CYR715(CYR715) - 药物靶点：sGC_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

sGC

作用方式

刺激剂

作用机制

sGC刺激剂(可溶性鸟苷酸环化酶复合体刺激剂)

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-

原研机构

Cyclerion Therapeutics

在研机构

Cyclerion Therapeutics

非在研机构-

最高研发阶段临床前

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C24H22F2N6O3

InChIKeyOREKZCCNTFVURN-SZNDQCEHSA-N

CAS号1628730-55-1

关联

100 项与 CYR715 相关的临床结果

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100 项与 CYR715 相关的转化医学

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100 项与 CYR715 相关的专利（医药）

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1

项与 CYR715 相关的文献（医药）

2021-05-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Discovery of CYR715: A novel carboxylic acid-containing soluble guanylate cyclase stimulator

4区 · 医学

Article

作者: Perl, Nicholas R ; Germano, Peter ; Zimmer, Daniel P ; Moore, Joel ; Jung, Joon ; Barden, Timothy C ; Rennie, Glen R ; Bernier, Sylvie G ; Deming, Renee ; Lee, Thomas W-H ; Mermerian, Ara ; Hudson, Colleen ; Jia, Lei ; Im, G-Yoon J ; Renhowe, Paul A ; Iyengar, Rajesh R ; Carvalho, Andrew ; Nakai, Takashi ; Kim, Elise ; Tobin, Jenny

Soluble guanylate cyclase (sGC) is a clinically validated therapeutic target in the treatment of pulmonary hypertension. Modulators of sGC have the potential to treat diseases that are affected by dysregulation of the NO-sGC-cGMP signal transduction pathway. This letter describes the SAR efforts that led to the discovery of CYR715, a novel carboxylic acid-containing sGC stimulator, with an improved metabolic profile relative to our previously described stimulator, IWP-051. CYR715 addressed potential idiosyncratic drug toxicity (IDT) liabilities associated with the formation of reactive, migrating acyl glucuronides (AG) found in related carboxylic acid-containing analogs and demonstrated high oral bioavailability in rat and dose-dependent hemodynamic pharmacology in normotensive Sprague-Dawley rats.

100 项与 CYR715 相关的药物交易

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