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1.发明授权Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 有权制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法公开(公告)号：US06215017B1
公开(公告)日：2001-04-10
申请号：US09497537
申请日：2000-02-03
申请人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
发明人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
IPC分类号： C07C67743
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： Intermediates of Formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译： 式（III）的中间体，其中Y1是酰氧基，其中酰基是式RC（O） - ，其中R是1-6个碳原子的烷基，Y2是芳烷氧基，Z是苯甲酰氧基或酰氧基，其中酰基如所定义 式（III）的中间体可用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1的单-L-缬氨酸酯的新方法 ，3-丙二醇（更昔洛韦）。 更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。
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2.发明授权Process for preparing a 2-(2-amino-1, 6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 有权制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法公开(公告)号：US06340756B1
公开(公告)日：2002-01-22
申请号：US09497319
申请日：2000-02-03
申请人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
发明人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
IPC分类号： C07D47318
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： wherein Z1 is hydrogen or an amino-protecting group selected from the group consisting of acyl of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms; trityl, optionally substituted with methoxy; and N-(9-fluorenylmethoxycarbonyl); Y1 is halo, aralkyloxy or acyloxy, wherein acyl is as defined above; and Y2 is aralkyloxy. These intermediates are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译： 其中Z1是氢或选自式R-C（O） - 的酰基的氨基保护基，其中R是1-6个碳原子的烷基; 三苯甲基，任选被甲氧基取代; 和N-（9-芴基甲氧基羰基）; Y1是卤素，芳烷氧基或酰氧基，其中酰基如上所定义; 而Y2是芳烷氧基。 这些中间体可用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇（更昔洛韦）的单-L-缬氨酸酯的新方法 ）。 更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。
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3.发明授权Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 有权制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法公开(公告)号：US06218568B1
公开(公告)日：2001-04-17
申请号：US09497538
申请日：2000-02-03
申请人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
发明人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
IPC分类号： C07C67743
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： Process for preparing intermediates of formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译： 制备式（III）的中间体的方法，其中Y1是酰氧基，其中酰基是式RC（O） - ，其中R是1-6个碳原子的烷基，Y2是芳烷氧基，Z是苯甲酰氧基或酰氧基，其中酰基 式（III）的中间体可用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基） - 的单-L-缬氨酸酯的新方法， 甲氧基-1,3-丙二醇（更昔洛韦）。 更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。
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4.发明授权Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3-propanediol derivative 失效制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US6040446A
公开(公告)日：2000-03-21
申请号：US127380
申请日：1998-07-31
申请人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
发明人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
IPC分类号： C07D473/00 , C07D473/18
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： Process and novel intermediates for preparing the L-mono-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts. The present process and intermediates provide for reduced impurities in the mono-valine ester end-product and lower overall production costs. The process involves the condensation of a silylated guanine compound with a substituted glycerol derivative and esterification of this product with an L-valine derivative. These mono-valine products are of value as antiviral agents with improved absorption.
摘要翻译： 用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇的L-缬氨酸酯的方法和新型中间体及其药学上可接受的盐。 本方法和中间体提供了单缬氨酸酯最终产物中减少的杂质，降低了总体生产成本。 该方法包括将甲硅烷基化鸟嘌呤化合物与取代的甘油衍生物缩合，并将该产物与L-缬氨酸衍生物酯化。 这些单缬氨酸产品具有改善吸收的抗病毒剂的价值。
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5.发明授权Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 失效制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US6103901A
公开(公告)日：2000-08-15
申请号：US121446
申请日：1998-07-23
CPC分类号： C07D473/18 , Y02P20/55
摘要： Intermediates of Formula (III) ##STR1## wherein P.sup.1 is hydrogen or an amino-protecting group, R is lower alkyl, allyl or aralkyl, and Z is hydrogen, lower alkyl, aryl or aralkyl; and Formula (VI) ##STR2## wherein P.sup.1 is hydrogen or an amino-protecting group, P.sup.2 is an amino protecting group, and Z is hydrogen, lower alkyl, aryl or aralkyl, are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译： 其中P1为氢或氨基保护基的式（III）中间体，R为低级烷基，烯丙基或芳烷基，Z为氢，低级烷基，芳基或芳烷基; 和式（VI）其中P1是氢或氨基保护基，P2是氨基保护基，Z是氢，低级烷基，芳基或芳烷基，可用于制备单-L-缬氨酸酯的新方法 的2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇（更昔洛韦）。 更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。
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6.发明授权Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 失效制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US5840890A
公开(公告)日：1998-11-24
申请号：US775424
申请日：1997-01-09
CPC分类号： C07D473/18 , Y02P20/55
摘要： Process and novel intermediates for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol ganciclovir) and its pharmaceutically acceptable salts. The present process and monoester intermediates provide for mono-esterification by an L-valine derivative, resulting in a monocarboxylate-monovalinate which is then selectively hydrolyzed under basic or enzymatic conditions to give the monovaline ester of ganciclovir in high yield and purity. These products are of value as antiviral agents with improved absorption.
