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51. 发明授权

US07645797B2 Amino acid conjugates providing for sustained systemic concentrations of GABA analogues 失效
标题翻译：提供持续全身浓度的GABA类似物的氨基酸缀合物
公开(公告)号：US07645797B2
公开(公告)日：2010-01-12
申请号：US12128225
申请日：2008-05-28
申请人： Mark Gallop , Kenneth C. Cundy , Randall A. Scheuerman , Ronald W. Barrett , Noa Zerangue
发明人： Mark Gallop , Kenneth C. Cundy , Randall A. Scheuerman , Ronald W. Barrett , Noa Zerangue
IPC分类号： A61K31/195 , C07C229/28
CPC分类号： C07D233/64 , A61K38/00 , A61K47/64 , C07C237/12 , C07C237/20 , C07C317/50 , C07C323/59 , C07C323/60 , C07C2601/14 , C07D207/16 , C07K5/0205 , G01N33/566
摘要： Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.
摘要翻译：公开了在口服给予动物后提供持续的全身浓度的GABA类似物的化合物。还公开了药物组合物，以及使用这些化合物的方法。

52. 发明申请

US20080226716A1 AMINO ACID CONJUGATES PROVIDING FOR SUSTAINED SYSTEMIC CONCENTRATION OF GABA ANALOGUES 失效
标题翻译：提供持续的GABA类似物系统浓度的氨基酸联合
公开(公告)号：US20080226716A1
公开(公告)日：2008-09-18
申请号：US12128225
申请日：2008-05-28
申请人： Mark Gallop , Kenneth C. Cundy , Randall A. Scheuerman , Ronald W. Barrett , Noa Zerangue
发明人： Mark Gallop , Kenneth C. Cundy , Randall A. Scheuerman , Ronald W. Barrett , Noa Zerangue
IPC分类号： C07C61/08 , A61K31/195 , A61K31/35 , C07D315/00 , A61K31/38 , A61K31/40 , A61K31/403 , C07D207/00 , A61P25/00 , A61P25/30 , A61P1/00 , A61P29/00 , A61K9/22
CPC分类号： C07D233/64 , A61K38/00 , A61K47/64 , C07C237/12 , C07C237/20 , C07C317/50 , C07C323/59 , C07C323/60 , C07C2601/14 , C07D207/16 , C07K5/0205 , G01N33/566
摘要： Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.
摘要翻译：公开了在口服给予动物后提供持续的全身浓度的GABA类似物的化合物。还公开了药物组合物，以及使用这些化合物的方法。

53. 发明授权

US07229757B2 Compounds displayed on icosahedral phage and methods of using same 失效
标题翻译：二十面体噬菌体上显示的化合物及其使用方法
公开(公告)号：US07229757B2
公开(公告)日：2007-06-12
申请号：US10105029
申请日：2002-03-21
申请人： Ronald W. Barrett , William J. Dower , Mark Gallop , Thomas F. Woiwode , Steven E. Cwirla
发明人： Ronald W. Barrett , William J. Dower , Mark Gallop , Thomas F. Woiwode , Steven E. Cwirla
IPC分类号： C12Q1/68
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。

54. 发明授权

US06426357B1 Antagonists of follicle stimulating hormone activity 失效
标题翻译：促卵泡激素活性的拮抗剂
公开(公告)号：US06426357B1
公开(公告)日：2002-07-30
申请号：US09629180
申请日：2000-07-31
申请人： Randall A. Scheuerman , Stephen D. Yanofsky , Christopher P. Holmes , Derek MacLean , Beatrice Ruhland , Ronald W. Barrett , Jay E. Wrobel , Ariamala Gopalsamy
发明人： Randall A. Scheuerman , Stephen D. Yanofsky , Christopher P. Holmes , Derek MacLean , Beatrice Ruhland , Ronald W. Barrett , Jay E. Wrobel , Ariamala Gopalsamy
IPC分类号： A61K31427
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention provides a compound of the formula: and methods for using the same, wherein R1, R2, R3, R4 and X are those defined herein.
摘要翻译：本发明提供下式的化合物及其使用方法：其中R1，R2，R3，R4和X为本文定义的化合物。

