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公开(公告)号：US07141648B2
公开(公告)日：2006-11-28
申请号：US10274437
申请日：2002-10-17
申请人： Selvaraj A. Naicker , Randall W. Yatscoff , Robert T. Foster , Mark Abel , Seetharaman Jayaraman , Hans-Jürgen Mair , Jean-Michel Adam , Bruno Lohri
发明人： Selvaraj A. Naicker , Randall W. Yatscoff , Robert T. Foster , Mark Abel , Seetharaman Jayaraman , Hans-Jürgen Mair , Jean-Michel Adam , Bruno Lohri
CPC分类号： C07K7/645 , A61K9/0095 , A61K9/1075 , A61K9/4858 , A61K38/00 , A61K38/13 , B82Y5/00 , C07K7/64 , Y10S530/806
摘要： The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. Stereoselective pathways may utilize a Wittig reaction, or an organometallic reagent comprising inorganic elements such as boron, silicon, titanium, and lithium. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.
摘要翻译： 本发明涉及结构类似于环孢霉素A的环孢菌素类似物的异构体混合物。该混合物具有比单个异构体和天然存在的和其它目前已知的环孢菌素和环孢菌素衍生物更强的功效和降低的毒性。 本发明的实施方案涉及被称为ISA 247的环孢菌素A类似物及其衍生物的顺式和反式异构体。 通过立体选择性途径合成烷基化，芳基化和氘代衍生物，其中反应的特定条件决定了立体选择性的程度。 立体选择性途径可以利用维蒂希反应或包含无机元素如硼，硅，钛和锂的有机金属试剂。 基于混合物的总重量，混合物中异构体的比例可以为（E） - 异构体的约10至90重量％至（Z） - 异构体的约90至10重量％。
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公开(公告)号：US06780995B2
公开(公告)日：2004-08-24
申请号：US10303048
申请日：2002-11-25
IPC分类号： C07D47104
CPC分类号： C07D213/86 , A61K31/166 , A61K31/426 , A61K31/4409 , A61K31/4745 , C07C233/65 , C07C233/78 , C07C237/30 , C07D213/87 , C07D277/46 , C07D285/135 , C07D311/16
摘要： A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.
摘要翻译： 一系列活化的碘代苯甲酰胺衍生物被描述为抗肿瘤和抗病毒药物化合物。 化合物通常具有螯合基团，硫醇捕获基团和活化基团。 预防癌细胞和病毒复制的推定机制是通过抑制转录因子与锌指结合结构域的结合。 该化合物在低浓度下有效抑制各种人和动物肿瘤和白血病细胞系的生长。
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23.发明授权公开(公告)号：US06602715B2
公开(公告)日：2003-08-05
申请号：US10228276
申请日：2002-08-27
IPC分类号： G01N3700
CPC分类号： A61K51/1206 , A61B5/0813 , A61B5/0836 , A61B5/14532 , G01N33/497 , Y10T436/104998 , Y10T436/13 , Y10T436/24 , Y10T436/25875
摘要： A breath test and kit for performing the breath test are described for the diagnosis of diabetic indications and monitoring of glycemic control. The breath test utilizes the measurement of expired 13C-labeled CO2 following the ingestion of a 13C-enriched glucose source.
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公开(公告)号：US06511988B2
公开(公告)日：2003-01-28
申请号：US09925814
申请日：2001-08-10
IPC分类号： A61K31437
CPC分类号： C07D213/86 , A61K31/166 , A61K31/426 , A61K31/4409 , A61K31/4745 , C07C233/65 , C07C233/78 , C07C237/30 , C07D213/87 , C07D277/46 , C07D285/135 , C07D311/16
摘要： A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.
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公开(公告)号：US06342507B1
公开(公告)日：2002-01-29
申请号：US09348015
申请日：1999-07-06
IPC分类号： C07D49116
CPC分类号： C07D498/18 , A61L31/16 , A61L2300/416
摘要： The synthesis of deuterated analogues of rapamycin is disclosed together with a method for use for inducing immunosupression and in the treatment of transplantation rejection, graft vs host disease, autoimmune diseases, diseases of inflammation leukemia/lymphoma, solid tumors, fungal infections, hyperproliferative vascular disorders. Also described is a method for the synthesis of water soluble deuteratred rapamycin compounds and their use as described above.
摘要翻译： 公开雷帕霉素的氘代类似物的合成以及用于诱导免疫抑制的方法和用于治疗移植排斥反应，移植物抗宿主病，自身免疫性疾病，炎症性白血病/淋巴瘤疾病，实体瘤，真菌感染，过度增殖性血管疾病 。 还描述了合成水溶性氘化雷帕霉素化合物的方法及其用途如上所述。
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公开(公告)号：US20110092669A1
公开(公告)日：2011-04-21
申请号：US12977602
申请日：2010-12-23
申请人： Selvaraj A. Naicker , Randall W. Yatscoff , Robert T. Foster , Mark Abel , Seetharaman Jayaraman , Hans-Jurgen Mair , Jean-Michel Adam , Bruno Lohri
发明人： Selvaraj A. Naicker , Randall W. Yatscoff , Robert T. Foster , Mark Abel , Seetharaman Jayaraman , Hans-Jurgen Mair , Jean-Michel Adam , Bruno Lohri
IPC分类号： C07K1/107
CPC分类号： C07K7/645 , A61K9/0095 , A61K9/1075 , A61K9/4858 , A61K38/13 , A61K47/10
摘要： The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. Stereoselective pathways may utilize a Wittig reaction, or an organometallic reagent comprising inorganic elements such as boron, silicon, titanium, and lithium. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.
