K-161(K-161) - 在研适应症：干眼综合征_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点-

作用方式-

作用机制-

治疗领域

眼部疾病

在研适应症

干眼综合征

非在研适应症-

原研机构

Kowa Co., Ltd.

在研机构

Kowa Research Institute, Inc.

非在研机构-

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C11H13ClO3

InChIKeyIPYOCBWUDXJNGI-UHFFFAOYSA-N

CAS号1206-38-8

关联

2

项与 K-161 相关的临床试验

NCT05403827

/ Completed临床3期

A Phase 3, Prospective, Double-masked, Randomized, Multi-center, Vehicle-controlled, Parallel-group, 12-week Administration and 40-week Extension Study Confirming the Efficacy and Safety of K-161 Ophthalmic Solution for the Treatment of Moderate to Severe Dry Eye Disease

The purpose of this study is to assess the efficacy and safety of K-161 ophthalmic solution for the treatment of moderate to severe dry eye disease.

开始日期2022-07-03

申办/合作机构

Kowa Research Institute, Inc.

NCT04084483

/ Completed临床2期

A Study Assessing the Safety, Efficacy, and Optimum Dosage of K-161 in Subjects With Moderate to Severe Dry Eye Disease

The objective of the study is to assess the safety, efficacy, optimum dosage, and dosing regimen of K-161 in adult subjects with moderate to severe dry eye disease.

开始日期2019-08-04

申办/合作机构

Kowa Research Institute, Inc.

100 项与 K-161 相关的临床结果

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100 项与 K-161 相关的转化医学

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100 项与 K-161 相关的专利（医药）

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16

项与 K-161 相关的文献（医药）

2020-03-01·Journal of Cell Science2区 · 生物学

Pan-SHIP1/2 inhibitors promote microglia effector functions essential for CNS homeostasis

2区 · 生物学

Article

作者: Viernes, Dennis R. ; Adhikari, Arijit A. ; Choi, Lydia B. ; Fernandes, Sandra ; Kerr, William G. ; De Jong, Ebbing P. ; Dormann, Shawn M. ; Pedicone, Chiara ; Chisholm, John D. ; Dungan, Otto M.

ABSTRACTWe show here that both SHIP1 (Inpp5d) and its paralog SHIP2 (Inppl1) are expressed at protein level in microglia. To examine whether targeting of SHIP paralogs might influence microglial physiology and function, we tested the capacity of SHIP1-selective, SHIP2-selective and pan-SHIP1/2 inhibitors for their ability to impact on microglia proliferation, lysosomal compartment size and phagocytic function. We find that highly potent pan-SHIP1/2 inhibitors can significantly increase lysosomal compartment size, and phagocytosis of dead neurons and amyloid beta (Aβ)1−42 by microglia in vitro. We show that one of the more-potent and water-soluble pan-SHIP1/2 inhibitors, K161, can penetrate the blood-brain barrier. Consistent with this, K161 increases the capacity of CNS-resident microglia to phagocytose Aβ and apoptotic neurons following systemic administration. These findings provide the first demonstration that small molecule modulation of microglia function in vivo is feasible, and suggest that dual inhibition of the SHIP1 and 2 paralogs can provide a novel means to enhance basal microglial homeostatic functions for therapeutic purposes in Alzheimer's disease and, possibly, other types of dementia where increased microglial function could be beneficial.

2017-08-01·Journal of Porous Materials

Synthesis of Hf/SBA-15 Lewis acid catalyst for converting glycerol to value-added chemicals

作者: A. Pandurangan ; V. Udayakumar

Hf/SBA-15 catalyst containing highly ordered two-dimensional hexagonal mesoporous silica with a large surface area is prepared in a facile one-step sol-gel method with hafnia content ranging from 2.5 to 10%.The synthesized catalyst is characterized by X-ray diffraction anal., N₂ adsorption-desorption isotherm, scanning electron microscope and transmission electron microscope.The oxidation state and Lewis acidic properties of 10% Hf/SBA-15 are investigated by diffuse reflectance UV-Vis technique, XPS and pyridine-adsorbed FT-IR anal.The catalytic activity of Hf/SBA-15 is employed in the acetalization of glycerol with acetophenone and benzaldehyde, order of activity of the catalyst is 10 > 5 > 2.5% Hf/SBA-15.The 10% Hf/SBA-15 is given 43 and 21% selectivity of six-membered (1,3-dioxane) and five-membered (1,3-dioxolane) acetals.Hence, this catalyst is further exploited in the acetalization of glycerol with substituted acetophenone and benzaldehyde.The catalyst could be recycled for five times without a significant decrease in activity.

1995-01-01·European Journal of Medicinal Chemistry

Synthesis and antifungal activity of novel (1-aryl-2-heterocyclyl)ethylideneaminooxymethyl-substituted dioxolanes

作者: T Kimny ; M Flammang ; H Baji ; F Gasquez ; PL Compagnon ; A Delcourt

A novel series of (1-aryl-2-heterocyclyl)ethylideneaminooxymethyl-substituted dioxolanes I (R¹ = Me, ClC₆H₄, 2,4-Cl₂C₆H₃, R² = H, imidazol-1-yl, 1,2,4-triazol-1-yl, X¹, X² = H, Cl, Ar = imidazol-1-yl, 1,2,4-triazol-1-yl) were prepared by condensation of dioxolanylmethyl tosylates II with 1-(hydroxyimino)-1-aryl-2-heterocyclylethanes III.I have effective in vitro antifungal activity against the pathogenic fungi Candida albicans, Aspergillus flavus and Fusarium solani with MIC (min. inhibitory concentration) values of 10 μg·mL^-1 and 5 μg·mL^-1.

100 项与 K-161 相关的药物交易

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