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1. 发明申请

WO2004089289A3 TREATING OR PREVENTING HOT FLASHES USING PRODRUGS OF GABA ANALOGS 审中-公开
标题翻译：使用GABA模拟原理处理或防止热水闪烁
公开(公告)号：WO2004089289A3
公开(公告)日：2005-03-10
申请号：PCT/US2004010137
申请日：2004-03-31
申请人： XENOPORT INC , BARRETT RONALD W , GALLOP MARK A
发明人： BARRETT RONALD W , GALLOP MARK A
IPC分类号： A61K20060101 , 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.
摘要翻译：本文公开了使用GABA类似物的前药和其药物组合物的方法来治疗或预防人类中的热潮红和用于治疗或预防潮热的GABA类似物的前药药物组合物。

2. 发明申请

WO2002100344A3 AMINO ACID CONJUGATES PROVIDING FOR SUSTAINED SYSTEMIC CONCENTRATIONS OF GABA ANALOGUES 审中-公开
公开(公告)号：WO2002100344A3
公开(公告)日：2002-12-19
申请号：PCT/US2002/018493
申请日：2002-06-11
申请人： XENOPORT, INC. , GALLOP, Mark, A. , CUNDY, Kenneth, C. , SCHEUERMAN, Randall, A. , BARRETT, Ronald, W. , ZERANGUE, Noa
发明人： GALLOP, Mark, A. , CUNDY, Kenneth, C. , SCHEUERMAN, Randall, A. , BARRETT, Ronald, W. , ZERANGUE, Noa
IPC分类号： C07C261/00
摘要： This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

3. 发明申请

WO0123619A9 COMPOUNDS DISPLAYED ON REPLICABLE GENETIC PACKAGES AND METHODS OF USING SAME 审中-公开
标题翻译：在可替代遗传包装上显示的化合物及其使用方法
公开(公告)号：WO0123619A9
公开(公告)日：2002-12-12
申请号：PCT/US0026849
申请日：2000-09-29
申请人： XENOPORT INC , BARRETT RONALD W , DOWER WILLIAM J , GALLOP MARK , WOIWODE THOMAS F , CWIRLA STEVEN E
发明人： BARRETT RONALD W , DOWER WILLIAM J , GALLOP MARK , WOIWODE THOMAS F , CWIRLA STEVEN E
IPC分类号： C12N15/10 , C12Q1/68 , C12Q1/70
CPC分类号： C12N15/1037
摘要： Replicable genetic packages and collections thereof that display various compounds are provided. In some instances, the replicable genetic packages include nucleic acid tags that serve to record a characteristic of the compound or compounds that are attached to the replicable genetic package. The invention further provides a number of different methods for using the replicable genetic packages to screen a library of compounds for a desired biological activity.
摘要翻译：提供显示各种化合物的可复制的遗传包装及其集合。在一些情况下，可复制遗传包装包括用于记录附着于可复制遗传包装的化合物或化合物的特征的核酸标签。本发明还提供了许多不同的使用可复制遗传包装以筛选化合物文库以获得所需生物学活性的方法。

4. 发明申请

WO1991007087A1 SPATIALLY-ADDRESSABLE IMMOBILIZATION OF ANTI-LIGANDS ON SURFACES 审中-公开
标题翻译：防辐射对表面的空间化处理
公开(公告)号：WO1991007087A1
公开(公告)日：1991-05-30
申请号：PCT/US1990006607
申请日：1990-11-13
申请人： AFFYMAX TECHNOLOGIES, N.V. , BARRETT, Ronald, W. , PIRRUNG, Michael, C. , STRYER, Lubert , HOLMES, Christopher, P. , SUNDBERG, Steven, A.
发明人： AFFYMAX TECHNOLOGIES, N.V.
IPC分类号： A01N01/02
CPC分类号： C07D495/04 , B01J2219/00608 , B01J2219/0061 , B01J2219/00612 , B01J2219/00619 , B01J2219/00621 , B01J2219/00626 , B01J2219/0063 , B01J2219/00659 , B01J2219/00722 , C07D233/38 , C40B40/06 , G01N33/54353 , G01N33/552 , Y02P20/55
摘要： Methods and compositions are described for immobilizing anti-ligands, such as antibodies or antigens, hormones or hormone receptors, oligonucleotides, and polysaccharides on surfaces of solid substrates for various uses. The methods provide surfaces covered with caged binding members which comprise protecting groups capable of being removed upon application of a suitable energy source. Spatially addressed irradiation of predefined regions on the surface permits immobilization of anti-ligands at the activated regions on the surface. Cycles of irradiation on different regions of the surface and immobilization of different anti-ligands allows formation of an immobilized matrix of anti-ligands at defined sites on the surface. The immobilized matrix of anti-ligands permits simultaneous screenings of a liquid sample for ligands having high affinities for certain anti-ligands of the matrix. A preferred embodiment of the invention involves attaching photoactivatable biotin derivatives to a surface. Photolytic activation of the biotin derivatives forms biotin analogs having strong binding affinity for avidin. Biotinylated anti-ligands can be immobilized on activated regions of the surface previously treated with avidin.
摘要翻译：描述了用于在固体底物的表面上固定抗配体如抗体或抗原，激素或激素受体，寡核苷酸和多糖的方法和组合物用于各种用途。这些方法提供了覆盖有笼式结合构件的表面，其包括在施加合适的能量源时能够被去除的保护基团。表面上预定区域的空间照射辐射允许在表面上的活化区域上固定抗配体。表面不同区域的照射周期和不同抗配体的固定允许在表面上限定的位点形成固定的抗配体基团。抗配体的固定化基质允许对基质的某些抗配体具有高亲和力的配体的液体样品的同时筛选。本发明的优选实施方案涉及将可光活化的生物素衍生物连接到表面。生物素衍生物的光解活化形成对抗生物素蛋白具有强结合亲和力的生物素类似物。生物素化的抗配体可以固定在先前用抗生物素蛋白处理的表面的活化区上。

