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1. 发明申请

WO2012090104A1 METHODS AND COMPOSITIONS FOR DESIGNING NOVEL CONJUGATE THERAPEUTICS 审中-公开
标题翻译：设计新型结合治疗方法和组合物
公开(公告)号：WO2012090104A1
公开(公告)日：2012-07-05
申请号：PCT/IB2011/055598
申请日：2011-12-12
申请人： KAREUS THERAPEUTICS, SA , AKELLA, Venkateswarlu , SAXENA, Uday , REDDY, Anji Reddy
发明人： AKELLA, Venkateswarlu , SAXENA, Uday , REDDY, Anji Reddy
IPC分类号： A61K51/00 , A61K39/00 , A61K39/385
CPC分类号： A61K47/48038 , A61K47/542 , A61K47/55
摘要： The present invention relates to novel drug conjugates, where in two drugs are linked together through an appropriate linker having at least two functional groups capable of forming covalent bond with drugs D1 and D2.The invention also relates to developing novel compositions, methods for their preparation and their use in treating various disease conditions.
摘要翻译：本发明涉及新的药物偶联物，其中两种药物通过具有至少两个能够与药物D1和D2形成共价键的官能团的适当接头连接在一起。本发明还涉及开发新的组合物，其制备方法并用于治疗各种疾病。

2. 发明申请

WO2011089576A2 NOVEL COMPOSITIONS FOR REDUCING Aß 42 PRODUCTION AND THEIR USE IN TREATING ALZHEIMER'S DISEASE (AD) 审中-公开
标题翻译：用于减少A42生产的新组合物及其在治疗阿尔茨海默病（AD）中的应用
公开(公告)号：WO2011089576A2
公开(公告)日：2011-07-28
申请号：PCT/IB2011/050290
申请日：2011-01-22
申请人： KAREUS THERAPEUTTICS SA , AKELLA, Venkateswarulu , SAXENA, Uday , KALLAM, Anji Reddy
发明人： AKELLA, Venkateswarulu , SAXENA, Uday , KALLAM, Anji Reddy
IPC分类号： C07D213/80 , C07D213/82 , C07D401/06 , C07D401/12 , A61K31/4406 , A61P25/28
CPC分类号： C07D213/82 , C07D213/56 , C07D213/80 , C07D401/06 , C07D401/12
摘要： Novel small molecule compounds for reduction of Aß 42 production and for treatment of Alzheimer's Disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
摘要翻译：描述了用于减少Aβ42产生和治疗阿尔茨海默病和其他神经变性疾病的新型小分子化合物，其制备方法和含有它们的药物组合物。

3. 发明申请

WO2008036966A2 METHODS AND COMPOSITIONS FOR THE TREATMENT OF INFLAMMATION, OBESITY AND RELATED METABOLIC DISORDERS 审中-公开
标题翻译：治疗炎症，肥胖和相关代谢障碍的方法和组合物
公开(公告)号：WO2008036966A2
公开(公告)日：2008-03-27
申请号：PCT/US2007/079284
申请日：2007-09-24
申请人： Reddy US Therapeutics, Inc. , PADMALAYAM, Indira , BHUNIYA, Debnath , REDDY, Dumbala Srinivas , KHANNA, Ish, K. , SAXENA, Uday , PILLARISETTI, Sivaram
发明人： PADMALAYAM, Indira , BHUNIYA, Debnath , REDDY, Dumbala Srinivas , KHANNA, Ish, K. , SAXENA, Uday , PILLARISETTI, Sivaram
IPC分类号： A61K31/385
CPC分类号： A61K31/385 , C12Q1/6883 , C12Q2600/136 , C12Q2600/158
摘要： This invention provides a method of reducing inflammation in a living cell of a subject. This method increases the level of lipoic acid synthase within the living cell thereby causing the reduction of the inflammation. Various embodiments and variants are contemplated, some of which are set forth in claim format at the end of this document. The aspects, embodiments, and variants so exemplified in the claims format should not be understood as limiting the invention.
摘要翻译：本发明提供减少受试者活细胞中的炎症的方法。该方法提高了活细胞内硫辛酸合成酶的水平，从而导致炎症的减少。考虑了各种实施例和变型，其中一些在本文件结尾处以权利要求格式阐述。在权利要求书格式中如此举例说明的方面，实施例和变型不应被理解为限制本发明。

