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1. 发明授权

US08168650B2 Therapeutic uses of bicyclic ligands of sigma 2 receptor 有权
标题翻译： sigma2受体双环配体的治疗用途
公开(公告)号：US08168650B2
公开(公告)日：2012-05-01
申请号：US12543647
申请日：2009-08-19
申请人： Robert H. Mach , Richard Hotchkiss , William Hawkins , Rebecca Aft , Zhude Tu
发明人： Robert H. Mach , Richard Hotchkiss , William Hawkins , Rebecca Aft , Zhude Tu
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D451/14 , C07D451/02
摘要： A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for σ2 versus σ1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the σ2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors.
摘要翻译：公开了一系列N-取代的9-氮杂双环[3.3.1]壬烷-3α-基苯基氨基甲酸酯类似物及其制备方法。描述了它们对西格玛（＆sgr。1和＆sgr; 2）受体的亲和力。两种新化合物N-（9-（4-氨基丁基）-9-氮杂双环[3.3.1]壬烷-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯和N-（9- 6-氨基己基）-9-氮杂双环[3.3.1]壬烷-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯显示出对于＆ 1受体。所公开的化合物中有生物素化和荧光类似物。这些化合物可以作为第二受体的探针。此外，一些公开的化合物可以通过胱天蛋白酶依赖性和半胱天冬酶非依赖性机制诱导凋亡细胞死亡，并且对于治疗肿瘤是有效的。该化合物可用作化学治疗剂或化学敏化剂，用于治疗各种实体瘤。

2. 发明授权

US07612085B2 Sigma 2 receptor ligands and therapeutic uses therefor 有权
标题翻译： Sigma 2受体配体及其治疗用途
公开(公告)号：US07612085B2
公开(公告)日：2009-11-03
申请号：US11776533
申请日：2007-07-11
申请人： Robert H. Mach , Zhude Tu , Wenhua Chu , Suwanna Vangveravong , Richard Hotchkiss , William Hawkins , Rebecca Aft
发明人： Robert H. Mach , Zhude Tu , Wenhua Chu , Suwanna Vangveravong , Richard Hotchkiss , William Hawkins , Rebecca Aft
IPC分类号： A01N43/42 , A61K31/44 , C07D221/02
CPC分类号： C07D451/14 , C07D451/02
摘要： A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for σ2 versus σ1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the σ2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors.
摘要翻译：公开了一系列N-取代的9-氮杂双环[3.3.1]壬烷-3-基苯基氨基甲酸酯类似物及其制备方法。描述了它们对西格玛（sigma1和sigma2）受体的亲和力。两种新化合物N-（9-（4-氨基丁基）-9-氮杂双环[3.3.1]壬-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯和N-（9- 6-氨基己基）-9-氮杂双环[3.3.1]壬-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯显示出对sigma2与σ1受体的高亲和力和选择性。所公开的化合物中有生物素化和荧光类似物。这些化合物可以作为sigma2受体的探针。此外，一些公开的化合物可以通过胱天蛋白酶依赖性和半胱天冬酶非依赖性机制诱导凋亡细胞死亡，并且对于治疗肿瘤是有效的。这些化合物可用作化学治疗剂或化学敏化剂，用于治疗各种实体瘤。

3. 发明申请

US20100048614A1 THERAPEUTIC USES OF BICYCLIC LIGANDS OF SIGMA 2 RECEPTOR 有权
标题翻译： SIGMA 2受体的双相配体的治疗用途
公开(公告)号：US20100048614A1
公开(公告)日：2010-02-25
申请号：US12543647
申请日：2009-08-19
申请人： Robert H. Mach , Richard Hotchkiss , William Hawkins , Rebecca Aft , Zhude Tu
发明人： Robert H. Mach , Richard Hotchkiss , William Hawkins , Rebecca Aft , Zhude Tu
IPC分类号： A61K31/439 , A61P35/00
CPC分类号： C07D451/14 , C07D451/02
摘要： A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for σ2 versus σ1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the σ2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors.
摘要翻译：公开了一系列N-取代的9-氮杂双环[3.3.1]壬烷-3α-基苯基氨基甲酸酯类似物及其制备方法。描述了它们对西格玛（＆sgr。1和＆sgr; 2）受体的亲和力。两种新化合物N-（9-（4-氨基丁基）-9-氮杂双环[3.3.1]壬烷-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯和N-（9- 6-氨基己基）-9-氮杂双环[3.3.1]壬烷-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯显示出对于＆ 1受体。所公开的化合物中有生物素化和荧光类似物。这些化合物可以作为第二受体的探针。此外，一些公开的化合物可以通过胱天蛋白酶依赖性和半胱天冬酶非依赖性机制诱导凋亡细胞死亡，并且对于治疗肿瘤是有效的。这些化合物可用作化学治疗剂或化学敏化剂，用于治疗各种实体瘤。

