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21. 发明授权

US658318A Broadcast seed-sower. 失效
标题翻译：广播种子
公开(公告)号：US658318A
公开(公告)日：1900-09-18
申请号：US1900020570
申请日：1900-06-16
申请人： JESSE ARNOLD , HOWARD BENJAMIN F
发明人： HOWARD BENJAMIN F
CPC分类号： A01C17/00

22. 发明申请

US20110009343A1 MODULATORS OF AMYLOID AGGREGATION 审中-公开
标题翻译：淀粉样聚集的调节剂
公开(公告)号：US20110009343A1
公开(公告)日：2011-01-13
申请号：US12643258
申请日：2009-12-21
申请人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Laura Kasman , Gary Musso , Ethan R. Signer , James Wakefield , Michael J. Reed
发明人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Laura Kasman , Gary Musso , Ethan R. Signer , James Wakefield , Michael J. Reed
IPC分类号： A61K38/16 , C07K14/00 , C07K7/08 , A61K38/10 , A61P43/00
CPC分类号： C07K14/4711 , A61K38/00
摘要： Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural β amyloid peptides (β-AP). In a preferred embodiment, the β amyloid modulator compounds of the invention are comprised of an Aβ aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural β amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural β-AP aggregation when the natural β-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译：公开了调节淀粉样蛋白形成蛋白或肽聚集的化合物。本发明的调节剂可以促进淀粉样蛋白聚集，更优选可以抑制天然淀粉样蛋白聚集。在优选的实施方案中，所述化合物调节天然物质的聚集。淀粉样蛋白肽（＆bgr; -AP）。在优选实施例中，本发明的淀粉样蛋白调节剂化合物由A＆Bgr; 聚集核心结构域和与其偶联的修饰基团，使得所述化合物改变聚集或抑制天然蛋白的神经毒性; 当与肽接触时，淀粉样蛋白肽。此外，当天然和重组相对于调节剂摩尔量过多时，调节剂能够改变天然和重组蛋白的聚集。还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。

23. 发明授权

US07658917B2 Modulators of amyloid aggregation 失效
标题翻译：淀粉样蛋白聚集的调节剂
公开(公告)号：US07658917B2
公开(公告)日：2010-02-09
申请号：US10463729
申请日：2003-06-17
申请人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Ethan R. Signer , James Wakefield , Laura Kasman , Gary Musso , Michael J. Reed
发明人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Ethan R. Signer , James Wakefield , Laura Kasman , Gary Musso , Michael J. Reed
IPC分类号： A61K38/02 , A61K38/17 , C07K1/113 , C07K14/47
CPC分类号： C07K14/4711 , A61K38/00
摘要： Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural β amyloid peptides (β-AP). In a preferred embodiment, the β amyloid modulator compounds of the invention are comprised of an Aβ aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural β amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural β-AP aggregation when the natural β-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译：公开了调节淀粉样蛋白形成蛋白或肽聚集的化合物。本发明的调节剂可以促进淀粉样蛋白聚集，更优选可以抑制天然淀粉样蛋白聚集。在优选的实施方案中，化合物调节天然β淀粉样肽（β-AP）的聚集。在优选的实施方案中，本发明的β淀粉样蛋白调节剂化合物由Abeta聚集核心结构域和与其偶联的修饰基团组成，使得当与肽接触时该化合物改变聚集或抑制天然β淀粉样肽的神经毒性。此外，当天然β-AP相对于调节剂为摩尔过量时，调节剂能够改变天然β-AP聚集。还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。