4. 发明申请

WO02087556A9 PROBUCOL MONOESTERS AND THEIR USE TO INCREASE PLASMA HDL CHOLESTEROL LEVELS AND IMPROVE HDL FUNCTIONALITY 审中-公开
标题翻译： PROBUCOL单酯类及其用于增加血浆HDL胆固醇水平并改善HDL功能
公开(公告)号：WO02087556A9
公开(公告)日：2003-03-20
申请号：PCT/US0212678
申请日：2002-04-11
申请人： ATHEROGENICS INC , LUCHOOMUN JAYRAZ , SAXENA UDAY , SUNDELL CYNTHIA L , SIKORSKI JAMES A
发明人： LUCHOOMUN JAYRAZ , SAXENA UDAY , SUNDELL CYNTHIA L , SIKORSKI JAMES A
IPC分类号： A61K45/00 , A61K31/05 , A61K31/10 , A61K31/138 , A61K31/198 , A61K31/216 , A61K31/22 , A61K31/225 , A61K31/235 , A61K31/255 , A61K31/275 , A61K31/40 , A61K31/4184 , A61K31/4422 , A61K31/4706 , A61K31/472 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/55 , A61K31/554 , A61K31/575 , A61K45/06 , A61P3/06 , A61P9/10 , C07C323/20 , C07C323/21
CPC分类号： C07C323/20 , A61K31/05 , A61K31/10 , A61K31/225 , A61K31/255 , A61K45/06 , A61K2300/00
摘要： It has been discovered that certain selected probucol monoesters, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.
摘要翻译：已经发现某些选择的普罗布考单酯及其药学上可接受的盐或前体药物可用于增加循环HDL胆固醇。这些化合物还可以通过（a）增加胆固醇酯的清除率，（b）增加HDL-粒子对肝细胞表面受体的亲和力或（c）增加apoAI-HDL的半衰期来改善HDL功能。

5. 发明申请

WO2002087556A2 METHODS TO INCREASE PLASMA HDL CHOLESTEROL LEVELS AND IMPROVE HDL FUNCTIONALITY WITH PROBUCOL MONOESTERS 审中-公开
标题翻译：增加血浆HDL胆固醇水平和提高高密度脂蛋白功能的方法与PROBUCOL MONOESTERS
公开(公告)号：WO2002087556A2
公开(公告)日：2002-11-07
申请号：PCT/US2002/012678
申请日：2002-04-11
申请人： ATHEROGENICS, INC. , LUCHOOMUN, JayRaz , SAXENA, Uday , SUNDELL, Cynthia, L. , SIKORSKI, James, A.
发明人： LUCHOOMUN, JayRaz , SAXENA, Uday , SUNDELL, Cynthia, L. , SIKORSKI, James, A.
IPC分类号： A61K31/00
CPC分类号： C07C323/20 , A61K31/05 , A61K31/10 , A61K31/225 , A61K31/255 , A61K45/06 , A61K2300/00
摘要： It has been discovered that certain selected probucol monoesters, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.
摘要翻译：已经发现，某些选择的普罗布考单酯及其药学上可接受的盐或前药可用于增加循环HDL胆固醇。这些化合物还可以通过（a）增加胆固醇酯的清除率，（b）增加对肝细胞表面受体的HDL-粒子亲和力或（c）增加apoAI-HDL的半衰期来改善HDL功能。

