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1. 发明授权

US07101907B2 Topical administration of statins for treatment of bone disorders 有权
标题翻译：用于治疗骨骼疾病的他汀类药物的局部给药
公开(公告)号：US07101907B2
公开(公告)日：2006-09-05
申请号：US10652159
申请日：2003-08-29
申请人： Shirley R. Gasper , Robert R. West , Theresa Martinez , Kirk G. Robbins , Patricia A. McKernan , Nand Baindur , Virender M. Labroo , Gregory R. Mundy
发明人： Shirley R. Gasper , Robert R. West , Theresa Martinez , Kirk G. Robbins , Patricia A. McKernan , Nand Baindur , Virender M. Labroo , Gregory R. Mundy
IPC分类号： A61K31/335
CPC分类号： C07D215/14 , A23L33/10 , A61K31/00 , A61K31/192 , A61K31/22 , A61K31/225 , A61K31/366 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/505 , A61K45/06 , A61K2300/00
摘要： The topical administration of statins for the treatment of bone disorders is disclosed.
摘要翻译：公开了用于治疗骨骼疾病的他汀类药物的局部给药。

2. 发明授权

US06642216B2 Isoprenoid pathway inhibitors for stimulating bone growth 有权
标题翻译：用于刺激骨生长的异戊二醛途径抑制剂
公开(公告)号：US06642216B2
公开(公告)日：2003-11-04
申请号：US09848839
申请日：2001-05-03
申请人： Shirley R. Gasper , Robert R. West , Theresa Martinez , Kirk G. Robbins , Patricia A. McKernan , Nand Baindur , Virender M. Labroo , Gregory R. Mundy
发明人： Shirley R. Gasper , Robert R. West , Theresa Martinez , Kirk G. Robbins , Patricia A. McKernan , Nand Baindur , Virender M. Labroo , Gregory R. Mundy
IPC分类号： A61K31665
CPC分类号： C07D215/14 , A23L33/10 , A61K31/00 , A61K31/192 , A61K31/22 , A61K31/225 , A61K31/366 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/505 , A61K45/06 , A61K2300/00
摘要： Compounds of the formula wherein X in each of formulas (1) and (2) represents a substituted or unsubstituted alkylene, alkenylene, or alkynylene linker of 2-6C; Y is of the formula or a stereoisomer thereof, wherein R1 is substituted or unsubstituted alkyl; each R2 is independently H, hydroxy, alkoxy (1-6C) or lower alkyl (1-4C); R3 is H, hydroxy, or alkoxy (1-6C); or Y is of the formula wherein each n is 1, Z is N, K comprises a substituted or unsubstituted aromatic carbocyclic or heterocyclic ring system which may optionally be spaced from the linkage position shown in formula (7) by a linker of 1-2C, or in formula (7), Z may be spaced from the carbon bonded to X by ═CR6— wherein R6 is H or linear, branded or cyclic alkyl (1-6C), R5 is H or linear, branched or cyclic alkyl, and R′ represents a cation, H or a substituted or unsubstituted alkyl group of 1-6C, promote bone formation and are thus useful in treating osteoporosis, bone fracture or deficiency, primary or secondary hyperparathyroidism, periodontal disease or defect, metastatic bone disease, osteolytic bone disease, post-plastic surgery, post-prosthetic joint surgery, and post-dental implantation. Also disclosed is a method to identify additional compounds which are inhibitors of enzymes in the isoprenoid scheme especially of HMG-CoA reductase which results in prenylation of proteins and in the synthesis of steroids or of inhibitors of their production which are useful in treating bone disorders.
摘要翻译：式（1）和（2）中的式（Ⅳ）化合物表示取代或未取代的2-6C的亚烷基，亚烯基或亚炔基接头; Y为其立体异构体，其中R 1为取代或每个R 2独立地是H，羟基，烷氧基（1-6C）或低级烷基（1-4C）; R 3是H，羟基或烷氧基（1-6C）; 或Y是每个n是1的烷基，其中Z是N，K包括取代或未取代的芳族碳环或杂环系统，其可以任选地与式（7）所示的连接位置与1-2C的连接体间隔开，或在式（7）中，Z可以与通过= CR 6键合到X的碳隔开，其中R 6是H或直链的，有品牌的或环状的烷基（1-6C），R 5是H或直链，支链或环状的烷基，R'表示1-6个C的阳离子H或取代或未取代的烷基，促进骨形成，因此可用于治疗骨质疏松症，骨折或缺陷，原发性或继发性甲状旁腺功能亢进，牙周病或缺损，转移性骨病，溶骨性骨病，整形后手术，假体后关节手术和牙后植入术。还公开了一种鉴定作为特异性HMG-CoA的异戊二烯方案中的酶抑制剂的其它化合物的方法导致蛋白质异戊烯化的还原酶在合成类固醇或其制备的抑制剂中可用于治疗骨骼疾病。