4. 发明申请

US20080161343A1 Sigma 2 Receptor Ligands and Therapeutic Uses Therefor 有权
标题翻译： Sigma 2受体配体及其治疗用途
公开(公告)号：US20080161343A1
公开(公告)日：2008-07-03
申请号：US11776533
申请日：2007-07-11
申请人： Robert H. Mach , Zhude Tu , Wenhua Chu , Suwanna Vangveravong , Richard Hotchkiss , William Hawkins , Rebecca Aft
发明人： Robert H. Mach , Zhude Tu , Wenhua Chu , Suwanna Vangveravong , Richard Hotchkiss , William Hawkins , Rebecca Aft
IPC分类号： A61K31/439 , C07D453/02 , C12N5/06 , A61P35/00
CPC分类号： C07D451/14 , C07D451/02
摘要： A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for σ2 versus σ1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the σ2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors.
摘要翻译：公开了一系列N-取代的9-氮杂双环[3.3.1]壬烷-3-基苯基氨基甲酸酯类似物及其制备方法。描述了它们对西格玛（sigma1和sigma2）受体的亲和力。两种新化合物N-（9-（4-氨基丁基）-9-氮杂双环[3.3.1]壬-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯和N-（9- 6-氨基己基）-9-氮杂双环[3.3.1]壬-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯显示出对sigma2与σ1受体的高亲和力和选择性。所公开的化合物中有生物素化和荧光类似物。这些化合物可以作为sigma2受体的探针。此外，一些公开的化合物可以通过胱天蛋白酶依赖性和半胱天冬酶非依赖性机制诱导凋亡细胞死亡，并且对于治疗肿瘤是有效的。这些化合物可用作化学治疗剂或化学敏化剂，用于治疗各种实体瘤。

5. 发明申请

US20050122655A1 Apparatus and method for fusing voltage surge and transient anomalies in a surge suppression device 有权
标题翻译：在浪涌抑制装置中对电压浪涌和瞬态异常进行定影的装置和方法
公开(公告)号：US20050122655A1
公开(公告)日：2005-06-09
申请号：US11003828
申请日：2004-12-03
申请人： Ronald Hotchkiss , Richard Hotchkiss
发明人： Ronald Hotchkiss , Richard Hotchkiss
IPC分类号： H02H9/04 , H02H5/04
CPC分类号： H02H9/044 , H02H9/042
摘要： A circuit board is enclosed in a housing containing rows of metal oxide varistors. Multiple surge ferrule type fuses are soldered directly to circuit board holes between the rows of metal oxide varistors. A ring connector electrically connects pairs of fuses and an electrical conductor connects the ring connector to an electrical circuit to be protected.
摘要翻译：电路板封装在包含行金属氧化物变阻器的外壳中。多个浪涌套管式保险丝直接焊接在金属氧化物变阻器行之间的电路板孔中。环形连接器电连接成对的保险丝，并且电导体将环形连接器连接到要保护的电路。

6. 发明申请

US20100121031A1 MEMBRANE-PERMEANT PEPTIDE COMPLEXES FOR TREATMENT OF SEPSIS 审中-公开
标题翻译：用于治疗SEPSIS的膜 - 渗透肽复合物
公开(公告)号：US20100121031A1
公开(公告)日：2010-05-13
申请号：US12617561
申请日：2009-11-12
申请人： Richard Hotchkiss , David Piwnica-Worms , Jonathan McDunn , Ernesto Bernal-Mizrachi
发明人： Richard Hotchkiss , David Piwnica-Worms , Jonathan McDunn , Ernesto Bernal-Mizrachi
IPC分类号： C07K14/435
CPC分类号： C07K14/005 , A61K47/64 , A61K47/645 , A61K51/088 , C07K14/4747 , C07K2319/10 , C07K2319/50 , C12N2740/16322
摘要： Methods and compositions for treating sepsis and diseases and conditions involving cellular apoptosis using cell membrane-permeant peptide conjugates of a cell membrane permeant peptide together with anti-apoptotic domains of the TCL1 protein are provided.
摘要翻译：提供了使用细胞膜透过肽的细胞膜透过肽缀合物与TCL1蛋白的抗凋亡结构域一起治疗败血症和涉及细胞凋亡的疾病和病症的方法和组合物。

