A Phase 2a, Multi Centre, Double-blind, Randomized, Placebo-controlled, Parallel-group Study to Assess the Effect of 12 Weeks Treatment With Oral PXS-4728A on Microglia Activation, as Measured by Positron Emission Tomography, in Participants With Isolated Rapid Eye Movement Sleep Behavior Disorder

This study is to investigate the safety and efficacy of PXS-4728A as an intervention therapy in participants with iRBD. This study will be conducted in participants aged 50 to 80 years of age and will investigate a single dose level.

开始日期2023-11-08

申办/合作机构

Syntara Ltd.

NCT03979820

/ Terminated临床1期

A Phase I Parallel Group Study in Healthy Subjects to Evaluate the Effect of Multiple Oral Doses of BI 1467335 and Phenelzine as Positive Control on Blood Pressure Response to Oral Tyramine (Double-blind, Randomised, Placebo-controlled Design for BI 1467335 Treatment Groups, Open Label for Phenelzine)

The main objective of the study is investigate the effect of escalating doses of oral tyramine on systolic blood pressure (SBP) at baseline and following an oral treatment with BI 1467335 up to 39 days at a low or high dose once daily compared to placebo and phenelzine (Nardil®) as positive control.

开始日期2019-07-31

申办/合作机构

Boehringer Ingelheim GmbH

100 项与 VAP-1 x MAO-B 相关的临床结果

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100 项与 VAP-1 x MAO-B 相关的转化医学

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0 项与 VAP-1 x MAO-B 相关的专利（医药）

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项与 VAP-1 x MAO-B 相关的文献（医药）

2025-01-01·Histology and histopathology

Expression of amine oxidase-related proteins in breast phyllodes tumor.

Article

作者: Kim, Hye Min ; Koo, Ja Seung

BACGROUNDBreast phyllodes tumors (BPTs) are difficult to differentiate from other tumor types. In-depth research is needed due to the insufficient description of the amine oxidase protein family, particularly in BPTs.OBJECTIVEThis study investigated the expression and clinical implications of amine oxidase-related proteins in BPTs.METHODSTissue microarrays were constructed (n=181), and amine oxidase-related proteins of monoamine oxidase (MAO) A, MAOB, lysyl oxidase (LOX), and primary-amine oxidase 3 (AOC3) were assessed using immunohistochemical staining. Staining patterns of these proteins were compared and analyzed with clinicopathologic parameters.RESULTSIn all, 149, 27, and 5 cases were classified as benign, borderline, and malignant, respectively. A higher grade of BPT was associated with increased MAOB (P<0.001), LOX (P=0.035), and AOC3 (P<0.001) expression. BPT cases with tumor recurrence and distant metastasis had higher proportions of MAOB positivity in stromal components (P=0.002 and 0.018, respectively). During follow-up, there was a significant association between MAOB positivity in the stromal component and shorter disease-free survival (DFS) (P=0.001) as well as overall survival (P=0.003). Moreover, MAOB positivity emerged as an independent factor for shorter DFS (hazard ratio: 4.253, 95% confidence interval: 1.034-17.49, P=0.045).CONCLUSIONSHigher MAOB, LOX, and AOC3 expression were observed in higher-grade BPTs, and MAOB expression was identified as a significant prognostic factor.

2023-07-04·Biomedicines

Expression of Amine Oxidase Proteins in Adrenal Cortical Neoplasm and Pheochromocytoma.

Article

作者: Koo, Ja Seung ; Kim, Eun Kyung

We delved into the expression of amine oxidase family proteins and their potential significance in adrenal gland neoplasm. Tissue microarrays were prepared for 132 cases of adrenal cortical neoplasm (ACN) consisting of 115 cases of adrenal cortical adenoma (ACA), 17 cases of adrenal cortical carcinoma (ACC), and 163 cases of pheochromocytoma (PCC). Immunohistochemical stainings for MAOA, MAOB, LOX, and AOC3 were performed to evaluate the H-scores and compare them with clinicopathological parameters. The H-scores of MAOA (T; p = 0.005) and MAOB (T; p = 0.006) in tumor cells (T) were high in ACN, whereas LOX (T, S; p < 0.001) in tumor and stromal cells (S) and AOC3 (T; p < 0.001) were higher in PCC. In stromal cells, MAOA (S; p < 0.001) and AOC3 (S; p = 0.010) were more expressed in ACA than in ACC. MAOB (S) in PCC showed higher H-scores when the grading of adrenal pheochromocytoma and paraganglioma (GAPP) score was 3 or higher (p = 0.027). In the univariate analysis, low MAOA expression in stromal cells of ACN was associated with shorter overall survival (p = 0.008). In conclusion, monoamine oxidase proteins revealed differences in expression between ACN and PCC and also between benign and malignant cells.

