盐酸美哌隆(Melperone Hydrochloride) - 药物靶点：DRDs_在研适应症：精神分裂症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Bunil、Melperon、Melperone

+ [10]

靶点

DRDs

作用方式

拮抗剂

作用机制

DRDs拮抗剂(多巴胺受体家族拮抗剂)

治疗领域

神经系统疾病

在研适应症

精神分裂症

非在研适应症-

原研机构-

在研机构-

非在研机构-

权益机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C16H23ClFNO

InChIKeyMQHYXXIJLKFQGY-UHFFFAOYSA-N

CAS号1622-79-3

关联

3

项与盐酸美哌隆相关的临床试验

EUCTR2007-002874-75-IT

/ Not yet recruitingN/A

Safety and effectivness of Open- Label Melperone in the treatment of Patients with Psycosis Associated with Parkinson's Disease'' - OV-1005

开始日期2007-09-10

申办/合作机构

OVATION Pharmaceuticals, Inc.

EUCTR2007-000307-15-IT

/ Not yet recruitingN/A

Safety and Efficacy of Melperone in the Treatment of Patients with Psychosis Associated with Parkinson's Disease.

开始日期2007-04-24

申办/合作机构

OVATION Pharmaceuticals, Inc.

NCT00125138

/ Completed临床2期

Safety and Efficacy of Melperone in the Treatment of Patients With Psychosis Associated With Parkinson's Disease

The purpose of this study is to evaluate the safety and efficacy of three target doses of melperone compared to placebo in the treatment of psychosis associated with Parkinson's disease. Subjects will be enrolled at approximately 20 investigational sites in the United States (U.S.) and 15 Ex-US sites. The maximum study duration will be 10 weeks. Subjects will have the option of continuing in an open-label extension study.

开始日期2005-07-01

申办/合作机构

Lundbeck LLC

100 项与盐酸美哌隆相关的临床结果

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100 项与盐酸美哌隆相关的转化医学

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100 项与盐酸美哌隆相关的专利（医药）

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427

项与盐酸美哌隆相关的文献（医药）

2025-03-17·CHEMICAL RESEARCH IN TOXICOLOGY

(Q)SAR Approaches to Predict the Extent of Nitrosation in Pharmaceutical Compounds

Article

作者: Chakravarti, Suman ; Saiakhov, Roustem ; Reiss, Krystle

Since their discovery as impurities in numerous pharmaceuticals beginning in 2018, there has been a strong push to predict and prevent the formation of mutagenic nitrosamines. Several experimental methods, particularly the Nitrosation Assay Procedure, have been developed to predict a molecule's susceptibility to nitrosation. Here, we have compiled the results of hundreds of these experiments from the literature to construct two structure-activity relationship models: a statistical model and an expert rule-based model. The statistical model has been built with graph neural networks and was trained on a dataset of 207 nitrogen-containing molecules. This model makes a binary call for each nitrogen center, predicting if it is likely to be nitrosated or not. Conversely, the rule-based model labels each possible nitrosamine product as one of four categories, ranging from "unlikely" to "very likely". It makes this determination based on 15 rules, which cover 12 deactivating (inhibit nitrosation) and 3 activating (favor nitrosation) features that have been drawn from the literature. Both models perform remarkably well, with accuracies of ∼80%. The rule-based model is generally biased toward favoring nitrosation while the statistical model is more likely to classify an amine as un-nitrosatable due to the makeup of the dataset. Using the models together can balance these biases and further improve the reliability of both.

2024-12-13·ORGANIC LETTERS

Photocatalyzed Selective α-Monoalkylation of Aqueous Acetaldehyde for Synthesis of α,β-Unsubstituted 1,4-Ketoaldehydes

Article

作者: Su, Yin ; Fu, Liang ; Zhao, Quansheng ; Liu, Xinyu

The direct utilization of aqueous acetaldehyde as an industrially important aqueous chemical has been hampered in organic synthesis due to the high reactivity of acetaldehyde. Herein, the first metal-free photocatalyzed selective α-monoalkylation of commercially available and safe to handle aqueous acetaldehyde (40 wt %) with inexpensive α-chloro/bromoacetophenones has been developed using 0.5 mol % 4CzIPN as an organic photosensitizer, which provides easy access to high-added-value α,β-unsubstituted 1,4-ketoaldehydes. The reaction features a broad substrate scope, high functional group tolerance, gram-scalability, operational simplicity, and mild reaction conditions. Moreover, the synthetic applications are demonstrated by directly using aqueous solutions of acetaldehyde as synthetically useful a C2 synthon for the modular and expeditious synthesis of various biologically active γ-aminoketones through the reductive amination of the α,β-unsubstituted 1,4-ketoaldehyde products with cyclic secondary amines, as well as the concise gram-scale total synthesis of pentabromo- and pentachloropseudilins.