3. 发明授权

US6022887A Compositions and methods for stimulating bone growth 失效
标题翻译：用于刺激骨骼生长的组合物和方法
公开(公告)号：US6022887A
公开(公告)日：2000-02-08
申请号：US989862
申请日：1997-12-12
申请人： Shirley R. Gasper , Robert R. West , Theresa Martinez , Kirk G. Robbins , Patricia A. McKernan , Nand Baindur , Virender M. Labroo
发明人： Shirley R. Gasper , Robert R. West , Theresa Martinez , Kirk G. Robbins , Patricia A. McKernan , Nand Baindur , Virender M. Labroo
IPC分类号： A61K31/216 , A61K31/22 , A61K31/366 , A61K31/381 , A61K31/404 , A61K31/405 , A61P19/08 , A61P19/10 , A01N43/16 , C07D309/00
CPC分类号： A61K31/405 , A61K31/22 , A61K31/366 , A61K31/404
摘要： Compounds of the formula ##STR1## wherein X in each of formulas (1) and (2) represents a substituted or unsubstituted alkylene, alkenylene, or alkynylene linker of 2-6C;Y represents one or more carbocyclic or heterocyclic rings; when two or more rings are present in Y, they may optionally be fused; andR' represents a cation, H or a substituted or unsubstituted alkyl group of 1-6C; andthe dotted lines represent optional .pi.-bonds,promote bone formation and are thus usefull in treating osteoporosis, bone fracture or deficiency, primary or secondary hyperparathyroidism, periodontal disease or defect, metastatic bone disease, osteolytic bone disease, post-plastic surgery, post-prosthetic joint surgery, and post-dental implantation.
摘要翻译：式（1）和（2）中的X表示取代或未取代的2-6C的亚烷基，亚烯基或亚炔基接头; Y表示一个或多个碳环或杂环; 当Y中存在两个或更多个环时，它们可以任选地稠合; 和R'表示1-6个C的阳离子，H或取代或未取代的烷基; 并且虚线代表可选的pi-键，促进骨形成，因此可用于治疗骨质疏松症，骨折或缺陷，原发性或继发性甲状旁腺功能亢进，牙周病或缺陷，转移性骨病，溶骨性骨病，整形后手术假体关节手术和牙植入后。

4. 发明授权

US06376476B1 Isoprenoid pathway inhibitors for stimulating bone growth 有权
标题翻译：用于刺激骨生长的异戊二醛途径抑制剂
公开(公告)号：US06376476B1
公开(公告)日：2002-04-23
申请号：US09488380
申请日：2000-01-20
申请人： Shirley R. Gasper , Robert R. West , Theresa Martinez , Kirk G. Robbins , Patricia A. McKernan , Nand Baindur , Virender M. Labroo , Gregory R. Mundy
发明人： Shirley R. Gasper , Robert R. West , Theresa Martinez , Kirk G. Robbins , Patricia A. McKernan , Nand Baindur , Virender M. Labroo , Gregory R. Mundy
IPC分类号： A61K31665
CPC分类号： C07D215/14 , A23L33/10 , A61K31/00 , A61K31/192 , A61K31/22 , A61K31/225 , A61K31/366 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/505 , A61K45/06 , A61K2300/00
摘要： Various embodiments of statin compounds are shown to enhance the formation of bone and are thus useful in treating osteoporosis, bone fracture or deficiency, primary or secondary hyperparathyroidism, periodontal disease or defect, metastatic bone disease, osteolytic bone disease, post-plastic surgery, post-prosthetic joint surgery, and post-dental implantation.
摘要翻译：他汀类化合物的各种实施方案被证明可增强骨的形成，因此可用于治疗骨质疏松症，骨折或缺陷，原发性或继发性甲状旁腺功能亢进，牙周病或缺损，转移性骨病，溶骨性骨病，整形外手术假体关节手术和牙植入后。