2022-10-01·Bioorganic & Medicinal Chemistry Letters

Combining monoamine oxidase B and semicarbazide-sensitive amine oxidase enzyme inhibition to address inflammatory disease

Article

作者: Buson, Alberto ; Deodhar, Mandar ; Yow, Tin ; Robertson, Alan D ; Turner, Craig I ; Zhou, Wenbin ; Jarolimek, Wolfgang ; Foot, Jonathan S ; Findlay, Alison D

The discovery of a dual MAO-B/SSAO inhibitor PXS-5131 is reported. The compound offers a compact and rigid three-dimensional structure with superior selectivity over MAO-A. Potency and selectivity are linked to both the double bond geometry and stereochemistry of the allylamine moiety, highlighting the importance of optimal set up of these features in the class of amine oxidase inhibitors. PXS-5131 possesses an attractive preclinical pharmacokinetic profile and has anti-inflammatory properties in models of acute inflammation and neuroinflammation.

项与 VAP-1 x MAO-B 相关的新闻（医药）

2023-05-19

·CPHI制药在线

研发 | 东阳光药业2016年以来重点专利布局分析

关注并星标CPHI制药在线“产品未动，专利先行。”是药品专利布局中的重要原则之一，对药企重点专利布局情况分析，有助于了解其研发动向与潜在的在研产品。通过调研发现，近年来东阳光药业的新分子实体化合物专利与晶型专利均有较高的申请量，故笔者针对东阳光药业2016年以来重点专利布局开展分析。因申请量较大，本文提高了用于分析的专利纳入标准，如下所示：①自主研发或受让获得权益的化合物（包括小分子与大分子）的外周专利，所述外周专利包括但不限于：已知化合物的新形式（包括晶型、盐、溶剂合物）专利、制备方法专利、组合物专利、用途专利、质量研究专利等；②至少在欧洲、美国与日本一地提交同族专利申请的化合物专利。一、东阳光药业2016年以来申请的重点专利1.1外周专利注：*未在欧洲、美国或日本提交同族专利申请，其余化合物专利均在欧洲、美国与日本中的至少一地提交同族专利申请。#以“A”结尾的号码为公开号，表示该专利申请截至2022年11月10日尚未获得授权；其余为公告号，表示该专利已获授权。1.2重点化合物专利小结2016年至今，东阳光药业在5-HT1F受体激动剂（偏头痛）、5-HT6受体拮抗剂（焦虑、抑郁等）、CRTH2受体拮抗剂（过敏性疾病）、FXR调控剂（NASH）、HBV抑制剂、HCV抑制剂、HIF-抑制剂（贫血）、MAO-B抑制剂（帕金森）、SGLT抑制剂（糖尿病）、SSRI/5-HT1A受体拮抗剂（抑郁症）、美金刚长效衍生物（阿尔茨海默氏病）、食欲素受体拮抗剂（睡眠障碍）、受体酪氨酸激酶抑制剂（肿瘤）、纤维化抑制剂与盐皮质激素受体拮抗剂（醛甾酮过多症）领域均有外周专利申请，提示相关的化合物可能即将或已经进入非临床或临床研究，无论是靶点还是治疗领域均呈现出高度的多元化特征。除了外周专利中涉及的化合物类别，2016年至今，东阳光药业的重点化合物专利还涉及A2A受体拮抗剂（帕金森综合征）、ACC抑制剂（NASH等）、FGF21多肽（1型糖尿病）、GnRH拮抗剂（性激素依赖性疾病）、RET抑制剂（癌症）、sGC刺激剂（心力衰竭等）、SSAO/VAP-1拮抗剂（炎症性疾病）、含免疫球蛋白Fc片断的融合蛋白（2型糖尿病）、抗TrkA抗体（疼痛）、流感病毒复制抑制剂、嵌合抗原受体（肿瘤），提示相关靶点或治疗领域可能是东阳光药业近期重点的研发方向。注：同族专利数量只是专利质量评价的一个方面，本文也发现部分有外周专利申请的化合物的化合物专利未在海外进行申请。专利申请至公开的时间滞后性，导致无法判定近三年内仅在中国申请的专利是否一定未在海外申请，因此专利监测与分析将是一个动态而持续的过程。由于作者精力与能力的限制，也会导致一定的遗漏甚至错误，还望广大读者朋友不吝指正、补充。【企业推荐】智药研习社近期课程报名来源：药智网声明：本文仅代表作者观点，并不代表制药在线立场。本网站内容仅出于传递更多信息之目的。如需转载，请务必注明文章来源和作者。投稿邮箱：Kelly.Xiao@imsinoexpo.com▼更多制药资讯，请关注CPHI制药在线▼点击阅读原文，进入智药研习社~