24. 发明授权

US06319498B1 Modulators of amyloid aggregation 失效
标题翻译：淀粉样蛋白聚集的调节剂
公开(公告)号：US06319498B1
公开(公告)日：2001-11-20
申请号：US08617267
申请日：1996-03-14
申请人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Laura Kasman , Gary Musso , Ethan R. Signer , James Wakefield , Michael J. Reed
发明人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Laura Kasman , Gary Musso , Ethan R. Signer , James Wakefield , Michael J. Reed
IPC分类号： A61K3802
CPC分类号： C07K14/4711 , A61K38/00
摘要： Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural &bgr; amyloid peptides (&bgr;-AP). In a preferred embodiment, the &bgr; amyloid modulator compounds of the invention are comprised of an A&bgr; aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural &bgr; amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural &bgr;-AP aggregation when the natural &bgr;-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译：公开了调节淀粉样蛋白形成蛋白或肽聚集的化合物。本发明的调节剂可以促进淀粉样蛋白聚集，更优选可以抑制天然淀粉样蛋白聚集。在优选的实施方案中，化合物调节天然β淀粉样肽（β-AP）的聚集。在优选的实施方案中，本发明的β淀粉样蛋白调节剂化合物由Abeta聚集核心结构域和与其偶联的修饰基团组成，使得当与肽接触时该化合物改变聚集或抑制天然β淀粉样肽的神经毒性。此外，当天然β-AP相对于调节剂为摩尔过量时，调节剂能够改变天然β-AP聚集。还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。

25. 发明申请

US20080032896A1 Methods for identifying compounds that bind to a target 审中-公开
标题翻译：用于鉴定结合靶标的化合物的方法
公开(公告)号：US20080032896A1
公开(公告)日：2008-02-07
申请号：US11704580
申请日：2007-02-09
申请人： Howard Benjamin , Mark Findeis , Malcolm Gefter , Gary Musso , Ethan Signer
发明人： Howard Benjamin , Mark Findeis , Malcolm Gefter , Gary Musso , Ethan Signer
IPC分类号： C40B20/02 , C40B20/08
CPC分类号： C07K1/047
摘要： Methods for identifying a compound that binds to a target are described. In general, the methods involve forming a first library comprising a multiplicity of peptides, identifying one or more peptides that bind to the target and determining a peptide motif therefrom, forming a second library comprising a multiplicity of compounds designed based on the peptide motif, selecting from the second library at least one compound that binds to the target, and determining the structure or structures of the at least one compound that binds to the target. Libraries of compounds based on a peptide motif and compounds identified by the methods of the invention are also disclosed.
摘要翻译：描述了用于鉴定与靶标结合的化合物的方法。通常，所述方法包括形成包含多个肽的第一文库，鉴定结合靶标的一种或多种肽，并从其中确定肽基序，形成包含基于肽基序设计的多种化合物的第二文库，选择来自第二文库的至少一种与靶标结合的化合物，以及确定结合靶标的至少一种化合物的结构或结构。还公开了基于肽基序的化合物和通过本发明的方法鉴定的化合物的文库。