5. 发明授权

US6080779A Compositions and methods for stimulating bone growth 失效
标题翻译：用于刺激骨骼生长的组合物和方法
公开(公告)号：US6080779A
公开(公告)日：2000-06-27
申请号：US96957
申请日：1998-06-12
申请人： Shirley R. Gasper , Robert R. West , Theresa Martinez , Kirk G. Robbins , Patricia A. McKernan , Nand Baindur , Virender M. Labroo , Gregory R. Mundy
发明人： Shirley R. Gasper , Robert R. West , Theresa Martinez , Kirk G. Robbins , Patricia A. McKernan , Nand Baindur , Virender M. Labroo , Gregory R. Mundy
IPC分类号： A61K31/22 , A61K31/366 , A61K31/404 , A61K31/335 , A61K31/33 , A61K31/66
CPC分类号： A61K31/404 , A61K31/22 , A61K31/366
摘要： Compounds of the formula ##STR1## wherein X in each of formulas (1) and (2) represents a substituted or unsubstituted alkylene, alkenylene, or alkynylene linker of 2-6 C;Y represents one or more carbocyclic or heterocyclic rings; when two or more rings are present in Y, they may optionally be fused; andR' represents a cation, H or a substituted or unsubstituted alkyl group of 1-6 C; andthe dotted lines represent optional .pi.-bonds,promote bone formation and are thus useful in treating osteoporosis, bone fracture or deficiency, primary or secondary hyperparathyroidism, periodontal disease or defect, metastatic bone disease, osteolytic bone disease, post-plastic surgery, post-prosthetic joint surgery, and post-dental implantation. These compounds can be used in combination with other bone growth-promoting compounds and/or estrogens and/or bisphosphonates for this purpose.
摘要翻译：式（1）和（2）各自表示X为2-6的取代或未取代的亚烷基，亚烯基或亚炔基连接基的式 Y表示一个或多个碳环或杂环; 当Y中存在两个或更多个环时，它们可以任选地稠合; R'表示1-6个C的阳离子，H或取代或未取代的烷基; 虚线表示可选的pi-键，促进骨形成，因此可用于治疗骨质疏松症，骨折或缺陷，原发性或继发性甲状旁腺功能亢进，牙周病或缺陷，转移性骨病，溶骨性骨病，整形外手术假体关节手术和牙植入后。为了此目的，这些化合物可以与其它骨生长促进化合物和/或雌激素和/或二膦酸盐组合使用。

6. 发明授权

US6124299A Calcitonin mimetics 失效
公开(公告)号：US6124299A
公开(公告)日：2000-09-26
申请号：US28085
申请日：1998-02-23
申请人： Nand Baindur , Virender Labroo , Steven Stroop , Stephanie Beigel , Theresa Martinez , Charles R. Petrie , Mark W. Orme , Patricia A. McKernan , Emma E. Moore
发明人： Nand Baindur , Virender Labroo , Steven Stroop , Stephanie Beigel , Theresa Martinez , Charles R. Petrie , Mark W. Orme , Patricia A. McKernan , Emma E. Moore
IPC分类号： C07D295/08 , A61K31/495 , A61P19/08 , A61P19/10 , A61P43/00 , C07D295/096 , C07D295/20 , C07D295/215 , A61K31/415 , A61K31/55
CPC分类号： C07D295/096 , A61K31/495 , C07D295/215
摘要： Compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. Included among the calcitonin mimetics of the present invention are substituted piperazines. The calcitonin mimetics of the present invention are also useful in libraries and in assays for the determination of calcitonin receptor activity.

7. 发明授权

US5508304A Glucagon antagonists and methods relating thereto 失效
标题翻译：胰高血糖素拮抗剂及其相关方法
公开(公告)号：US5508304A
公开(公告)日：1996-04-16
申请号：US288875
申请日：1994-08-10
申请人： Robert R. West , Virender Labroo , James R. Piggott , Robert A. Smith , Patricia A. McKernan
发明人： Robert R. West , Virender Labroo , James R. Piggott , Robert A. Smith , Patricia A. McKernan
IPC分类号： A61K31/12 , A61K31/122 , A61K31/22 , A61K31/27 , C12P15/00 , A61K31/21
CPC分类号： A61K31/122 , A61K31/12 , A61K31/22 , A61K31/27 , C12P15/00
摘要： Glucagon antagonists and methods relating thereto are disclosed. The glucagon antagonists include skyrin and skyrin analogs, and serve to inhibit the stimulation of a glucagon-induced response pathway, such as the adenylate cyclase response pathway or the inositol phosphate response pathway. The glucagon antagonists may be used within therapeutic compositions to treat disease states associate with elevated glucose levels, including diabetes and hyperglycemia. The present invention also discloses a biologically pure culture of ATCC accession number 74200, as well as methods relating to the production of glucagon antagonists by cultivating the same in a nutrient medium and recovering the glucagon antagonist therefrom.
摘要翻译：公开了胰高血糖素拮抗剂及其相关方法。胰高血糖素拮抗剂包括天冬氨酸和天冬氨酸类似物，并且用于抑制胰高血糖素诱导的应答途径的刺激，例如腺苷酸环化酶应答途径或肌醇磷酸应答途径。胰高血糖素拮抗剂可用于治疗组合物内以治疗与升高的葡萄糖水平相关的疾病状态，包括糖尿病和高血糖。本发明还公开了ATCC保藏号74200的生物纯纯培养物，以及通过在营养培养基中培养并从其中回收胰高血糖素拮抗剂来产生胰高血糖素拮抗剂的方法。

