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公开(公告)号：US20070293528A9
公开(公告)日：2007-12-20
申请号：US11344690
申请日：2006-01-31
申请人： Lin Zhi , Cornelis Van Oeveren , Jyun-Hung Chen , Robert Higuchi
发明人： Lin Zhi , Cornelis Van Oeveren , Jyun-Hung Chen , Robert Higuchi
IPC分类号： A61K31/4743 , A61K31/4741 , A61K31/382 , A61K31/366 , C07D495/02 , C07D493/02 , C07D491/02
CPC分类号： C07D471/04 , C07D491/04 , C07D493/04
摘要： This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.
摘要翻译： 本发明涉及作为雄激素受体调节剂的非甾体三环化合物以及制备和使用这些化合物的方法。
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公开(公告)号：US20070167445A1
公开(公告)日：2007-07-19
申请号：US11340282
申请日：2006-01-25
申请人： Robert Higuchi , Kristen Arienti , Neelakandha Mani , Barbara Pio , Lin Zhi , Penghui Chen , Thomas Caferro
发明人： Robert Higuchi , Kristen Arienti , Neelakandha Mani , Barbara Pio , Lin Zhi , Penghui Chen , Thomas Caferro
IPC分类号： A61K31/538 , A61K31/498
CPC分类号： C07D471/04 , C07D498/04 , C07D498/14 , C07D513/04
摘要： Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.
摘要翻译： 用于调节由类固醇受体介导的过程的化合物，药物组合物和方法。 特别地，描述了使用作为雄激素受体（AR）的激动剂，部分激动剂和拮抗剂的非类固醇化合物和组合物的制备方法和方法。 此外，描述了制备和使用关键中间体的方法，其包括用于AR调节剂的中间体的立体选择性合成路线。
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公开(公告)号：US06462038B1
公开(公告)日：2002-10-08
申请号：US09648684
申请日：2000-08-25
申请人： Robert Higuchi , Kristen L. Arienti , Mani Neelakandha , Barbara Pio , Lin Zhi , Penghui Chen , Thomas R. Caferro
发明人： Robert Higuchi , Kristen L. Arienti , Mani Neelakandha , Barbara Pio , Lin Zhi , Penghui Chen , Thomas R. Caferro
IPC分类号： A61K31536
CPC分类号： C07D471/04 , C07D498/04 , C07D498/14 , C07D513/04
摘要： Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.
摘要翻译： 用于调节由类固醇受体介导的过程的化合物，药物组合物和方法。 特别地，描述了使用作为雄激素受体（AR）的激动剂，部分激动剂和拮抗剂的非类固醇化合物和组合物的制备方法和方法。 此外，描述了制备和使用关键中间体的方法，所述关键中间体包括用于AR调节剂的中间体的立体选择性合成路线。
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14.发明授权Boron containing polybasic bacterial efflux pump inhibitors and therapeutic uses thereof 有权含有多碱性细菌外排泵抑制剂的硼及其治疗用途公开(公告)号：US08933018B2
公开(公告)日：2015-01-13
申请号：US13983747
申请日：2012-02-06
申请人： Tomasz Glinka , Robert Higuchi , Scott Hecker , Brian Eastman , Olga Rodny
发明人： Tomasz Glinka , Robert Higuchi , Scott Hecker , Brian Eastman , Olga Rodny
CPC分类号： C07K5/06191 , A61K38/05 , C07F5/025
摘要： Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.
摘要翻译： 本文公开了含有硼酸官能团的多碱性细菌外排泵抑制剂及其合成方法，使用方法和药物组合物。 一些实施方案包括通过与感染细菌的受试者共同施用或具有另外的抗细菌剂的外排泵抑制剂感染细菌的风险来治疗或预防细菌感染的方法。
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公开(公告)号：US06534516B1
公开(公告)日：2003-03-18
申请号：US09448992
申请日：1999-11-24
IPC分类号： C07D48704
CPC分类号： C07D471/04 , C07D471/14
摘要： Non-steroidal compounds that are high affinity, high selectivity modulators for androgen receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring androgen receptor agonist, partial agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the androgen receptor modulator compounds.
摘要翻译： 公开了用于雄激素受体的高亲和力，高选择性调节剂的非甾体化合物。 还公开了掺入这种化合物的药物组合物，使用所公开的化合物的方法和用于治疗需要雄激素受体激动剂的患者的组合物，部分激动剂或拮抗剂治疗，可用于制备化合物的中间体和用于制备雄激素受体调节剂化合物的方法 。
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16.发明申请BORON CONTAINING POLYBASIC BACTERIAL EFFLUX PUMP INHIBITORS AND THERAPEUTIC USES THEREOF 有权含硼多孔酚醛树脂泵抑制剂及其治疗用途公开(公告)号：US20130316943A1
公开(公告)日：2013-11-28
申请号：US13983747
申请日：2012-02-06
申请人： Tomasz Glinka , Robert Higuchi , Scott Hecker , Brian Eastman , Olga Rodny
发明人： Tomasz Glinka , Robert Higuchi , Scott Hecker , Brian Eastman , Olga Rodny
CPC分类号： C07K5/06191 , A61K38/05 , C07F5/025
摘要： Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.
摘要翻译： 本文公开了含有硼酸官能团的多碱性细菌外排泵抑制剂及其合成方法，使用方法和药物组合物。 一些实施方案包括通过与感染细菌的受试者共同施用或具有另外的抗细菌剂的外排泵抑制剂感染细菌的风险来治疗或预防细菌感染的方法。
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公开(公告)号：US6017924A
公开(公告)日：2000-01-25
申请号：US373460
申请日：1999-08-12
IPC分类号： C07D471/04 , C07D471/14 , C07D498/16 , A61K31/44
CPC分类号： C07D471/04 , C07D471/14
摘要： Non-steroidal compounds that are high affinity, high selectivity modulators for androgen receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring androgen receptor agonist, partial agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the androgen receptor modulator compounds.
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