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主要目的：评估单次给药后TPN729MA片原形及其代谢产物TPN-M3在不同程度肝功能不全及健康男性受试者中的药代动力学特征。次要目的：（1）评估单次给药后TPN729MA片在不同程度肝功能不全及健康男性受试者中的安全性。（2）评估单次给药后TPN729MA片原形及其代谢产物TPN-M3在不同程度肝功能不全及健康男性受试中的血浆蛋白结合率。

开始日期2024-08-05

申办/合作机构

山东特珐曼药业有限公司

[+3]

CTR20242204 / Completed临床1期

评价TPN729MA片在肾功能不全和健康男性受试者中的药代动力学特征及安全性的单剂量、开放、平行对照的I期临床试验

主要目的：评估单次给药后TPN729MA片原形及其代谢产物TPN-M3在不同程度肾功能不全及健康男性受试者中的药代动力学特征。次要目的： 1）评估单次给药后TPN729MA片在不同程度肾功能不全及健康男性受试者中的安全性； 2）评估单次给药后TPN729MA片原形及其代谢产物TPN-M3在不同程度肾功能不全及健康男性受试中的血浆蛋白结合率。

开始日期2024-07-08

申办/合作机构

山东特珐曼药业有限公司

[+3]

CTR20242200 / Completed临床1期

评价TPN729MA片在老年男性受试者中的药代动力学特征及安全性的单剂量、开放的I期临床试验

主要目的：评估单次给药后TPN729MA片原形及其代谢产物TPN-M3在老年男性受试者（年龄≥65岁）中的药代动力学（PK）特征。次要目的： 1）评估单次给药后TPN729MA片在老年男性受试者（年龄≥65岁）中的安全性。 2）评估单次给药后TPN729MA片原形及其代谢产物TPN-M3在老年男性受试者（年龄≥65岁）中的血浆蛋白结合率。

开始日期2024-06-28

申办/合作机构

山东特珐曼药业有限公司

[+3]

100 项与上海特化医药科技有限公司相关的临床结果

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0 项与上海特化医药科技有限公司相关的专利（医药）

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13

项与上海特化医药科技有限公司相关的文献（医药）

2024-05-17·The Journal of Organic Chemistry

An Alternative Approach to Synthesize Sildenafil via Improved Copper-Catalyzed Cyclization

Article

作者: Gong, Xudong ; Yang, Feipu ; Zhu, Fuqiang ; Shen, Jingshan ; Bonku, Emmanuel Mintah ; Qin, Hongjian ; Odilov, Abdullajon

A facile synthetic pathway for sildenafil has been developed. This approach is characterized by a ligand-free Ullmann-type copper-catalyzed coupling reaction to construct sildenafil and its derivative, pyrrazolo[4,3-d]pyrimidin-7-one ring, with yields of 79% and 82%, respectively, in a convergent fashion by connecting key building blocks halo-pyrazole moiety 16c with 2-ethoxybenzamidine and 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]benzamidine in a one-pot reaction. Thus, this approach circumvents the need to use nitric/sulfuric acid for nitration, a costly Pd-catalyst for reduction, and coupling agents encountered in the reported processes.

2023-11-17·Organic Process Research & Development

Optimized Synthesis of the Key Intermediate of Telmisartan via the Cyclization of 2-Bromoarylamine with n-Butyronitrile

作者: Odilov, Abdullajon ; Zhu, Fuqiang ; Liu, Yongjian ; Shen, Jingshan ; Mintah Bonku, Emmanuel ; Qin, Hongjian ; Aisa, Haji A. ; Wu, Mingjun

Herein, a facile and sustainable synthesis method of bis-benzimidazole which is the key intermediate of telmisartan is described using com. available 3-methyl-4-nitrobenzoic acid and 2-chloronitrobenzene as starting materials.Aniline was produced in 98% isolated yield using a one-pot reduction/cyclization procedure.Subsequently, 2-bromoarylamine was prepared in 96% isolated yield via the bromination of aniline with bromine.Finally, bis-benzimidazole synthesis was completed via the cyclization of 2-bromoarylamine with n-butyronitrile; the isolated yield of bis-benzimidazole was 95% and its high-performance liquid chromatog. purity based on area was 99.8%.Each reaction step was optimized to achieve high yields and the optimal conditions were identified in the final step via the design of experimentsThe developed process provides an alternative sustainable route for synthesizing bis-benzimidazole; this route avoid undesired nitration using nitric/sulfuric acid and cyclization in polyphosphoric acid, which are used in the current methods.

2021-01-01·Neuroscience Letters4区 · 医学

Chronic administration of synthetic cannabidiol induces antidepressant effects involving modulation of serotonin and noradrenaline levels in the hippocampus

4区 · 医学

Article

作者: Zhang, Jian ; He, Yang ; Wu, Song ; Gong, Xudong ; Abame, Melkamu Alemu ; Xie, Zhifei ; Shen, Jingshan ; Wu, Chunhui

Cannabidiol (CBD) is a non-psychotomimetic compound derived from Cannabis sativa. Preclinical and clinical studies have shown therapeutic potential of CBD in a variety of disorders. Despite several research efforts on CBD, its antidepressant activity has been poorly investigated and the exact mechanism of action remains unclear. Thus, this study aimed to further explore the mechanism of CBD after chronic administration (7 days). First, the dose level of CBD that is enough to produce antidepressant effects after chronic administration was explored. Second, the changes in key proteins and neurotransmitters through such methods as real-time polymerase chain reaction (RT-PCR), western blotting, and high-performance liquid chromatography-electrochemical detection (HPLC-ECD) were critically studied. Furthermore, correlation between behavioral phenotypes with protein and neurotransmitters was established and the possible mechanism was herein postulated. The results showed that only the high dose CBD 100 mg/kg chronic administration induced antidepressant-like effects in mice subjected to forced swim test. Chronic CBD 100 mg/kg administration resulted in significant increases in serotonin (5-HT) and noradrenaline (NA) levels in the hippocampus (HPC). Similarly, the chronic administration of CBD 30 mg/kg and CBD 100 mg/kg significantly decreased nuclear factor kappa B (NF-κB) expression in the HPC. Moreover, none of the treatments were observed to induce locomotor effects. Thus, we concluded that chronic administration of CBD (100 mg/kg) induced antidepressant-like effects by increasing 5-HT and NA levels in the HPC. These results shed new light on further discovery of the antidepressant effect of CBD.

100 项与上海特化医药科技有限公司相关的药物交易

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100 项与上海特化医药科技有限公司相关的转化医学

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药物(靶点)	适应症	全球最高研发状态

TPN729MA ( PDE5A )	勃起功能障碍更多	临床3期
斯美瑞非 ( PDE5A )	肺动脉高压更多	无进展
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