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31. 发明授权

US5145975A Naphthoquinone derivatives 失效
标题翻译：萘醌衍生物
公开(公告)号：US5145975A
公开(公告)日：1992-09-08
申请号：US549410
申请日：1990-07-06
申请人： Graeme B. Henderson , Peter C. Ulrich , Anthony Cerami
发明人： Graeme B. Henderson , Peter C. Ulrich , Anthony Cerami
IPC分类号： A61K31/00 , A61K31/175 , A61K31/345 , A61K31/495
CPC分类号： A61K31/00 , A61K31/175 , A61K31/345 , A61K31/495
摘要： The present invention relates to the treatment of diseases caused by invading organisms in a host by first identifying an enzymatic difference between the host and the invading organism and then administering to the host a pharmaceutically effective amount of a subversive substrate for the differing enzyme of the invading organism, whereby the action of the differing enzyme causes a result counter to the intended result and function of the enzyme that results in its debilitation or death. In particular, treatment of parasitic diseases caused by kinetoplastids including trypanosomes and leishmanias, e.g., African sleeping sickness, Chagas' disease, oriental sore and kala-azar is accomplished by administration of a pharmaceutically effective antiparasitic amount of a competitive toxigenic substrate for trypanothione reductase. Methods of treatment and compositions therefor contain a competitive toxigenic substrate for trypanothione reductase. Numerous compounds and corresponding compositions are disclosed.
摘要翻译：本发明涉及通过首先鉴定宿主与入侵生物体之间的酶差异，然后向宿主施用药物有效量的侵入性不同酶的颠覆性底物，来治疗宿主入侵生物引起的疾病由此不同酶的作用导致与预期的导致其衰弱或死亡的酶的预期结果和功能相反的结果。特别地，通过给予药学有效的寄生虫剂量的用于锥虫硫酮还原酶的竞争性产毒底物来实现由包括锥虫和利什曼原虫在内的动粒细胞引起的寄生虫病的治疗，例如非洲昏睡病，恰加斯病，东方疮和卡拉 - 氮芥。治疗方法及其组合物包含用于锥虫硫酮还原酶的竞争性产毒底物。公开了许多化合物和相应的组合物。

32. 发明授权

US5128360A Method and agents for inhibiting protein aging 失效
标题翻译：抑制蛋白质老化的方法和试剂
公开(公告)号：US5128360A
公开(公告)日：1992-07-07
申请号：US481869
申请日：1990-02-20
申请人： Anthony Cerami , Peter C. Ulrich , Michael Brownlee
发明人： Anthony Cerami , Peter C. Ulrich , Michael Brownlee
IPC分类号： C07H3/02 , A61K8/40 , A61K8/42 , A61K8/43 , A61K8/44 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/19 , A61K38/20 , A61K38/21 , A61K38/38 , A61K39/00 , A61Q11/00 , A61Q19/00 , A61Q19/08 , C07D405/00 , C07D405/14 , C07K14/00 , C07K14/435 , C07K14/76 , C07K16/00 , C07K16/28 , C09K11/06 , C12Q1/00 , G01N21/76 , G01N21/78 , G01N33/53 , G01N33/533 , G01N33/573 , G01N33/58 , G01N33/66 , G01N33/68
CPC分类号： G01N33/6893 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/40 , A61K8/42 , A61K8/43 , A61K8/44 , A61Q11/00 , A61Q19/00 , A61Q19/08 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/582 , G01N33/68 , G01N33/6842 , A61K2039/6081 , G01N2333/922 , Y10S435/968 , Y10S514/866
摘要： The present invention relates to compositions and methods for inhibiting protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents may contain an active nitrogen-containing group, such as a hydrazine group. Particular agents comprise aminoguanidine, .alpha.-hydrazinohistidine and mixtures thereof. 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形成的试剂或化合物。合适的试剂可以含有活性含氮基团，例如肼基团。具体的试剂包括氨基胍，α-肼基组氨酸及其混合物。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。

