Delving into the Latest Updates on Phenchlobenpyrrone with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

GlyR x VDCCs

Action

antagonists, blockers

Mechanism

GlyR antagonists(Glycine receptor antagonists), VDCCs blockers(Voltage-gated calcium channel blockers)

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Alzheimer Disease

Originator Organization

Yunnan Province Shipurui Biology Engineering Co. Ltd.

Active Organization-

Inactive Organization

Chinese Academy of Sciences

Yunnan Province Shipurui Biology Engineering Co. Ltd.

License Organization-

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC17H16ClNO

InChIKeyVKZXZQUFDSNROH-VTLFJGNJSA-N

CAS Registry215036-81-0

Observe the speed and extent of the test drug reaching the cerebrospinal fluid, as well as the correlation between the cerebrospinal fluid drug concentration and the blood drug concentration. At the same time, evaluate the safety and effectiveness of Fenclotone tablets in the treatment of mild and moderate Alzheimer's disease and preliminarily judge the consistency between the blood drug concentration and the overall efficacy.

Start Date03 Feb 2015

Sponsor / Collaborator

Chinese Academy of Sciences

[+2]

CTR20130335

/ CompletedPhase 2

评价芬克罗酮片治疗轻中度阿尔茨海默病安全性、有效性的单中心、随机、双盲、安慰剂对照Ⅱa期临床试验

[Translation] A single-center, randomized, double-blind, placebo-controlled phase IIa clinical trial to evaluate the safety and efficacy of fenclofenone tablets in the treatment of mild to moderate Alzheimer's disease

初步评价芬克罗酮片治疗轻、中度阿尔茨海默病的安全性、有效性和初步判断血药浓度与总体疗效的吻合度。

[Translation]

To preliminarily evaluate the safety and efficacy of Fenclotone Tablets in the treatment of mild and moderate Alzheimer's disease and to preliminarily determine the consistency between blood drug concentration and overall efficacy.

Start Date21 Jan 2014

Sponsor / Collaborator

Chinese Academy of Sciences

[+2]

100 Clinical Results associated with Phenchlobenpyrrone

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100 Translational Medicine associated with Phenchlobenpyrrone

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100 Patents (Medical) associated with Phenchlobenpyrrone

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4

Literatures (Medical) associated with Phenchlobenpyrrone

01 Apr 2022·Bioorganic & Medicinal ChemistryQ3 · MEDICINE

Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells

Q3 · MEDICINE

Article

Author: Yang, Lishou ; Li, Qiji ; Yang, Xiaosheng ; Yang, Juan ; Wang, Li ; Yang, Yan ; Cao, Jiafu ; Yang, Qian ; Wang, Enhua ; Liao, Xiu

A range of novel 1-phenyl-benzopyrrolizidin-3-one derivatives were synthesized and evaluated for neuroprotective effects against N-methyl-ᴅ-aspartate (NMDA)-induced injury in PC12 cells. Interestingly, derivatives that 1-phenyl moiety bearing electron-donating group, especially benzyloxy, and the trans-forms exhibited better protective activity against NMDA-induced neurotoxicity. Compound 11 m demonstrated the best neuroprotective potency and shown a dose-dependent prevention. The increased intracellular calcium (Ca²⁺) influx caused by NMDA in PC12 cells was reversed in the case of compound 11 m pretreatment at 15 μM. These results suggested that the synthesized 1-phenyl-benzopyrrolizidin-3-one derivatives exerted neuroprotective effect on NMDA-induced excitotoxicity in PC12 cells associated with inhibition of Ca²⁺ overload and can be further optimized for the development of neuroprotective agents.

01 Nov 2021·Tetrahedron

DBU-catalyzed Michael addition of bulky glycine imine to α,β-unsaturated isoxazoles and pyrazolamides

Author: Hu, Xiao-Mu ; Bai, Ya-Jun ; Zhang, Sheng-Yong ; Zheng, Xiao-Hui ; Ping-AnWang ; Bai, Yu-Jun

An efficient DBU-catalyzed syn-Michael addition of β-substituted α,β-unsaturated isoxazoles or pyrazolamides with a bulky glycine imine to provide Michael adducts in good to excellent yields and diastereoselectivities in THF by using LiBr as an additive was developed.Several types of substrates with high pK_a values like nitroalkanes and N-methylindolin-2-one were also used as Michael donor in the above-mentioned additionA practical preparation of a key intermediate for Phenchlobenpyrrone was realized based on this DBU-assisted Michael reaction.These Michael adducts can be converted into various bioactive mols. through several simple steps.

01 Aug 2018·Natural Products and BioprospectingQ4 · CHEMISTRY

An Explorer of Chemical Biology of Plant Natural Products in Southwest China, Xiaojiang Hao

Q4 · CHEMISTRY

Review

Author: Chen, Duo-Zhi ; Shen, Yue-Mao

Xiaojiang Hao, who obtained Master Degree from Kunming Institute of Botany (KIB), Chinese Academy of Sciences (CAS) in 1985, and Doctor in Pharmacy degree in Pharmacy from Institute for Chemical Research, Kyoto University, in 1990, was born in Chongqing in July, 1951. In 1991, he returned to KIB, CAS, as an Associate professor and served as the chair of the Department of Phytochemistry. In 1994, he was promoted to a full professor at the current institute. He served as the Deputy Director of KIB and the Director of Open Laboratory of Phytochemistry from 1995 to 1997, and the Director of KIB from 1997 to 2005. Professor Hao has published more than 450 peer-reviewed SCI papers, which have been cited over 6000 times. He has obtained one PCT patent and 23 patents in China. Due to his tremendous efforts, one candidate drug, phenchlobenpyrrone, has entered the Phase II clinical trail for the treatment of Alzheimer's disease. Moreover, he won the First Prize of Natural Sciences in Yunnan Province for three times, and Ho Leung Ho Lee Fund Science and Technology Innovation Award in 2017.

100 Deals associated with Phenchlobenpyrrone

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 2	China	Chinese Academy of Sciences	21 Jan 2014
Alzheimer Disease	Phase 2	China	Yunnan Province Shipurui Biology Engineering Co. Ltd.	21 Jan 2014