26. 发明授权

US06214795B1 Peptide compounds useful for modulating FGF receptor activity 失效
标题翻译：可用于调节FGF受体活性的肽化合物
公开(公告)号：US06214795B1
公开(公告)日：2001-04-10
申请号：US08747599
申请日：1996-11-12
申请人： Howard Benjamin , Ling Chai , Mark A. Findeis , William Goodwin , Arvind Hundal , David I. Israel , Michael Kelley , Martin P. Keough , Kuanghui Lu , Farah Natoli , Alicia Peticolas , Ethan R. Signer , Malcolm L. Gefter
发明人： Howard Benjamin , Ling Chai , Mark A. Findeis , William Goodwin , Arvind Hundal , David I. Israel , Michael Kelley , Martin P. Keough , Kuanghui Lu , Farah Natoli , Alicia Peticolas , Ethan R. Signer , Malcolm L. Gefter
IPC分类号： C07K700
CPC分类号： C07K7/06 , A61K38/00 , C07K14/50
摘要： This invention provides peptide compounds that bind to either a fibroblast growth factor (FGF) or a fibroblast growth factor receptor (FGFR) and, accordingly, are useful for modulating FGFR activity. Preferably, the FGFR is FGFR2-IIIC. Preferably, the FGF is basic FGF. Preferably the peptide compound comprises an amino acid sequence: (Y/F)-(L/F/I)-(R/D/E/S/Y/G)-(Q/L/Y)-Y-(M/L/K/R)-(L/M/D/E/N/S)-(R/L/S/T)-(L/F/M/V) (SEQ ID NO: 1). The invention further comprises pharmaceutical compositions comprising the peptide compounds of the invention and a pharmaceutically acceptable carrier. The invention still further provides methods of modulating FGFR activity using the peptide compounds of the invention.
摘要翻译：本发明提供了与成纤维细胞生长因子（FGF）或成纤维细胞生长因子受体（FGFR）结合的肽化合物，因此可用于调节FGFR活性。优选地，FGFR是FGFR2-IIIC。优选地，FGF是碱性FGF。优选地，肽化合物包含氨基酸序列：（Y / F） - （L / F / I） - （R / D / E / S / Y / G） - （Q / L / Y）-Y-（M / L / K / R） - （L / M / D / E / N / S） - （R / L / S / T） - （L / F / M / V）（SEQ ID NO：1）。本发明还包括包含本发明的肽化合物和药学上可接受的载体的药物组合物。本发明还提供使用本发明的肽化合物调节FGFR活性的方法。

27. 发明授权

US5854215A Modulators of .beta.-amyloid peptide aggregation 失效
标题翻译： β-淀粉样肽聚集的调节剂
公开(公告)号：US5854215A
公开(公告)日：1998-12-29
申请号：US475579
申请日：1995-06-07
申请人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Laura Kasman , Gary Musso , Ethan R. Signer , James Wakefield , Michael J. Reed
发明人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Laura Kasman , Gary Musso , Ethan R. Signer , James Wakefield , Michael J. Reed
IPC分类号： A61K38/00 , C07K14/47 , A61K38/17 , C07K1/113
CPC分类号： C07K14/4711 , A61K38/00
摘要： Compounds that act to modulate the aggregation of natural .beta. amyloid peptides (.beta.-AP) are disclosed. The .beta. amyloid modulators of the invention can promote .beta.-AP aggregation or, more preferably, can inhibit natural .beta.-AP aggregation. Furthermore, the modulators are capable of altering natural .beta.-AP aggregation when the natural .beta.-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and methods of altering natural .beta.-AP aggregation using the compounds of the invention, are also disclosed.
摘要翻译：公开了用于调节天然β淀粉样肽（β-AP）聚集的化合物。本发明的β淀粉样蛋白调节剂可以促进β-AP聚集，更优选可以抑制天然β-AP聚集。此外，当天然β-APs相对于调节剂摩尔过量时，调节剂能够改变天然的β-AP聚集。还公开了包含本发明化合物的药物组合物和使用本发明化合物改变天然β-AP聚集的方法。

