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1. 发明专利

CA2969839A1 HETEROCYCLIC COMPOUNDS AS BIOGENIC AMINE TRANSPORT MODULATORS 未知
公开(公告)号：CA2969839A1
公开(公告)日：2016-06-09
申请号：CA2969839
申请日：2015-12-04
申请人： ANANTHAN SUBRAMANIAM , ROTHMAN RICHARD B
发明人： ANANTHAN SUBRAMANIAM , ROTHMAN RICHARD B
IPC分类号： A61K31/517 , A61P25/00 , C07D401/12
摘要： The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

2. 发明专利

CA2969856A1 NOVEL QUINAZOLINES AS BIOGENIC AMINE TRANSPORT MODULATORS 未知
公开(公告)号：CA2969856A1
公开(公告)日：2016-06-09
申请号：CA2969856
申请日：2015-12-04
申请人： ANANTHAN SUBRAMANIAM , ROTHMAN RICHARD B
发明人： ANANTHAN SUBRAMANIAM , ROTHMAN RICHARD B
IPC分类号： A61K31/517 , A61P25/00 , C07D401/12
摘要： The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

3. 发明公开

EP3226868A1 NOVEL QUINAZOLINES AS BIOGENIC AMINE TRANSPORT MODULATORS 审中-公开
标题翻译：新型喹唑啉作为生物胺运输调节剂
公开(公告)号：EP3226868A1
公开(公告)日：2017-10-11
申请号：EP15865587.8
申请日：2015-12-04
申请人： Ananthan, Subramaniam , Rothman, Richard B.
发明人： Ananthan, Subramaniam , Rothman, Richard B.
IPC分类号： A61K31/517 , C07D401/12 , A61P25/00
CPC分类号： C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：本公开涉及抑制生物胺转运体，多巴胺转运蛋白（DAT），血清素转运蛋白（SERT）和去甲肾上腺素转运蛋白（NET）的胺再摄取功能的稠合双环杂环的某些胺衍生物。本公开的化合物是具有全部或部分最大功效的多巴胺（DA），血清素（5-羟色胺，5-HT）和去甲肾上腺素（NE）的重摄取的有效抑制剂。在抑制全部三种生物胺的再摄取方面具有部分最大功效的化合物在本文中称为部分三重摄取抑制剂（PTRI）。本公开化合物可用于治疗抑郁症，疼痛和药物滥用以及药物滥用和对诸如可卡因，甲基苯丙胺，尼古丁和酒精的物质成瘾的复发。该摘要旨在作为用于在特定领域中进行搜索的目的的扫描工具，并且不旨在限制本发明。

4. 发明公开

EP3226867A4 HETEROCYCLIC COMPOUNDS AS BIOGENIC AMINE TRANSPORT MODULATORS 审中-公开
公开(公告)号：EP3226867A4
公开(公告)日：2018-05-09
申请号：EP15864354
申请日：2015-12-04
申请人： ANANTHAN SUBRAMANIAM , ROTHMAN RICHARD B
发明人： ANANTHAN SUBRAMANIAM , ROTHMAN RICHARD B
IPC分类号： A61K31/517 , A61P25/00 , C07D401/12
CPC分类号： C07D487/04 , C07D239/95 , C07D401/04 , C07D401/14 , C07D403/04 , C07D409/04 , C07D471/04 , C07D473/00
摘要： The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

