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1. 发明授权

US5821249A Anhydroecogonine compounds and their use as anticholinergic agents 失效
标题翻译：脱氢嘌呤类化合物及其作为抗胆碱剂的用途
公开(公告)号：US5821249A
公开(公告)日：1998-10-13
申请号：US706105
申请日：1996-08-30
申请人： Ronald W. Wood , Hassan A. N. El-Fawal , John F. Graefe , Lung C. Chen , Jalil Shojaie
发明人： Ronald W. Wood , Hassan A. N. El-Fawal , John F. Graefe , Lung C. Chen , Jalil Shojaie
IPC分类号： C07D451/02 , C07D213/20 , A61K31/44
CPC分类号： C07D451/02
摘要： Methylecgonidine (MEG; anhydroecgonine methylester), is produced when cocaine base ("crack") is heated. MEG alone and in combination with cocaine was tested for action on isolated tracheal rings stimulated to contact with acetylcholine. At micromolar concentrations, cocaine sensitized tracheal rings, increasing both the potency and efficacy of acetylcholine-induced contraction. Surprisingly, MEG, at nanomolar concentrations and above, non-competitively and irreversibly antagonized acetylcholine-induced contraction independently of the actions of cocaine. MEG also displayed antihistaminic activity. Therefore, MEG and anticholinergically active derivatives or analogues thereof are useful in the prevention or treatment of a disease or disorder treatable by an antimuscarinic anticholinergic agent, an anti-histaminic agent or a spasmolytic agent, in particular bronchoconstriction in a number of pulmonary diseases such as asthma.
摘要翻译：当可卡因碱（“裂纹”）被加热时，产生甲基氢醌（MEG;脱氢莽草啶甲酯）。测试单独的和与可卡因组合的MEG对被刺激与乙酰胆碱接触的分离的气管环的作用。在微摩尔浓度下，可卡因致敏气管环，增加了乙酰胆碱诱导的收缩的效力和功效。令人惊讶的是，纳米摩尔浓度以上的MEG与可卡因的作用无关，不可逆地和不可逆地拮抗乙酰胆碱诱导的收缩。 MEG还显示抗组胺活性。因此，MEG和抗胆碱能活性衍生物或其类似物可用于预防或治疗由抗毒蕈碱性抗胆碱能药，抗组胺药或解痉药治疗的疾病或病症，特别是在多种肺部疾病中的支气管收缩哮喘。

2. 发明申请

US20100168198A1 Mitochondria-targeted antioxidant prodrugs and methods of use 失效
标题翻译：线粒体靶向抗氧化剂前药及其使用方法
公开(公告)号：US20100168198A1
公开(公告)日：2010-07-01
申请号：US12694337
申请日：2010-01-27
申请人： Marion W. Anders , James L. Robotham , Shey-Shing Sheu , Paul Spencer Brookes , Jalil Shojaie , Leif Olson , Richard L. Parton
发明人： Marion W. Anders , James L. Robotham , Shey-Shing Sheu , Paul Spencer Brookes , Jalil Shojaie , Leif Olson , Richard L. Parton
IPC分类号： A61K31/4164 , C07C59/90 , C07C63/04 , C07D233/54 , C07C229/04 , C07C229/28 , C07F11/00 , C07D339/08 , A61K31/195 , A61K31/19 , A61K31/28 , A61K31/385 , A61K31/192 , A61P39/06
CPC分类号： C07D233/54 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/28 , A61K31/385 , A61K31/4164 , C07C323/52 , C07D233/84 , C07D271/12 , C07D311/72 , C07D339/06 , C07D339/08 , C07D471/04 , C07F9/65324
摘要： The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation.
摘要翻译：本发明是线粒体靶向的抗氧化剂前药，其可用于预防或治疗由线粒体氧化还原环境的变化引起的线粒体功能障碍相关的疾病或病症。通过将抗氧化剂改性为脂肪酸来制备本发明的抗氧化剂前药，以使得到的前药被靶向并被线粒体脂肪酸β-氧化酶活化。

