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1. 发明授权

US6121300A Reversing advanced glycosylation cross-links using heterocyclic-substituted thiazolium salts 失效
公开(公告)号：US6121300A
公开(公告)日：2000-09-19
申请号：US189200
申请日：1998-11-10
申请人： Dilip R. Wagle , Sheng-Ding Fang , Taikyun Rho , John J. Egan , Sara Vasan , Peter Ulrich , Anthony Cerami
发明人： Dilip R. Wagle , Sheng-Ding Fang , Taikyun Rho , John J. Egan , Sara Vasan , Peter Ulrich , Anthony Cerami
IPC分类号： C07D277/20 , A61K8/00 , A61K8/49 , A61K31/426 , A61K31/427 , A61K31/431 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5355 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P9/14 , A61P13/12 , A61P17/00 , A61P27/02 , A61Q19/00 , C07D277/22 , C07D277/24 , C07D277/44 , C07D417/06
CPC分类号： C07D277/22 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5355 , A61K31/541 , A61K31/55 , C07D277/44 , C07D417/06
摘要： The present invention relates to compositions and methods for reversing advanced glycosylation end product-mediated cross-linking and protein aging. Accordingly, compositions are described which comprise thiazolium compounds substituted with heterocyclic groups which are capable of reversing the formation of advanced glycosylation end product cross-links. Both industrial and therapeutic applications for the invention are disclosed, as food spoilage and animal protein aging can be treated. Such compounds have particular application in the treatment of protein aging such as is responsible for the complications of aging and diabetes.

2. 发明授权

US06319934B1 Reversing advanced glycosylation cross-links using heterocyclic-substituted thiazolium compounds 失效
标题翻译：使用杂环取代的噻唑化合物逆转先进的糖基化交联
公开(公告)号：US06319934B1
公开(公告)日：2001-11-20
申请号：US09644024
申请日：2000-08-23
申请人： Dilip R. Wagle , Sheng-Ding Fang , Taikyun Rho , John J. Egan , Sara Vasan , Peter Ulrich , Anthony Cerami
发明人： Dilip R. Wagle , Sheng-Ding Fang , Taikyun Rho , John J. Egan , Sara Vasan , Peter Ulrich , Anthony Cerami
IPC分类号： C07D27724
CPC分类号： C07D277/22 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5355 , A61K31/541 , A61K31/55 , C07D277/44 , C07D417/06
摘要： The present invention relates to compositions and methods for reversing advanced glycosylation end product-mediated cross-linking and protein aging. Accordingly, compositions are described which comprise thiazolium compounds substituted with heterocyclic groups which are capable of reversing the formation of advanced glycosylation end product cross-links. Both industrial and therapeutic applications for the invention are disclosed, as food spoilage and animal protein aging can be treated. Such compounds have particular application in the treatment of protein aging such as is responsible for the complications of aging and diabetes.
摘要翻译：本发明涉及用于逆转晚期糖基化终产物介导的交联和蛋白质老化的组合物和方法。因此，描述了包含被能够逆转高级糖基化终产物交联的形成的杂环基取代的噻唑鎓化合物的组合物。公开了用于本发明的工业和治疗应用，因为可以处理食物腐败和动物蛋白质老化。这些化合物在治疗老化和糖尿病并发症等蛋白质老化中具有特殊的应用。

3. 发明授权

US06790859B2 Reversing advanced glycosylation cross-links using heterocyclic-substituted thiazolium compounds 失效
标题翻译：使用杂环取代的噻唑化合物逆转先进的糖基化交联
公开(公告)号：US06790859B2
公开(公告)日：2004-09-14
申请号：US10348378
申请日：2003-01-21
申请人： Dilip R. Wagle , Sheng-Ding Fang , Taikyun Rho , John J. Egan , Sara Vasan , Peter Ulrich , Anthony Cerami
发明人： Dilip R. Wagle , Sheng-Ding Fang , Taikyun Rho , John J. Egan , Sara Vasan , Peter Ulrich , Anthony Cerami
IPC分类号： A61K31425
CPC分类号： C07D277/22 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5355 , A61K31/541 , A61K31/55 , C07D277/44 , C07D417/06
摘要： The present invention relates to compositions and methods for reversing advanced glycosylation end product-mediated cross-linking and protein aging. Accordingly, compositions are described which comprise thiazolium compounds substituted with heterocyclic groups which are capable of reversing the formation of advanced glycosylation end product cross-links. Both industrial and therapeutic applications for the invention are disclosed, as food spoilage and animal protein aging can be treated. Such compounds have particular application in the treatment of protein aging such as is responsible for the complications of aging and diabetes.
摘要翻译：本发明涉及用于逆转晚期糖基化终产物介导的交联和蛋白质老化的组合物和方法。因此，描述了包含被能够逆转高级糖基化终产物交联的形成的杂环基取代的噻唑鎓化合物的组合物。公开了用于本发明的工业和治疗应用，因为可以处理食物腐败和动物蛋白质老化。这些化合物在治疗老化和糖尿病并发症等蛋白质老化中具有特殊的应用。