5. 发明公开

EP3226867A1 HETEROCYCLIC COMPOUNDS AS BIOGENIC AMINE TRANSPORT MODULATORS 审中-公开
标题翻译：作为生物胺运输调节剂的杂环化合物
公开(公告)号：EP3226867A1
公开(公告)日：2017-10-11
申请号：EP15864354.4
申请日：2015-12-04
申请人： Ananthan, Subramaniam , Rothman, Richard B.
发明人： Ananthan, Subramaniam , Rothman, Richard B.
IPC分类号： A61K31/517 , C07D401/12 , A61P25/00
CPC分类号： C07D487/04 , C07D239/95 , C07D401/04 , C07D401/14 , C07D403/04 , C07D409/04 , C07D471/04 , C07D473/00
摘要： The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：本公开涉及抑制生物胺转运体，多巴胺转运蛋白（DAT），血清素转运蛋白（SERT）和去甲肾上腺素转运蛋白（NET）的胺再摄取功能的稠合双环杂环的某些胺衍生物。本公开的化合物是具有全部或部分最大功效的多巴胺（DA），血清素（5-羟色胺，5-HT）和去甲肾上腺素（NE）的重摄取的有效抑制剂。在抑制全部三种生物胺的再摄取方面具有部分最大功效的化合物在本文中称为部分三重摄取抑制剂（PTRI）。本公开化合物可用于治疗抑郁症，疼痛和药物滥用以及药物滥用和对诸如可卡因，甲基苯丙胺，尼古丁和酒精的物质成瘾的复发。该摘要旨在作为用于在特定领域中进行搜索的目的的扫描工具，并且不旨在限制本发明。

6. 发明申请

WO2009023299A2 ANTI-ANGIOGENIC AGENTS AND METHODS OF USE 审中-公开
公开(公告)号：WO2009023299A2
公开(公告)日：2009-02-19
申请号：PCT/US2008060186
申请日：2008-04-14
申请人： SOUTHERN RES INST , QU ZHICAN , ROY ANSHU MITTAL , ANANTHAN SUBRAMANIAM
发明人： QU ZHICAN , ROY ANSHU MITTAL , ANANTHAN SUBRAMANIAM
IPC分类号： A61K31/542
CPC分类号： A61K31/445 , A61K31/095 , A61K31/343 , A61K31/519 , A61K31/5415 , A61K31/55
摘要： The present disclosure relates generally to treating or preventing diseases associated with angiogenesis by administering to a patient certain compounds found to inhibit or substantially reduce angiogenesis. Compounds employed according to the present disclosure exhibit good anti-angiogenic activity as well as demonstrate a prophylactic effect for preventing and substantially reducing angiogenesis. Examples of such compounds include Ritanserin, Amiodarone, Terfenadinc, Perphenazine, Bithionol, and Clomipramine.

7. 发明申请

WO2016090299A1 NOVEL QUINAZOLINES AS BIOGENIC AMINE TRANSPORT MODULATORS 审中-公开
标题翻译：作为生物胺运输调节剂的新型五氮杂环己烷
公开(公告)号：WO2016090299A1
公开(公告)日：2016-06-09
申请号：PCT/US2015/064079
申请日：2015-12-04
申请人： ANANTHAN, Subramaniam , ROTHMAN, Richard, B.
发明人： ANANTHAN, Subramaniam , ROTHMAN, Richard, B.
IPC分类号： A61K31/517 , C07D401/12 , A61P25/00
CPC分类号： C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：本公开涉及抑制生物胺转运蛋白，多巴胺转运蛋白（DAT），血清素转运蛋白（SERT）和去甲肾上腺素转运蛋白（NET））的胺再摄取功能的稠合双环杂环的某些胺衍生物。本公开的化合物是具有完全或部分最大功效的多巴胺（DA），5-羟色胺（5-羟色胺，5-HT）和去甲肾上腺素（NE））再摄取的有效抑制剂。在抑制所有三种生物胺的再摄取中具有部分最大功效的化合物在本文中称为部分三重摄取抑制剂（PTRI）。本公开的化合物可用于治疗抑郁症，疼痛和药物滥用以及物质滥用和对诸如可卡因，甲基苯丙胺，尼古丁和酒精的物质的成瘾的复发。该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