6. 发明申请

WO0177072A3 COMPOUNDS AND METHODS TO INCREASE PLASMA HDL CHOLESTEROL LEVELS AND IMPROVE HDL FUNCTIONALITY 审中-公开
标题翻译：提高血浆HDL胆固醇水平并提高HDL功能的化合物和方法
公开(公告)号：WO0177072A3
公开(公告)日：2002-07-18
申请号：PCT/US0111899
申请日：2001-04-11
申请人： ATHEROGENICS INC , LUCHOOMUN JAYRAZ , MENG CHARLES Q , SAXENA UDAY , SIKORSKI JAMES
发明人： LUCHOOMUN JAYRAZ , MENG CHARLES Q , SAXENA UDAY , SIKORSKI JAMES
IPC分类号： A61K31/7034 , A61K31/10 , A61K31/192 , A61K31/198 , A61K31/255 , A61P3/06 , C07C323/20 , G01N33/92
CPC分类号： G01N33/92 , C07C323/20 , G01N2500/00 , G01N2500/10 , G01N2800/044
摘要： It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.
摘要翻译：已经发现，普罗布考的某些选择的醚及其药学上可接受的盐或前药可用于增加循环HDL胆固醇。这些化合物还可以通过（a）增加胆固醇酯的清除率，（b）增加对肝细胞表面受体的HDL-粒子亲和力或（c）增加apoAI-HDL的半衰期来改善HDL功能。

7. 发明申请

WO2008036835A2 METHODS AND COMPOSITIONS FOR UPREGULATION OF PEROXIREDOXIN ACTIVITY 审中-公开
标题翻译：过氧化物酶活性升高的方法和组合物
公开(公告)号：WO2008036835A2
公开(公告)日：2008-03-27
申请号：PCT/US2007079068
申请日：2007-09-20
申请人： REDDY US THERAPEUTICS , KHANNA ISH , PILLARISETTI RAM , SAXENA UDAY
发明人： KHANNA ISH , PILLARISETTI RAM , SAXENA UDAY
IPC分类号： A61K31/47
CPC分类号： C12Q1/28 , G01N33/92 , G01N2500/10 , G01N2800/044
摘要： A novel method of identifying compounds capable of upregulating Peroxiredoxin activity is disclosed. The method includes providing a sample of cells that express Peroxiredoxin, providing a sample of a candidate compound, contacting the cell sample and the compound sample, and measuring a quantitative indicator of Peroxiredoxin activity within the cell sample after the contacting step. Peroxiredoxin inducers identified by the method and uses therefore to upregulate Peroxiredoxin activity in subjects and to reduce LDL and/or VLDL levels and to prevent or treat atherosclerosis and inflammatory disorders such as arthritis in subjects are also described. The invention also provides a method of treatment of inflammatory and cardiovascular diseases which comprises providing a patient in need of treatment with an effective amount of a composition that increases Peroxiredoxin protein or activity.
摘要翻译：公开了鉴定能够上调过氧化还原毒素活性的化合物的新方法。该方法包括提供表达过氧化还原毒素的细胞样品，提供候选化合物样品，接触细胞样品和化合物样品，以及在接触步骤后测量细胞样品内过氧化还原毒素活性的定量指标。本文还描述了通过该方法和用途鉴定的过氧化还原毒素诱导剂，以上调受试者中的过氧化还原毒素活性并降低LDL和/或VLDL水平，并预防或治疗动脉粥样硬化和炎症性疾病如受试者中的关节炎。本发明还提供了一种治疗炎性和心血管疾病的方法，其包括提供需要治疗的患者，所述治疗有效量的增加过氧化还原蛋白或活性的组合物。

