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1. 发明申请

US20130078280A1 CYCLOSPORINE ANALOGUE MIXTURES AND THEIR USE AS IMMUNOMODULATING AGENTS 审中-公开
标题翻译：环孢素类似物混合物及其作为免疫调节剂的使用
公开(公告)号：US20130078280A1
公开(公告)日：2013-03-28
申请号：US13684574
申请日：2012-11-26
申请人： Selvaraj A. Naicker , Randall W. Yatscoff , Robert T Foster
发明人： Selvaraj A. Naicker , Randall W. Yatscoff , Robert T Foster
IPC分类号： A61K38/13
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％。

2. 发明授权

US07829533B2 Cyclosporin analog formulations 有权
标题翻译：环孢菌素类似物制剂
公开(公告)号：US07829533B2
公开(公告)日：2010-11-09
申请号：US12197199
申请日：2008-08-22
申请人： Selvaraj A. Naicker , Randall W. Yatscoff , Robert T. Foster
发明人： Selvaraj A. Naicker , Randall W. Yatscoff , Robert T. Foster
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。

3. 发明申请

US20090054311A1 Novel Cyclosporin Analog Formulations 有权
标题翻译：新型环孢菌素类似物制剂
公开(公告)号：US20090054311A1
公开(公告)日：2009-02-26
申请号：US12197199
申请日：2008-08-22
申请人： Selvaraj A. Naicker , Randall W. Yatscoff , Robert T. Foster
发明人： Selvaraj A. Naicker , Randall W. Yatscoff , Robert T. Foster
IPC分类号： A61K38/13 , A61P37/06
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。

4. 发明申请

US20080171850A1 Cyclosporine Analogue Mixtures and their Use as Immunomodulating Agents 审中-公开
标题翻译：环孢霉素类似物混合物及其作为免疫调节剂的用途
公开(公告)号：US20080171850A1
公开(公告)日：2008-07-17
申请号：US11969174
申请日：2008-01-03
申请人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
发明人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
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。 ISA 247异构体的混合物显示了与天然存在的和目前已知的环孢菌素相比增强的效力和降低的毒性的组合。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。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％。

5. 发明授权

US07141648B2 Synthesis of cyclosporin analogs 有权
标题翻译：环孢菌素类似物的合成
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
IPC分类号： C07K1/00 , C07K1/107 , A61K38/13
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％。

6. 发明授权

US06780995B2 Activated iododerivatives for the treatment of cancer and aids 失效
标题翻译：活化的碘衍生物用于治疗癌症和辅助物质
公开(公告)号：US06780995B2
公开(公告)日：2004-08-24
申请号：US10303048
申请日：2002-11-25
申请人： Randall W. Yatscoff , Robert T. Foster , Selvaraj Naicker
发明人： Randall W. Yatscoff , Robert T. Foster , Selvaraj Naicker
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。

7. 发明授权

US06602715B2 13C glucose breath test for the diagnosis of diabetic indications and monitoring glycemic control 失效
公开(公告)号：US06602715B2
公开(公告)日：2003-08-05
申请号：US10228276
申请日：2002-08-27
申请人： Randall W. Yatscoff , Robert T. Foster , Launa J. Aspeslet , Richard Lewanczuk
发明人： Randall W. Yatscoff , Robert T. Foster , Launa J. Aspeslet , Richard Lewanczuk
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.

8. 发明授权

US06511988B2 Activated iododerivatives for the treatment of cancer and aids 失效
公开(公告)号：US06511988B2
公开(公告)日：2003-01-28
申请号：US09925814
申请日：2001-08-10
申请人： Randall W. Yatscoff , Robert T. Foster , Selvaraj Naicker
发明人： Randall W. Yatscoff , Robert T. Foster , Selvaraj Naicker
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.

9. 发明授权

US06476058B2 Methods of pharmacological treatment using S(−) amlodipine 失效
标题翻译：使用S（ - ）氨氯地平进行药理学治疗的方法
公开(公告)号：US06476058B2
公开(公告)日：2002-11-05
申请号：US09987661
申请日：2001-11-15
申请人： Robert T. Foster
发明人： Robert T. Foster
IPC分类号： A61K3144
CPC分类号： C07D211/90 , C07B2200/05
摘要： Methods and compositions are disclosed utilizing the optically pure S(−) isomer of amlodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the administration of the racemic mixture of amlodipine. The S(−) isomer of amlodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of S(−) amlodipine as a calcium channel antagonist without the concomitant liability of adverse effects associated with the racemic mixture of amlodipine.
摘要翻译：公开了使用旋光纯的氨氯地平的S（ - ）异构体的方法和组合物。该化合物是用于治疗高血压的有效药物，同时避免与施用氨氯地平的外消旋混合物相关的副作用的伴随责任。氨氯地平的S（ - ）异构体也可用于治疗心绞痛和其他可能与S（ - ）氨氯地平作为钙通道拮抗剂的活性有关的其他病症，而与外消旋混合物有关的不良反应伴随起作用的氨氯地平。

10. 发明授权

US06342507B1 Deuterated rapamycin compounds, method and uses thereof 失效
标题翻译：氘代雷帕霉素化合物，其方法和用途
公开(公告)号：US06342507B1
公开(公告)日：2002-01-29
申请号：US09348015
申请日：1999-07-06
申请人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
发明人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
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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