4. 发明授权

US5358960A Method for inhibiting advanced glycosylation of proteins using aminosubstituted imidazoles 失效
标题翻译：使用氨基取代咪唑抑制蛋白质晚期糖基化的方法
公开(公告)号：US5358960A
公开(公告)日：1994-10-25
申请号：US986662
申请日：1992-12-08
申请人： Peter Ulrich , Anthony Cerami , Dilip R. Wagle
发明人： Peter Ulrich , Anthony Cerami , Dilip R. Wagle
IPC分类号： A61K8/43 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/19 , A61K38/20 , A61K38/21 , A61K38/38 , A61K39/00 , A61Q11/00 , A61Q19/08 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/58 , G01N33/68
CPC分类号： A61K8/43 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61Q19/08 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/582 , G01N33/68 , G01N33/6842 , G01N33/6893 , A61K2039/6081 , G01N2333/922 , Y10S514/866
摘要： The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging), Accordingly, a composition is disclosed which comprises 2-aminoimidazoles capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation, The method comprises contacting the target protein with the composition, Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
摘要翻译：本发明涉及抑制非酶交联（蛋白质老化）的组合物和方法。因此，公开了一种组合物，其包含2-氨基咪唑，其能够通过与靶蛋白的羰基部分反应来抑制靶蛋白的高级糖基化终产物的形成通过其初始糖基化形成的这种靶蛋白的早期糖基化产物。该方法包括使靶蛋白与组合物接触。本发明的工业和治疗应用都是可以想象的，因为可以处理食物腐败和动物蛋白质老化。

5. 发明申请

US20070025926A1 Preventing and reversing the formation of advance glycosylation endproducts 审中-公开
标题翻译：预防和逆转先进的糖基化终产物的形成
公开(公告)号：US20070025926A1
公开(公告)日：2007-02-01
申请号：US11351655
申请日：2006-02-09
申请人： Anthony Cerami , Peter Ulrich , Dilip Wagle , San-Bao Hwang , Sara Vasan , John Egan
发明人： Anthony Cerami , Peter Ulrich , Dilip Wagle , San-Bao Hwang , Sara Vasan , John Egan
IPC分类号： A61K31/426 , A61K8/49 , C07D277/30
CPC分类号： G01N33/6842 , A61K8/49 , A61K31/425 , A61K31/426 , A61K31/428 , A61Q11/00 , A61Q19/00 , A61Q19/08 , C07D277/22 , C07D277/40 , G01N33/68 , G01N33/6854 , G01N2500/02
摘要： The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain useful agents are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.
摘要翻译：本发明涉及用于抑制和逆转非酶交联（蛋白质老化）的组合物和方法。因此，公开了包含能够抑制靶蛋白的高级糖基化终产物形成的试剂的组合物，并且还通过切割高级糖基化终产物中存在的基于α-二羰基的蛋白质交联来进一步反转高级糖基化终产物中的预形成交联。某些有用的试剂是噻唑鎓盐。该方法包括使靶蛋白与组合物接触。预想到本发明的工业和治疗应用，因为可以处理食物腐败和动物蛋白质老化。还公开了用于检测非酶交联反转的新型免疫测定。

6. 发明授权

US5854289A Guanylhydrazones and their use to treat inflammatory conditions 失效
标题翻译：桂脒及其用于治疗炎症的用途
公开(公告)号：US5854289A
公开(公告)日：1998-12-29
申请号：US632305
申请日：1996-04-15
申请人： Marina Bianchi , Anthony Cerami , Kevin J. Tracey , Peter Ulrich
发明人： Marina Bianchi , Anthony Cerami , Kevin J. Tracey , Peter Ulrich
IPC分类号： C07D233/61 , A61K31/00 , A61K31/155 , A61K31/167 , A61K31/17 , A61K31/175 , A61K31/195 , A61K31/198 , A61K31/415 , A61K31/4164 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/60 , A61P3/00 , A61P9/00 , A61P29/00 , A61P31/00 , A61P33/00 , A61P35/00 , A61P43/00 , C07C275/38 , C07C275/40 , C07C281/18 , C07D213/42 , A61K31/16
CPC分类号： A61K31/621 , A61K31/00 , A61K31/155 , A61K31/167 , A61K31/17 , A61K31/175 , A61K31/195 , A61K31/4164 , A61K31/44 , A61K31/60 , C07C275/38 , C07C275/40 , C07C281/18 , Y10S514/825 , Y10S514/886 , Y10S514/903
摘要： This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections, and autoimmune or other diseases in which activated macrophages are involved, such as septic shock, heumatoid arthritis and multiple sclerosis.
摘要翻译：本发明涉及可用于预防和改善恶病质的新方法和组合物，与癌症和其它慢性疾病相关的营养状况不佳的临床综合征以及身体的消耗。更具体地说，本发明涉及芳香脒腙（更合适地称为脒基腙）组合物及其用于抑制巨噬细胞摄取精氨酸和/或转化成尿素的用途。这些组合物和方法也可用于预防细胞产生一氧化氮（NO），并且因此可以防止需要相同的人的NO介导的炎症和其他反应。在另一个实施方案中，所述化合物可用于抑制精氨酸依赖性肿瘤和感染中的精氨酸摄取，以及涉及活化的巨噬细胞的自身免疫性或其它疾病，例如败血性休克，类风湿性关节炎和多发性硬化症。