5. 发明申请

WO2009094563A3 CRYSTALLINE FORM OF CALCIUM-SALTS OF (3S)-AMINOMETHYL-B-METHYL-HEXANOIC ACIDS AND METHODS OF USE 审中-公开
标题翻译：（3S） - 氨基乙基 - 甲基 - 十六烷酸的钙盐的结晶形式及其使用方法
公开(公告)号：WO2009094563A3
公开(公告)日：2009-10-01
申请号：PCT/US2009031867
申请日：2009-01-23
申请人： XENOPORT INC , GALLOP MARK A , YAO FENMEI , BARRETT RONALD W , VIRSIK PETER A
发明人： GALLOP MARK A , YAO FENMEI , BARRETT RONALD W , VIRSIK PETER A
IPC分类号： C07C269/08 , A61K31/325 , A61P25/00 , C07C271/22
CPC分类号： C07C271/22 , A61K31/325 , C07B2200/07 , C07B2200/13 , C07C329/06 , C12P11/00 , C12P41/005
摘要： A crystalline form of Ca-salts of (3S) -aminomethyl-5-hexanoic acids and methods of preparing a crystalline form of a (3S) -aminomethyl-5-hexanoic acid and methods of using a crystalline form of a (3S) -aminomethyl-5-hexanoic acid are provided.
摘要翻译：（3S） - 氨基甲基-5-己酸的Ca-盐的结晶形式和（3S） - 氨基甲基-5-己酸的结晶形式的制备方法和使用（3S） - 提供氨基甲基-5-己酸。

6. 发明申请

WO2009094563A2 CRYSTALLINE FORM OF A (3S)-AMINOMETHYL-5-METHYL-HEXANOIC ACID PRODRUG AND METHODS OF USE 审中-公开
标题翻译：（3S） - 氨基甲酰基-5-甲基 - 十六烷酸的制备方法及其使用方法
公开(公告)号：WO2009094563A2
公开(公告)日：2009-07-30
申请号：PCT/US2009/031867
申请日：2009-01-23
申请人： XENOPORT, INC. , BARRETT, Ronald W. , VIRSIK, Peter A. , GALLOP, Mark A. , YAO, Fenmei
发明人： BARRETT, Ronald W. , VIRSIK, Peter A. , GALLOP, Mark A. , YAO, Fenmei
IPC分类号： C07C269/08 , C07C271/22 , A61K31/325 , A61P25/00
CPC分类号： C07C271/22 , A61K31/325 , C07B2200/07 , C07B2200/13 , C07C329/06 , C12P11/00 , C12P41/005
摘要： A crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug and methods of preparing a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug, and methods of using a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug are provided.
摘要翻译：（3S） - 氨基甲基-5-己酸前药的结晶形式和（3S） - 氨基甲基-5-己酸前药的结晶形式的制备方法，以及使用（3S） - 提供氨基甲基-5-己酸前药。

7. 发明申请

WO2002077182A2 COMPOUNDS DISPLAYED ON ICOSAHEDRAL PHAGE AND METHODS OF USING SAME 审中-公开
标题翻译：在ICOSAHEDRAL PHAGE上显示的化合物及其使用方法
公开(公告)号：WO2002077182A2
公开(公告)日：2002-10-03
申请号：PCT/US2002/009095
申请日：2002-03-21
申请人： XENOPORT, INC. , BARRETT, Ronald, W. , DOWER, William, J. , GALLOP, Mark , WOIWODE, Thomas, F. , CWIRLA, Steven, E.
发明人： BARRETT, Ronald, W. , DOWER, William, J. , GALLOP, Mark , WOIWODE, Thomas, F. , CWIRLA, Steven, E.
IPC分类号： C12N
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.
摘要翻译：提供显示各种化合物的二十面体噬菌体及其收集物。在一些情况下，二十面体噬菌体包括用于记录附着于噬菌体的化合物或化合物的特征的核酸标签。还提供了许多用于使用二十面体噬菌体筛选化合物文库以获得所需生物学活性的不同方法，特别是用于受体介导的转运过程例如内吞作用和转胞吞作用的底物的化合物的测定。

