BMS-986308(BMS-986308) - 药物靶点：KCNJ1_在研适应症：心脏衰竭_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

KCNJ1

作用机制

KCNJ1抑制剂(potassium inwardly rectifying channel subfamily J member 1 inhibitors)

治疗领域

心血管疾病

在研适应症

心脏衰竭

非在研适应症-

原研机构

Bristol Myers Squibb Co.

在研机构

Bristol Myers Squibb Co.

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-

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结构

分子式C24H25N7O2

InChIKeyNRCYDDLRPFXMNA-NYHFZMIOSA-N

CAS号2254333-97-4

关联

1

项与 BMS-986308 相关的临床试验

NCT04763226 / Completed临床1期

A Randomized, Double-Blinded, Placebo-Controlled, Single Ascending Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of BMS-986308 in Healthy Participants

The purpose of this study is to evaluate the safety, tolerability, drug levels, and drug effects of BMS-986308 compared to placebo in healthy participants.

开始日期2021-04-14

申办/合作机构

Bristol Myers Squibb Co.

100 项与 BMS-986308 相关的临床结果

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100 项与 BMS-986308 相关的转化医学

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100 项与 BMS-986308 相关的专利（医药）

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1

项与 BMS-986308 相关的文献（医药）

2024-06-13·Journal of Medicinal Chemistry

Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure

Article

作者: Govindrajan, Arun ; Wexler, Ruth R ; Kamble, Shyam ; Bora, Rajesh Onkardas ; Gulia, Jyoti ; Gunaga, Prashantha ; Rajugowda, Nagendra ; Sivaprasad Lvj, Sankara ; Lentz, Kimberley A ; Kole, Prashant ; Bhide, Rajeev ; Levesque, Paul C ; Priestley, E Scott ; Soleman, Sharif I ; Mathur, Arvind ; Akuthota, Nagarjuna ; Chacko, Silvi ; Godesi, Sreenivasulu ; Govindrajulu, Kavitha ; Sivaraman, Aneesh ; Rao, Prasanna ; Thatipamula, Rajendra Prasad ; Gordon, David A ; Yadav, Navnath ; Panda, Manoranjan ; Richter, Jeremy M ; Gupta, Anuradha ; Ramarao, Manjunath ; Sridhar, Srikanth ; Kaspady, Mahammed ; Dokania, Manoj

Recent literature reports highlight the importance of the renal outer medullary potassium (ROMK) channel in renal sodium and potassium homeostasis and emphasize the potential impact that ROMK inhibitors could have as a novel mechanism diuretic in heart failure patients. A series of piperazine-based ROMK inhibitors were designed and optimized to achieve excellent ROMK potency, hERG selectivity, and ADME properties, which led to the identification of compound 28 (BMS-986308). BMS-986308 demonstrated efficacy in the volume-loaded rat diuresis model as well as promising in vitro and in vivo profiles and was therefore advanced to clinical development.

100 项与 BMS-986308 相关的药物交易

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