公开(公告)号：EP1751087B1

公开(公告)日：2012-06-27

申请号：EP05758073.0

申请日：2005-06-03

申请人： XenoPort, Inc.

发明人： XIANG, Jia-Ning ,  GALLOP, Mark, A. ,  ZHOU, Cindy, X. ,  NGUYEN, Mark ,  DAI, Xuedong ,  LI, Jianhua ,  CUNDY, Kenneth, C. ,  JUMBE, Nelson, L.

IPC分类号： C07C229/36 ,  C07C235/60 ,  C07D213/80 ,  C07D213/79 ,  A61K31/216 ,  A61K31/24 ,  A61K31/618 ,  A61K31/609 ,  A61K31/455 ,  A61K31/4409 ,  A61P25/16

CPC分类号： C07C235/60 ,  C07C229/34 ,  C07C229/36 ,  C07C235/48 ,  C07C2601/14 ,  C07D213/79 ,  C07D213/80 ,  C07D213/803

摘要： Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed. Wherein Q is selected from X-CO-, and -CO-X-; X is selected from-O-, and -NR6-; n is an integer from 2 to 4; R5 is selected from hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, cycloalkyl, substituted cycloalkyl, heteroalkyl, substituted heteroalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, and substituted heteroarylalkyl; and when Q is -X--CO-, R5 is further selected from alkoxy, substituted alkoxy, cycloalkoxy, and substituted cycloalkoxy.

摘要翻译： 公开了左旋多巴的前药，制备左旋多巴的前药的方法，使用左旋多巴的前药的方法和左旋多巴的前药组合物。

公开(公告)号：EP1751087A1

公开(公告)日：2007-02-14

申请号：EP05758073.0

申请日：2005-06-03

申请人： Xenoport, Inc.

发明人： XIANG, Jia-Ning ,  GALLOP, Mark, A. ,  ZHOU, Cindy, X. ,  NGUYEN, Mark ,  DAI, Xuedong ,  LI, Jianhua ,  CUNDY, Kenneth, C. ,  JUMBE, Nelson, L.

IPC分类号： C07C229/36 ,  C07C235/60 ,  C07D213/80 ,  C07D213/79 ,  A61K31/216 ,  A61K31/24 ,  A61K31/618 ,  A61K31/609 ,  A61K31/455 ,  A61K31/4409 ,  A61P25/16

CPC分类号： C07C235/60 ,  C07C229/34 ,  C07C229/36 ,  C07C235/48 ,  C07C2601/14 ,  C07D213/79 ,  C07D213/80 ,  C07D213/803

摘要： Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed. Wherein Q is selected from X-CO-, and -CO-X-; X is selected from-O-, and -NR6-; n is an integer from 2 to 4; R5 is selected from hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, cycloalkyl, substituted cycloalkyl, heteroalkyl, substituted heteroalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, and substituted heteroarylalkyl; and when Q is -X--CO-, R5 is further selected from alkoxy, substituted alkoxy, cycloalkoxy, and substituted cycloalkoxy.

公开(公告)号：EP1485082A1

公开(公告)日：2004-12-15

申请号：EP02746514.5

申请日：2002-06-11

申请人： Xenoport, Inc.

发明人： GALLOP, Mark, A. ,  XIANG, Jia-Ning ,  YAO, Fenmei ,  BHAT, Laxminarayan ,  ZHOU, Cindy, X.

IPC分类号： A61K31/225 ,  C07C271/22

CPC分类号： C07C269/06 ,  C07C271/12 ,  C07C271/22 ,  C07C2601/14 ,  C07F9/4087

摘要： The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amenable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug compounds and methods for synthesizing these 1-acyl-alkyl derivatives.

摘要翻译： 本发明提供了从1-酰基 - 烷基衍生物合成1-（酰氧基） - 烷基衍生物的方法，其通常以高产率立体特异性地进行，不需要使用活化的中间体和/或有毒化合物并且易于修饰 放大。 本发明还提供已知药物成分的1-酰基 - 烷基衍生物和合成这些1-酰基 - 烷基衍生物的方法。

公开(公告)号：EP1404324B1

公开(公告)日：2007-12-05

申请号：EP02744314.2

申请日：2002-06-11

申请人： Xenoport, Inc.

发明人： GALLOP, Mark, A. ,  CUNDY, Kenneth, C. ,  ZHOU, Cindy, X. ,  QIU, Fayang, G. ,  YAO, Fenmei ,  XIANG, Jia-Ning ,  OLLMAN, Ian, R.

IPC分类号： A61K31/44 ,  A61K31/335 ,  A61K31/27 ,  A61K31/225 ,  A61K31/195 ,  A61P25/00 ,  C07D213/02 ,  C07D317/00 ,  C07C205/00 ,  C07C229/00 ,  C07C261/00 ,  C07C269/00 ,  C07C271/00

CPC分类号： C07C201/12 ,  A61K31/19 ,  A61K31/197 ,  A61K31/22 ,  A61K31/27 ,  A61K31/341 ,  A61K47/54 ,  A61K47/555 ,  C07C271/22 ,  C07C323/58 ,  C07C2601/14 ,  C07D213/79 ,  C07D213/80 ,  C07D267/06 ,  C07D307/33 ,  C07D307/58 ,  C07D307/60 ,  C07D317/32 ,  C07D317/40 ,  C07C205/43

摘要： The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using phannaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

公开(公告)号：EP1404324A2

公开(公告)日：2004-04-07

申请号：EP02744314.2

申请日：2002-06-11

申请人： Xenoport, Inc.

发明人： GALLOP, Mark, A. ,  CUNDY, Kenneth, C. ,  ZHOU, Cindy, X. ,  QIU, Fayang, G. ,  YAO, Fenmei ,  XIANG, Jia-Ning ,  OLLMAN, Ian, R.