33. 发明授权

US4983604A Inhibitors of nonenzymatic cross-linking 失效
标题翻译：非酶交联剂的抑制剂
公开(公告)号：US4983604A
公开(公告)日：1991-01-08
申请号：US264930
申请日：1988-11-02
申请人： Peter C. Ulrich , Anthony Cerami
发明人： Peter C. Ulrich , Anthony Cerami
IPC分类号： A61K8/43 , A61K31/15 , A61K31/155 , A61K31/16 , A61K31/415 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P3/08 , A61P3/10 , A61P35/00 , A61P39/02 , A61Q11/00 , A61Q19/08 , C07C281/16 , C07D233/02 , C07D233/46 , C07D233/52 , C07D239/04 , C07D243/04 , C07D295/12 , C07D295/215
CPC分类号： A61K8/43 , A61K31/15 , A61K31/155 , A61K31/415 , A61K31/495 , A61K31/535 , A61Q11/00 , A61Q19/08 , C07D233/02 , C07D239/04 , C07D243/04 , C07D295/215 , G01N33/6842 , A61K2800/88
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. Suitable agents contain an active nitrogen-containing group, such as a hydrazine group. Particular agents comprise aminoguanidine derivatives. 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.

34. 发明授权

US4758583A Method and agents for inhibiting protein aging 失效
标题翻译：抑制蛋白质老化的方法和试剂
公开(公告)号：US4758583A
公开(公告)日：1988-07-19
申请号：US798032
申请日：1985-11-14
申请人： Anthony Cerami , Peter C. Ulrich , Michael Brownlee
发明人： Anthony Cerami , Peter C. Ulrich , Michael Brownlee
IPC分类号： C07H3/02 , A23J3/00 , A23L3/3526 , A61K8/40 , A61K8/42 , A61K8/43 , A61K8/44 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/19 , A61K38/20 , A61K38/21 , A61K38/38 , A61K39/00 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P17/00 , A61P27/02 , A61P43/00 , A61Q11/00 , A61Q19/00 , A61Q19/08 , C07D405/00 , C07D405/14 , C07K14/00 , C07K14/435 , C07K14/76 , C07K16/00 , C07K16/28 , C09K11/06 , C12Q1/00 , G01N21/76 , G01N21/78 , G01N33/53 , G01N33/533 , G01N33/573 , G01N33/58 , G01N33/66 , G01N33/68 , C07C128/00 , C07C129/00 , C12N1/06
CPC分类号： G01N33/6842 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/40 , A61K8/42 , A61K8/43 , A61K8/44 , A61Q11/00 , A61Q19/00 , 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 protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents may contain an active nitrogen-containing group, such as a hydrazine group, and may further be at least partially derived from amino acids. Particular agents comprise aminoguanidine, .alpha.-hydrazinohistidine and lysine. 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形成的试剂或化合物。合适的试剂可以含有活性含氮基团，例如肼基团，并且还可以至少部分地衍生自氨基酸。特定的药剂包括氨基胍，α-肼基组氨酸和赖氨酸。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。

