T-6932(T-6932) - 药物靶点：PDE5A_专利_临床

概要

基本信息

药物类型

小分子化药

别名

T 6932、T6932

靶点

PDE5A

作用机制

PDE5A抑制剂(磷酸二酯酶-5A抑制剂)

治疗领域

泌尿生殖系统疾病

在研适应症-

非在研适应症

勃起功能障碍

原研机构

Mitsubishi Tanabe Pharma Corp.

在研机构-

非在研机构

Mitsubishi Tanabe Pharma Corp.

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构/序列

分子式C28H27ClN4O6

InChIKeyDJVBNZMSHDWOSI-UHFFFAOYSA-N

CAS号372112-75-9

关联

100 项与 T-6932 相关的临床结果

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100 项与 T-6932 相关的转化医学

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100 项与 T-6932 相关的专利（医药）

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2

项与 T-6932 相关的文献（医药）

2014-12-01·Bioorganic & medicinal chemistry letters4区 · 医学

The discovery of avanafil for the treatment of erectile dysfunction: A novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor

4区 · 医学

Article

作者: Matsuki, Kenji ; Sakamoto, Toshiaki ; Kotera, Jun ; Hikota, Masataka ; Koga, Yuichi ; Morimoto, Hiroshi ; Omori, Kenji ; Fujishige, Kotomi ; Murakami, Michino ; Yamada, Koichiro ; Kikkawa, Kohei

Novel pyrimidine-5-carboxamide derivatives bearing a 3-chloro-4-methoxybenzylamino group at the 4-position were identified as potent and highly selective phosphodiesterase 5 inhibitors. Among them, we successfully found 10j (avanafil) which exhibited a potent relaxant effect on isolated rabbit cavernosum (EC30=2.1 nM) and a high isozyme selectivity.

2014-11-01·Bioorganic & medicinal chemistry letters4区 · 医学

Design and synthesis of novel 5-(3,4,5-trimethoxybenzoyl)-4-aminopyrimidine derivatives as potent and selective phosphodiesterase 5 inhibitors: Scaffold hopping using a pseudo-ring by intramolecular hydrogen bond formation

4区 · 医学

Article

作者: Matsuki, Kenji ; Sakamoto, Toshiaki ; Kotera, Jun ; Hikota, Masataka ; Koga, Yuichi ; Omori, Kenji ; Morimoto, Hiroshi ; Fujishige, Kotomi ; Murakami, Michino ; Yamada, Koichiro ; Kikkawa, Kohei

5-(3,4,5-Trimethoxybenzoyl)-4-amimopyrimidine derivatives were found as a novel chemical class of potent and highly selective phosphodiesterase 5 inhibitors. A pseudo-ring formed by an intramolecular hydrogen bond constrained the conformation of 3-chloro-4-methoxybenzylamino and 3,4,5-trimethoxybenzoyl substituents and led to the discovery of T-6932 (19a) with a potent PDE5 inhibitory activity (IC50 = 0.13 nM) and a high selectivity over PDE6 (IC50 ratio: PDE6/PDE5 = 2400). Further modification at the 2-position of T-6932 resulted in the finding of 26, which exhibited potent relaxant effects on isolated rabbit corpus cavernosum (EC30 = 11 nM) with a high PDE5 selectivity over PDE6 (IC50 ratio: PDE6/PDE5 = 2800).

100 项与 T-6932 相关的药物交易

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