55. 发明授权

US06251864B1 Peptides and compounds that bind to a receptor 有权
标题翻译：结合受体的肽和化合物
公开(公告)号：US06251864B1
公开(公告)日：2001-06-26
申请号：US09516704
申请日：2000-03-01
申请人： William J. Dower , Ronald W. Barrett , Steven E. Cwirla , Christian M. Gates , Peter J. Schatz , Palaniappan Balasubramanian , Christopher R. Wagstrom , Richard Wayne Hendren , Randolph B. Deprince , Surekha Podduturi , Qun Yin
发明人： William J. Dower , Ronald W. Barrett , Steven E. Cwirla , Christian M. Gates , Peter J. Schatz , Palaniappan Balasubramanian , Christopher R. Wagstrom , Richard Wayne Hendren , Randolph B. Deprince , Surekha Podduturi , Qun Yin
IPC分类号： A61K3800
CPC分类号： C07K14/524
摘要： Described are peptides and peptide mimetics that bind to and activate the thrombopoietin receptor. Such peptides and peptide mimetics are useful in methods for treating hematological disorders and particularly, thrombocytopenia resulting from chemotherapy, radiation therapy, or bone marrow transfusions as well as in diagnostic methods employing labeled peptides and peptide mimetics.
摘要翻译：描述了结合并激活血小板生成素受体的肽和肽模拟物。这样的肽和肽模拟物可用于治疗血液学疾病，特别是由化疗，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肽模拟物的诊断方法。

56. 发明授权

US6143497A Method of synthesizing diverse collections of oligomers 失效
公开(公告)号：US6143497A
公开(公告)日：2000-11-07
申请号：US36599
申请日：1998-03-06
申请人： William J. Dower , Ronald W. Barrett , Mark A. Gallop
发明人： William J. Dower , Ronald W. Barrett , Mark A. Gallop
IPC分类号： C12N15/09 , B01J19/00 , C07B61/00 , C07H19/10 , C07H19/14 , C07H21/00 , C07H21/02 , C07H21/04 , C07K1/04 , C07K1/06 , C07K5/00 , C07K7/00 , C08F8/00 , C08G85/00 , C40B40/06 , C40B40/10 , C40B40/12 , C40B60/14 , C40B70/00 , C12Q1/68 , C12P19/34 , C12Q1/70
CPC分类号： C07K1/047 , B01J19/0046 , B01J19/0093 , C07H19/10 , C07H19/14 , C07H21/00 , B01J2219/00306 , B01J2219/00313 , B01J2219/00459 , B01J2219/00466 , B01J2219/005 , B01J2219/00502 , B01J2219/00536 , B01J2219/00542 , B01J2219/00545 , B01J2219/00547 , B01J2219/00554 , B01J2219/00563 , B01J2219/00565 , B01J2219/00572 , B01J2219/00574 , B01J2219/00576 , B01J2219/00585 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00689 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , B01J2219/00731 , C07B2200/11 , C40B40/06 , C40B40/10 , C40B40/12 , C40B60/14 , C40B70/00 , Y10S435/81 , Y10T436/143333
摘要： A general stochastic method for synthesizing random oligomers on particles is disclosed. A further aspect of the invention relates to the use of identification tags on the particles to facilitate identification of the sequence of the monomers in the oligomer.

