C07D307/58 ,  C07D307/60 ,  C07D409/04 ,  C07D417/10

摘要： The present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their regioisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

摘要翻译： 本发明涉及通式（I）的新型杂环化合物，其衍生物，其类似物，其互变异构形式，其立体异构体，其区域异构体，其多晶型物，其药学上可接受的盐，其药学上可接受的溶剂合物和含有它们的药学上可接受的组合物 。

公开(公告)号：US07335656B2

公开(公告)日：2008-02-26

申请号：US11512863

申请日：2006-08-30

申请人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Sesha Sridevi Alluri ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

发明人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Sesha Sridevi Alluri ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

IPC分类号： A61M31/00 ,  A61F2/86 ,  C07D251/70 ,  C07D251/52 ,  C07D251/30 ,  A61P35/00

CPC分类号： A61K31/53 ,  C07D251/30 ,  C07D251/44 ,  C07D251/46 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/66 ,  C07D251/70 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D453/02 ,  C07D487/04 ,  C07F9/6521 ,  C07F9/65583

摘要： The present invention relates to methods, compounds, and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses, and is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention also relates to compounds that inhibit smooth muscle proliferation, for example, by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis. This invention also relates to medical devices, such as a stent, comprising a compound or composition of this invention disposed on or within the medical device.

摘要翻译： 本发明涉及包含治疗由炎性反应引起的病理生理状况的化合物的方法，化合物和组合物，并且涉及抑制或阻断糖基化蛋白质产生内皮细胞中信号传导相关炎症反应诱导的化合物。 本发明还涉及抑制平滑肌增殖的化合物，例如通过调节HSPG如Perlecan。 本发明还涉及化合物用于治疗以平滑肌增生为特征的血管闭塞症状，例如再狭窄和动脉粥样硬化。 本发明还涉及包括设置在医疗装置上或内部的本发明的化合物或组合物的医疗装置，例如支架。

公开(公告)号：US07112587B2

公开(公告)日：2006-09-26

申请号：US10400134

申请日：2003-03-26

申请人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Bhatlapenumarthy Sesha Sridevi ,  Potlapally Rajendar Kumar ,  Gaddam Om Reddy

发明人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Bhatlapenumarthy Sesha Sridevi ,  Potlapally Rajendar Kumar ,  Gaddam Om Reddy

IPC分类号： C07D251/30 ,  C07D251/46 ,  C07D251/48 ,  A61K31/53 ,  A61P35/00

CPC分类号： A61K31/53 ,  C04B35/632 ,  C07D251/30 ,  C07D251/44 ,  C07D251/46 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/66 ,  C07D251/70 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D453/02 ,  C07D487/04 ,  C07F9/6521 ,  C07F9/65583

摘要： The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.

公开(公告)号：US07820654B2

公开(公告)日：2010-10-26

申请号：US11234695

申请日：2005-09-23

申请人： Manojit Pal ,  Srinivas Kalleda ,  Srinivas Padakanti ,  Nalivela Kumara Swamy ,  Koteswar Rao Yeleswarapu ,  Christopher W. Alexander ,  Ish Khanna ,  Javed Iqbal ,  Sivaram Pillarisetti ,  Deepak Barange

发明人： Manojit Pal ,  Srinivas Kalleda ,  Srinivas Padakanti ,  Nalivela Kumara Swamy ,  Koteswar Rao Yeleswarapu ,  Christopher W. Alexander ,  Ish Khanna ,  Javed Iqbal ,  Sivaram Pillarisetti ,  Deepak Barange

IPC分类号： A61K31/54 ,  A61K31/535 ,  A61K31/497 ,  A61K31/505 ,  C07D417/00 ,  C07D413/00 ,  C07D403/00 ,  C07D239/02

CPC分类号： C07D405/14 ,  C07D239/30 ,  C07D239/40 ,  C07D239/42 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D239/54 ,  C07D401/04 ,  C07D403/12 ,  C07D405/12

摘要： The present invention is directed to a compounds, methods and compositions for making the compounds and methods of treating a variety of diseases and disease states including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease states mediated by the low expression of Perlecan, comprising the administration of new heterocyclic compounds, particularly substituted pyrimidines. The present invention is directed to novel compounds represented by the general formula:

摘要翻译： 本发明涉及用于制备化合物的化合物，方法和组合物以及治疗各种疾病和疾病状态的方法，包括动脉粥样硬化，关节炎，再狭窄，糖尿病性肾病或血脂异常或由Perlecan低表达介导的疾病 包括施用新的杂环化合物，特别是取代的嘧啶。 本发明涉及由以下通式表示的新化合物：

公开(公告)号：US07268134B2

公开(公告)日：2007-09-11

申请号：US10951305

申请日：2004-09-27

申请人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Sesha Sridevi Alluri ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

发明人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Sesha Sridevi Alluri ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

IPC分类号： A61M31/00 ,  A61F2/86 ,  C07D251/70 ,  C07D251/52 ,  C07D251/30 ,  A61K31/53 ,  A61P35/00

CPC分类号： A61K31/53 ,  C04B35/632 ,  C07D251/30 ,  C07D251/44 ,  C07D251/46 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/66 ,  C07D251/70 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D453/02 ,  C07D487/04 ,  C07F9/6521 ,  C07F9/65583

摘要： The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.

公开(公告)号：US07163943B2

公开(公告)日：2007-01-16

申请号：US10397968

申请日：2003-03-26

申请人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Bhatlapenumarthy Sesha Sridevi ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

发明人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Bhatlapenumarthy Sesha Sridevi ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

IPC分类号： C07D251/30 ,  C07D251/46 ,  C07D251/52 ,  C07D251/54 ,  A61K31/53

CPC分类号： A61K31/53 ,  C04B35/632 ,  C07D251/30 ,  C07D251/44 ,  C07D251/46 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/66 ,  C07D251/70 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D453/02 ,  C07D487/04 ,  C07F9/6521 ,  C07F9/65583

摘要： The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.