摘要翻译： 用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇更昔洛韦的单-L-缬氨酸酯的方法和新型中间体及其药学上可接受的 盐。 本方法和单酯中间体通过L-缬氨酸衍生物提供单酯化，得到单羧酸酯 - 单戊酸酯，然后在碱性或酶条件下选择性水解，以高产率和纯度得到更昔洛韦的单戊酸酯。 这些产品具有改善吸收的抗病毒药物的价值。
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7.发明授权Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 失效制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US5756736A
公开(公告)日：1998-05-26
申请号：US592283
申请日：1996-01-26
IPC分类号： C07D473/18
CPC分类号： C07D473/18
摘要： Process for preparing the L-monovaline ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts. The present process provides an N,O-bis-trityl intermediate of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol which allows for mono-esterification by an L-valine derivative. These products are of value as antiviral agents with improved absorption.
摘要翻译： 制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇的L-缬氨酸酯及其可药用盐的方法。 本方法提供2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇的N，O-双三苯甲基中间体，其允许单酯化 通过L-缬氨酸衍生物。 这些产品具有抗病毒药物的价值，具有改善的吸收。
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公开(公告)号：US5948939A
公开(公告)日：1999-09-07
申请号：US870841
申请日：1992-04-20
IPC分类号： C07C279/14 , C07K5/02 , C07K5/068 , C07C229/18 , C07C229/26
CPC分类号： C07K5/0222 , C07C279/14 , C07K5/06086
摘要： An .omega.-guanidino-.alpha.-amino-acid (or its functional derivative) or a compound containing it may be prepared by the reaction of the .omega.-amino group of an .alpha.,.omega.-diamino acid (or its functional derivative) or a compound containing it with a formamidinesulfonic acid.
摘要翻译： ω-胍基-α-氨基酸（或其功能衍生物）或含有它的化合物可以通过α，ω-二氨基酸（或其官能衍生物）或化合物 含有甲酰胺磺酸。
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9.发明授权Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3-propanediol valinate 失效制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇缬氨酸酯的方法
公开(公告)号：US5700936A
公开(公告)日：1997-12-23
申请号：US592080
申请日：1996-01-26
申请人： Humberto B. Arzeno
发明人： Humberto B. Arzeno
IPC分类号： C07D473/18 , C07B43/06
CPC分类号： C07D473/18
摘要： Process for preparing the L-monovaline ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts. The present process relates to an improved process whereby ganciclovir is esterified with an L-valine derivative to provide a di-valine ganciclovir intermediate. Removal of one of the valine groups with a lower alkyl amine, benzylamine or benzyl methylamine provides the mono-valine ester compound of Formula I. These products are of value as antiviral agents with improved absorption.
摘要翻译： 制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇的L-缬氨酸酯及其可药用盐的方法。 本方法涉及一种改进方法，其中更昔洛韦与L-缬氨酸衍生物酯化以提供二缬氨酸更昔洛韦中间体。 用低级烷基胺，苄胺或苄基甲胺除去缬氨酸基团之一提供了式I的单缬氨酸酯化合物。这些产品具有改善吸收的抗病毒剂的价值。
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