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11. 发明授权

US5585387A Prepration of cisapride 失效
标题翻译：西沙必利的制备
公开(公告)号：US5585387A
公开(公告)日：1996-12-17
申请号：US319681
申请日：1994-10-07
申请人： Yee-Fung Lu , Raymond So , Clarke Slemon , Jan Oudenes , Teng-Ko Ngooi
发明人： Yee-Fung Lu , Raymond So , Clarke Slemon , Jan Oudenes , Teng-Ko Ngooi
IPC分类号： C07D211/58 , C07D211/74 , A61K31/445 , C07D211/42
CPC分类号： C07D211/58 , C07D211/74
摘要： Cisapride, i.e. cis-4-amino-5-chloro-N-[1-[3-(4 fluoro-phenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxy-benzamide, and similar benzamide derivatives, are prepared from novel 1-aryloxyalkyl- or 1-aralkyl-3-arylcarbonyloxy-4-oxo-piperidines, by nuclear substituent re arrangement involving acyl transfer under animal forming conditions, to give the corresponding 1-aryloxyalkyl- or 1-aralkyl-3-hydroxy-4-lower alkoxy-4-arylamido piperidine. This in turn is readily converted to the corresponding 3-oxo-4-arylamido-piperidine by reaction with strong organic acid, which can then be reduced, deprotected and 3-methylated to give the final compound, e.g. cisapride.
摘要翻译：西萨必利，即顺式-4-氨基-5-氯-N- [1- [3-（4-氟 - 苯氧基）丙基] -3-甲氧基-4-哌啶基] -2-甲氧基 - 苯甲酰胺和类似的苯甲酰胺衍生物，通过在动物形成条件下涉及酰基转移的核取代基重排，由新的1-芳氧基烷基 - 或1-芳烷基-3-芳基羰基氧基-4-氧代 - 哌啶制备，得到相应的1-芳氧基烷基 - 或1-芳烷基-3 - 羟基-4-低级烷氧基-4-芳基酰氨基哌啶。这又通过与强有机酸反应而容易地转化为相应的3-氧代-4-芳基氨基 - 哌啶，然后可以将其还原，脱保护和3-甲基化，得到最终化合物，例如。西沙必利

12. 发明授权

US5470983A Preparation of omeprazole and lansoprazole, and intermediates useful therein 失效
标题翻译：奥美拉唑和兰索拉唑的制备及其中有用的中间体
公开(公告)号：US5470983A
公开(公告)日：1995-11-28
申请号：US276378
申请日：1994-07-18
申请人： Clarke Slemon , Bob Macel
发明人： Clarke Slemon , Bob Macel
IPC分类号： A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61P1/00 , A61P1/04 , C07D401/12
CPC分类号： C07D401/12
摘要： Omeprazole and lansoprazole, which are chemically pyridine-benzimidazole sulfinyl compounds, are produced from the corresponding acetamide-sulfide compounds by a process of oxidation to form the amide sulfinyl compound, followed by alkaline hydrolysis to the sulfinyl carboxylate or salt, and decarboxylation.
摘要翻译：化学式为吡啶 - 苯并咪唑亚磺酰基化合物的奥美拉唑和兰索拉唑通过氧化形成酰亚胺亚磺酰基化合物，然后碱性水解成亚磺酰基羧酸盐或盐，并脱羧由相应的乙酰胺 - 硫化物化合物制备。

