AZD-2716(AZD-2716) - 药物靶点：sPLA2_在研适应症：冠心病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

sPLA2(AstraZeneca)

靶点

sPLA2

作用机制

sPLA2抑制剂(分泌型磷脂酶A2抑制剂)

治疗领域

心血管疾病

在研适应症

冠心病

非在研适应症-

原研机构

AstraZeneca AB

在研机构

AstraZeneca AB

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

分子式C24H23NO3

InChIKeyPXRCDPVYRPKGGI-MRXNPFEDSA-N

CAS号1845753-81-2

关联

100 项与 AZD-2716 相关的临床结果

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100 项与 AZD-2716 相关的转化医学

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100 项与 AZD-2716 相关的专利（医药）

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2

项与 AZD-2716 相关的文献（医药）

2022-01-03·Angewandte Chemie International Edition1区 · 化学

Enantioselective Synthesis of Chiral Carboxylic Acids from Alkynes and Formic Acid by Nickel‐Catalyzed Cascade Reactions: Facile Synthesis of Profens

1区 · 化学

Article

作者: Yang, Peng ; Ma, Yu ; Zhou, Jianrong Steve ; Zhang, Li ; Tang, Bo ; Yue, Jieyu ; Fu, Kaiyue ; Yang, Guang ; Sun, Yaxin

AbstractWe report a stereoselective conversion of terminal alkynes to α‐chiral carboxylic acids using a nickel‐catalyzed domino hydrocarboxylation‐transfer hydrogenation reaction. A simple nickel/BenzP* catalyst displayed high activity in both steps of regioselective hydrocarboxylation of alkynes and subsequent asymmetric transfer hydrogenation. The reaction was successfully applied in enantioselective preparation of three nonsteroidal anti‐inflammatory profens (>90 % ees) and the chiral fragment of AZD2716.

2016-10-13·ACS Medicinal Chemistry Letters3区 · 医学

Discovery of AZD2716: A Novel Secreted Phospholipase A₂ (sPLA₂) Inhibitor for the Treatment of Coronary Artery Disease

3区 · 医学

Article

作者: Dekker, Niek ; Pettersen, Daniel ; Larsson, Lars-Olof ; Nordberg, Peter ; Karlsson, Ulla ; Dahlström, Mikael ; Hurt-Camejo, Eva ; Knerr, Laurent ; Selmi, Nidhal ; Rosengren, Birgitta ; Sandmark, Jenny ; Castaldo, Marie ; Starke, Ingemar ; Giordanetto, Fabrizio

Expedited structure-based optimization of the initial fragment hit 1 led to the design of (R)-7 (AZD2716) a novel, potent secreted phospholipase A₂ (sPLA₂) inhibitor with excellent preclinical pharmacokinetic properties across species, clear in vivo efficacy, and minimized safety risk. Based on accumulated profiling data, (R)-7 was selected as a clinical candidate for the treatment of coronary artery disease.

100 项与 AZD-2716 相关的药物交易

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