RGH-560(RGH-560) - 药物靶点：CHRNA7_在研适应症：遗忘_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

CHRNA7

作用机制

α7 receptor调节剂(神经性乙酰胆碱受体蛋白α-7亚基调节剂)

治疗领域

神经系统疾病

在研适应症

遗忘

非在研适应症-

原研机构

Gedeon Richter Romania SA

在研机构

Gedeon Richter Romania SA

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C22H20FN3O3

InChIKeyLXOXUGXUUINWLS-UHFFFAOYSA-N

CAS号2408799-43-7

关联

100 项与 RGH-560 相关的临床结果

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100 项与 RGH-560 相关的转化医学

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100 项与 RGH-560 相关的专利（医药）

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1

项与 RGH-560 相关的文献（医药）

2023-12-14·Journal of Medicinal Chemistry1区 · 医学

Optimization of Novel α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulators and the Discovery of a Preclinical Development Candidate Molecule (RGH-560)

1区 · 医学

Article

作者: Balázs, Ottilia ; Makó, Attila ; Némethy, Zsolt ; Greiner, István ; Vastag, Mónika ; Laszy, Judit ; Éles, János ; Fodor, László ; Vágó, István ; Thán, Márta ; Tapolcsányi, Pál ; Kolok, Sándor ; Ledneczki, István ; Visegrády, András ; Ilkei, Viktor ; Molnár, Katalin Dudásné ; Szigetvári, Áron ; Bata, Imre ; Lendvai, Balázs ; Krámos, Balázs ; Lévay, György

During optimization of a previously identified lead compound, attempts were made to optimize the reactive indole structural element, the suboptimal metabolic stability, as well as the low kinetic solubility. It was concluded that the indole was important for in vitro activity. With the aim of further improvements, more thorough modifications were also carried out. As a result, a new chemotype (the azetidinespirochromone family) was identified, which proved to be 1 order of magnitude less lipophilic retaining the same high level of in vitro potency as the lead series itself, however, with improved metabolic stability and kinetic solubility. Compound 53 showed the most balanced physicochemical and pharmacological profile with significant in vivo efficacy in the scopolamine-induced amnesia test. Based on these promising results, cognitive enhancement through the positive modulation of α7 nAChRs appears to be a viable approach. Compound 53 was selected to be a preclinical development candidate (as RGH-560).

100 项与 RGH-560 相关的药物交易

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