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1. 发明授权

US06800653B2 Epothilone derivatives 有权
标题翻译：埃博霉素衍生物
公开(公告)号：US06800653B2
公开(公告)日：2004-10-05
申请号：US10144879
申请日：2002-05-14
申请人： Alicia Regueiro-Ren , Robert M. Borzilleri , Gregory D. Vite , Soong-Hoon Kim
发明人： Alicia Regueiro-Ren , Robert M. Borzilleri , Gregory D. Vite , Soong-Hoon Kim
IPC分类号： A61K31425
CPC分类号： C07D417/06 , A61K31/427 , A61K31/5377 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor.
摘要翻译：本发明涉及12,13位修饰的埃坡霉素衍生物，衍生物的制备方法及其中间体。

2. 发明授权

US06790859B2 Reversing advanced glycosylation cross-links using heterocyclic-substituted thiazolium compounds 失效
标题翻译：使用杂环取代的噻唑化合物逆转先进的糖基化交联
公开(公告)号：US06790859B2
公开(公告)日：2004-09-14
申请号：US10348378
申请日：2003-01-21
申请人： Dilip R. Wagle , Sheng-Ding Fang , Taikyun Rho , John J. Egan , Sara Vasan , Peter Ulrich , Anthony Cerami
发明人： Dilip R. Wagle , Sheng-Ding Fang , Taikyun Rho , John J. Egan , Sara Vasan , Peter Ulrich , Anthony Cerami
IPC分类号： A61K31425
CPC分类号： C07D277/22 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5355 , A61K31/541 , A61K31/55 , C07D277/44 , C07D417/06
摘要： The present invention relates to compositions and methods for reversing advanced glycosylation end product-mediated cross-linking and protein aging. Accordingly, compositions are described which comprise thiazolium compounds substituted with heterocyclic groups which are capable of reversing the formation of advanced glycosylation end product cross-links. Both industrial and therapeutic applications for the invention are disclosed, as food spoilage and animal protein aging can be treated. Such compounds have particular application in the treatment of protein aging such as is responsible for the complications of aging and diabetes.
摘要翻译：本发明涉及用于逆转晚期糖基化终产物介导的交联和蛋白质老化的组合物和方法。因此，描述了包含被能够逆转高级糖基化终产物交联的形成的杂环基取代的噻唑鎓化合物的组合物。公开了用于本发明的工业和治疗应用，因为可以处理食物腐败和动物蛋白质老化。这些化合物在治疗老化和糖尿病并发症等蛋白质老化中具有特殊的应用。

3. 发明授权

US06750235B1 Pramipexole as a treatment for cocaine craving 有权
标题翻译：普拉克索作为可卡因渴望的治疗方法
公开(公告)号：US06750235B1
公开(公告)日：2004-06-15
申请号：US10088628
申请日：2002-06-12
申请人： Jerrold Rosenbaum
发明人： Jerrold Rosenbaum
IPC分类号： A61K31425
CPC分类号： A61K45/06 , A61K31/428 , A61K31/53 , A61K2300/00
摘要： Disclosed herein are methods foe reducing stimulant dependency or craving, involving administration of a therapeutically-effective amount of a dopamine agonist, such as pramipexole.
摘要翻译：本文公开了减少兴奋剂依赖性或渴望的方法，涉及施用治疗有效量的多巴胺激动剂如普拉克索。

4. 发明授权

US06706745B1 Biphenylamidine derivatives 失效
标题翻译：联苯脒衍生物
公开(公告)号：US06706745B1
公开(公告)日：2004-03-16
申请号：US09554799
申请日：2000-05-18
申请人： Takayuki Hara , Tomohisa Nakada , Yasunobu Takano , Satoshi Sugiura , Takaharu Tsutsumi , Yoshiharu Takazawa , Reiko Takarada
发明人： Takayuki Hara , Tomohisa Nakada , Yasunobu Takano , Satoshi Sugiura , Takaharu Tsutsumi , Yoshiharu Takazawa , Reiko Takarada
IPC分类号： A61K31425
CPC分类号： C07D207/08 , C07C251/18 , C07C257/18 , C07C2601/14 , C07D207/09 , C07D207/16 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/40 , C07D211/62
摘要： The present invention relates to a biphenylamidine derivative of the general formula (1): or a pharmaceutically acceptable salt thereof, which is a novel compound functioning as a clinically applicable FXa inhibitor.
摘要翻译：本发明涉及通式（1）的联苯基脒衍生物或其药学上可接受的盐，它是作为临床适用的FXa抑制剂起作用的新化合物。