摘要翻译： 本发明涉及结构类似于环孢霉素A的环孢菌素类似物的异构体混合物。该混合物具有比单个异构体和天然存在的和其它目前已知的环孢菌素和环孢菌素衍生物更强的功效和降低的毒性。 本发明的实施方案涉及称为ISATX247的环孢菌素A类似物的顺式和反式异构体及其衍生物。 ISATX247异构体和烷基化，芳基化和氘代衍生物通过立体选择性途径合成，其中反应的特定条件决定了立体选择性的程度。 立体选择性途径可以利用维蒂希反应或包含无机元素如硼，硅，钛和锂的有机金属试剂。 基于混合物的总重量，混合物中异构体的比例可以为（E） - 异构体的约10至90重量％至（Z） - 异构体的约90至10重量％。
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27.发明申请公开(公告)号：US20100311944A1
公开(公告)日：2010-12-09
申请号：US12796616
申请日：2010-06-08
IPC分类号： C07K7/64
CPC分类号： C07K7/645 , A61K9/0095 , A61K9/1075 , A61K9/4858 , A61K38/00 , A61K38/13 , B82Y5/00 , C07K7/64 , Y10S530/806
摘要： The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. Mixtures of ISATX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.
摘要翻译： 本发明涉及结构类似于环孢霉素A的环孢菌素类似物的异构体混合物。该混合物具有比单个异构体和天然存在的和其它目前已知的环孢菌素和环孢菌素衍生物更强的功效和降低的毒性。 本发明的实施方案涉及称为ISATX247的环孢菌素A类似物的顺式和反式异构体及其衍生物。 ISATX247异构体的混合物显示与天然存在的和目前已知的环孢菌素相比，其效力和毒性降低的组合。 ISATX247异构体和烷基化，芳基化和氘代衍生物通过立体选择性途径合成，其中反应的特定条件决定了立体选择性的程度。 基于混合物的总重量，混合物中异构体的比例可以为（E） - 异构体的约10至90重量％至（Z） - 异构体的约90至10重量％。
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公开(公告)号：US20090318336A1
公开(公告)日：2009-12-24
申请号：US12427692
申请日：2009-04-21
CPC分类号： C07K7/645 , A61K38/00 , C07B59/008 , C07K1/13 , C07K7/64 , Y10S530/806 , Y10S530/807
摘要： Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.
摘要翻译： 公开了与天然存在的和其他目前已知的环孢菌素和环孢菌素衍生物相比具有增强的功效和降低的毒性的环孢菌素衍生物。 本发明的环孢菌素衍生物通过以下方式通过环孢菌素A（CsA）分子的化学和同位素取代产生：（1）氨基酸1的化学取代和任选的氘取代; 和（2）在环孢菌素A分子的代谢关键位置的氘代替，例如氨基酸1,4,9。还公开了产生环孢菌素衍生物的方法和与所公开的环孢菌素衍生物一起产生具有降低的毒性的免疫抑制的方法。
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公开(公告)号：US07429562B2
公开(公告)日：2008-09-30
申请号：US11375532
申请日：2006-03-13
IPC分类号： A61K38/13
CPC分类号： A61K9/1075 , A61K9/0095 , A61K9/4858 , A61K38/13 , A61K47/10
摘要： The present invention relates to formulations containing cyclosporin analogs that are structurally similar to cyclosporin A, in particular isomeric mixtures of cyclosporin analogs that are structurally similar to cyclosporin A. The formulations form stable microemulsion preconcentrates and may provide superior drug bioavailability and/or may reduce one or more adverse effects associated with the administration of cyclosporin. Also disclosed are methods for using and preparing the formulations.
摘要翻译： 本发明涉及结构上类似于环孢菌素A的环孢菌素类似物的制剂，特别是在结构上类似于环孢菌素A的环孢菌素类似物的异构体混合物中。制剂形成稳定的微乳液预浓缩物，并可提供优异的药物生物利用度和/或减少一种 或更多与施用环孢菌素相关的不良反应。 还公开了使用和制备制剂的方法。
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30.发明授权13C glucose breath test for the diagnosis of diabetic indications and monitoring glycemic control 失效13C葡萄糖呼吸试验用于诊断糖尿病适应症并监测血糖控制公开(公告)号：US07118919B2
公开(公告)日：2006-10-10
申请号：US11069169
申请日：2005-02-28
IPC分类号： G01N37/00
CPC分类号： A61K51/1206 , A61B5/0813 , A61B5/0836 , A61B5/14532 , G01N33/497 , Y10T436/104998 , Y10T436/13 , Y10T436/24 , Y10T436/25875
摘要： Use of 13C glucose in an analytical assay to monitor glucose metabolism by measurement of labeled exhaled CO2 is provided. A breath test and kit for performing the breath test are described for the diagnosis of diabetic indications and monitoring of glycemic control. The breath test utilizes the measurement of expired 13C-labeled CO2 following the ingestion of a 13C-enriched glucose source.
摘要翻译： 提供了在分析测定中使用13 C葡萄糖以通过测量标记的呼出的CO 2 2监测葡萄糖代谢。 描述了用于进行呼吸试验的呼吸试验和试剂盒，用于诊断糖尿病适应症和监测血糖控制。 呼吸试验利用了摄入富含13 C的葡萄糖源后测量过期的13 C-标记的CO 2。
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