WS-75624B(WS-75624B) - 药物靶点：ECE_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

ECE

作用方式

抑制剂

作用机制

ECE抑制剂(内皮素转化酶-1抑制剂)

治疗领域

心血管疾病

在研适应症-

非在研适应症

心血管疾病

原研机构

Fujisawa Pharmaceutical Co., Ltd.

在研机构-

非在研机构

Fujisawa Pharmaceutical Co., Ltd.

权益机构-

最高研发阶段终止药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 WS-75624B 相关的临床结果

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100 项与 WS-75624B 相关的转化医学

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100 项与 WS-75624B 相关的专利（医药）

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2

项与 WS-75624B 相关的文献（医药）

2004-04-01·The Journal of Organic Chemistry2区 · 化学

Use of Thiazoles in the Halogen Dance Reaction: Application to the Total Synthesis of WS75624 B

2区 · 化学

Article

作者: Sammakia, Tarek ; Stangeland, Eric L.

The total synthesis of the pyridine-thiazole-containing natural product WS75624 B (1) is described. This synthesis proceeds via the Stille coupling of appropriately functionalized pyridine and thiazole components, and this paper details our studies on the use of the halogen dance reaction to prepare the desired thiazole. Various halogen dance reactions on thizoles are described, including a novel one-pot multistep reaction in which 2-bromothiazole is treated with LDA in the presence of a silyl chloride at -78 degrees C and quenched with an electrophile to provide the highly functionalized thiazole derivatives 27.

1995-01-01·The Journal of Antibiotics4区 · 医学

WS75624 A and B, New Endothelin Converting Enzyme Inhibitors Isolated from Saccharothrix sp. No. 75624. I. Taxonomy, Fermentation, Isolation, Physico-chemical Properties and Biological Activities.

4区 · 医学

Article

作者: Motoaki Nishikawa ; Masakuni Okuhara ; Sumio Kiyoto ; Yasuhisa Tsurumi ; Hirotugu Ueda ; Kenichi Hayashi ; Shigehiro Takase

Novel endothelin converting enzyme (ECE) inhibitors, WS75624 A and B, have been isolated from the fermentation broth of Saccharothrix sp. No. 75624. These inhibitors were purified from an acetone extract of whole culture broth followed by HP-20 column chromatography, silica gel column chromatography and HPLC. WS75624 A and B showed highly potent ECE inhibitory activity, and both had IC50 values of 0.03 microgram/ml. WS75624 A and B also showed other metalloprotease (collagenase and neutral endopeptidase) inhibitory activity with IC50 values of 1 microgram/ml. Since large amount of WS75624 B was isolated, we tried in vivo evaluation using WS75624 B. WS75624 B inhibited big endothelin-induced pressor effect when administered to SD rat intravenously with big ET-1.

100 项与 WS-75624B 相关的药物交易

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