公开(公告)号：US20120129774A1

公开(公告)日：2012-05-24

申请号：US13294371

申请日：2011-11-11

申请人： Fernand GOBEIL ,  Witold A. NEUGEBAUER ,  Domenico REGOLI ,  David FORTIN

发明人： Fernand GOBEIL ,  Witold A. NEUGEBAUER ,  Domenico REGOLI ,  David FORTIN

IPC分类号： A61K38/08 ,  A61P13/12 ,  A61P9/00

CPC分类号： C07K7/18 ,  A61K38/08

摘要： The present invention provides for novel kinin B1 receptors peptide agonists of formula (1) having very good to excellent affinities and selectivity for the B1 receptor, in vitro and in vivo increased resistance to enzymatic degradation, superior pharmacokinetic properties to those of naturally occurring agents, capacity to significantly enhance delivery of chemotherapeutic substances across the blood brain barrier and within peripheral tissues for the treatment of tumors, capacity to protect and restore kidney, heart, brain and other organ functions, when given alone or in combination with other therapies in the treatment of hypertension, diabetes and other cardiovascular diseases particularly, but not limited to, atherosclerosis and arteriosclerosis. aay-aax-aa0-aa1-aa2-aa3-aa4-aa5-Ser6-Pro7-D-Phe8-X(1)

摘要翻译： 本发明提供了新颖的激肽B1受体式（1）的肽激动剂，其对B1受体具有非常好的至优异的亲和力和选择性，体外和体内增加了对酶降解的抗性，优于天然存在的药物的药代动力学性质， 当治疗单独或与治​​疗中的其他疗法组合时，能够显着增强穿过血脑屏障和外周组织的化疗物质的递送以治疗肿瘤的能力，保护和恢复肾，心脏，脑和其他器官功能的能力 高血压，糖尿病和其他心血管疾病，特别但不限于动脉粥样硬化和动脉硬化。 aay-aax-aa0-aa1-aa2-aa3-aa4-aa5-Ser6-Pro7-D-Phe8-X（1）