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1. 发明授权

US06677453B1 Production of polymorphic forms I and II of finasteride by complexation with group I or II metal salts 失效
标题翻译：通过与I或II族金属盐络合生产非那雄胺的多晶型I和II
公开(公告)号：US06677453B1
公开(公告)日：2004-01-13
申请号：US10111979
申请日：2002-06-18
申请人： Clarke Slemon
发明人： Clarke Slemon
IPC分类号： C07D22118
CPC分类号： C07J73/005
摘要： Polymorphic Form (I) finasteride is prepared by first forming a substantially insoluble complex of finasteride and a Group (I) or Group (II) metal salt, such as lithium bromide, and then dissociating the complex by dissolving away the salt component with water, so as to obtain substantially pure Form (I) polymorphic crystalline finasteride.
摘要翻译：多晶型（I）非那雄胺通过首先形成非那雄胺和第（I）或（II）族金属盐如溴化锂的基本上不溶的络合物，然后通过用水溶解盐组分来解离络合物来制备，以获得基本上纯的形式（I）多晶型结晶非那雄胺。

2. 发明授权

US07316900B2 Methylated nucleotide regulation of gene expression 失效
标题翻译：甲基化核苷酸调控基因表达
公开(公告)号：US07316900B2
公开(公告)日：2008-01-08
申请号：US10332542
申请日：2001-07-13
申请人： Shafaat A. Rabbani , Clarke Slemon
发明人： Shafaat A. Rabbani , Clarke Slemon
IPC分类号： C12Q1/68 , C12P19/34 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C12N15/1137 , A61K38/00 , C12N2310/3341 , C12Q1/6886 , C12Q2600/154 , C12Q2600/156 , C12Y304/21073
摘要： The present invention provides a method of regulating the expression of the urokinase type plasminogen activator (“uPA”) gene in a mammalian cell comprising the steps of: identifying a target nucleotide sequence in a gene of interest, obtaining a methylated antisense oligonucleotide sequence complementary to the target sequence, said oligonucleotide sequence having 5 methylated cytosine in place of unmethylated cytosine in the region complementary to the CpG region in the target nucleotide sequence, and exposing the cell to copies of the oligonucleotide sequence under suitable conditions, such that the oligonucleotide sequence enters the nucleus and interacts with the target sequence to promote methylation of the target nucleotide sequence.
摘要翻译：本发明提供一种调节哺乳动物细胞中尿激酶型纤溶酶原激活物（“uPA”）基因表达的方法，包括以下步骤：鉴定目的基因中的靶核苷酸序列，获得互补的甲基化反义寡核苷酸序列所述靶序列，所述寡核苷酸序列在与靶核苷酸序列中的CpG区域互补的区域中代替未甲基化的胞嘧啶，并在合适的条件下将细胞暴露于寡核苷酸序列的拷贝，使得寡核苷酸序列进入核并与靶序列相互作用以促进靶核苷酸序列的甲基化。

3. 发明授权

US07119068B2 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：US07119068B2
公开(公告)日：2006-10-10
申请号：US10651659
申请日：2003-08-29
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： C07C65/01 , C07C65/03 , C07C65/10 , A01N37/36 , A01N31/60
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。