13. 发明申请

US20100310540A1 METHODS OF SCREENING FOR COMPOUNDS THAT MODULATE TAFIA ACTIVITY, COMPOUNDS, AND METHODS OF USING THE COMPOUNDS 审中-公开
标题翻译：用于调节TAFIA活性的化合物的筛选方法，化合物和使用该化合物的方法
公开(公告)号：US20100310540A1
公开(公告)日：2010-12-09
申请号：US12795152
申请日：2010-06-07
申请人： Robert S. Greenfield , Seong Soo A. An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
发明人： Robert S. Greenfield , Seong Soo A. An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
IPC分类号： A61K38/48 , C12Q1/37 , A61P9/10 , A61P7/02 , A61P7/06 , A61P19/02 , A61K31/609 , C07C271/20 , C07C235/60 , A61K31/60 , A61K38/17 , A61K38/49 , A61K31/616
CPC分类号： C12Q1/37 , A61K31/60 , C12Q1/56 , G01N33/573 , G01N33/6893 , G01N33/86 , G01N33/9486 , G01N2500/00
摘要： Provided are methods of screening compounds for any aspirin-related activity other than TAFI inhibition, and also for non-inhibition of TAFI. Compounds identified by the screening methods can be used to treat, prevent or manage in a patient pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder. Also provided is a method of evaluating test compounds for TAFI inhibitory activity wherein the TAFI inhibitory activity of these test compounds is compared to the TAFI inhibitory activity of aspirin or its derivatives or metabolites. Further provided is a method of treating, preventing or managing in a patient, a hemorrhagic or thrombotic disease or disorder with high dose aspirin or aspirin derivatives or metabolites. Also contemplated is a method of treating, preventing or managing in a patient, pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder comprising administering aspirin or a derivative thereof or any other therapeutic having at least one desired therapeutic or prophylactic activity of aspirin to a patient in need thereof and administering to the patient a factor that promotes TAFIa activity, e.g. stabilized TAFIa, to ameliorate one or more adverse side effects of the therapeutic. Compounds identified by the methods of the invention are also provided.
摘要翻译：提供了筛选化合物除了TAFI抑制以外的任何阿司匹林相关活性的方法，以及用于非抑制TAFI的方法。通过筛选方法鉴定的化合物可用于治疗，预防或控制患者疼痛，发烧，结肠癌，胰腺癌或炎症，血小板聚集，纤维蛋白溶解或出血性疾病或病症。还提供了评价试验化合物对TAFI抑制活性的方法，其中将这些试验化合物的TAFI抑制活性与阿司匹林或其衍生物或代谢物的TAFI抑制活性进行比较。还提供了一种治疗，预防或控制患者出血性或血栓性疾病或病症的方法，其中高剂量阿司匹林或阿司匹林衍生物或代谢物。还考虑了治疗，预防或控制患者的疼痛，发烧，结肠癌，胰腺癌或炎性，血小板聚集，纤维蛋白溶解或出血性疾病或病症的方法，包括给予阿司匹林或其衍生物或任何其它具有对有需要的患者的阿司匹林的至少一种期望的治疗或预防活性，并向患者施用促进TAFIa活性的因子，例如稳定的TAFIa，以改善治疗的一种或多种不良副作用。还提供了通过本发明的方法鉴定的化合物。

14. 发明申请

US20050222096A1 Methods of screening for compounds that modulate TAFIa activity, compounds, and methods of using the compounds 失效
标题翻译：筛选调节TAFIa活性的化合物的方法，化合物和使用该化合物的方法
公开(公告)号：US20050222096A1
公开(公告)日：2005-10-06
申请号：US10651659
申请日：2003-08-29
申请人： Robert Greenfield , Seong An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
发明人： Robert Greenfield , Seong An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
IPC分类号： A61K31/60 , C12Q1/00 , C12Q1/56 , G01N33/573 , G01N33/68 , G01N33/86 , G01N33/94
CPC分类号： C12Q1/37 , A61K31/60 , C12Q1/56 , G01N33/573 , G01N33/6893 , G01N33/86 , G01N33/9486 , G01N2500/00
摘要： Provided are methods of screening compounds for any aspirin-related activity other than TAFI inhibition, and also for non-inhibition of TAFI. Compounds identified by the screening methods can be used to treat, prevent or manage in a patient pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder. Also provided is a method of evaluating test compounds for TAFI inhibitory activity wherein the TAFI inhibitory activity of these test compounds is compared to the TAFI inhibitory activity of aspirin or its derivatives or metabolites. Further provided is a method of treating, preventing or managing in a patient, a hemorrhagic or thrombotic disease or disorder with high dose aspirin or aspirin derivatives or metabolites. Also contemplated is a method of treating, preventing or managing in a patient, pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder comprising administering aspirin or a derivative thereof or any other therapeutic having at least one desired therapeutic or prophylactic activity of aspirin to a patient in need thereof and administering to the patient a factor that promotes TAFIa activity, e.g. stablized TAFIa, to ameliorate one or more adverse side effects of the therapeutic. Compounds identified by the methods of the invention are also provided.
摘要翻译：提供了筛选化合物除了TAFI抑制以外的任何阿司匹林相关活性的方法，以及用于非抑制TAFI的方法。通过筛选方法鉴定的化合物可用于治疗，预防或控制患者疼痛，发烧，结肠癌，胰腺癌或炎症，血小板聚集，纤维蛋白溶解或出血性疾病或病症。还提供了评价试验化合物对TAFI抑制活性的方法，其中将这些试验化合物的TAFI抑制活性与阿司匹林或其衍生物或代谢物的TAFI抑制活性进行比较。还提供了一种治疗，预防或控制患者出血性或血栓性疾病或病症的方法，其中高剂量阿司匹林或阿司匹林衍生物或代谢物。还考虑了治疗，预防或控制患者的疼痛，发烧，结肠癌，胰腺癌或炎性，血小板聚集，纤维蛋白溶解或出血性疾病或病症的方法，包括给予阿司匹林或其衍生物或任何其它具有对有需要的患者的阿司匹林的至少一种期望的治疗或预防活性，并向患者施用促进TAFIa活性的因子，例如稳定TAFIa，以改善治疗的一种或多种不良副作用。还提供了通过本发明的方法鉴定的化合物。

