Delving into the Latest Updates on 上海特化医药科技有限公司 with Synapse

主要目的： 1)定量分析健康男性受试者单次口服[14C]TPN729MA后排泄物中的总放射性，获得人体放射性的累计排泄率和主要排泄途径； 2)考察健康男性受试者单次口服[14C]TPN729MA后全血和血浆中的分配情况和血浆中总放射性的药代动力学特征； 3)评价健康男性受试者单次口服[14C]TPN729MA后血浆、尿液、粪便中的主要代谢产物，确定主要生物转化途径和主要代谢产物（接近或>10%总放射性AUC）。次要目的： 1)采用已验证的液相色谱串联质谱联用法（LC-MS/MS）定量分析血浆中TPN729MA和主要代谢产物（如适用），获得相应药动学参数； 2)评价健康男性受试者单次口服[14C]TPN729MA后的安全性。

开始日期2024-08-22

申办/合作机构

山东特珐曼药业有限公司

[+3]

CTR20242709

/ Completed临床1期

评价TPN729MA片在肝功能损伤受试者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期临床研究

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]

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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16

项与上海特化医药科技有限公司相关的文献（医药）

2025-01-01·Synlett

An Improved Iodine-Catalyzed Aromatization Reaction and Its Application in the Synthesis of a Key Intermediate of Cannabidiol

作者: Qin, Hongjian ; Abduahadi, Safomuddin ; Odilov, Abdullajon ; Aisa, Haji Akber ; Shen, Jingshan ; Zhu, Fuqiang ; Mintah Bonku, Emmanuel

AbstractIn this study, the development of an improved process for the synthesis of a key cannabidiol intermediate, methyl olivetolate, is described. The process involves an improvement of the iodine-catalyzed aromatization of cyclohexanone using potassium persulfate as an oxidant. This approach enabled for the efficient synthesis of methyl olivetolate with a 90% yield and 99.84% HPLC purity on a 5 kg scale. Additionally, a total of 19 cyclohexanone substrates afforded higher yields (71–92%) of m-diphenol compounds compared to the established methods.

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 ; Liu, Yongjian ; Zhu, Fuqiang ; 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.

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
TPN102 ( GABAA receptor )	癫痫更多	无进展