7. 发明授权

US5620983A Compounds and methods of use to derivatize neighboring lysine residues in proteins under physiological conditions 失效
标题翻译：用于在生理条件下衍生蛋白质中相邻赖氨酸残基的化合物和方法
公开(公告)号：US5620983A
公开(公告)日：1997-04-15
申请号：US470103
申请日：1995-06-06
申请人： Michael I. Bukrinsky , Anthony Cerami , Peter Ulrich
发明人： Michael I. Bukrinsky , Anthony Cerami , Peter Ulrich
IPC分类号： C07C279/16 , C07C279/26 , C07D239/48 , C07D251/48 , A61K31/52
CPC分类号： C07D239/48 , C07C279/16 , C07C279/26 , C07D251/48
摘要： The present invention concerns compounds that block the movement of viral particles through the nuclear membrane and thereby prevent the productive infection of terminally differentiated cells by virus the life cycle of which includes such an importation step. The invention encompasses methods of use of such compounds. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.
摘要翻译：本发明涉及阻止病毒颗粒通过核膜的运动，从而通过其生命周期包括这种进口步骤的病毒来防止终末分化细胞的生产性感染的化合物。本发明包括使用这些化合物的方法。还教导了使用化合物来检测存在于核定位序列中的某些特定蛋白质结构。

8. 发明申请

US20050245512A1 Method and composition for rejuvinating cells, tissues organs, hair and nails 审中-公开
标题翻译：用于恢复细胞，组织器官，头发和指甲的方法和组合物
公开(公告)号：US20050245512A1
公开(公告)日：2005-11-03
申请号：US11175098
申请日：2005-07-05
申请人： Peter Ulrich , Sheng Fang , Michael Brines , Qiao-Wen Xie , Anthony Cerami
发明人： Peter Ulrich , Sheng Fang , Michael Brines , Qiao-Wen Xie , Anthony Cerami
IPC分类号： C07D233/60 , A61K8/49 , A61K31/415 , A61K31/4174 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/44 , A61K31/452 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/519 , A61K31/535 , A61K31/5377 , A61K31/5383 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/02 , A61P13/12 , A61P17/00 , A61P19/02 , A61P25/02 , A61P25/28 , A61P27/02 , A61P27/12 , A61P27/16 , A61P43/00 , A61Q3/00 , A61Q3/02 , A61Q5/00 , A61Q5/12 , A61Q19/00 , A61Q19/08 , C07D213/20 , C07D213/50 , C07D213/57 , C07D213/73 , C07D233/54 , C07D239/26 , C07D239/42 , C07D265/36 , C07D277/22 , C07D277/24 , C07D277/84 , C07D417/06 , C07D487/04 , C07D498/02 , C07D513/04 , C07D521/00
CPC分类号： C07D213/20 , A61K8/49 , A61K8/4986 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/535 , A61Q3/00 , A61Q3/02 , A61Q5/00 , A61Q5/02 , A61Q5/12 , A61Q7/00 , A61Q19/08 , A61Q19/10 , C07D213/50 , C07D213/57 , C07D213/73 , C07D231/12 , C07D233/54 , C07D233/56 , C07D233/64 , C07D239/26 , C07D239/42 , C07D249/08 , C07D277/22 , C07D277/24 , C07D277/84 , C07D417/06 , C07D487/04 , C07D513/04
摘要： In one embodiment, the present invention relates to compounds and compositions including pharmaceutical compositions containing the compounds and associated methods that uncouple sugar-mediated coupling of proteins, lipids, nucleic acids, and other biomaterials, and any combination thereof. In another embodiment, the compositions and associated methods have utility in vivo to reduce the deleterious effects of sugar-mediated coupling processes in an organism, when the organism is exposed to the compound or composition internally, by ingestion, transdermal application, or other means. In yet another embodiment, the compositions and associated methods are useful for the ex-vivo treatment of organs, cells and tissues and external treatment of hair, nails and skin to rejuvenate them by changing deformability and increase the tissue diffusion coefficient. In a further embodiment, the present invention relates to novel compounds and pharmaceutical compositions.
摘要翻译：在一个实施方案中，本发明涉及包含药物组合物的化合物和组合物，所述药物组合物含有化合物和解离糖介导的蛋白质，脂质，核酸和其他生物材料偶联的相关方法及其任何组合。在另一个实施方案中，组合物和相关方法在体内通过摄入，经皮施用或其它方式在生物体内部暴露于化合物或组合物时，有效地降低糖介导的生物体中的偶联过程的有害作用。在另一个实施方案中，组合物和相关方法可用于器官，细胞和组织的离体处理以及毛发，指甲和皮肤的外部治疗，以通过改变变形性和增加组织扩散系数使其恢复活力。在另一个实施方案中，本发明涉及新化合物和药物组合物。

