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51. 发明授权

US09169247B2 Tetrahydro-beta-carboline derivatives, synthesis and use thereof 有权
标题翻译：四氢-β-咔啉衍生物，其合成和用途
公开(公告)号：US09169247B2
公开(公告)日：2015-10-27
申请号：US13510810
申请日：2010-11-19
申请人： Gary A. Piazza , Ashraf H. Abadi
发明人： Gary A. Piazza , Ashraf H. Abadi
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Certain 2-halophenyl, 2,4-dihalophenyl (e.g. 2,4-dichlorophenyl), 3,4-dichlorophenyl (e.g. 3,4-dichlorophenyl), 2,6-dichlorophenyl (2,6-dichlorophenyl) and 2,5-diakoxyphenyl (e.g. 2,5-dimethoxyphenyl) derivatives of tetrahydro-β-carbolines are provided, along with their pharmaceutically acceptable salts; prodrugs and solvates, and compositions containing the compounds. The compounds are useful for the prevention and treatment of cancer, and other indications where PDE5 inhibitors have shown benefits including erectile dysfunction, pulmonary hypertension, enhancing cognitive function, cystic fibrosis, or enhancing the activity of conventional chemotherapeutic drugs. Methods for fabricating the compounds are also provided.
摘要翻译：某些2-卤代苯基，2,4-二卤苯基（如2,4-二氯苯基），3,4-二氯苯基（如3,4-二氯苯基），2,6-二氯苯基（2,6-二氯苯基）提供四氢 - 咔咔啉的二烷氧基苯基（例如2,5-二甲氧基苯基）衍生物及其药学上可接受的盐; 前药和溶剂合物，以及含有这些化合物的组合物。这些化合物可用于预防和治疗癌症，以及PDE5抑制剂已显示益处的其他适应症，包括勃起功能障碍，肺动脉高压，增强认知功能，囊性纤维化或增强常规化学治疗药物的活性。还提供了制备化合物的方法。

52. 发明申请

US20140171477A1 DERIVATIVES OF CELEBOXIB, USE THEREOF AND PREPARATION THEREOF 有权
标题翻译： CELEBOXIB的衍生物，其使用及其制备
公开(公告)号：US20140171477A1
公开(公告)日：2014-06-19
申请号：US14005462
申请日：2012-03-16
申请人： Gary A. Piazza , Ashraf H. Abadi
发明人： Gary A. Piazza , Ashraf H. Abadi
IPC分类号： C07D231/06
CPC分类号： C07D231/06 , C07D231/12
摘要： Derivatives of celecoxib that lack cyclooxygenase inhibitory activity but have improved PDE5 inhibitory activity are provided along with pharmaceutical compositions containing them for the treatment or prevention of cancer. Such compounds are expected to have reduced toxicity compared with celecoxib and other cyclooxygenase inhibitors, and greater efficacy compared with conventional PDE5 inhibitors. Derivatives of celecoxib are also suitable for treating chronic inflammatory conditions, erectile dysfunction, pulmonary hypertension, congestive heart failure, and enhancement of cognitive function.
摘要翻译：提供缺乏环加氧酶抑制活性但具有改善的PDE5抑制活性的塞来考昔衍生物以及含有它们的药物组合物用于治疗或预防癌症。与塞来昔布和其他环加氧酶抑制剂相比，这些化合物预期具有降低的毒性，与常规PDE5抑制剂相比具有更大的功效。塞来昔布的衍生物也适用于治疗慢性炎症，勃起功能障碍，肺动脉高压，充血性心力衰竭和增强认知功能。

53. 发明申请

US20140094492A1 DERIVATIVES OF SULINDAC, USE THEREOF AND PREPARATION THEREOF 有权
标题翻译： SULINDAC的衍生物，其使用及其制备
公开(公告)号：US20140094492A1
公开(公告)日：2014-04-03
申请号：US14008271
申请日：2012-03-30
申请人： Robert Reynolds , Bini Mathew , Gary A. Piazza
发明人： Robert Reynolds , Bini Mathew , Gary A. Piazza
IPC分类号： C07D307/52 , C07D213/38 , C07C211/19 , C07D295/13
CPC分类号： C07D295/13 , C07C211/19 , C07D211/26 , C07D213/38 , C07D307/52
摘要： Derivatives of sulindac that lack cyclooxygenase inhibitory activity are provided along with pharmaceutical compositions containing them and use for treatment or prevention of cancer. The derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.
摘要翻译：提供缺乏环氧合酶抑制活性的舒林酸衍生物以及含有它们的药物组合物，并用于治疗或预防癌症。舒林酸的衍生物也适用于治疗慢性炎症病症。还提供了制备衍生物的方法。

54. 发明授权

US5565439A Methods of using lysophosphatidic acid for treating hyperproliferative conditions 失效
标题翻译：使用溶血磷脂酸治疗过度增殖症状的方法
公开(公告)号：US5565439A
公开(公告)日：1996-10-15
申请号：US334888
申请日：1994-11-04
申请人： Gary A. Piazza , Adam W. Mazur
发明人： Gary A. Piazza , Adam W. Mazur
IPC分类号： A61K31/665 , A61K31/66
CPC分类号： A61K31/661 , A61K31/662 , A61K31/665 , Y10S514/859 , Y10S514/88
摘要： The subject invention involves a method for treating hyperproliferative conditions in mammalian epithelial cells comprising administering to the mammal a composition containing a safe and effective amount of a lysophosphatidic acid compound or derivative having the structure ##STR1## or a cyclic derivative thereof having the structure ##STR2## or a pharmaceutically acceptable salt thereof, wherein: a) --Y-- is --0-- or --CH.sub.2 --;b) --Z is --XH, --H or halo;c) each --X-- is independently --0-- or --S--; andd) --R is unsubstituted or substituted, saturated or unsaturated, straight or branched chain alkyl having from 11 to about 23 carbon atoms.
摘要翻译：本发明涉及一种用于治疗哺乳动物上皮细胞中过度增殖病症的方法，其包括向哺乳动物施用含有安全有效量的具有结构为“IMAGE”的结构为“IMAGE”或其环状衍生物的抗凝血磷酸化合物或其衍生物的组合物或其药学上可接受的盐，其中：a）-Y-是-O-或-CH 2 - ; b）-Z是-XH，-H或卤素; c）每个-X-独立地为-O-或-S-; 和d）-R是未取代或取代的饱和或不饱和的具有11至约23个碳原子的直链或支链烷基。

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