57. 发明授权

US6140493A Method of synthesizing diverse collections of oligomers 失效
公开(公告)号：US6140493A
公开(公告)日：2000-10-31
申请号：US151467
申请日：1998-09-11
申请人： William J. Dower , Ronald W. Barrett , Mark A. Gallop , Michael C. Needels
发明人： William J. Dower , Ronald W. Barrett , Mark A. Gallop , Michael C. Needels
IPC分类号： C12N15/09 , B01J19/00 , C07B61/00 , C07H19/10 , C07H19/14 , C07H21/00 , C07H21/02 , C07H21/04 , C07K1/04 , C07K1/06 , C07K5/00 , C07K7/00 , C08F8/00 , C08G85/00 , C40B40/06 , C40B40/10 , C40B40/12 , C40B60/14 , C40B70/00 , B01J20/26
CPC分类号： C07K1/047 , B01J19/0046 , B01J19/0093 , C07H19/10 , C07H19/14 , C07H21/00 , B01J2219/00306 , B01J2219/00313 , B01J2219/00459 , B01J2219/00466 , B01J2219/005 , B01J2219/00502 , B01J2219/00536 , B01J2219/00542 , B01J2219/00545 , B01J2219/00547 , B01J2219/00554 , B01J2219/00563 , B01J2219/00565 , B01J2219/00572 , B01J2219/00574 , B01J2219/00576 , B01J2219/00585 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00689 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , B01J2219/00731 , C07B2200/11 , C40B40/06 , C40B40/10 , C40B40/12 , C40B60/14 , C40B70/00 , Y10S435/81 , Y10T436/143333
摘要： A general stochastic method for synthesizing random oligomers can be used to synthesize compounds to screen for desired properties. The use of identification tags on the oligomers facilitates identification of oligomers with desired properties.

58. 发明授权

US5932546A Peptides and compounds that bind to the thrombopoietin receptor 失效
标题翻译：结合血小板生成素受体的肽和化合物
公开(公告)号：US5932546A
公开(公告)日：1999-08-03
申请号：US726464
申请日：1996-10-04
申请人： Ronald W. Barrett , William J. Dower , Steven E. Cwirla , Sherril S. Johnson , Nicholas C. Wrighton , David J. Duffin , Christopher R. Wagstrom
发明人： Ronald W. Barrett , William J. Dower , Steven E. Cwirla , Sherril S. Johnson , Nicholas C. Wrighton , David J. Duffin , Christopher R. Wagstrom
IPC分类号： A61K38/00 , C07K7/06 , C07K7/08 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： C07K7/06 , C07K7/08 , A61K38/00
摘要： Described are peptides and peptide mimetics that bind to and activate the thrombopoietin receptor. Such peptides and peptide mimetics are useful in methods for treating hematological disorders and particularly, thrombocytopenia resulting from chemotherapy, radiation therapy, or bone marrow transfusions as well as in diagnostic methods employing labeled peptides and peptide mimetics.
摘要翻译：描述了结合并激活血小板生成素受体的肽和肽模拟物。这样的肽和肽模拟物可用于治疗血液学疾病，特别是由化疗，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肽模拟物的诊断方法。