专利无效专利到期

2023-05-16

·药智网

干货！东阳光药业2016年以来重点专利布局分析

“产品未动，专利先行。”是药品专利布局中的重要原则之一，对药企重点专利布局情况分析，有助于了解其研发动向与潜在的在研产品。通过调研发现，近年来东阳光药业的新分子实体化合物专利与晶型专利均有较高的申请量，故笔者针对东阳光药业2016年以来重点专利布局开展分析。因申请量较大，本文提高了用于分析的专利纳入标准，如下所示：①自主研发或受让获得权益的化合物（包括小分子与大分子）的外周专利，所述外周专利包括但不限于：已知化合物的新形式（包括晶型、盐、溶剂合物）专利、制备方法专利、组合物专利、用途专利、质量研究专利等；②至少在欧洲、美国与日本一地提交同族专利申请的化合物专利。一、东阳光药业2016年以来申请的重点专利1.1外周专利注：*未在欧洲、美国或日本提交同族专利申请，其余化合物专利均在欧洲、美国与日本中的至少一地提交同族专利申请。#以“A”结尾的号码为公开号，表示该专利申请截至2022年11月10日尚未获得授权；其余为公告号，表示该专利已获授权。1.2重点化合物专利小结2016年至今，东阳光药业在5-HT1F受体激动剂（偏头痛）、5-HT6受体拮抗剂（焦虑、抑郁等）、CRTH2受体拮抗剂（过敏性疾病）、FXR调控剂（NASH）、HBV抑制剂、HCV抑制剂、HIF-抑制剂（贫血）、MAO-B抑制剂（帕金森）、SGLT抑制剂（糖尿病）、SSRI/5-HT1A受体拮抗剂（抑郁症）、美金刚长效衍生物（阿尔茨海默氏病）、食欲素受体拮抗剂（睡眠障碍）、受体酪氨酸激酶抑制剂（肿瘤）、纤维化抑制剂与盐皮质激素受体拮抗剂（醛甾酮过多症）领域均有外周专利申请，提示相关的化合物可能即将或已经进入非临床或临床研究，无论是靶点还是治疗领域均呈现出高度的多元化特征。除了外周专利中涉及的化合物类别，2016年至今，东阳光药业的重点化合物专利还涉及A2A受体拮抗剂（帕金森综合征）、ACC抑制剂（NASH等）、FGF21多肽（1型糖尿病）、GnRH拮抗剂（性激素依赖性疾病）、RET抑制剂（癌症）、sGC刺激剂（心力衰竭等）、SSAO/VAP-1拮抗剂（炎症性疾病）、含免疫球蛋白Fc片断的融合蛋白（2型糖尿病）、抗TrkA抗体（疼痛）、流感病毒复制抑制剂、嵌合抗原受体（肿瘤），提示相关靶点或治疗领域可能是东阳光药业近期重点的研发方向。注：同族专利数量只是专利质量评价的一个方面，本文也发现部分有外周专利申请的化合物的化合物专利未在海外进行申请。专利申请至公开的时间滞后性，导致无法判定近三年内仅在中国申请的专利是否一定未在海外申请，因此专利监测与分析将是一个动态而持续的过程。由于作者精力与能力的限制，也会导致一定的遗漏甚至错误，还望广大读者朋友不吝指正、补充。声明：本内容为作者独立观点，不代表药智网立场。如需转载，请务必注明文章作者和来源。对本文有异议或投诉，请联系maxuelian@yaozh.com。责任编辑 | 八角转载开白 | 马老师 18996384680（同微信）商务合作 | 张武龙 13368443108（同微信）阅读原文，是昨天最受欢迎的文章哦

专利无效专利到期