15. 发明授权

US5665884A Preparation of cisapride 失效
标题翻译：西沙必利的制备
公开(公告)号：US5665884A
公开(公告)日：1997-09-09
申请号：US701125
申请日：1996-08-21
申请人： Yee-Fung Lu , Raymond So , Clarke Slemon , Jan Oudenes , Teng-Ko Ngooi
发明人： Yee-Fung Lu , Raymond So , Clarke Slemon , Jan Oudenes , Teng-Ko Ngooi
IPC分类号： C07D211/58 , C07D211/74
CPC分类号： C07D211/58 , C07D211/74
摘要： Cisapride, i.e. cis-4-amino-5-chloro-N-[1-[3-(4 fluoro-phenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxy-benzamide, and similar benzamide derivatives, are prepared from novel 1-aryloxyalkyl- or 1-aralkyl-3-arylcarbonyloxy-4-oxo-piperidines, by nuclear substituent re arrangement involving acyl transfer under animal forming conditions, to give the corresponding 1-aryloxyalkyl- or 1-aralkyl-3-hydroxy-4-lower alkoxy-4-arylamido piperidine. This in turn is readily converted to the corresponding 3-oxo-4-arylamido-piperidine by reaction with strong organic acid, which can then be reduced, deprotected and 3-methylated to give the final compound, e.g. cisapride.
摘要翻译：西萨必利，即顺式-4-氨基-5-氯-N- [1- [3-（4-氟 - 苯氧基）丙基] -3-甲氧基-4-哌啶基] -2-甲氧基 - 苯甲酰胺和类似的苯甲酰胺衍生物，通过在动物形成条件下涉及酰基转移的核取代基重排，由新的1-芳氧基烷基 - 或1-芳烷基-3-芳基羰基氧基-4-氧代 - 哌啶制备，得到相应的1-芳氧基烷基 - 或1-芳烷基-3 - 羟基-4-低级烷氧基-4-芳基酰氨基哌啶。这又通过与强有机酸反应而容易地转化为相应的3-氧代-4-芳基氨基 - 哌啶，然后可以将其还原，脱保护和3-甲基化，得到最终化合物，例如。西沙必利

16. 发明授权

US5502195A Sulfoxide-carboxylate intermediates of omeprazole and lansoprazole 失效
标题翻译：奥美拉唑和兰索拉唑的亚磺酸 - 羧酸中间体
公开(公告)号：US5502195A
公开(公告)日：1996-03-26
申请号：US345725
申请日：1994-11-22
申请人： Clarke Slemon , Bob Macel
发明人： Clarke Slemon , Bob Macel
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Omeprazole and lansoprazole, which are chemically pyridine-benzimidazole sulfinyl compounds, are produced from the corresponding acetamide-sulfide compounds by a process of oxidation to form the amide sulfinyl compound, followed by alkaline hydrolysis to the sulfinyl carboxylate or salt, and decarboxylation.
摘要翻译：化学式为吡啶 - 苯并咪唑亚磺酰基化合物的奥美拉唑和兰索拉唑通过氧化形成酰亚胺亚磺酰基化合物，然后碱性水解成亚磺酰基羧酸盐或盐，并脱羧由相应的乙酰胺 - 硫化物化合物制备。

17. 发明授权

US5677286A Glycosylated analogs of camptothecin 失效
标题翻译：喜树碱的糖基化类似物
公开(公告)号：US5677286A
公开(公告)日：1997-10-14
申请号：US429941
申请日：1995-04-27
申请人： Brian K. Shull , Clarke Slemon , Masato Koreeda
发明人： Brian K. Shull , Clarke Slemon , Masato Koreeda
IPC分类号： C07H15/26 , C07H17/00 , A61K31/70 , C07H15/24
CPC分类号： C07H15/26 , C07H17/00
摘要： The present invention relates to chemotherapeutic agents, and more particularly, to novel analogs of camptothecin. The camptothecin analogs display increased solubility through the hydrophilicity of added non-ionic sugar substituents. In accordance with the present invention, a member from the class of novel camptothecin analogs is to be delivered in vivo as a chemotherapeutic agent to fight cancer growth in the body.
摘要翻译：本发明涉及化学治疗剂，更具体地涉及喜树碱的新型类似物。喜树碱类似物通过添加的非离子糖取代基的亲水性显示增加的溶解度。根据本发明，来自新兴喜树碱类似物类的成员将作为化学治疗剂在体内递送以抵抗体内的癌症生长。

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