Delving into the Latest Updates on Fazamorexant with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

OX1R x OX2R

Action

antagonists

Mechanism

OX1R antagonists(Orexin receptor type 1 antagonists), OX2R antagonists(Orexin receptor type 2 antagonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Sleep Initiation and Maintenance DisordersCentral Nervous System Diseases

Inactive Indication-

Originator Organization

Jiangsu Yangtze River Pharmaceutical Group Co., Ltd.

Active Organization

Jiangsu COAST PHARMACEUTICAL CO., LTD

Shanghai Haiyan Pharmaceutical Technology Co Ltd

Inactive Organization-

Drug Highest PhaseNDA/BLA

First Approval Date-

RegulationSpecial Review Project (China)

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Structure/Sequence

Molecular FormulaC25H25FN4O2

InChIKeyPMJPLAGTPPVSRL-JLMWRMLUSA-N

CAS Registry1808918-69-5

Primary Objective：
1) To evaluate the pharmacodynamic interaction between YZJ-1139 tablets and Escitalopram oxalate tablets in healthy subjects; 2) To evaluate the pharmacokinetic interaction between YZJ-1139 tablets and Escitalopram oxalate tablets in healthy subjects; To observe the safety of YZJ-1139 tablets taken together with Escitalopram oxalate tablets.

Start Date31 Aug 2024

Sponsor / Collaborator

Shanghai Haiyan Pharmaceutical Technology Co Ltd

CTR20242936

/ Active, not recruitingPhase 1

YZJ-1139片与草酸艾司西酞普兰片的药物相互作用研究

[Translation] Study on drug interaction between YZJ-1139 tablets and escitalopram oxalate tablets

主要目的：评价健康受试者口服YZJ-1139片与草酸艾司西酞普兰片的药效学相互作用；次要目的：评价健康受试者口服YZJ-1139片与草酸艾司西酞普兰片的药代动力学相互作用；观察YZJ-1139片与草酸艾司西酞普兰片同服的安全性。

[Translation]

Primary objective: To evaluate the pharmacodynamic interaction between YZJ-1139 tablets and escitalopram oxalate tablets in healthy subjects; Secondary objective: To evaluate the pharmacokinetic interaction between YZJ-1139 tablets and escitalopram oxalate tablets in healthy subjects; To observe the safety of taking YZJ-1139 tablets and escitalopram oxalate tablets together.

Start Date26 Aug 2024

Sponsor / Collaborator

Yangtze River Pharmacy Group Jiangsu Haici Biological Pharmacy

[+2]

NCT06671470

/ Active, not recruitingPhase 1

Drug Interaction Study of YZJ-1139 Tablets With Ticagrelor Tablets

Primary Objective :
To evaluate the effect of ticagrelor tablets on the pharmacokinetic characteristics of YZJ-1139 in healthy subjects;
Secondary Objective:
To evaluate the safety of ticagrelor tablets in combination with YZJ-1139 tablets in healthy subjects.

Start Date22 Aug 2024

Sponsor / Collaborator

Shanghai Haiyan Pharmaceutical Technology Co Ltd

100 Clinical Results associated with Fazamorexant

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100 Translational Medicine associated with Fazamorexant

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100 Patents (Medical) associated with Fazamorexant

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3

Literatures (Medical) associated with Fazamorexant

05 Aug 2022·ACS Catalysis

Asymmetric Synthesis of Nortropanes via Rh-Catalyzed Allylic Arylation

Article

Author: Zhang, Yan ; Christensen, Kirsten E. ; Goetzke, F. Wieland ; Fletcher, Stephen P.

Tropane derivatives are extensively used in medicine, but catalytic asymmetric methods for their synthesis are underexplored. Here, we report Rh-catalyzed asymmetric Suzuki-Miyaura-type cross-coupling reactions between a racemic N-Boc-nortropane-derived allylic chloride and (hetero)aryl boronic esters. The reaction proceeds via an unexpected kinetic resolution, and the resolved enantiopure allyl chloride can undergo highly enantiospecific reactions with N-, O-, and S-containing nucleophiles. The method was applied in a highly stereoselective formal synthesis of YZJ-1139(1), a potential insomnia treatment that recently completed Phase II clinical trials. Our report represents an asymmetric catalytic method for the synthesis of YZJ-1139(1) and related compounds.

18 Feb 2022·Organic Process Research & Development

Development of a Scalable Route with Efficient Stereoisomer Control to YZJ-1139, an Orexin Receptor Antagonist

Author: Fei, Zonglei ; Gao, Qingfu ; Ma, Youhong ; Zhang, Xingsong ; Jia, Miao ; Feng, Yixiao ; Wu, Bo ; Cai, Xunzhi ; Zhang, Jiangbo ; Zeng, Zhenya

An effort toward the synthesis and process development of the orexin receptor antagonist YZJ-1139 I was described in this article.I contains the azabicyclic nortropane structure with three chiral centers.By the original process, highly pure intermediates or API could be obtained by chromatog. with a relatively low yield.To remove the undesirable stereoisomers as early as possible, an N-(R)-α-phenethyl was synthesized by the Robinson-Schopf reaction and easily purified as its hydrochloride.The single crystal X-ray study was used to confirm the stereo configuration of I.The protecting group could be easily removed by transfer hydrogenation, resulting in an enantiomerically pure intermediate as its D-tartrate.The overall yield for preparing I was significantly increased, and this cost-efficient process might be promising in future com. productions.

ChemRxiv

Asymmetric synthesis of nortropanes via Rh-catalysed allylic arylation

Author: Zhang, Yan ; Christensen, Kirsten E. ; Goetzke, F. Wieland ; Fletcher, Stephen P.

Tropane derivatives are extensively used in medicine, but catalytic asym. methods for their synthesis are underexplored.Here we report Rh-catalyzed asym. Suzuki-Miyaura type cross-coupling reactions between a racemic N-Boc-nortropane-derived allylic chloride and (hetero-)aryl-boronic esters.The reaction proceeds via an unexpected kinetic resolution, and the resolved enantiopure allyl chloride can undergo highly enantiospecific reactions with N, O, and S-containing nucleophiles.The method was applied in a highly stereoselective formal synthesis of YZJ-1139(1) (I), a potential insomnia treatment that recently completed Phase II clin. trials.Our report represents the first synthesis of YZJ-1139(1) and related compounds using asym. catalysis.

100 Deals associated with Fazamorexant

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Sleep Initiation and Maintenance Disorders	NDA/BLA	China	Jiangsu COAST PHARMACEUTICAL CO., LTD	22 Jan 2025
Central Nervous System Diseases	Phase 1	China	Shanghai Haiyan Pharmaceutical Technology Co Ltd	31 Aug 2024