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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：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％。
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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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4.发明授权公开(公告)号：US06998385B2
公开(公告)日：2006-02-14
申请号：US10274255
申请日：2002-10-17
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％。
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公开(公告)号：US20110136744A1
公开(公告)日：2011-06-09
申请号：US12941907
申请日：2010-11-08
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。
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公开(公告)号：US07060672B2
公开(公告)日：2006-06-13
申请号：US10274419
申请日：2002-10-17
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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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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8.发明申请公开(公告)号：US20130078280A1
公开(公告)日：2013-03-28
申请号：US13684574
申请日：2012-11-26
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％。
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公开(公告)号：US07829533B2
公开(公告)日：2010-11-09
申请号：US12197199
申请日：2008-08-22
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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公开(公告)号：US20090054311A1
公开(公告)日：2009-02-26
申请号：US12197199
申请日：2008-08-22
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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