8. 发明申请

WO2011031974A9 ACRIDINE ANALOGS IN THE TREATMENT OF GLIOMAS 审中-公开
标题翻译：吡啶类似物治疗糖尿病
公开(公告)号：WO2011031974A9
公开(公告)日：2011-05-05
申请号：PCT/US2010048435
申请日：2010-09-10
申请人： SOUTHERN RES INST , GRIMALDI MAURIZIO , ANANTHAN SUBRAMANIAM
发明人： GRIMALDI MAURIZIO , ANANTHAN SUBRAMANIAM
IPC分类号： A61K31/4706 , A61K31/473 , A61P35/00 , A61P35/04
CPC分类号： A61K31/4706 , A61K31/473
摘要： Disclosed are methods and compositions for treating gliomas that involve quinacrine and other acridine analogs.
摘要翻译：公开了用于治疗涉及奎纳克胺和其他吖啶类似物的胶质瘤的方法和组合物。

9. 发明申请

WO2011047129A1 TREATMENT OF NEURODEGENERATIVE DISEASES, CAUSATION OF MEMORY ENHANCEMENT, AND ASSAY FOR SCREENING COMPOUNDS FOR SUCH 审中-公开
标题翻译：治疗神经细胞增生性疾病，记忆增强的原因及其筛选化合物的测定
公开(公告)号：WO2011047129A1
公开(公告)日：2011-04-21
申请号：PCT/US2010/052624
申请日：2010-10-14
申请人： SOUTHERN RESEARCH INSTITUTE , GRIMALDI, Maurizio , HOBRATH, Judith, Varady , ANANTHAN, Subramaniam , MADDRY, Joseph, A.
发明人： GRIMALDI, Maurizio , HOBRATH, Judith, Varady , ANANTHAN, Subramaniam , MADDRY, Joseph, A.
IPC分类号： A01N57/00 , A61K31/675
CPC分类号： A61K31/5377 , A61K31/136 , A61K31/36 , A61K31/426 , A61K31/427 , A61K31/444 , A61K31/675
摘要： Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, and Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.
摘要翻译：描述了通过施用某些杂环和芳族化合物增强记忆和/或学习和预防神经变性的方法。这些方法对于治疗患有神经变性疾病的患者特别有用，例如（但不限于）阿尔茨海默病，帕金森氏症和Lou Gehrig氏病（ALS）疾病或记忆障碍或学习障碍。还提供了使用荧光素酶报告基因评估NF-kB基因上调的基于神经元的基于人细胞的测定法，其筛选用于增强记忆或学习的方法中的化合物。

10. 发明申请

WO2009023299A3 ANTI-ANGIOGENIC AGENTS AND METHODS OF USE 审中-公开
标题翻译：抗血管生成药物和使用方法
公开(公告)号：WO2009023299A3
公开(公告)日：2009-05-22
申请号：PCT/US2008060186
申请日：2008-04-14
申请人： SOUTHERN RES INST , QU ZHICAN , ROY ANSHU MITTAL , ANANTHAN SUBRAMANIAM
发明人： QU ZHICAN , ROY ANSHU MITTAL , ANANTHAN SUBRAMANIAM
IPC分类号： A01N43/54 , C07D239/42 , C07D471/04
CPC分类号： A61K31/445 , A61K31/095 , A61K31/343 , A61K31/519 , A61K31/5415 , A61K31/55
摘要： The present disclosure relates generally to treating or preventing diseases associated with angiogenesis by administering to a patient certain compounds found to inhibit or substantially reduce angiogenesis. Compounds employed according to the present disclosure exhibit good anti-angiogenic activity as well as demonstrate a prophylactic effect for preventing and substantially reducing angiogenesis. Examples of such compounds include Ritanserin, Amiodarone, Terfenadinc, Perphenazine, Bithionol, and Clomipramine.
摘要翻译：本发明通常涉及通过向患者施用某些发现抑制或基本上减少血管生成的化合物来治疗或预防与血管生成相关的疾病。根据本公开使用的化合物表现出良好的抗血管生成活性以及表现出预防和显着减少血管生成的预防效果。这样的化合物的实例包括利坦色林，胺碘酮，特芬芬丹，奋乃静，比硫洛尔和氯米帕明。

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