IPC分类号： A61K31/44 ,  A61K31/335 ,  A61K31/27 ,  A61K31/225 ,  A61K31/195 ,  A61P25/00 ,  C07D213/02 ,  C07D317/00 ,  C07C205/00 ,  C07C229/00 ,  C07C261/00 ,  C07C269/00 ,  C07C271/00

CPC分类号： C07C201/12 ,  A61K31/19 ,  A61K31/197 ,  A61K31/22 ,  A61K31/27 ,  A61K31/341 ,  A61K47/54 ,  A61K47/555 ,  C07C271/22 ,  C07C323/58 ,  C07C2601/14 ,  C07D213/79 ,  C07D213/80 ,  C07D267/06 ,  C07D307/33 ,  C07D307/58 ,  C07D307/60 ,  C07D317/32 ,  C07D317/40 ,  C07C205/43

摘要： The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using phannaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

摘要翻译： 本发明提供了GABA类似物的前药，GABA类似物前药的药物组合物和制备GABA类似物的前药的方法。 本发明还提供使用GABA类似物前药的方法和使用GABA类似物前药的药物组合物治疗或预防常见疾病和/或病症的方法。

公开(公告)号：EP1959948B1

公开(公告)日：2012-07-18

申请号：EP06844799.4

申请日：2006-12-04

申请人： XenoPort, Inc.

发明人： XIANG, Jia-Ning ,  DAI, Xuedong ,  ZHOU, Cindy X. ,  LI, Jianhua ,  NGUYEN, Mark Q.

IPC分类号： A61K31/24 ,  C07C229/36 ,  C07C309/04

CPC分类号： C07C229/36 ,  C07B2200/07 ,  C07B2200/13 ,  C07C229/34 ,  C07C309/04

摘要： (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.

公开(公告)号：EP1404324B2

公开(公告)日：2011-04-06

申请号：EP02744314.2

申请日：2002-06-11

申请人： XenoPort, Inc.

发明人： GALLOP, Mark, A. ,  CUNDY, Kenneth, C. ,  ZHOU, Cindy, X. ,  QIU, Fayang, G. ,  YAO, Fenmei ,  XIANG, Jia-Ning ,  OLLMANN, Ian, R.

IPC分类号： A61K31/44 ,  A61K31/335 ,  A61K31/27 ,  A61K31/225 ,  A61K31/195 ,  A61P25/00 ,  C07D213/02 ,  C07D317/00 ,  C07C205/00 ,  C07C229/00 ,  C07C261/00 ,  C07C269/00 ,  C07C271/00

CPC分类号： C07C201/12 ,  A61K31/19 ,  A61K31/197 ,  A61K31/22 ,  A61K31/27 ,  A61K31/341 ,  A61K47/54 ,  A61K47/555 ,  C07C271/22 ,  C07C323/58 ,  C07C2601/14 ,  C07D213/79 ,  C07D213/80 ,  C07D267/06 ,  C07D307/33 ,  C07D307/58 ,  C07D307/60 ,  C07D317/32 ,  C07D317/40 ,  C07C205/43

摘要： The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using phannaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

摘要翻译： 本发明提供GABA类似物的前药，GABA类似物前药的药物组合物和制备GABA类似物前药的方法。 本发明还提供使用GABA类似物前药的方法和使用GABA类似物前药药物组合物治疗或预防常见疾病和/或病症的方法。

公开(公告)号：EP2125702A1

公开(公告)日：2009-12-02

申请号：EP07867956.0

申请日：2007-12-20

申请人： XenoPort, Inc.

发明人： XIANG, Jia-Ning ,  ZHOU, Cindy X. ,  YAO, Fenmei ,  NGUYEN, Mark Q.

IPC分类号： C07C229/36 ,  A61K31/24 ,  A61P25/16 ,  A61P25/18 ,  A61P25/00

CPC分类号： C07C229/36

摘要： Levodopa dimethyl-substituted diester prodrugs, pharmaceutical, compositions comprising levodopa dimethyl-substituted diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided. Formula (I)

公开(公告)号：EP1554237A1

公开(公告)日：2005-07-20

申请号：EP03757492.8

申请日：2003-06-11

申请人： Xenoport, Inc.

发明人： RAILLARD, Stephen, P. ,  ZHOU, Cindy, X. ,  YAO, Fenmei ,  MANTHATI, Suresh, Kumar ,  XIANG, Jia-Ning ,  GALLOP, Mark, A.

IPC分类号： C07C205/00 ,  C07C261/00 ,  C07C269/00 ,  C07C271/00

CPC分类号： C07C271/22 ,  C07C269/06 ,  C07C2601/14 ,  C07D309/06 ,  C07D335/02

摘要： The synthesis of 1-(acyloxy)-alkyl carbamates of GABA analogs from 1-haloalkyl carbamates of GABA analogs are described. Also described are new 1-haloalkyl carbamates of GABA analogs.

摘要翻译： 本发明涉及结晶1 - {[（±）异丁酰氧基乙氧基）羰基]氨基甲基} -1-环己烷乙酸。

公开(公告)号：EP1959948A2

公开(公告)日：2008-08-27

申请号：EP06844799.4

申请日：2006-12-04

申请人： Xenoport, Inc.

发明人： XIANG, Jia-Ning ,  DAI, Xuedong ,  ZHOU, Cindy X. ,  LI, Jianhua ,  NGUYEN, Mark Q.

IPC分类号： A61K31/24

CPC分类号： C07C229/36 ,  C07B2200/07 ,  C07B2200/13 ,  C07C229/34 ,  C07C309/04

摘要： (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.