公开(公告)号：EP1212619B1

公开(公告)日：2007-05-23

申请号：EP00966735.3

申请日：2000-09-14

申请人： Xenoport, Inc.

发明人： DOWER, William, J. ,  GALLOP, Mark ,  BARRETT, Ronald, W. ,  CUNDY, Kenneth, C. ,  CHERNOV-ROGAN, Tania

IPC分类号： G01N33/566 ,  G01N33/542 ,  G01N33/50

CPC分类号： G01N33/5088 ,  A61K49/0004 ,  C07C271/22 ,  C07C2603/18 ,  C07D271/08 ,  C07D277/32 ,  C07D311/16 ,  C07K1/047 ,  C12N15/1034 ,  C12N15/1086 ,  C40B40/00 ,  G01N33/5008 ,  G01N33/533 ,  G01N33/566 ,  G01N33/92

摘要： A variety of methods for assaying libraries of test compounds as ligands and/or substrates of transport proteins, including both carrier-type and receptor-type transport proteins, are provided. Both in vitro and in vivo screening methods are disclosed. Also provided are methods for screening DNA libraries to identify members that encode transport proteins. Pharmaceutical compositions including compounds identified via the screening methods are also provided.

公开(公告)号：EP1781596A1

公开(公告)日：2007-05-09

申请号：EP05770911.5

申请日：2005-07-12

申请人： Xenoport, Inc.

发明人： XU, Feng ,  GALLOP, Mark A. ,  SASIKUMAR, Vivek

IPC分类号： C07C237/12 ,  C07K5/062 ,  C07C323/60 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078 ,  C07D233/54 ,  C07C237/20 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/28 ,  A61K38/05 ,  A61K31/16

CPC分类号： C07C323/60 ,  A61K38/00 ,  C07C229/22 ,  C07C237/12 ,  C07C237/20 ,  C07D233/64 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06069 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/06113 ,  C07K5/06147 ,  C07K5/06165

摘要： The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post?chemotherapy or post?operative surgery nausea and vomiting.

公开(公告)号：EP1716115A2

公开(公告)日：2006-11-02

申请号：EP04815821.6

申请日：2004-12-30

申请人： Xenoport, Inc.

发明人： GALLOP, Mark A. ,  DAI, Xuedong ,  SCHEUERMAN, Randall A. ,  RAILLARD, Stephen P. ,  MANTHATI, Suresh K. ,  YAO, Fenmei ,  PHAN, Thu ,  LUDWIKOW, Maria ,  PENG, Ge ,  BHAT, Seema

IPC分类号： C07D207/40

CPC分类号： C07D207/46 ,  C07D207/404 ,  C07D207/416

摘要： Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

公开(公告)号：EP1554237A4

公开(公告)日：2006-11-02

申请号：EP03757492

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： C07D213/803 ,  A61K31/325 ,  A61K31/553 ,  A61K31/66 ,  A61K31/675 ,  A61K38/04 ,  C07B61/00 ,  C07C205/00 ,  C07C261/00 ,  C07C269/00 ,  C07C269/06 ,  C07C271/00 ,  C07C271/10 ,  C07C271/18 ,  C07C271/22 ,  C07D213/55 ,  C07F9/02 ,  C07K1/04 ,  C07K5/04

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.

公开(公告)号：EP1608357A2

公开(公告)日：2005-12-28

申请号：EP04749644.3

申请日：2004-03-31

申请人： Xenoport, Inc.

发明人： BARRETT, Ronald, W. ,  GALLOP, Mark, A.

IPC分类号： A61K31/195

CPC分类号： A61K31/195

摘要： Disclosed herein are methods of using prodrugs of GABA analogs and pharmaceutical compositions thereof to treat or prevent hot flashes in humans and pharmaceutical compositions of prodrugs of GABA analogs useful in treating or preventing hot flashes.

公开(公告)号：EP1569895A1

公开(公告)日：2005-09-07

申请号：EP03812817.9

申请日：2003-12-05

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： C07C271/22

CPC分类号： C07C205/43 ,  A61K38/00 ,  C07C45/567 ,  C07C209/48 ,  C07C229/28 ,  C07C271/22 ,  C07C2601/10 ,  C07C2601/14 ,  C07D213/80 ,  C07D267/04 ,  C07D307/58 ,  C07D317/32 ,  C07D317/40 ,  C07K5/0205 ,  C07C49/83 ,  C07C49/17

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 pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

公开(公告)号：EP1385984A2

公开(公告)日：2004-02-04

申请号：EP02728558.4

申请日：2002-03-21

申请人： Xenoport, Inc.

发明人： BARRETT, Ronald, W. ,  DOWER, William, J. ,  GALLOP, Mark ,  WOIWODE, Thomas, F. ,  CWIRLA, Steven, E.