28. 发明授权

US06475806B1 Anchor libraries and identification of peptide binding sequences 失效
标题翻译：锚定文库和肽结合序列的鉴定
公开(公告)号：US06475806B1
公开(公告)日：2002-11-05
申请号：US08479660
申请日：1995-06-07
申请人： Howard Benjamin , Ethan Signer , Malcolm Gefter
发明人： Howard Benjamin , Ethan Signer , Malcolm Gefter
IPC分类号： G01N33543
CPC分类号： C40B40/02 , C07K1/047 , C12N15/1037
摘要： An anchor library is described. A collection of recombinant vectors having a nucleic acid encoding a displayed peptide sequence is provided. The displayed peptide sequence of each of the vectors comprises X1(Y1)c1X2(Y2)c2X3(Y3)c3X4, wherein each X1, X2, X3 and X4 is an amino acid residue and any of X1, X2, X3 and X4 can be the same or different from any one other, wherein each Y1, Y2 and Y3 is alanine or glycine or a combination of alanine and glycine that is respectively c1, c2 and c3 amino acid residues long and any of Y1, Y2 and Y3 if present can be the same or different from any one other, wherein each of c1, c2 and c3 is 0 to about 20, wherein X1 and X4 are each attached to an amino acid residue that flanks the displayed peptide sequence. Preferably, at least about 105 to about 108 permutations of all possible permutations of the displayed peptide sequence are present in the anchor library. Preferably, the library does not contain more than about 10% of displayed peptide sequences different from the first mentioned displayed peptide sequences. Also described are methods of making anchor libraries and methods of using anchor libraries to identify a peptide sequence that binds to a target. Recombinant vectors, filamentous phage, nucleic acid molecules and proteins are also provided.
摘要翻译：描述了一个锚库。提供了具有编码显示的肽序列的核酸的重组载体的集合。每个载体的显示的肽序列包含X1（Y1）c1X2（Y2）c2X3（Y3）c3X4，其中X1，X2，X3和X4是氨基酸残基，X1，X2，X3和X4中的任一个可以是其中每个Y1，Y2和Y3分别是丙氨酸或甘氨酸或分别为c1，c2和c3氨基酸残基长的丙氨酸和甘氨酸的组合，如果存在，Y1，Y2和Y3中的任何一个可以可以相同或不同，其中c1，c2和c3各自为0至约20，其中X1和X4各自连接于所显示的肽序列侧翼的氨基酸残基。优选地，显示的肽序列的所有可能排列的至少约105至约108个排列存在于锚库中。优选地，文库不含超过约10％的显示肽序列，其不同于第一个提到的显示的肽序列。还描述了制备锚定文库的方法以及使用锚定文库来鉴定与靶标结合的肽序列的方法。还提供了重组载体，丝状噬菌体，核酸分子和蛋白质。

29. 发明授权

US1379567A Vehicle 失效
公开(公告)号：US1379567A
公开(公告)日：1921-05-24
申请号：US41622320
申请日：1920-10-11
申请人： WEST HOWARD BENJAMIN
发明人： WEST HOWARD BENJAMIN
IPC分类号： B62B13/02
CPC分类号： B62B13/02

30. 发明授权

US5854204A A.beta. peptides that modulate .beta.-amyloid aggregation 失效
标题翻译：调节β-淀粉样蛋白聚集的β肽
公开(公告)号：US5854204A
公开(公告)日：1998-12-29
申请号：US612785
申请日：1996-03-14
申请人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Laura Kasman , Gary Musso , Ethan R. Signer , James Wakefield , Michael Reed , Susan Molineaux , William Kubasek , Joseph Chin , Jung-Ja Lee , Michael Kelley
发明人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Laura Kasman , Gary Musso , Ethan R. Signer , James Wakefield , Michael Reed , Susan Molineaux , William Kubasek , Joseph Chin , Jung-Ja Lee , Michael Kelley
IPC分类号： A61K39/02 , A61K31/00 , A61K38/00 , A61K51/00 , A61P25/00 , C07K7/06 , C07K14/47 , C07K14/435 , C07K7/08
CPC分类号： C07K14/4711 , A61K38/00
摘要： Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural .beta. amyloid peptides (.beta.-AP). In a preferred embodiment, the .beta. amyloid modulator compounds of the invention are comprised of an A.beta. aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural .beta. amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural .beta.-AP aggregation when the natural .beta.-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译：公开了调节淀粉样蛋白形成蛋白或肽聚集的化合物。本发明的调节剂可以促进淀粉样蛋白聚集，更优选可以抑制天然淀粉样蛋白聚集。在优选的实施方案中，化合物调节天然β淀粉样蛋白肽（β-AP）的聚集。在优选的实施方案中，本发明的β淀粉样蛋白调节剂化合物由Aβ聚集核心结构域和与其偶联的修饰基团组成，使得当与肽接触时，该化合物改变聚集或抑制天然β淀粉样肽的神经毒性。此外，当天然β-APs相对于调节剂摩尔过量时，调节剂能够改变天然的β-AP聚集。还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。

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