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11. 发明授权

US5318982A Inhibition of the advanced glycosylation of proteins using substituted-1,2,4-triazoles 失效
标题翻译：使用取代的1,2,4-三唑抑制蛋白质的高级糖基化
公开(公告)号：US5318982A
公开(公告)日：1994-06-07
申请号：US986661
申请日：1992-12-08
申请人： Peter C. Ulrich , Anthony Cerami , Dilip R. Wagle
发明人： Peter C. 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 , A61K31/41 , A61K7/16
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
摘要： The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises substituted 1,2,4-triazoles 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，其包含通过与通过其初始糖基化形成的这些靶蛋白的早期糖基化产物的羰基部分反应而能够抑制靶蛋白的高级糖基化终产物形成的取代的1,2,4-三唑。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。

12. 发明授权

US5612332A Di- and triaminoguanidines, and methods of use 失效
标题翻译：二胺和三氨基胍，以及使用方法
公开(公告)号：US5612332A
公开(公告)日：1997-03-18
申请号：US487059
申请日：1995-06-07
申请人： Dilip R. Wagle , Peter C. Ulrich , Anthony Cerami
发明人： Dilip R. Wagle , Peter C. Ulrich , Anthony Cerami
IPC分类号： A61K8/43 , A61K31/15 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K31/4468 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/55 , A61K38/19 , A61K38/20 , A61K38/21 , A61K38/38 , A61K39/00 , A61Q11/00 , A61Q19/08 , C07C281/16 , C07D233/02 , C07D239/04 , C07D243/04 , C07D295/215 , C07D295/28 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/68 , C07C277/00 , C07C281/00 , C07D211/56 , C07D265/30
CPC分类号： G01N33/6842 , A61K31/15 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K31/4468 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/55 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/43 , A61Q11/00 , A61Q19/08 , C07C281/16 , C07D233/02 , C07D239/04 , C07D243/04 , C07D295/215 , C07D295/32 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/68 , G01N33/6893 , A61K2039/6081 , G01N2333/922
摘要： The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a di- or tri-aminoguanidine capable of inhibiting the formation of advanced glycosylation endproducts of target proteins. 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）的化合物，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二 - 或三氨基胍的组合物。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。

13. 发明授权

US5476849A Methods for glycosylation inhibition using amino-benzoic acids and derivatives 失效
标题翻译：使用氨基 - 苯甲酸及其衍生物进行糖基化抑制的方法
公开(公告)号：US5476849A
公开(公告)日：1995-12-19
申请号：US162538
申请日：1993-12-03
申请人： Peter C. Ulrich , Anthony Cerami , Dilip R. Wagle
发明人： Peter C. Ulrich , Anthony Cerami , Dilip R. Wagle
IPC分类号： A61K8/40 , A61K8/42 , A61K31/15 , A61K31/155 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/235 , A61K31/245 , 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 , G01N33/68 , A61K31/535 , A61K31/14 , A61K31/16 , A61K31/445 , A61K31/55
CPC分类号： G01N33/6842 , A61K31/15 , A61K31/155 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/235 , A61K31/245 , A61K31/415 , A61K31/4178 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/40 , A61K8/42 , A61Q11/00 , A61Q19/08 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/68 , G01N33/6893 , A61K2039/6081 , G01N2333/922 , G01N2800/042 , Y10S514/866 , Y10S514/913
摘要： The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with a 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）的化合物，组合物和方法。因此，公开了一种组合物，其包含能够通过与通过其初始糖基化形成的这些靶蛋白的早期糖基化产物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的试剂。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。

14. 发明授权

US5500439A Aminopyrazoles 失效
标题翻译：氨基吡唑
公开(公告)号：US5500439A
公开(公告)日：1996-03-19
申请号：US164466
申请日：1993-12-09
申请人： Peter C. Ulrich , Dilip R. Wagle
发明人： Peter C. Ulrich , Dilip R. Wagle
IPC分类号： A61K31/415
CPC分类号： A61K31/415
摘要： The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises aminopyrazoles capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of an 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）的化合物，组合物和方法。因此，公开了一种组合物，其包含氨基吡唑，其能够通过与通过其初始糖基化形成的这种靶蛋白的早期糖基化产物的羰基部分反应来抑制靶蛋白的晚期糖基化终产物的形成。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。