IPC分类号： C12Q1/00 ,  C12Q1/70 ,  C12Q1/68 ,  G01N33/53 ,  G01N33/543 ,  C12N7/00 ,  C12N15/00 ,  C12N15/09 ,  C12N15/63 ,  C12N15/70 ,  C12N15/74 ,  A61K38/00

CPC分类号： C40B40/02 ,  C12N15/1037 ,  G01N33/6845

摘要： Icosahedral phage and collections thereof that display various compounds are provided. In some instances, the icosahedral phage include nucleic acid tags that serve to record a characteristic of the compound or compounds that are attached to the phage. A number of different methods for using the icosahedral phage to screen a library of compounds for a desired biological activity are also provided, especially assays for compounds that are substrates for receptor-mediated transport processes such as endocytosis and transcytosis.

公开(公告)号：EP1361847A2

公开(公告)日：2003-11-19

申请号：EP01987653.1

申请日：2001-10-05

申请人： Xenoport, Inc.

发明人： GALLOP, Mark A. ,  CUNDY, Kenneth C. ,  ZHOU, Cindy X

IPC分类号： A61K6/00

CPC分类号： C07D233/64 ,  A61K38/00 ,  A61K47/554 ,  A61K47/64 ,  A61K47/65 ,  C07C237/12 ,  C07C237/20 ,  C07C323/60 ,  C07C2601/14 ,  C07D207/16 ,  C07K5/0205 ,  C07K5/06 ,  C07K5/08

摘要： This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

摘要翻译： 本发明涉及在对动物施用后提供持续全身浓度的治疗剂或预防剂的化合物。 本发明还涉及药物组合物以及使用这些化合物的方法。

公开(公告)号：EP1343805A1

公开(公告)日：2003-09-17

申请号：EP01979953.5

申请日：2001-10-05

申请人： Xenoport, Inc.

发明人： GALLOP, Mark, A. ,  CUNDY, Kenneth, C. ,  ZHOU, Cindy, X.

IPC分类号： C07J5/00 ,  C07J9/00 ,  C07J17/00 ,  C07J41/00 ,  C07J43/00 ,  A61K31/56 ,  A61K31/58

CPC分类号： C07K5/0205 ,  A61K31/56 ,  A61K38/00 ,  A61K47/54 ,  A61K47/554 ,  A61K47/64 ,  A61K47/65 ,  C07C237/12 ,  C07C237/20 ,  C07C323/60 ,  C07C2601/14 ,  C07D207/16 ,  C07D233/64

摘要： This invention is directed to methods for providing sustained systemic concentrations of therapeutic or prophylactic agents such as GABA analogs following oral administration to animals. This invention is also directed to compounds and pharmaceutical compositions that are used in such methods.

摘要翻译： 本发明涉及到的方法，用于提供治疗或预防剂的持续的全身浓度：如GABA类似物口服给药于动物。 因此，本发明涉及化合物和药物组合物也被在搜索方法中使用。

公开(公告)号：EP1259823A2

公开(公告)日：2002-11-27

申请号：EP01912936.0

申请日：2001-02-22

申请人： Xenoport, Inc.

发明人： GALLOP, Mark A. ,  DOWER, William J. ,  BARRETT, Ron W.

IPC分类号： G01N33/68 ,  C07K1/04

CPC分类号： C07K1/047 ,  B01J19/0046 ,  B01J2219/005 ,  B01J2219/00563 ,  B01J2219/00572 ,  B01J2219/00576 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00592 ,  B01J2219/00596 ,  B01J2219/00702 ,  B01J2219/00707 ,  B01J2219/0072 ,  B01J2219/00722 ,  B01J2219/00725 ,  B01J2219/00731 ,  B01J2219/00734 ,  C07B2200/11 ,  C40B40/06 ,  C40B40/10 ,  C40B40/12

摘要： The present invention provides a variety of methods for synthesizing, encoding and decoding compounds in a combinatorial library. One step or cycle in the synthetic methods of the invention is a self-encoding step in which different pairs of components, each pair with a known and different molecular weight difference, are reacted with supports, whereby two compounds differing in molecular weight are formed on each support. The molecular weight difference between the two compounds on the support encodes for a particular component pair. Libraries of compounds formed according to the methods of the invention are also provided.

摘要翻译： 本发明提供了用于在组合文库中合成，编码和解码化合物的多种方法。 本发明的合成方法中的一个步骤或循环是自编码步骤，其中不同配对的组分（每对具有已知且不同的分子量差异）与载体反应，由此形成分子量不同的两种化合物 每个支持。 载体上两种化合物之间的分子量差异编码特定组分对。 还提供了根据本发明的方法形成的化合物文库。