5. 发明授权

US06696473B2 Heterocyclic modulators of nuclear receptors 有权
公开(公告)号：US06696473B2
公开(公告)日：2004-02-24
申请号：US10329668
申请日：2002-12-20
申请人： Richard Martin , Brenton Todd Flatt , Jeffrey Dean Kahl , Tie-Lin Wang
发明人： Richard Martin , Brenton Todd Flatt , Jeffrey Dean Kahl , Tie-Lin Wang
IPC分类号： A61K31425
CPC分类号： C07D277/20 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/64 , C07D417/04 , C07D417/06 , C07D417/14 , C07D513/04
摘要： Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. In certain embodiments, the compounds are thiazolidinone derivatives.

6. 发明授权

US06696441B1 Inhibition of p53-induced stress response 失效
标题翻译：抑制p53诱导的应激反应
公开(公告)号：US06696441B1
公开(公告)日：2004-02-24
申请号：US09637531
申请日：2000-08-11
申请人： Howard B. Cottam , Lorenzo M. Leoni , Dennis A. Carson
发明人： Howard B. Cottam , Lorenzo M. Leoni , Dennis A. Carson
IPC分类号： A61K31425
CPC分类号： C07D513/04 , A61K31/519 , C07D487/04
摘要： The present invention provides compounds that act to suppress p53 activity in mammalian cells, and a method to effectively suppress p53 activity in the cells of a mammal subject to a stress or pathology that is ameliorated by such suppression.
摘要翻译：本发明提供了用于抑制哺乳动物细胞中p53活性的化合物，以及有效抑制经受这种抑制而改善的应激或病理学的哺乳动物细胞中p53活性的方法。

7. 发明授权

US06689803B2 Compositions and methods for treating surgical adhesions 失效
标题翻译：用于治疗手术粘连的组合物和方法
公开(公告)号：US06689803B2
公开(公告)日：2004-02-10
申请号：US10067467
申请日：2002-02-05
申请人： William L. Hunter
发明人： William L. Hunter
IPC分类号： A61K31425
CPC分类号： A61K31/7064 , A61K9/0014 , A61K9/0019 , A61K9/0048 , A61K9/1075 , A61K9/12 , A61K9/1647 , A61K9/5153 , A61K9/7007 , A61K31/047 , A61K31/08 , A61K31/138 , A61K31/16 , A61K31/17 , A61K31/22 , A61K31/223 , A61K31/28 , A61K31/335 , A61K31/337 , A61K31/352 , A61K31/36 , A61K31/366 , A61K31/4015 , A61K31/4025 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/443 , A61K31/4745 , A61K31/475 , A61K31/519 , A61K31/70 , A61K33/00 , A61K33/06 , A61K33/16 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/34 , B82Y5/00
摘要： Methods and compositions for treating or preventing inflammatory diseases such as psoriasis or multiple sclerosis are provided, comprising the step of delivering to the site of inflammation an anti-microtubule agent, or analogue or derivative thereof.
摘要翻译：提供了用于治疗或预防诸如牛皮癣或多发性硬化症的炎性疾病的方法和组合物，其包括向炎症部位递送抗微管剂或其类似物或衍生物的步骤。