15. 发明授权

US5877217A N-acylaminoalkyl-hydrazinecarboximidamides 失效
标题翻译： N-酰氨基烷基 - 肼甲脒
公开(公告)号：US5877217A
公开(公告)日：1999-03-02
申请号：US771959
申请日：1996-12-23
申请人： Peter C. Ulrich , Dilip R. Wagle
发明人： Peter C. Ulrich , Dilip R. Wagle
IPC分类号： C07C281/16 , A61K31/16 , C07C307/00
CPC分类号： C07C281/16
摘要： The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging) using compounds of the following formula I ##STR1## wherein alk is a straight or branched chain alkylene group containing from 2 to 8 carbon atoms, and R is a lower alkyl group containing from 1 to 6 carbon atoms; and their biologically or pharmaceutically acceptable acid addition salts. Accordingly, a compositions are disclosed which comprises these N-acylaminoalkylhydrazinecarboximidamides, which are capable of inhibiting the formation of advanced glycosylation endproducts of target proteins. 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：本发明涉及使用下列式I化合物（I）抑制非酶交联（蛋白质老化）的组合物和方法，其中alk是含有2至8个碳原子的直链或支链亚烷基，以及 R是含有1至6个碳原子的低级烷基; 及其生物学或药学上可接受的酸加成盐。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N-酰基氨基烷基肼甲酰胺的组合物。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。

16. 发明授权

US5534540A Methods of inhibiting the advanced glycosylation of proteins using tetramic and tetronic acids and compositions therefor 失效
标题翻译：使用四聚和四氢酸抑制蛋白质高级糖基化的方法及其组合物
公开(公告)号：US5534540A
公开(公告)日：1996-07-09
申请号：US95095
申请日：1993-07-20
申请人： Peter C. Ulrich , Dilip R. Wagle
发明人： Peter C. Ulrich , Dilip R. Wagle
IPC分类号： A61K8/49 , A61K31/00 , A61K31/12 , A61K31/155 , A61K31/16 , A61K31/19 , A61K31/195 , A61K31/22 , A61K31/275 , A61K31/365 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , A61K38/19 , A61K38/20 , A61K38/21 , A61K38/38 , A61K39/00 , A61Q11/00 , A61Q19/08 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/68 , A61K31/34
CPC分类号： G01N33/6842 , A61K31/00 , A61K31/12 , A61K31/155 , A61K31/16 , A61K31/19 , A61K31/195 , A61K31/22 , A61K31/275 , A61K31/365 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/4973 , A61Q11/00 , A61Q19/08 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/68 , G01N33/6893 , A61K2039/6081 , G01N2333/922
摘要： The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises substituted or unsubstituted tetramic and tetronic acids capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with a carbonyl moiety of an 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，其包含能够通过其初始糖基化形成的这种靶蛋白的早期糖基化产物的羰基部分的反应而能够抑制靶蛋白的晚期糖基化终产物形成的取代或未取代的四聚和四氢酸。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。

17. 发明授权

US5468777A Method and agents for preventing and reversing the staining of teeth 失效
标题翻译：防止和反转牙齿染色的方法和试剂
公开(公告)号：US5468777A
公开(公告)日：1995-11-21
申请号：US236228
申请日：1994-04-29
申请人： Dennis S. France , Anthony Cerami , Peter C. Ulrich , Laura A. Norton , David L. Neer
发明人： Dennis S. France , Anthony Cerami , Peter C. Ulrich , Laura A. Norton , David L. Neer
IPC分类号： A61K8/44 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/19 , A61K38/20 , A61K38/21 , A61K38/38 , A61K39/00 , A61Q11/00 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/68 , A61K7/16
CPC分类号： C07D405/14 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/447 , A61Q11/00 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/68 , G01N33/6893 , A61K2039/6081 , G01N2333/922
摘要： The present invention relates to methods and agents for preventing and reversing the staining of teeth caused by the nonenzymatic browning of proteins in the oral cavity. Suitable agents for the inhibition of nonenzymatic browning may be formulated as rinses and toothpastes, and include cysteine and cysteine derivatives. These preparations may further include known anti-plaque agents, such as chlorhexidine.
摘要翻译：本发明涉及用于预防和逆转由口腔内的蛋白质的非酶褐变引起的牙齿染色的方法和试剂。用于抑制非酶褐变的合适的试剂可以配制成漂洗剂和牙膏，并且包括半胱氨酸和半胱氨酸衍生物。这些制剂还可以包括已知的抗斑块剂，如氯己定。