3. 发明授权

US08470861B2 Mitochondria-targeted antioxidant prodrugs and methods of use 失效
标题翻译：线粒体靶向抗氧化剂前药及其使用方法
公开(公告)号：US08470861B2
公开(公告)日：2013-06-25
申请号：US12694337
申请日：2010-01-27
申请人： Marion W. Anders , James L. Robotham , Shey-Shing Sheu , Paul Spencer Brookes , Jalil Shojaie , Leif Olson , Richard L. Parton
发明人： Marion W. Anders , James L. Robotham , Shey-Shing Sheu , Paul Spencer Brookes , Jalil Shojaie , Leif Olson , Richard L. Parton
IPC分类号： A01N43/50 , A01N43/32 , A01N43/26 , A01N43/16 , A01N31/14 , A61K31/415 , A61K31/385 , A61K31/35 , A61K31/075 , A61K31/08 , C07D339/00 , C07D339/02 , C07D341/00 , C07D409/00 , C07D239/00 , C07D239/02
CPC分类号： C07D233/54 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/28 , A61K31/385 , A61K31/4164 , C07C323/52 , C07D233/84 , C07D271/12 , C07D311/72 , C07D339/06 , C07D339/08 , C07D471/04 , C07F9/65324
摘要： The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation.
摘要翻译：本发明是线粒体靶向的抗氧化剂前药，其可用于预防或治疗由线粒体氧化还原环境的变化引起的线粒体功能障碍相关的疾病或病症。通过将抗氧化剂改性为脂肪酸来制备本发明的抗氧化剂前药，以使得到的前药被靶向并被线粒体脂肪酸β-氧化酶活化。

4. 发明授权

US5552407A Anhydroecgonine compounds and their use as anticholinergic agents 失效
标题翻译：脱氢化合物化合物及其作为抗胆碱剂的用途
公开(公告)号：US5552407A
公开(公告)日：1996-09-03
申请号：US76315
申请日：1993-06-11
申请人： Ronald W. Wood , Hassan A. N. El-Fawal , John F. Graefe , Lung C. Chen , Jalil Shojaie
发明人： Ronald W. Wood , Hassan A. N. El-Fawal , John F. Graefe , Lung C. Chen , Jalil Shojaie
IPC分类号： C07D451/02 , A61K31/44 , C07D213/20
CPC分类号： C07D451/02
摘要： Methylecgonidine (MEG; anhydroecgonine methylester), is produced when cocaine base ("crack") is heated. MEG alone and in combination with cocaine was tested for action on isolated tracheal rings stimulated to contact with acetylcholine. At micromolar concentrations, cocaine sensitized tracheal rings, increasing both the potency and efficacy of acetylcholine-induced contraction. Surprisingly, MEG, at nanomolar concentrations and above, non-competitively and irreversibly antagonized acetylcholine-induced contraction independently of the actions of cocaine. MEG also displayed antihistaminic activity. Therefore, MEG and anticholinergically active derivatives or analogues thereof are useful in the prevention or treatment of a disease or disorder treatable by an antimuscarinic anticholinergic agent, an anti-histaminic agent or a spasmolytic agent, in particular bronchoconstriction in a number of pulmonary diseases such as asthma.
摘要翻译：当可卡因碱（“裂纹”）被加热时，产生甲基氢醌（MEG;脱氢莽草啶甲酯）。测试单独的和与可卡因组合的MEG对被刺激与乙酰胆碱接触的分离的气管环的作用。在微摩尔浓度下，可卡因致敏气管环，增加了乙酰胆碱诱导的收缩的效力和功效。令人惊讶的是，纳米摩尔浓度以上的MEG与可卡因的作用无关，不可逆地和不可逆地拮抗乙酰胆碱诱导的收缩。 MEG还显示抗组胺活性。因此，MEG和抗胆碱能活性衍生物或其类似物可用于预防或治疗由抗毒蕈碱性抗胆碱能药，抗组胺药或解痉药治疗的疾病或病症，特别是在多种肺部疾病中的支气管收缩哮喘。

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