9. 发明授权

US06906076B2 Compounds and methods of use to treat infectious diseases 失效
标题翻译：用于治疗传染病的化合物和方法
公开(公告)号：US06906076B2
公开(公告)日：2005-06-14
申请号：US10660748
申请日：2003-09-12
申请人： Michael I. Bukrinsky , Anthony Cerami , Peter Ulrich , Bradley Berger
发明人： Michael I. Bukrinsky , Anthony Cerami , Peter Ulrich , Bradley Berger
IPC分类号： C07D251/70 , A61K31/155 , A61K31/505 , A61K31/52 , A61K31/53 , A61P31/12 , A61P33/06 , C07D239/42 , C07D239/48 , C07D473/34 , C07D239/28
CPC分类号： C07D239/48 , A61K31/505 , A61K31/53 , Y02A50/402 , Y02A50/411 , Y02A50/423 , Y10T436/173845 , Y10T436/200833
摘要： The present invention concerns alkyl aryl carbonyl compounds that possess anti-infective activity. The compounds of the invention can be used to target specific nuclear localization signal, thereby blocking importation of specific proteins or molecular complex into the nucleus of a cell. The invention encompasses methods of use of such compounds for treatment or prevention of infectious diseases, such as parasitic and viral diseases, including, for example, malaria and acquired immunodeficiency syndrome. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.
摘要翻译：本发明涉及具有抗感染活性的烷基芳基羰基化合物。本发明的化合物可用于靶向特异性核定位信号，从而阻止特异性蛋白质或分子复合物进入细胞核。本发明包括使用这些化合物治疗或预防感染性疾病如寄生虫病和病毒性疾病，包括例如疟疾和获得性免疫缺陷综合征的方法。还教导了使用化合物来检测存在于核定位序列中的某些特定蛋白质结构。

10. 发明授权

US6119701A Methods, agents and devices for removing nucleophilic toxins from tobacco and tobacco smoke 失效
标题翻译：用于从烟草和烟草烟雾中去除亲核毒素的方法，试剂和装置
公开(公告)号：US6119701A
公开(公告)日：2000-09-19
申请号：US23569
申请日：1998-02-13
申请人： Anthony Cerami , Carla Cerami , Peter Ulrich
发明人： Anthony Cerami , Carla Cerami , Peter Ulrich
IPC分类号： A24D3/10 , A24D3/14 , A24B15/00 , A24B15/10
CPC分类号： A24D3/14 , A24D3/10
摘要： This invention provides methods, devices and agents for the removal of nucleophilic toxins present in tobacco and tobacco smoke, without the removal of nicotine. The filter element of a tobacco smoking device or an air filtration device used in conjunction with a tobacco smoking device may comprise chemical moieties reactive with nucleophilic compounds, or agents that trap nucleophilic compounds may be incorporated into the filter element of tobacco smoking device such as a cigarette, cigar, pipe, or in a separate filter through which tobacco smoke passes before entering the mouth. The agents may also be incorporated into air filters for removing tobacco combustion product toxins from room air. The agents may also be incorporated into smoking or smokeless tobacco to remove toxins.
摘要翻译：本发明提供了除去烟草和烟草烟雾中存在的亲核毒素的方法，装置和试剂，而不除去尼古丁。与烟草吸烟装置一起使用的烟草吸烟装置或空气过滤装置的过滤元件可以包括与亲核化合物反应的化学部分，或者捕获亲核化合物的试剂可以并入烟草吸烟装置的过滤元件中，例如香烟，雪茄，烟斗，或烟草烟雾在进入口腔之前通过的单独过滤器。还可以将这些试剂并入空气过滤器中，以从室内空气中除去烟草燃烧产物毒素。这些药剂也可以并入吸烟或无烟烟草中以去除毒素。

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