2024-09-01·PSYCHIATRY RESEARCH

Dopamine D2 receptor antagonism of antipsychotics and the risk of death due to choking

Article

作者: Correll, Christoph U ; Lähteenvuo, Markku ; Luykx, Jurjen J ; Lieslehto, Johannes ; Hasan, Alkomiet ; Tanskanen, Antti ; Manu, Peter ; Taipale, Heidi ; Tiihonen, Jari

The risk of fatal choking for people with schizophrenia and associations with antipsychotic medication are largely unknown. Therefore, we calculated the choking-related standardized mortality ratio for schizophrenia relative to the general population (SMR_choking). We also computed adjusted hazard ratios (aHR) of choking-related mortality for antipsychotics in a nationwide cohort of patients with schizophrenia (N = 59,916). SMR_choking was 20.5 (95 % confidence interval (CI)=17.1-23.9). The aHR was 1.74 (95 %CI=1.19-2.55) for strong dopamine 2-antagonists. For other antipsychotics, CIs included 1. Importantly, aHRs were particularly high for high dose categories of strong dopamine D2 receptor (D2R) antagonists. In conclusion, a schizophrenia diagnosis is associated with a 20-fold risk of death due to choking. This risk is elevated during use of strong D2R antagonist antipsychotics, particularly when prescribed in high dosages.

1

项与盐酸美哌隆相关的新闻（医药）

2025-01-30

·SYNAPSE

EQL Pharma AB completes the asset purchase of a product portfolio from Medilink A/S

EQL Pharma AB (publ) (the “Company” or “EQL”) has today completed the previously announced acquisition of a product portfolio (the “Product portfolio”) from Medilink A/S, through its wholly owned subsidiary EQL Pharma Int AB. All conditions for the completion of the transaction have been satisfied. As per previous press release the acquisition price amounts to DKK 120 million (corresponding to approximately SEK 185 million). The Product portfolio consists of Buronil (melperone), Folimet (folic acid/B-vitamin), Hydromed (hydrochlorothiazide) and Marplan (isocarboxazid). The Product Portfolio consists of well-established products, limiting the need for additional promotional activities. From a strategic perspective the products fit very well with EQL’s existing portfolio of niche generics. The products have a stable financial development and are expected to be accretive to EQL’s sales and margins, in addition to increasing the Company’s geographical presence. As of 31 October 2024, the Product Portfolio generates annual revenues of approximately SEK 51 million and gross profit of SEK 36 million, corresponding to a gross margin of 71% annually. If the Product Portfolio had been part of EQL during the twelve-month period that ended on 31st of December 2024, EQL assesses that the combined turnover and adjusted EBITDA would have amounted to approximately SEK 389 million and SEK 94 million, respectively. CEO Axel Schörling: “We are very happy for having completed the portfolio acquisition from Medilink and are looking forward to integrating the products to our portfolio in collaboration with the sellers, our new suppliers and distributors. In parallel with the integration of the portfolio the EQL team will start working with the different upsides and synergies that have been identified during the due diligence process. The full integration of the portfolio is expected to take approximately one year but the sales will be included in EQLs accounts already from 1st of February, from when we also will start receiving the cash flow from the acquisition” This disclosure contains information that EQL Pharma is obliged to make public pursuant to the EU Market Abuse Regulation (EU nr 596/2014) and the Swedish Securities Markets Act (2007:528). The information was submitted for publication, through the agency of the contact person, on 31-01-2025 12:35 CET.

并购生物类似药

100 项与盐酸美哌隆相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D08172	盐酸美哌隆	N05AD03	DB09224

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
精神分裂症	-	-	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00125138 (CTgov)	临床2期	精神障碍 \| 帕金森病	90	Melperone HCl (Melperone HCl - 20 mg)	構窪繭網憲鬱夢廠淵鹹(願窪構範簾憲淵觸膚網) = 範獵選艱蓋積鬱淵鹽簾鹽憲廠廠廠夢鹽鹽艱糧 (餘築夢鹽願鬱鏇願糧鑰, 4.4) 更多	-	2011-06-17
				Melperone HCl (Melperone HCl - 40 mg)	構窪繭網憲鬱夢廠淵鹹(願窪構範簾憲淵觸膚網) = 艱範艱築餘網廠夢顧夢鹽憲廠廠廠夢鹽鹽艱糧 (餘築夢鹽願鬱鏇願糧鑰, 4.0) 更多