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：US20100216858A1

公开(公告)日：2010-08-26

申请号：US12711979

申请日：2010-02-24

申请人： Tomasz Popek ,  Kishore Patel ,  Valery Alakhov ,  Grzegorz Pietrzynski

发明人： Tomasz Popek ,  Kishore Patel ,  Valery Alakhov ,  Grzegorz Pietrzynski

IPC分类号： A61K31/4184 ,  A61P35/00

CPC分类号： A61K31/4184 ,  A61K9/0019 ,  A61K9/19 ,  A61K47/38 ,  A61K47/40

摘要： The present invention is directed to pharmaceutical compositions comprising: (a) bendamustine, (b) a charged cyclopolysaccharide, and (c) a stabilizing agent having a charge opposite to that of the cyclopolysaccharide. Such composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. Such compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.

摘要翻译： 本发明涉及药物组合物，其包含：（a）苯达莫司汀，（b）带电荷的多环多糖，和（c）具有与环多糖相反的电荷的稳定剂。 这样的组合物在诸如血浆的反应性环境中提供了意想不到的期望的稳定性，偶联期望的抗癌活性。 这样的组合物适用于需要用苯达莫司汀治疗的患者的注射或输注。

公开(公告)号：US08436032B2

公开(公告)日：2013-05-07

申请号：US12711979

申请日：2010-02-24

申请人： Tomasz Popek ,  Kishore Patel ,  Valery Alakhov ,  Grzegorz Pietrzynski

发明人： Tomasz Popek ,  Kishore Patel ,  Valery Alakhov ,  Grzegorz Pietrzynski

IPC分类号： A61K31/415

CPC分类号： A61K31/4184 ,  A61K9/0019 ,  A61K9/19 ,  A61K47/38 ,  A61K47/40

摘要： The present invention is directed to pharmaceutical compositions comprising: (a) bendamustine, (b) a charged cyclopolysaccharide, and (c) a stabilizing agent having a charge opposite to that of the cyclopolysaccharide. Such composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. Such compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.

摘要翻译： 本发明涉及药物组合物，其包含：（a）苯达莫司汀，（b）带电荷的多环多糖，和（c）具有与环多糖相反的电荷的稳定剂。 这样的组合物在诸如血浆的反应性环境中提供了意想不到的期望的稳定性，偶联期望的抗癌活性。 这样的组合物适用于需要用苯达莫司汀治疗的患者的注射或输注。