8. 发明授权

US5698521A Native calcitonin mimetics 失效
标题翻译：天然降钙素模拟物
公开(公告)号：US5698521A
公开(公告)日：1997-12-16
申请号：US416602
申请日：1995-04-04
申请人： Patricia A. McKernan , Lennie Chen , Charles Petrie , James Piggott , Robert R. West , Shirley Gasper , Colin Lellis
发明人： Patricia A. McKernan , Lennie Chen , Charles Petrie , James Piggott , Robert R. West , Shirley Gasper , Colin Lellis
IPC分类号： A61K38/00 , C07K14/575 , C07K5/00 , C07K7/00
CPC分类号： C07K14/57527 , A61K38/00
摘要： The invention provides isolated, biologically active native calcitonin mimetics and related methods. These small 16 and 17 amino acid proteins mimic the interaction of calcitonin on its receptor, and also exhibit bone resorptive inhibiting activity.
摘要翻译：本发明提供了分离的，生物活性的天然降钙素模拟物和相关方法。这些小的16和17氨基酸蛋白质模拟降钙素对其受体的相互作用，并且还表现出骨吸收抑制活性。

9. 发明授权

US5677334A Method for inhibiting the stimulation of a glucagon-induced response pathway in a warm-blooded animal in need thereof 失效
标题翻译：在有需要的温血动物中抑制胰高血糖素诱导的应答途径的刺激的方法
公开(公告)号：US5677334A
公开(公告)日：1997-10-14
申请号：US526722
申请日：1995-09-11
申请人： Robert R. West , Virender Labroo , James R. Piggott , Robert A. Smith , Patricia A. McKernan
发明人： Robert R. West , Virender Labroo , James R. Piggott , Robert A. Smith , Patricia A. McKernan
IPC分类号： A61K31/12 , A61K31/122 , A61K31/22 , A61K31/27 , C12P15/00 , A61K31/21
CPC分类号： A61K31/122 , A61K31/12 , A61K31/22 , A61K31/27 , C12P15/00
摘要： Glucagon antagonists and methods relating thereto are disclosed. The glucagon antagonists include skyrin and skyrin analogs, and serve to inhibit the stimulation of a glucagon-induced response pathway, such as the adenylate cyclase response pathway or the inositol phosphate response pathway. The glucagon antagonists may be used within therapeutic compositions to treat disease states associate with elevated glucose levels, including diabetes and hyperglycemia. The present invention also discloses a biologically pure culture of ATCC accession number 74200, as well as methods relating to the production of glucagon antagonists by cultivating the same in a nutrient medium and recovering the glucagon antagonist therefrom.
摘要翻译：公开了胰高血糖素拮抗剂及其相关方法。胰高血糖素拮抗剂包括天冬氨酸和天冬氨酸类似物，并且用于抑制胰高血糖素诱导的应答途径的刺激，例如腺苷酸环化酶应答途径或肌醇磷酸应答途径。胰高血糖素拮抗剂可用于治疗组合物内以治疗与升高的葡萄糖水平相关的疾病状态，包括糖尿病和高血糖。本发明还公开了ATCC保藏号74200的生物纯纯培养物，以及通过在营养培养基中培养并从其中回收胰高血糖素拮抗剂来产生胰高血糖素拮抗剂的方法。

10. 发明授权

US07323164B2 Use of interleukin-24 to treat ovarian cancer 有权
标题翻译：使用白介素24治疗卵巢癌
公开(公告)号：US07323164B2
公开(公告)日：2008-01-29
申请号：US10410447
申请日：2003-04-08
申请人： Yasmin A. Chandrasekher , Patricia A. McKernan
发明人： Yasmin A. Chandrasekher , Patricia A. McKernan
IPC分类号： A61K45/00 , A61K38/21 , C07K14/54
CPC分类号： A61K31/7048 , A61K31/337 , A61K31/4745 , A61K31/555 , A61K31/675 , A61K31/704 , A61K38/14 , A61K38/164 , A61K38/168 , A61K38/20 , A61K41/0038 , A61K47/642 , A61K2300/00
摘要： The present invention relates to the anti-cancer activity of IL-24 polypeptide molecules. IL-24 is a cytokine involved in inflammatory processes and human disease. The present invention includes Use of IL-24 for decreasing proliferation of ovarian cancer cells, treating ovarian cancer, amongst other uses disclosed. IL-24 polypeptides can be administered alone, or can be fused to cytotoxic moieties, and can be administered in conjunction with radiation or chemotherapeutic agents.
摘要翻译：本发明涉及IL-24多肽分子的抗癌活性。 IL-24是涉及炎症过程和人类疾病的细胞因子。本发明包括使用IL-24降低卵巢癌细胞的增殖，治疗卵巢癌以及所公开的其它用途。 IL-24多肽可以单独施用，或可以与细胞毒素部分融合，并且可以与辐射或化学治疗剂一起施用。

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