FR-158999(FR-158999) - 药物靶点：Fibrinogen x GP IIb/IIIa_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

Fibrinogen x GP IIb/IIIa

作用方式

抑制剂、拮抗剂

作用机制

纤维蛋白原抑制剂、GP IIb/IIIa拮抗剂(糖蛋白 IIb/IIIa拮抗剂)、血小板聚集抑制剂

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

Astellas Pharma, Inc.

在研机构-

非在研机构

Fujisawa Pharmaceutical Co., Ltd.

Astellas Pharma, Inc.

权益机构-

最高研发阶段终止临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C24H35N5O8S

InChIKeyFPOQHPVEVPIFME-RXVVDRJESA-N

CAS号160138-41-0

关联

100 项与 FR-158999 相关的临床结果

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100 项与 FR-158999 相关的转化医学

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100 项与 FR-158999 相关的专利（医药）

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3

项与 FR-158999 相关的文献（医药）

1998-09-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

QSAR study of the peptidic fibrinogen inhibitors FK633, FR158999 and related derivatives, using a novel and useful hydrophobic descriptor (logPmw)

4区 · 医学

Article

作者: Akito Tanaka ; Masayoshi Murata ; Hideaki Fujiwara

A QSAR study using the novel hydrophobic descriptor (logPmw), which is a descriptor for membrane affinity, of our fibrinogen inhibitors FK633 (1), FR158999 (21), and related derivatives was performed, and resulted in good correlation (n = 19, s = 0.268, F = 6.38**, r = 0.667). Based on these results, we constructed a hypothesis by which these potent inhibitors bind to the receptor via the biomembrane and the C-terminal moiety functions as an anchor moiety.

1997-03-01·Bioorganic & Medicinal Chemistry Letters

Design, synthesis, and evaluation of orally active fibrinogen inhibitors

作者: Takatoshi Ishikawa ; Hiroyoshi Sakai ; Akito Tanaka ; Hisashi Takasugi ; Yukio Motoyama ; Toshiaki Aoki

Low mol. weight and orally active fibrinogen inhibitors are described.The compounds studied in this work were rationally designed based on a metabolic study of a peptidic fibrinogen inhibitor, 4-(4-amidinophenoxy)butanoylaspartylvaline (FK633), which led to the synthesis of a potent and orally active antiplatelet agent, 4-(4-amidinophenoxy)butanoylaspartylvalylthiomorpholine 1,1-dioxide (FR158999).Structure-activity relations are discussed.

Drugs of the Future

Rational drug design of the fibrinogen inhibitors FK633 and FR158999

作者: Sakai, Hiroyoshi ; Motoyama, Yukio ; Aoki, Toshiaki ; Tanaka, Akito ; Fujiwara, Hideaki ; Takasugi, Hisashi ; Ishikawa, Takatoshi

A review with 38 references of design, synthesis, pharmacol., metabolism, and structure-activity relationships of novel peptidal fibrinogen inhibitors.

100 项与 FR-158999 相关的药物交易

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