35. 发明申请

US20080167228A1 Screening assay for the identification of inhibitors of macrophage migration inhibitory factor 审中-公开
标题翻译：用于鉴定巨噬细胞迁移抑制因子抑制剂的筛选试验
公开(公告)号：US20080167228A1
公开(公告)日：2008-07-10
申请号：US11812061
申请日：2007-06-14
申请人： Richard Bucala , Peter C. Ulrich , Xini Xhang , Anthony Cerami
发明人： Richard Bucala , Peter C. Ulrich , Xini Xhang , Anthony Cerami
IPC分类号： A61K38/16 , G01N33/68 , A61P37/02 , A61P29/00 , A61K38/02
CPC分类号： A61K31/122 , A61K31/167 , A61K31/404 , A61K38/00 , C07K14/52
摘要： The present invention encompasses assays to identify compounds that inhibit the enzymatic activity of MIF which catalyzes the tautomerization of MIF-substrates, such as D-dopachrome to DHICA. In general, the assay is conducted in vitro by adding, mixing or combining MIF and a suitable substrate in the presence or absence of a test compound, and measuring the tautomerization of the substrate. The test compounds that inhibit tautomerization in the assay are identified as MIF inhibitors.
摘要翻译：本发明包括鉴定抑制MIF的酶活性的化合物的测定，所述化合物催化MIF-底物如D多巴胺与DHICA的互变异构。通常，通过在存在或不存在测试化合物的情况下通过加入，混合或组合MIF和合适的底物并测量底物的互变异构体进行测定。在测定中抑制互变异构化的测试化合物被鉴定为MIF抑制剂。

36. 发明授权

US6025401A Method and agents for inhibiting protein aging 失效
标题翻译：抑制蛋白质老化的方法和试剂
公开(公告)号：US6025401A
公开(公告)日：2000-02-15
申请号：US62354
申请日：1998-04-17
申请人： Anthony Cerami , Yousef Al Abed , Richard J. Bucala , Peter C. Ulrich
发明人： Anthony Cerami , Yousef Al Abed , Richard J. Bucala , Peter C. Ulrich
IPC分类号： A61K31/045 , A61K31/11
CPC分类号： G01N33/6842
摘要： The present invention relates to compositions and methods for inhibiting the aging of amino-containing amino acid, peptides, proteins and biomolecules. Accordingly, a composition is disclosed which comprises an agent or compound capable of reacting with the glycosyl-amino moiety of the early glycosylation product (also known as the Amadori product or the Heyns product) formed by the reaction of glucose, or other reactive sugars, with an amino-containing peptide, protein or biomolecule, thus stabilizing this early glycosylation product, and preventing its further reaction to form open-chain, carbonyl-containing advanced glycosylation end products. Suitable agents may contain a reactive aldehyde group. A preferred agent is acetaldehyde. The method comprises contacting the target biomolecule 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：本发明涉及抑制含氨基酸，肽，蛋白质和生物分子的老化的组合物和方法。因此，公开了一种组合物，其包含能够与葡萄糖或其它反应性糖反应形成的早期糖基化产物（也称为Amadori产物或Heyns商品）的糖基 - 氨基部分反应的试剂或化合物，含有氨基的肽，蛋白质或生物分子，从而稳定该早期糖基化产物，并防止其进一步反应形成开链的含羰基的高级糖基化终产物。合适的试剂可以含有反应性醛基。优选的试剂是乙醛。该方法包括使目标生物分子与组合物接触。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。

37. 发明授权

US5770571A Method and agents for inhibiting protein aging 失效
公开(公告)号：US5770571A
公开(公告)日：1998-06-23
申请号：US746742
申请日：1996-11-15
申请人： Anthony Cerami , Yousef Al-Abed , Richard J. Bucala , Peter C. Ulrich
发明人： Anthony Cerami , Yousef Al-Abed , Richard J. Bucala , Peter C. Ulrich
IPC分类号： A23L3/3562 , A21D4/00 , A61K31/00 , A61K31/11 , A61K38/00 , A61K45/00 , A61P3/00 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/00 , A61P13/12 , A61P17/00 , A61P19/00 , A61P19/02 , A61P25/00 , A61P27/00 , A61P27/02 , A61P27/12 , A61P43/00 , C07H9/06 , C07H19/01 , G01N33/15 , G01N33/50 , G01N33/68 , C07K13/00 , C08J89/06
CPC分类号： G01N33/6842 , A61K31/11 , C07H19/01 , C07H9/06 , G01N33/68
摘要： The present invention relates to compositions and methods for inhibiting the aging of amino-containing amino acid, peptides, proteins and biomolecules. Accordingly, a composition is disclosed which comprises an agent or compound capable of reacting with the glycosyl-amino moiety of the early glycosylation product (also known as the Amadori product or the Heyns product) formed by the reaction of glucose, or other reactive sugars, with an amino-containing peptide, protein or biomolecule, thus stabilizing this early glycosylation product, and preventing its further reaction to form open-chain, carbonyl-containing advanced glycosylation end products. Suitable agents may contain a reactive aldehyde group. A preferred agent is acetaldehyde. The method comprises contacting the target biomolecule with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.