18. 发明授权

US5272176A Advanced glycation inhibitors containing amino-benzoic acids and derivatives, and methods of use 失效
标题翻译：含氨基苯甲酸及其衍生物的高级糖化抑制剂及其使用方法
公开(公告)号：US5272176A
公开(公告)日：1993-12-21
申请号：US896854
申请日：1992-06-12
申请人： Peter C. Ulrich , Anthony Cerami
发明人： Peter C. Ulrich , Anthony Cerami
IPC分类号： A61K8/44 , A61K8/46 , A61K31/15 , A61K31/155 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/235 , A61K31/245 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , 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 , A61K31/24
CPC分类号： G01N33/6842 , A61K31/15 , A61K31/155 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/235 , A61K31/245 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/44 , A61K8/445 , A61K8/466 , A61Q11/00 , A61Q19/08 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/582 , G01N33/68 , G01N33/6893 , A61K2039/6081 , G01N2333/922 , Y10S514/866 , Y10S514/913
摘要： The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent 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，其包含能够通过与通过其初始糖基化形成的这些靶蛋白的早期糖基化产物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的试剂。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。

19. 发明授权

US5254593A Compositions containing biguanides and derivatives thereof as inhibitors of nonenzymatic cross-linking 失效
标题翻译：含有双胍类及其衍生物作为非酶交联抑制剂的组合物
公开(公告)号：US5254593A
公开(公告)日：1993-10-19
申请号：US807609
申请日：1991-12-16
申请人： Peter C. Ulrich , Anthony Cerami
发明人： Peter C. Ulrich , Anthony Cerami
IPC分类号： A61K8/43 , A61K31/155 , A61K31/195 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , 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： C07D405/14 , A61K31/155 , A61K31/195 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/43 , A61Q11/00 , A61Q19/08 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/582 , G01N33/68 , G01N33/6893 , A61K2039/6081 , G01N2333/922 , Y10S514/824 , Y10S514/866 , Y10S514/878 , Y10S514/912 , Y10S514/913
摘要： The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent 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，其包含能够通过与通过其初始糖基化形成的这些靶蛋白的早期糖基化产物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的试剂。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。

20. 发明授权

US5218001A Inhibitors of the advanced glycosylation of proteins and methods of use therefor 失效
标题翻译：蛋白质高级糖基化的抑制剂及其使用方法
公开(公告)号：US5218001A
公开(公告)日：1993-06-08
申请号：US672946
申请日：1991-03-25
申请人： Peter C. Ulrich , Anthony Cerami
发明人： Peter C. Ulrich , Anthony Cerami
IPC分类号： A61K8/35 , A61K8/40 , A61K8/42 , A61K8/44 , A61K8/49 , A61K31/00 , A61K31/12 , A61K31/155 , A61K31/16 , A61K31/19 , A61K31/195 , A61K31/22 , A61K31/275 , A61K31/365 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , 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 , A61K31/33 , A61K7/16 , A61K31/335 , A61K31/505
CPC分类号： G01N33/6842 , A61K31/00 , A61K31/12 , A61K31/155 , A61K31/16 , A61K31/19 , A61K31/195 , A61K31/22 , A61K31/275 , A61K31/365 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/35 , A61K8/40 , A61K8/42 , A61K8/44 , A61K8/498 , A61Q11/00 , A61Q19/08 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/582 , G01N33/68 , G01N33/6893 , A61K2039/6081 , G01N2333/922
摘要： The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with a carbonyl moiety of an early glycosylation product of such target proteins resulting from 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，其包含能够通过与由其初始糖基化产生的此类靶蛋白的早期糖基化产物的羰基部分反应来抑制靶蛋白的高级糖基化终产物形成的试剂。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。

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