59. 发明授权

US5880096A Peptides and compounds that bind to the IL-1 receptor 失效
标题翻译：结合IL-1受体的肽和化合物
公开(公告)号：US5880096A
公开(公告)日：1999-03-09
申请号：US463076
申请日：1995-06-05
申请人： Ronald W. Barrett , Stephen D. Yanofsky
发明人： Ronald W. Barrett , Stephen D. Yanofsky
IPC分类号： A61K38/00 , C07K14/545 , A61K38/04
CPC分类号： C07K14/545 , A61K38/00
摘要： Peptides that bind to the interleukin-1 type I receptor (IL-1RtI) can be used to assay the amount of IL-1R, or an IL-1R agonist or antagonist, in a sample and comprise a sequence of amino acids selected from the group consisting of (1) WXXXGZ.sub.1 W where Z.sub.1 is L, I, A, or Q (SEQ ID NO:2); (2) XXQZ.sub.5 YZ.sub.6 XX where Z.sub.5 is P or Aze where Aze is azetidine; and Z.sub.6 is S, A, V, or L (SEQ ID NO:1); and (3) Z.sub.23 NZ.sub.24 SZ.sub.25 Z.sub.26 Z.sub.27 Z.sub.28 Z.sub.29 Z.sub.30 L where Z.sub.23 is D or Y; Z.sub.24 is D or S; Z.sub.25 is S or W; Z.sub.26 is S or Y; Z.sub.27 is D or V; Z.sub.28 is S or W; Z.sub.29 is F or L; and Z.sub.30 is D or L (SEQ ID NO:27); and where each amino acid is indicated by standard one letter abbreviation; and each X can be selected from any one of the 20 genetically coded L-amino acids or the stereoisomeric D-amino acids. Also provided are peptides which bind to the IL-1RtI, which are 11 to 40 amino acids in length, which comprise the core sequence of amino acids:Z.sub.31 XWZ.sub.32 Z.sub.33 Z.sub.34 Z.sub.35 Z.sub.36 QZ.sub.37 Z.sub.38where each letter represents the standard one letter abbreviation for an amino acid or an analog thereof; X is selected from the group of natural or unnatural amino acids; Z.sub.37 is a natural or unnatural cyclic amino acid; Z.sub.31 is selected from phenylalanine and acetylated phenylalanine; Z.sub.32 is a natural or unnatural amino acid; Z.sub.33 is selected from proline and pipecolic acid; Z.sub.34 is selected from glycine, d-alanine, d-valine, sarcosine and aminoisobutyric acid; Z.sub.35 is a natural or unnatural amino acid and Z.sub.36 is selected from tyrosine, phosphotyrosine, phenylalanine and tryptophan; and Z.sub.38 is selected from tyrosinamide and substituted tyrosinamide (SEQ ID NO:392).
摘要翻译：结合白细胞介素-1 I型受体（IL-1RtI）的肽可用于测定样品中IL-1R或IL-1R激动剂或拮抗剂的量，并且包含选自以下的氨基酸序列：由（1）WXXXGZ1W组成的组，其中Z1是L，I，A或Q（SEQ ID NO：2）; （2）XXQZ5YZ6XX其中Z5为P或Aze，其中Aze为氮杂环丁烷; Z6是S，A，V或L（SEQ ID NO：1）; 和（3）Z23NZ24SZ25Z26Z27Z28Z29Z30L其中Z23为D或Y; Z24是D或S; Z25为S或W; Z26为S或Y; Z27为D或V; Z28为S或W; Z29为F或L; Z30为D或L（SEQ ID NO：27）; 并且其中每个氨基酸由标准单字母缩写指示; 并且每个X可以选自20个遗传编码的L-氨基酸或立体异构体D-氨基酸中的任一个。还提供了与IL-1RtI结合的肽，其长度为11至40个氨基酸，其包含氨基酸核心序列：Z31XWZ32Z33Z34Z35Z36QZ37Z38，其中每个字母表示氨基酸或其类似物的标准单字母缩写; X选自天然或非天然氨基酸组; Z37是天然或非天然环状氨基酸; Z31选自苯丙氨酸和乙酰化苯丙氨酸; Z32是天然或非天然氨基酸; Z33选自脯氨酸和哌啶酸; Z34选自甘氨酸，d-丙氨酸，d-缬氨酸，肌氨酸和氨基异丁酸; Z35是天然或非天然氨基酸，Z36选自酪氨酸，磷酸酪氨酸，苯丙氨酸和色氨酸; Z38选自酪氨酰胺和取代的酪氨酰胺（SEQ ID NO：392）。

60. 发明授权

US5869451A Peptides and compounds that bind to a receptor 失效
公开(公告)号：US5869451A
公开(公告)日：1999-02-09
申请号：US764640
申请日：1996-12-11
申请人： William J. Dower , Ronald W. Barrett , Steven E. Cwirla , Christian M. Gates , Peter J. Schatz , Palaniappan Balasubramanian , Christopher R. Wagstrom , Richard Wayne Hendren , Randoph B. DePrince , Surekha Podduturi , Qun Yin
发明人： William J. Dower , Ronald W. Barrett , Steven E. Cwirla , Christian M. Gates , Peter J. Schatz , Palaniappan Balasubramanian , Christopher R. Wagstrom , Richard Wayne Hendren , Randoph B. DePrince , Surekha Podduturi , Qun Yin
IPC分类号： A61K38/00 , A61K38/02 , A61P7/00 , A61P43/00 , C07K5/00 , C07K7/00 , C07K14/52 , C07K17/08
CPC分类号： C07K14/524 , A61K38/00
摘要： Described are peptides and peptide mimetics that bind to and activate the thrombopoietin receptor. Such peptides and peptide mimetics are useful in methods for treating hematological disorders and particularly, thrombocytopenia resulting from chemotherapy, radiation therapy, or bone marrow transfusions as well as in diagnostic methods employing labeled peptides and peptide mimetics.

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