专利检索 ap:("M. Robert Leanna" OR "Steven M. Hannick" OR "Michael Rasmussen" OR "Jien-Heh J. Tien" OR "Lakshmi Bhagavatula" OR "Pulla Reddy Singam" OR "Bradley D. Gates" OR "Lawrence Kolaczkowski" OR "Ramesh R. Patel" OR "Greg Wayne" OR "Greg Lannoye" OR "Weijiang Zhang" OR "Zhenping Tian" OR "Kirill A. Lukin" OR "Bikshandarkoil A. Narayanan" OR "David A. Riley" OR "Howard Morton" OR "Sou-Jen Chang" OR "Cynthia B. Curty" OR "Daniel Plata" OR "John Bellettini" OR "Bhadra Shelat" OR "Tiffany Spitz" OR "Cheng-Xi Yang") AND inv:"John Bellettini" 第 1 页

1.

发明授权
Synthesis of acyclic nucleoside derivatives 有权
标题翻译：无环核苷衍生物的合成

公开(公告)号：US06184376B2

公开(公告)日：2001-02-06

申请号：US09130214

申请日：1998-08-06

申请人： M. Robert Leanna , Steven M. Hannick , Michael Rasmussen , Jien-Heh J. Tien , Lakshmi Bhagavatula , Pulla Reddy Singam , Bradley D. Gates , Lawrence Kolaczkowski , Ramesh R. Patel , Greg Wayne , Greg Lannoye , Weijiang Zhang , Zhenping Tian , Kirill A. Lukin , Bikshandarkoil A. Narayanan , David A. Riley , Howard Morton , Sou-Jen Chang , Cynthia B. Curty , Daniel Plata , John Bellettini , Bhadra Shelat , Tiffany Spitz , Cheng-Xi Yang

发明人： M. Robert Leanna , Steven M. Hannick , Michael Rasmussen , Jien-Heh J. Tien , Lakshmi Bhagavatula , Pulla Reddy Singam , Bradley D. Gates , Lawrence Kolaczkowski , Ramesh R. Patel , Greg Wayne , Greg Lannoye , Weijiang Zhang , Zhenping Tian , Kirill A. Lukin , Bikshandarkoil A. Narayanan , David A. Riley , Howard Morton , Sou-Jen Chang , Cynthia B. Curty , Daniel Plata , John Bellettini , Bhadra Shelat , Tiffany Spitz , Cheng-Xi Yang

IPC分类号： C07D47318

CPC分类号： C07D473/00 , C07C309/73 , C07D473/18 , Y02P20/55

摘要： Methods and novel intermediates of the formula: wherein R6 and R7 are lower alkyl or benzyl or R6 and R7 taken together are —CH2CH2—, —CH2CH2CH2— or —CH2CH2CH2CH2CH2—, R8 is C1-C21 alkyl or a C2-C21 monounsaturated alkenyl, which may optionally be substituted with substitution substituents independently selected from the group consisting of hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy C1-C6 alkyl, C1-C6 alkanoyl, amino, halo, cyano, azido, oxo, mercapto and nitro, and R9 is an alcohol protecting group. The intermediates are useful for the preparation of acyclic nucleoside derivatives of the formula: where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a —C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl and R3 is OH or H; or a pharmaceutically acceptable salt thereof.

摘要翻译： 下式的方法和新型中间体：其中R6和R7是低级烷基或苄基或R6和R7一起是-CH 2 CH 2 - ， - CH 2 CH 2 CH 2 - 或-CH 2 CH 2 CH 2 CH 2 CH 2 - ，R 8是C 1 -C 21烷基或C 2 -C 21单不饱和链烯基，其可以任选地被独立地选自羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6烷氧基C 1 -C 6烷基，C 1 -C 6烷酰基，氨基，卤素，氰基，叠氮基，氧代，巯基和硝基，R9是醇保护基。中间体可用于制备下式的无环核苷衍生物：其中R 1和R 2中的一个是氨基酸酰基，R 1和R 2中的另一个是-C（O）C 3 -C 21饱和或单不饱和的，任选取代的烷基和R 3是OH或H; 或其药学上可接受的盐。

2.

发明授权
Synthesis of acyclic nucleoside derivatives 失效
标题翻译：无环核苷衍生物的合成

公开(公告)号：US07189849B2

公开(公告)日：2007-03-13

申请号：US11131646

申请日：2005-05-18

申请人： M. Robert Leanna , Michael Rasmussen , Steven M. Hannick , Jien-Heh J. Tien , Kirill A. Lukin , Zhenping Tian , Sou-Jen Chang , Cynthia B. Curty , Bikshandarkoil A. Narayanan , John Bellettini , Bhadra Shelat , Tiffany Spitz

发明人： M. Robert Leanna , Michael Rasmussen , Steven M. Hannick , Jien-Heh J. Tien , Kirill A. Lukin , Zhenping Tian , Sou-Jen Chang , Cynthia B. Curty , Bikshandarkoil A. Narayanan , John Bellettini , Bhadra Shelat , Tiffany Spitz

IPC分类号： C07D473/18 , C07D473/40 , C07F7/18 , C07C69/66

CPC分类号： C07D473/00 , C07C309/73 , C07D473/18 , Y02P20/55

摘要： Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.

摘要翻译： 合成抗病毒伐莫西洛维硬脂酸酯的新方法，其中将酯化的鸟嘌呤缩醛还原成相应的醇，与活化的氨基酸反应并进行N-去保护。酯化鸟嘌呤缩醛由带有无环羟甲基丁缩醛的9-鸟嘌呤衍生物制备。这些过程可以修改为一锅反应。