Delving into the Latest Updates on Jiangsu Carefree Pharmaceutical Co., Ltd. with Synapse

概览

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

RORγt(视黄酸相关孤儿受体γt)	1

关联

1

项与 Jiangsu Carefree Pharmaceutical Co., Ltd. 相关的药物

b12(Jiangsu Carefree Pharmaceutical)

靶点

RORγt

作用机制

RORγt反向激动剂

在研机构

Jiangsu Carefree Pharmaceutical Co., Ltd. [+1]

原研机构

东南大学 [+1]

在研适应症

炎症

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

1

项与 Jiangsu Carefree Pharmaceutical Co., Ltd. 相关的临床试验

NCT01637675 / Unknown status临床2/3期IIT

Clinical Study of Effects of Sodium Tanshinone IIA Sulfonate on Pulmonary Hypertension

Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine,the dried root of Salvia miltiorrhiza Bunge known as Danshen. Danshen has been known for the function of improving body functions such as activating blood circulation and removing blood stasis according to the theory of traditional Chinese medicine. Danshen and its various formula products including STS have been long-time widely used in oriental countries, especially China to treat various inflammatory and cardiovascular diseases for its pharmacological actions, including vasodilatation, anticoagulation, anti-inflammation, and free radical scavenging,with negligible adverse effects observed.
The investigator's objective is to evaluate whether STS exhibits beneficial effects on pulmonary hypertension. This is a randomized, controlled, multicentre clinical trial study. 90 patients with pulmonary hypertension will be enrolled in this study.

开始日期2013-05-01

申办/合作机构

广州医科大学第一附属医院

[+10]

100 项与 Jiangsu Carefree Pharmaceutical Co., Ltd. 相关的临床结果

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0 项与 Jiangsu Carefree Pharmaceutical Co., Ltd. 相关的专利（医药）

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3

项与 Jiangsu Carefree Pharmaceutical Co., Ltd. 相关的文献（医药）

2022-02-01·European Journal of Medicinal Chemistry1区 · 医学

Discovery of 2H-chromone-4-one based sulfonamide derivatives as potent retinoic acid receptor-related orphan receptor γt inverse agonists

1区 · 医学

Article

作者: Chen, Lei ; Kang, Yang-Yang ; Su, Mei ; Huang, Ri-Zhen ; Zhao, Shi-Feng ; Li, Yan ; Assani, Israa ; Wu, Xian-Zhi ; Sun, Bo ; Jin, Qiu ; Lv, Shen-Min ; Liao, Zhi-Xin ; Wang, Jia-Wei ; Wang, De-Zhong ; Wang, Mu-Xuan ; Wang, Chun-Gu

Retinoic acid receptor related orphan receptor γt (RORγt), identified as the essential functional regulator of IL-17 producing Th17 cells, is an attractive drug target for treating autoimmune diseases. Starting from the reported GSK2981278 (Phase II), we structurally modified and synthesized a series of 2H-chromone-4-one based sulfonamide derivatives as novel RORγt inverse agonists, which significantly improved their human metabolic stabilities while maintaining a potent RORγt inverse agonist profile. Efforts in reducing the lipophilicity and improving the LLE values led to the discovery of c9, which demonstrated potent RORγt inverse agonistic activity and consistent metabolic stability. During in vivo studies, oral administration of compound c9 exhibited a robust and dose-dependent inhibition of IL-17A cytokine expression and significantly lessened the skin inflammatory symptoms in the mouse imiquimod-induced skin inflammation model. Docking analysis of the binding mode revealed that c9 can suitably occupy the active pocket, and the introduction of the morpholine pyridine group can interact with Leu396, His479, and Cys393. Thus, compound c9 was selected as a preclinical compound for treating Th17-driven autoimmune diseases.

2022-02-01·Bioorganic Chemistry2区 · 化学

Discovery of N-(2-benzyl-4-oxochroman-7-yl)-2-(5-(ethylsulfonyl) pyridin-2-yl) acetamide (b12) as a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist

2区 · 化学

Article

作者: Liao, Zhi-Xin ; Li, Yan ; Wang, Mu-Xuan ; Chen, Lei ; Wang, Chun-Gu ; Assani, Israa ; Wang, Jia-Wei ; Zhao, Shi-Feng ; Su, Mei ; Sun, Bo ; Lv, Shen-Min ; Jin, Qiu

The nuclear receptor retinoic acid receptor-related orphan receptor γ (RORγ, NR1F3, or RORc) exists in two isoforms, with one isoform (RORγ or RORc1) widely expressed in a variety of tissues, and the expression of the second isoform (RORγt or RORc2) restricted to the thymus and cells of the immune system. RORγt is a key regulator of the development and functions of T-helper 17 (Th17) cells. Clinical proof-of-concept (PoC) with small molecule inverse agonists of RORγt has been achieved with VTP-43742 (Phase II) for the treatment of psoriasis, and pre-clinical PoC for this mechanism has also been established for the treatment of autoimmune diseases. A series of aryl sulfonyl derivatives as novel RORγt inverse agonists were designed and synthesized based on VTP-43742. We conducted structural modifications that improved the activity profile. In pharmacodynamic (PD) studies, oral administration of compound b12 showed robust and dose-dependent inhibition of IL-6 and IL-17A cytokine expression. The ability of compound b12 to reduce the levels of IL-6 and IL-17A in vivo after oral dosing in mice, and a corresponding reduction in skin inflammation further supports the potential of small molecule RORγt modulation as a therapeutic target for the treatment of inflammatory diseases.

Guangzhou Huagong

Optimum extraction technology of egg white lysozyme and determination of enzyme activity

作者: Wu, Xu-ya ; You, Qing-hong ; Yin, Xiu-lian

Using egg white as material, enzyme activity as target, the salting-out method and ion exchange extraction methods were studied by orthogonal experiment design.The optimal process conditions for extraction lysozyme were adding 5% sodium chloride, crystallization temperature 4 degree, and crystallization time for 4 days.The best conditions of ion exchange were egg white resin ratio 5:1, pH 7.0, and stirred adsorption time for 4 h.The output and enzyme activity of enzyme derived from ion exchange was higher than that from the salting-out method.

100 项与 Jiangsu Carefree Pharmaceutical Co., Ltd. 相关的药物交易

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100 项与 Jiangsu Carefree Pharmaceutical Co., Ltd. 相关的转化医学

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