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1. 发明申请

US20100062976A1 Synthesis of Cyclosporin Analogs 审中-公开
标题翻译：环孢菌素类似物的合成
公开(公告)号：US20100062976A1
公开(公告)日：2010-03-11
申请号：US12555787
申请日：2009-09-08
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： 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％。

2. 发明申请

US20110092669A1 SYNTHESIS OF CYCLOSPORIN ANALOGS 审中-公开
标题翻译： CYPOSPORIN类似物的合成
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％。

3. 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％。

4. 发明授权

US06998385B2 Cyclosporine analogue mixtures and their use as immunomodulating agents 有权
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：US06998385B2
公开(公告)日：2006-02-14
申请号：US10274255
申请日：2002-10-17
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. 发明申请

US20110136744A1 CYCLOSPORIN ANALOG FORMULATIONS 审中-公开
标题翻译：环磷酰胺类似物制剂
公开(公告)号：US20110136744A1
公开(公告)日：2011-06-09
申请号：US12941907
申请日：2010-11-08
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 disclosure 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：本公开内容涉及在结构上类似于环孢菌素A的环孢菌素类似物的制剂，特别是在环孢菌素类似物的结构上类似于环孢菌素A的异构体混合物中。制剂形成稳定的微乳液预浓缩物并且可以提供优异的药物生物利用度和/或可以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。

6. 发明授权

US07060672B2 Cyclosporin analog formulations 有权
标题翻译：环孢菌素类似物制剂
公开(公告)号：US07060672B2
公开(公告)日：2006-06-13
申请号：US10274419
申请日：2002-10-17
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。

7. 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。

8. 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。

9. 发明授权

US07429562B2 Cyclosporin analog formulations 有权
标题翻译：环孢菌素类似物制剂
公开(公告)号：US07429562B2
公开(公告)日：2008-09-30
申请号：US11375532
申请日：2006-03-13
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。

10. 发明授权

US07160867B2 Rapamycin carbohydrate derivatives 失效
标题翻译：雷帕霉素碳水化合物衍生物
公开(公告)号：US07160867B2
公开(公告)日：2007-01-09
申请号：US10845747
申请日：2004-05-13
申请人： Mark Abel , Roman Szweda , Daniel Trepanier , Randall W Yatscoff , Robert T. Foster
发明人： Mark Abel , Roman Szweda , Daniel Trepanier , Randall W Yatscoff , Robert T. Foster
IPC分类号： A61K31/70 , A61K31/44 , C07H15/00 , C07D487/00 , A61F13/00
CPC分类号： A61K31/7052 , A61K31/436 , C07D498/18 , C07H15/04 , C07H19/01
摘要： This invention provides modified rapamycins that have specific monosaccharide(s), oligosaccharide(s), pseudosugar(s) or derivatives thereof attached through a linker to create rapamycin carbohydrate derivatives having enhanced pharmacokinetic and/or pharmacodynamic profiles. For example, administration of the rapamycin carbohydrate derivative results in altered pharmacokinetic profiles and reduced toxicities. Thus, the present invention provides compounds with characteristics that are distinct from other drugs in its class such as rapamycin.
摘要翻译：本发明提供了具有通过连接体连接的具有增强的药代动力学和/或药效学特征的雷帕霉素碳水化合物衍生物的特异性单糖，寡糖，假糖或其衍生物的修饰的雷帕霉素。例如，雷帕霉素碳水化合物衍生物的施用导致药代动力学特征改变和毒性降低。因此，本发明提供具有与其同类其他药物不同的特征的化合物，例如雷帕霉素。

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