基本信息:
- 专利标题: MODIFIED NATURETIC COMPOUNDS, CONJUGATES, AND USES THEREOF
- 专利标题(中):改性天然化合物,结合物及其用途
- 申请号:PCT/US0337996 申请日:2003-11-12
- 公开(公告)号:WO2004047871A3 公开(公告)日:2005-03-17
- 发明人: JAMES KENNETH D , RADHAKRISHNAN BALASINGAM , MALKAR NAVDEEP B , MILLER MARK A , EKWURIBE NNOCHIRI N
- 申请人: NOBEX CORP
- 专利权人: NOBEX CORP
- 当前专利权人: NOBEX CORP
- 优先权: US42915102 2002-11-26
- 主分类号: A61K47/48
- IPC分类号: A61K47/48 ; C07K14/58 ; C07K14/72 ; C08G65/329 ; A61K38/22 ; C08G65/32 ; C08G65/333
摘要:
Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, subcutaneous, and intravenous forms to of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.
摘要(中):
本发明公开了改进的利尿钠化合物及其缀合物。 特别地,提供了缀合形式的hBNP,其包括与其连接的至少一个修饰部分。 修饰的利尿钠化合物缀合物保留刺激cGMP产生,结合NPR-A受体的活性,并且在一些实施方案中,与未修饰的对应利钠化合物相比,循环中的半衰期改善。 可以制备化合物和缀合物的口服,肠胃外,皮下和静脉内形式作为心脏状况的治疗和/或治疗,特别是充血性心力衰竭。 还公开了包含具有各种长度和构型的寡聚结构的修饰部分。 还公开了利尿钠化合物的类似物,其具有不同于天然序列的氨基酸序列。
IPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品 |
------A61K47/00 | 以所用的非有效成分为特征的医用配制品,如载体、惰性添加剂 |
--------A61K47/48 | .非有效成分被化学键键合到有效成分上,例如聚合物药物轭合物 |