8. 发明申请

WO03065008A3 METHODS AND COMPOSITIONS FOR IDENTIFICATION AND THERAPEUTIC USE OF GENES INVOLVED IN VASCULAR AND PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于鉴定和治疗参与血管和增殖性疾病的基因的方法和组合物
公开(公告)号：WO03065008A3
公开(公告)日：2005-03-10
申请号：PCT/US0302940
申请日：2003-01-31
申请人： REDDY US THERAPEUTICS INC , PILLARISETTI SIVRAM , SAXENA UDAY
发明人： PILLARISETTI SIVRAM , SAXENA UDAY
IPC分类号： C07H21/04 , C12Q1/00 , C12Q1/68 , G01N20060101 , G01N33/48 , G01N33/50 , G06F19/00
CPC分类号： C12Q1/6883 , C12Q2600/158
摘要： The present invention comprises compositions and methods for identification of genes involved in vascular diseases using human endothelial and smooth cell "artery wall" models to capture the cell-cell and cell-matrix communications that are operative in normal and diseases conditions. The present invention further comprises the capture of the complexity of multiple chronic pathologies that coexist in humans by simultaneous treatment of the cells with disease specific stimuli and the identification and use of genes that are regulated by such multiple established disease mediators. The present invention additionally comprises compositions and methods of treatment of vascular disease.
摘要翻译：本发明包括使用人内皮和光滑细胞“动脉壁”模型鉴定参与血管疾病的基因的组合物和方法，以捕获在正常和疾病状况下操作的细胞 - 细胞和细胞 - 基质通讯。本发明还包括通过用疾病特异性刺激同时治疗细胞以及鉴定和使用由这种多种既定疾病介质调节的基因来捕获人类共存的多种慢性病理学的复杂性。本发明另外包括治疗血管疾病的组合物和方法。

9. 发明申请

WO0223197A3 METHODS AND COMPOSITIONS FOR GLYCOSIDASE ASSAYS 审中-公开
标题翻译：用于糖苷酶测定的方法和组合物
公开(公告)号：WO0223197A3
公开(公告)日：2003-07-24
申请号：PCT/US0128862
申请日：2001-09-14
申请人： REDDY US THERAPEUTICS INC , PILLARISETTI SIVARAM , SAXENA UDAY , WANG DONGYAN
发明人： PILLARISETTI SIVARAM , SAXENA UDAY
IPC分类号： C12Q1/527 , G01N33/573 , G01N33/574 , C12Q1/34
CPC分类号： G01N33/573 , G01N33/574 , G01N33/57484 , G01N2333/924
摘要： The present invention is directed to compositions and methods for measuring enzymatic activity, particularly glycosidase activity. Methods of the present invention include assays for quantitatively determining the amount of glycosidase activity in a sample. The present invention also provides methods for the diagnosis of metastatic and inflammatory processes in vitro and in vivo. The present invention further provides compositions and methods for high throughput assays for identifying compounds that effect glycosidase activity.
摘要翻译：本发明涉及用于测量酶活性，特别是糖苷酶活性的组合物和方法。本发明的方法包括用于定量测定样品中糖苷酶活性的量的测定法。本发明还提供用于诊断体外和体内转移和炎症过程的方法。本发明还提供用于鉴定影响糖苷酶活性的化合物的高通量测定的组合物和方法。

10. 发明申请

WO2002087556A3 PROBUCOL MONOESTERS AND THEIR USE TO INCREASE PLASMA HDL CHOLESTEROL LEVELS AND IMPROVE HDL FUNCTIONALITY 审中-公开
公开(公告)号：WO2002087556A3
公开(公告)日：2002-11-07
申请号：PCT/US2002/012678
申请日：2002-04-11
申请人： ATHEROGENICS, INC. , LUCHOOMUN, JayRaz , SAXENA, Uday , SUNDELL, Cynthia, L. , SIKORSKI, James, A.
发明人： LUCHOOMUN, JayRaz , SAXENA, Uday , SUNDELL, Cynthia, L. , SIKORSKI, James, A.
IPC分类号： A61K31/225
摘要： It has been discovered that certain selected probucol monoesters, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.

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