8. 发明授权

US06686380B2 Treatment of refractory tumors using epothilone derivatives 有权
$Treatment of refractory tumors using epothilone derivatives$
标题翻译：使用埃坡霉素衍生物治疗难治性肿瘤
公开(公告)号：US06686380B2
公开(公告)日：2004-02-03
申请号：US10072123
申请日：2002-02-08
申请人： Francis Y. F. Lee
发明人： Francis Y. F. Lee
IPC分类号： A61K31425
CPC分类号： A61K31/395 , A61K31/427 , Y10S514/922 , A61K2300/00
摘要： Methods of treating tumors in a mammal, especially a human that has demonstrated resistance to other chemotherapeutic agents, is disclosed. Specifically, methods of the present invention are effective in tumors that have initially been unresponsive to taxane therapy, or have developed resistance during the course of treatment. The methods of the present invention comprise administering epothilone derivatives selected from those represented by the formula: The subject epothilone derivatives are advantageous in addition to their enhanced potency and effectiveness against tumors that have demonstrated resistance to therapy with taxane oncology agents in that they are efficacious upon oral administration.
摘要翻译：公开了治疗哺乳动物，特别是已证明对其它化学治疗剂具有抗性的人的肿瘤的方法。具体而言，本发明的方法在最初对紫杉烷疗法无反应或在治疗过程中产生抗药性的肿瘤中有效。本发明的方法包括施用选自由下式表示的埃坡霉素衍生物：除了它们对抗紫杉烷类肿瘤药物抗药性的肿瘤的效力和效力之外，受试者埃坡霉素衍生物是有利的，因为它们有效口服。

9. 发明授权

US06613785B2 Use of glucose uptake enhancer for reducing post-ischemic injury of the heart 失效
标题翻译：使用葡萄糖摄取增强剂减少心脏缺血后损伤
公开(公告)号：US06613785B2
公开(公告)日：2003-09-02
申请号：US10348456
申请日：2003-01-21
申请人： Antoine Michel Alain Bril , Robin Edwin Buckingham , Nassirah Khandoudi
发明人： Antoine Michel Alain Bril , Robin Edwin Buckingham , Nassirah Khandoudi
IPC分类号： A61K31425
CPC分类号： A61K31/4439 , A61K31/00 , A61K31/426 , A61K31/427
摘要： A method for reducing post-ischaemic injury of the heart and/or improving the functional recovery of the heart following myocardial ischaemia which method comprises administration of an effective, non-toxic amount of a glucose uptake enhancer to a human or non-human mammal in need thereof.
摘要翻译：一种用于减少心脏缺血后损伤和/或改善心肌缺血后心脏功能恢复的方法，该方法包括向人或非人哺乳动物施用有效的无毒量的葡萄糖摄取增强剂需要。

10. 发明授权

US06569878B1 Substituted 4-amino-thiazol-2-yl compounds as cyclin-dependent kinase inhibitors 失效
标题翻译：取代的4-氨基 - 噻唑-2-基化合物作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US06569878B1
公开(公告)日：2003-05-27
申请号：US09179744
申请日：1998-10-27
申请人： Wesley K. M. Chong , Shao Song Chu , Lin Li , Rohit K. Duvadie , Yi Yang , Wei Xiao
发明人： Wesley K. M. Chong , Shao Song Chu , Lin Li , Rohit K. Duvadie , Yi Yang , Wei Xiao
IPC分类号： A61K31425
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/42 , C07D417/06 , C07D417/12 , C07D417/14
摘要： Pharmaceutical compositions containing effective amounts of CDK-inhibiting diaminothiazole compounds of the following formula (where R1 and R2 are as defined in the specification) or their salts, or prodrugs or active metabolites of such compounds or salts, are useful for treating disorders and diseases such as cancer: In preferred embodiments, R1 and R2 are independently unsubstituted or substituted carbocyclic or heterocyclic aryl ring structures. Compounds where R2 is ortho-substituted aryl are especially potent inhibitors of CDKs such as CDK4.
摘要翻译：含有有效量的下式（其中R1和R2如本说明书中所定义）的有效量的CDK抑制性二氨基噻唑化合物或其盐或这些化合物或其盐的前体药物或活性代谢物可用于治疗疾病和疾病，例如作为癌症：在优选的实施方案中，R 1和R 2独立地是未取代或取代的碳环或杂环芳环结构。其中R2是邻位取代的芳基的化合物是CDK如CDK4的特别有效的抑制剂。

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