YM-96765(YM-96765) - 药物靶点：factor Xa_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

factor Xa

作用方式

抑制剂

作用机制

factor Xa抑制剂(激活型凝血因子X抑制剂)

治疗领域

心血管疾病

在研适应症-

非在研适应症

血栓形成

原研机构

Yamanouchi Pharmaceutical Co., Ltd.

在研机构-

非在研机构

Yamanouchi Pharmaceutical Co., Ltd.

权益机构-

最高研发阶段终止临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 YM-96765 相关的临床结果

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100 项与 YM-96765 相关的转化医学

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100 项与 YM-96765 相关的专利（医药）

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2

项与 YM-96765 相关的文献（医药）

2005-01-01·Chemical & pharmaceutical bulletin4区 · 医学

An Easy Access to 7-Methyl-2-naphthalenecarbonitrile

4区 · 医学

Article

作者: Matsumoto, Yuzo ; Yanagisawa, Isao ; Yamada, Hiroyoshi ; Ishihara, Tsukasa ; Koshio, Hiroyuki ; Hirayama, Fukushi

A practical and cost-effective procedure has been developed for the synthesis of 7-methyl-2-naphthalenecarbonitrile, the precursor of the anticoagulant agents YM-60828 or YM-96765. This new route generates the key intermediate in only two steps from readily available 3-cyanopropionaldehyde dimethyl acetal and m-tolualdehyde, without requiring chromatographic purification. The synthesis involves condensation of the cyano derivative with the aldehyde and subsequent cyclodehydration.

2004-05-01·Bioorganic & medicinal chemistry3区 · 医学

Synthesis and biological activity of novel 1,4-diazepane derivatives as factor Xa inhibitor with potent anticoagulant and antithrombotic activity

3区 · 医学

Article

作者: Ishihara, Tsukasa ; Hirayama, Fukushi ; Taniuchi, Yuta ; Matsumoto, Yuzo ; Sakamoto, Shuichi ; Tsukamoto, Shin-ichi ; Sakai-Moritani, Yumiko ; Kawasaki, Tomihisa ; Sato, Kazuo ; Koshio, Hiroyuki ; Kaku, Seiji

Factor Xa (fXa) is a serine protease involved in the coagulation cascade, which has received great interest as a potential target for the development of new antithrombotic drugs. Herein we report a novel series of fXa inhibitors in which the 1,4-diazepane moiety was designed to interact with the S4 aryl-binding domain of the fXa active site. Compound 13 (YM-96765) showed potent fXa inhibitory activity (IC(50) = 6.8 nM) and effective antithrombotic activity without prolonging bleeding time.

100 项与 YM-96765 相关的药物交易

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