8. 发明申请

WO2001020331A1 SUBSTRATES AND SCREENING METHODS FOR TRANSPORT PROTEINS 审中-公开
标题翻译：运输蛋白的基质和筛选方法
公开(公告)号：WO2001020331A1
公开(公告)日：2001-03-22
申请号：PCT/US2000/025439
申请日：2000-09-14
申请人： XENOPORT, INC. , DOWER, William, J. , GALLOP, Mark , BARRETT, Ronald, W. , CUNDY, Kenneth, C. , CHERNOV-ROGAN, Tania
发明人： DOWER, William, J. , GALLOP, Mark , BARRETT, Ronald, W. , CUNDY, Kenneth, C. , CHERNOV-ROGAN, Tania
IPC分类号： G01N33/566
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.
摘要翻译：提供了用于测定测试化合物的文库作为载体蛋白质（包括载体型和受体型转运蛋白）的转运蛋白质的配体和/或底物的多种方法。公开了体外和体外的筛选方法。还提供了筛选DNA文库以鉴定编码转运蛋白的成员的方法。还提供了包括通过筛选方法鉴定的化合物的药物组合物。

9. 发明申请

WO1998025965A2 PEPTIDES AND COMPOUNDS THAT BIND TO A RECEPTOR 审中-公开
标题翻译：与受体结合的肽和化合物
公开(公告)号：WO1998025965A2
公开(公告)日：1998-06-18
申请号：PCT/EP1997006850
申请日：1997-12-09
申请人： GLAXO GROUP LIMITED , DOWER, William, J. , BARRETT, Ronald, W. , CWIRLA, Steven, E. , GATES, Christian, M. , SCHATZ, Peter, J. , BALASUBRAMANIAN, Palaniappan , WAGSTROM, Christopher, R. , HENDREN, Richard, Wayne , DEPRINCE, Randolph, B. , PODDUTURI, Surekha , YIN, Qun
发明人： GLAXO GROUP LIMITED
IPC分类号： C07K14/52
CPC分类号： C07K14/524 , A61K38/00
摘要： Described are peptides and compounds that bind to and activate the thrombopoietin receptor. Such peptides and compounds are useful in methods for treating haematological disorders and particularly, thrombocytopenia resulting from chemotherapy, radiation therapy, or bone marrow transfusions as well as in diagnostic methods employing labelled peptides and compounds.
摘要翻译：描述了结合并激活血小板生成素受体的肽和化合物。这样的肽和化合物可用于治疗血液病，特别是化疗，放射治疗或骨髓输注引起的血小板减少症以及使用标记肽和化合物的诊断方法。

10. 发明申请

WO1995031210A1 PEPTIDES AND COMPOUNDS THAT BIND SELECTINS INCLUDING ENDOTHELIUM LEUKOCYTE ADHESION MOLECULE 1 (ELAM-1) 审中-公开
标题翻译：肽类和化合物，其包括内含子白蛋白粘附分子1（ELAM-1）
公开(公告)号：WO1995031210A1
公开(公告)日：1995-11-23
申请号：PCT/US1995006315
申请日：1995-05-11
申请人： AFFYMAX TECHNOLOGIES NV , BARRETT, Ronald, W. , CWIRLA, Steven, E. , DOWER, William, J. , KOLLER, Kerry, J. , LEE, Jung , MARTENS, Christine, L. , RUHLAND-FRITSCH, Beatrice
发明人： AFFYMAX TECHNOLOGIES NV
IPC分类号： A61K38/00
CPC分类号： A61K49/0056 , A61K38/00 , A61K47/62 , A61K51/08 , A61K2123/00 , C07K1/047 , C07K7/06 , C07K7/08 , C07K14/001
摘要： Disclosed are peptides and peptide mimetics that bind selectins, including endothelial leukocyte adhesion molecule 1 (ELAM-1). Such peptides and peptide mimetics are useful in methods for blocking adhesion of leukocytes to the selectins for the purpose of inhibiting inflammation as well as in diagnostic methods employing labeled peptides and peptide mimetics that bind selectins for the purpose of determining the site of inflammation in mammals which inflammation is mediated by the presence of one or more selectins.
摘要翻译：公开了结合选择素的肽和肽模拟物，包括内皮细胞粘附分子1（ELAM-1）。这样的肽和肽模拟物可用于阻止白细胞粘附到选择素上用于抑制炎症的方法以及使用结合选择素的标记肽和肽模拟物的诊断方法，以确定哺乳动物的炎症位点炎症由一种或多种选择素的存在介导。

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