7. 发明申请

US20090012025A1 Methods and Compositions for Treatment of Sepsis 审中-公开
标题翻译：脓毒症治疗方法和组成
公开(公告)号：US20090012025A1
公开(公告)日：2009-01-08
申请号：US12029412
申请日：2008-02-11
申请人： Richard Hotchkiss , Jonathan McDunn , David Piwnica-Worms , Steven Schwulst
发明人： Richard Hotchkiss , Jonathan McDunn , David Piwnica-Worms , Steven Schwulst
IPC分类号： A61K31/7105 , A61P31/04
CPC分类号： A61K47/6455 , A61K47/64 , A61K47/645
摘要： Methods of treatment of sepsis are disclosed. These methods comprise administering to a subject a composition comprising at least one siRNA directed against at least one gene encoding a pro-apoptotic polypeptide. The pro-apoptotic polypeptide, in some aspects, can be other than Fas or caspase-8. In some embodiments, an siRNA can be directed against a pro-apoptotic component of the mitochondrial pathway, such as a pro-apoptotic bcl-2 protein. In some aspects, an siRNA can be directed against a BH3-only bcl-2 protein, while in other aspects, siRNAs can be directed against multi BH domain Bcl-2 family members such as bax and bak. In some embodiments, an siRNA can be directed against a death receptor pathway molecule such as FADD. In various configurations, a composition can also comprise a cationic lipid such as DOTAP, or nanoparticles comprising a cyclodextrin-containing polycation and a polymer such as a poly(ethylene glycol).
摘要翻译：公开了治疗败血症的方法。这些方法包括向受试者施用包含针对至少一种编码促细胞凋亡多肽的基因的至少一种siRNA的组合物。促凋亡多肽在某些方面可能不同于Fas或caspase-8。在一些实施方案中，siRNA可以针对线粒体途径的促凋亡组分，例如促细胞凋亡的bcl-2蛋白。在一些方面，siRNA可以针对仅BH3的bcl-2蛋白，而在其它方面，siRNA可以针对多BH结构域Bcl-2家族成员，例如bax和bak。在一些实施方案中，siRNA可以针对死亡受体途径分子如FADD。在各种构型中，组合物还可以包含阳离子脂质，例如DOTAP，或包含含环糊精的聚阳离子和聚合物如聚（乙二醇）的纳米颗粒。

8. 发明申请

US20060166881A1 Membrane-permeant peptide complexes for treatment of sepsis 有权
标题翻译：用于治疗败血症的膜 - 透性肽复合物
公开(公告)号：US20060166881A1
公开(公告)日：2006-07-27
申请号：US11286920
申请日：2005-11-23
申请人： Richard Hotchkiss , David Piwnica-Worms , Jonathan McDunn
发明人： Richard Hotchkiss , David Piwnica-Worms , Jonathan McDunn
IPC分类号： A61K48/00 , C07K14/475
CPC分类号： C07K14/4747 , A61K38/00 , A61K49/0043 , A61K49/0056 , A61K51/088 , C07K14/005 , C07K14/4702 , C07K2319/10 , C07K2319/21 , C07K2319/50 , C12N2740/16322
摘要： Methods and compositions for treating sepsis using cell membrane-permeant peptide conjugate covalent compounds having target cell specificity are provided.
摘要翻译：提供了使用具有靶细胞特异性的细胞膜透过肽缀合物共价化合物治疗败血症的方法和组合物。

9. 发明授权

US08038984B2 Membrane-permeant peptide complexes for treatment of sepsis 有权
标题翻译：用于治疗败血症的膜 - 透性肽复合物
公开(公告)号：US08038984B2
公开(公告)日：2011-10-18
申请号：US11286920
申请日：2005-11-23
申请人： Richard Hotchkiss , David Piwnica-Worms , Jonathan McDunn
发明人： Richard Hotchkiss , David Piwnica-Worms , Jonathan McDunn
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07K14/4747 , A61K38/00 , A61K49/0043 , A61K49/0056 , A61K51/088 , C07K14/005 , C07K14/4702 , C07K2319/10 , C07K2319/21 , C07K2319/50 , C12N2740/16322
摘要： Methods and compositions for treating sepsis using cell membrane-permeant peptide conjugate covalent compounds having target cell specificity are provided.
摘要翻译：提供了使用具有靶细胞特异性的细胞膜透过肽缀合物共价化合物治疗败血症的方法和组合物。

10. 发明授权

US07417841B2 Apparatus and method for fusing voltage surge and transient anomalies in a surge suppression device 有权
标题翻译：在浪涌抑制装置中对电压浪涌和瞬态异常进行定影的装置和方法
公开(公告)号：US07417841B2
公开(公告)日：2008-08-26
申请号：US11003828
申请日：2004-12-03
申请人： Ronald Hotchkiss , Richard Hotchkiss
发明人： Ronald Hotchkiss , Richard Hotchkiss
IPC分类号： H02H5/04 , H02H3/22
CPC分类号： H02H9/044 , H02H9/042
摘要： A circuit board is enclosed in a housing containing rows of metal oxide varistors. Multiple surge ferrule type fuses are soldered directly to circuit board holes between the rows of metal oxide varistors. A ring connector electrically connects pairs of fuses and an electrical conductor connects the ring connector to an electrical circuit to be protected.
摘要翻译：电路板封装在包含行金属氧化物变阻器的外壳中。多个浪涌套管式保险丝直接焊接在金属氧化物变阻器行之间的电路板孔中。环形连接器电连接成对的保险丝，并且电导体将环形连接器连接到要保护的电路。

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