摘要翻译： 本发明涉及包含治疗由炎性反应引起的病理生理状况的化合物的方法和组合物。 特别地，本发明涉及抑制或阻断糖基化蛋白质产生内皮细胞中信号传导相关炎症反应诱导的化合物。 本发明涉及抑制平滑肌增殖的化合物。 特别地，本发明涉及通过调节HSPG例如Perlecan抑制平滑肌细胞增殖的化合物。 本发明还涉及化合物用于治疗以平滑肌增生为特征的血管闭塞症状，例如再狭窄和动脉粥样硬化。

公开(公告)号：US07332490B2

公开(公告)日：2008-02-19

申请号：US11441326

申请日：2006-05-25

申请人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Sesha Sridevi Alluri ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

发明人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Sesha Sridevi Alluri ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

IPC分类号： C07D251/70 ,  C07D251/52 ,  C07D401/12 ,  C07D403/12 ,  A61K31/53 ,  A61P35/00

CPC分类号： A61K31/53 ,  C07D251/30 ,  C07D251/44 ,  C07D251/46 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/66 ,  C07D251/70 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D453/02 ,  C07D487/04 ,  C07F9/6521 ,  C07F9/65583

摘要： The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.

摘要翻译： 本发明涉及包含治疗由炎性反应引起的病理生理状况的化合物的方法和组合物。 特别地，本发明涉及抑制或阻断糖基化蛋白质产生内皮细胞中信号传导相关炎症反应诱导的化合物。 本发明涉及抑制平滑肌增殖的化合物。 特别地，本发明涉及通过调节HSPG例如Perlecan抑制平滑肌细胞增殖的化合物。 本发明还涉及化合物用于治疗以平滑肌增生为特征的血管闭塞症状，例如再狭窄和动脉粥样硬化。

公开(公告)号：US07332489B2

公开(公告)日：2008-02-19

申请号：US10528724

申请日：2003-03-26

申请人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Sesha Sridevi Alluri ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

发明人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krishna Reddy ,  Sesha Sridevi Alluri ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

IPC分类号： C07D251/70 ,  C07D403/12 ,  C07D401/12 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D413/04 ,  A61K31/53 ,  C07D251/30 ,  C07D251/44 ,  C07D251/46 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/66 ,  C07D251/70 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D453/02 ,  C07D487/04 ,  C07F9/6521 ,  C07F9/65583

摘要： The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.

公开(公告)号：US07238692B2

公开(公告)日：2007-07-03

申请号：US10951120

申请日：2004-09-27

申请人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krisha Reddy ,  Sesha Sridevi Alluri ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

发明人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Koteswar Rao Yeleswarapu ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Velagala Venkata Rama Murali Krisha Reddy ,  Sesha Sridevi Alluri ,  Potlapally Rajender Kumar ,  Gaddam Om Reddy

IPC分类号： A61M31/00 ,  A61F2/86 ,  C07D251/70 ,  C07D251/52 ,  C07D251/30

CPC分类号： A61K31/53 ,  C04B35/632 ,  C07D251/30 ,  C07D251/44 ,  C07D251/46 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/54 ,  C07D251/66 ,  C07D251/70 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07F9/6521 ,  C07F9/65583

摘要： The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.

摘要翻译： 本发明涉及包含治疗由炎性反应引起的病理生理状况的化合物的方法和组合物。 特别地，本发明涉及抑制或阻断糖基化蛋白质产生内皮细胞中信号传导相关炎症反应诱导的化合物。 本发明涉及抑制平滑肌增殖的化合物。 特别地，本发明涉及通过调节HSPG例如Perlecan抑制平滑肌细胞增殖的化合物。 本发明还涉及化合物用于治疗以平滑肌增生为特征的血管闭塞症状，例如再狭窄和动脉粥样硬化。

公开(公告)号：US07335770B2

公开(公告)日：2008-02-26

申请号：US10808210

申请日：2004-03-24

申请人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Sesha Sridevi Alluri ,  Velagala Venkata Rama Murali Krishna Reddy ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Koteswar Rao Yeleswarapu ,  Gaddam Om Reddy ,  Potlapally Rajender Kumar

发明人： Richard T. Timmer ,  Christopher W. Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Sesha Sridevi Alluri ,  Velagala Venkata Rama Murali Krishna Reddy ,  Manojit Pal ,  Jangalgar Tirupathy Reddy ,  Koteswar Rao Yeleswarapu ,  Gaddam Om Reddy ,  Potlapally Rajender Kumar

IPC分类号： C07D251/54 ,  C07D251/48 ,  C07D251/18 ,  C07D251/42 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D251/46

摘要： The present invention relates to triazine compounds and their analogs and derivatives, and methods and compositions comprising these compounds. The compounds and compositions of this invention are useful for, among other things, treating pathophysiological conditions arising from inflammatory responses, inhibiting or blocking glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells, inhibiting smooth muscle proliferation, treating vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis, and the like.

摘要翻译： 本发明涉及三嗪化合物及其类似物和衍生物，以及包含这些化合物的方法和组合物。 本发明的化合物和组合物尤其可用于治疗由炎症反应引起的病理生理学病症，抑制或阻断糖基化蛋白产生内皮细胞中信号传导相关炎症反应的诱导，抑制平滑肌增生，治疗血管闭塞症状 其特征在于平滑肌增生如再狭窄和动脉粥样硬化等。