38. 发明授权

US5137916A 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：US5137916A
公开(公告)日：1992-08-11
申请号：US561066
申请日：1990-08-01
申请人： Peter C. Ulrich , Anthony Cerami
发明人： Peter C. Ulrich , Anthony Cerami
IPC分类号： A61K31/155 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , A61K39/00 , C07K16/28 , G01N33/573 , A01N37/12 , A01N37/18 , A01N43/50
CPC分类号： G01N33/6842 , A61K31/155 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , A61K39/0005 , C07K16/28 , G01N33/573 , 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 glycosylaton 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。

39. 发明授权

US5130337A Amidrazones and derivatives thereof 失效
标题翻译：氨基腙及其衍生物
公开(公告)号：US5130337A
公开(公告)日：1992-07-14
申请号：US697213
申请日：1991-05-07
申请人： Peter C. Ulrich , Anthony Cerami
发明人： Peter C. Ulrich , Anthony Cerami
IPC分类号： C07H3/02 , A61K8/40 , A61K8/42 , A61K8/43 , A61K8/44 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/19 , A61K38/20 , A61K38/21 , A61K38/38 , A61K39/00 , A61Q11/00 , A61Q19/00 , A61Q19/08 , C07D405/00 , C07D405/14 , C07K14/00 , C07K14/435 , C07K14/76 , C07K16/00 , C07K16/28 , C09K11/06 , C12Q1/00 , G01N21/76 , G01N21/78 , G01N33/53 , G01N33/533 , G01N33/573 , G01N33/58 , G01N33/66 , G01N33/68
CPC分类号： G01N33/6893 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/40 , A61K8/42 , A61K8/43 , A61K8/44 , A61Q11/00 , A61Q19/00 , A61Q19/08 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/582 , G01N33/68 , G01N33/6842 , A61K2039/6081 , G01N2333/922 , Y10S435/968 , Y10S514/866
摘要： The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging) which contain novel amidrazones and derivatives thereof. 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：本发明涉及抑制含有新型氨基腙及其衍生物的非酶交联（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。

40. 发明授权

US5106877A Aminoalcohol compounds in methods of use as inhibitors of the advanced glycosylation of proteins and methods of use therefor 失效
标题翻译：用作蛋白质高级糖基化抑制剂的方法中的氨基醇化合物及其使用方法
公开(公告)号：US5106877A
公开(公告)日：1992-04-21
申请号：US606697
申请日：1990-10-31
申请人： Peter C. Ulrich , Anthony Cerami
发明人： Peter C. Ulrich , Anthony Cerami
IPC分类号： A61K8/40 , A61K8/41 , A61K8/42 , 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 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/55 , A61K38/19 , A61K38/20 , A61K38/21 , A61K38/38 , A61K39/00 , A61Q11/00 , A61Q19/00 , A61Q19/08 , C07D405/14 , C07K16/28 , G01N33/533 , G01N33/573 , G01N33/58 , G01N33/68
CPC分类号： A61K8/40 , 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 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/55 , A61K38/191 , A61K38/2006 , A61K38/217 , A61K38/38 , A61K39/0005 , A61K8/41 , A61K8/42 , A61K8/494 , A61K8/4953 , A61Q11/00 , A61Q19/00 , 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 an agent capable of inhibiting the formation of advanced glycosylation end products 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。

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