公开(公告)号：US20080139664A1

公开(公告)日：2008-06-12

申请号：US12029209

申请日：2008-02-11

申请人： Faustinus YEBOAH ,  Yasuo KONISHI ,  Sung Ju CHO ,  Jittiwud LERTVORACHON ,  Taira KIYOTA ,  Tomasz Popek

发明人： Faustinus YEBOAH ,  Yasuo KONISHI ,  Sung Ju CHO ,  Jittiwud LERTVORACHON ,  Taira KIYOTA ,  Tomasz Popek

IPC分类号： A61K31/135 ,  A61P3/00

CPC分类号： A61K31/47 ,  A61K31/00 ,  A61K31/04 ,  A61K31/137 ,  A61K31/195 ,  A61K31/222 ,  A61K31/345 ,  A61K31/352 ,  A61K31/4164 ,  A61K31/4168 ,  A61K31/65 ,  C07C219/30

摘要： The invention provides new inhibitors of protein glycation, identified from compound libraries by a high throughput screening assay. The anti-glycation agents so identified are characterized by a variety of chemical structures and are useful for the prevention or treatment of age-, diabetes-, and smoking-related complications, including neuropathy, nephropathy, ocular pathologies, or the loss of mechanical properties of collagenous tissues. Among compounds identified as having the anti-glycation activity, of special interest are epinephrine and its analogs, in particular D-epinephrine and its analogs, which are particularly useful for the prevention or treatment of age-, diabetes-, and smoking-related ocular pathologies.

摘要翻译： 本发明提供了通过高通量筛选测定从化合物文库鉴定的蛋白质糖基化的新抑制剂。 如此确定的抗糖化剂的特征在于各种化学结构，并且可用于预防或治疗年龄，糖尿病和吸烟相关并发症，包括神经病，肾病，眼病变或机械性能的丧失 的胶原组织。 鉴定为具有抗糖基化活性的化合物是特别有用的肾上腺素及其类似物，特别是D-肾上腺素及其类似物，其特别可用于预防或治疗年龄，糖尿病和吸烟相关眼 病态。

公开(公告)号：US20100204468A1

公开(公告)日：2010-08-12

申请号：US12764537

申请日：2010-04-21

申请人： Faustinus YEBOAH ,  Mahmood PIRAEE

发明人： Faustinus YEBOAH ,  Mahmood PIRAEE

IPC分类号： C07D243/10 ,  C12P17/10 ,  C12N1/00 ,  C12N1/20

CPC分类号： C12P17/10 ,  B01D15/00 ,  B01D61/145 ,  C07D243/38 ,  C12N1/20 ,  C12P17/12 ,  C12R1/29

摘要： The present invention provides a scalable process for producing a concentrate containing a mass of a farnesylated dibenzodiazepinone by fermenting in an aqueous culture medium a strain of a microorganism that is capable of producing the farnesylated dibenzodiazepinone, upon completion of fermentation harvesting the fermentation broth and extracting the fermentation broth to provide an extract, and thereafter treating the extract to form the concentrate. The concentrate so produced may be utilized in downstream processes for producing pharmaceutical compounds. A strain of a Micromonospora species capable of producing a farnesylated dibenzodiazepinone at a high yield rate is provided, together with culture media for culturing microorganisms, and fermentation conditions for production of the farnesylated dibenzodiazepinone of the concentrate.

摘要翻译： 本发明提供了一种可扩展的方法，用于生产含有大量法呢基化二苯并二氮杂酮的浓缩物，其通过在水性培养基中发酵能够产生法呢基化二苯并二氮杂酮的微生物菌株，在完成发酵收获发酵液并提取 发酵液提供提取物，然后处理提取物以形成浓缩物。 如此生产的浓缩物可用于生产药物化合物的下游方法。 提供能够以高产率生产法呢基化二苯并二氮杂酮的小单孢菌属菌株，以及用于培养微生物的培养基和用于生产浓缩物的法呢基化二苯并二氮杂酮的发酵条件。