4. 发明授权

US06703504B2 Conformationally constrained compounds as dendrimer cores 失效
标题翻译：构象约束的化合物作为树枝状聚合物核心
公开(公告)号：US06703504B2
公开(公告)日：2004-03-09
申请号：US10071206
申请日：2002-02-11
申请人： Clarke Slemon , Bohumil Macel , Latchazar Trifonov , Jean Vaugeois
发明人： Clarke Slemon , Bohumil Macel , Latchazar Trifonov , Jean Vaugeois
IPC分类号： C07D23900
CPC分类号： C08G83/003 , C07C39/17 , C07C39/27 , C07C49/747 , C07C49/753 , C07C237/10 , C07C2603/94
摘要： There are provided novel chemical compounds and their uses in the preparation of polymers and oligomers, and the preparation of such compounds. In certain embodiments there are provided dendritic polymers and oligomers, of a type having at least four polymeric or oligomeric organic chains emanating from a single chemical core, each of the chains being of substantially equal length and substantially the same chemical composition. Such compounds may be referred to as dendrimers. Also provided are novel chemical entities useful as core entities in the preparation of dentrimers. Dendrimers can recognize a core substructure to which the polymeric/oligomeric chains (“dendrons”) are covalenty attached and from which they extend with systematic branching radially outward in a three dimensional fashion, to approximately the same extent to each other. Together, core and dendrons constitute macromolecules possessing a high degree of internal structural replication attributable to the branches.
摘要翻译：提供新颖的化合物及其在制备聚合物和低聚物中的用途以及这些化合物的制备。在某些实施方案中，提供了具有从单个化学核发出的至少四个聚合物或低聚有机链的类型的树枝状聚合物和低聚物，每条链具有基本相同的长度和基本上相同的化学组成。这些化合物可以称为树枝状大分子。还提供了新颖的化学实体，可用作制备残留物的核心实体。树枝状聚合物可以识别聚合物/低聚链（“树枝状”）被共价连接的核心亚结构，并且它们以三维方式径向向外以系统分支延伸到彼此大致相同的程度。核心和树突一起构成具有归属于分枝的高度内部结构复制的大分子。

5. 发明授权

US5932709A Process for preparing glycosylated analogs of camptothecin 失效
标题翻译：制备喜树碱糖基化类似物的方法
公开(公告)号：US5932709A
公开(公告)日：1999-08-03
申请号：US876824
申请日：1997-06-16
申请人： Brian Keith Shull , Clarke Slemon , Masato Koreeda
发明人： Brian Keith Shull , Clarke Slemon , Masato Koreeda
IPC分类号： C07H15/26 , C07H17/00 , C07H1/00
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。

6. 发明授权

US5374730A Preparation of omeprazole and lansoprazole 失效
标题翻译：奥美拉唑和兰索拉唑的制备
公开(公告)号：US5374730A
公开(公告)日：1994-12-20
申请号：US145572
申请日：1993-11-04
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。

7. 发明授权

US5371240A Process for the preparation of pure thiophene derivatives 失效
标题翻译：制备纯噻吩衍生物的方法
公开(公告)号：US5371240A
公开(公告)日：1994-12-06
申请号：US983316
申请日：1992-11-30
申请人： Clarke Slemon
发明人： Clarke Slemon
IPC分类号： C07D333/46 , C07D333/22 , C07D333/08 , C07D333/28 , C07D333/38
CPC分类号： C07D333/46
摘要： 3-substituted thiophene compounds contaminating the analogous 2-substituted thiophene compounds, e.g. 3-acetylthiophene contaminating 2-acetyl thiophene, are removed by a selective electrophilic substitution process, e.g. bromination, followed by fractional distillation. It has been found that electrophilic substitution as exemplified by bromination is highly selective towards the 3-substituted thiophenes, yielding compounds of significantly higher molecular weights for separation purposes, to give high purity 2-substituted thiophene compounds.
摘要翻译：污染类似的2-取代噻吩化合物的3-取代噻吩化合物，例如污染2-乙酰基噻吩的3-乙酰基噻吩通过选择性亲电取代方法，例如，溴化，然后分馏。已经发现，通过溴化示例的亲电取代对于3-取代的噻吩是高选择性的，产生用于分离目的的显着更高分子量的化合物，得到高纯度2-取代的噻吩化合物。

8. 发明授权

US07767646B2 Methods of screening for compounds that modulate TAFIa activity, compounds, and methods of using the compounds 有权
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：US07767646B2
公开(公告)日：2010-08-03
申请号：US11544906
申请日：2006-10-06
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： C12Q1/00
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。

9. 发明申请

US20080305508A1 Methods of screening for compounds that modulate TAFIa activity, compounds, and methods of using the compounds 有权
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：US20080305508A1
公开(公告)日：2008-12-11
申请号：US11544906
申请日：2006-10-06
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： A61K31/60
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。

10. 发明授权

US5783702A Preparation of cisapride 失效
标题翻译：西沙必利的制备
公开(公告)号：US5783702A
公开(公告)日：1998-07-21
申请号：US700907
申请日：1996-08-21
申请人： Yee-Fung Lu , Clarke Slemon , Raymond So , Jan Oudenes , Teng-Ko Ngooi
发明人： Yee-Fung Lu , Clarke Slemon , Raymond So , 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

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