OPC-18750(OPC-18750) - 在研适应症：心血管疾病_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点-

作用机制-

治疗领域

心血管疾病

在研适应症

心血管疾病

非在研适应症

心脏衰竭

原研机构

Otsuka Holdings Co., Ltd.

在研机构

Otsuka Pharmaceutical Co., Ltd.

非在研机构

Otsuka Holdings Co., Ltd.

最高研发阶段药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

登录后查看时间轴

结构

分子式C20H22N2O4

InChIKeySMFUDVJKOUBSBI-UHFFFAOYSA-N

CAS号128667-63-0

关联

100 项与 OPC-18750 相关的临床结果

登录后查看更多信息

100 项与 OPC-18750 相关的转化医学

登录后查看更多信息

100 项与 OPC-18750 相关的专利（医药）

登录后查看更多信息

1

项与 OPC-18750 相关的文献（医药）

1992-10-01·Journal of Medicinal Chemistry1区 · 医学

Novel positive inotropic agents: synthesis and biological activities of 6-(3-amino-2-hydroxypropoxy)-2(1H)-quinolinone derivatives

1区 · 医学

Article

作者: Tominaga, Michiaki ; Mori, Toyoki ; Teramoto, Shuji ; Hosokawa, Tetsumi ; Yabuuchi, Youichi ; Sumida, Takumi ; Fujioka, Takafumi

A series of 6-(3-amino-2-hydroxypropoxy)-2(1H)-quinolinones has been synthesized and evaluated for positive inotropic activity on the canine heart. Some of these derivatives have a potent activity with none or negative chronotropic effect in isolated, blood-perfused dog heart preparations. They also display a high selectivity for positive inotropic effect over chronotropic and vasodilatory effects in anesthetized dogs. (+/-)-6-[2-Hydroxy-3-[(3-methoxybenzyl)amino]propoxy]-2(1H)-quinolinone (39) and (+/-)-6-[3-(3,4-dimethoxybenzyl)amino]-2-hydroxypropoxy]-2 (1H)-quinolinone (40) were further investigated in conscious dogs. After iv administration, they did not affect heart rate or mean blood pressure at the dose producing a 50% increase in the peak of the first derivative of the left ventricular pressure. The compounds (39, OPC-18750, and 40, OPC-18790) are the most promising agents with desirable biological activities, and now are currently undergoing clinical evaluation.

100 项与 OPC-18750 相关的药物交易

登录后查看更多信息