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公开(公告)号：US5840697A
公开(公告)日：1998-11-24
申请号：US660747
申请日：1996-06-06
摘要： The present invention relates to novel family of peptides which inhibit calmodulin and which have the general structure Ac-A1-B2-C3-D4-E5-F6-NH.sub.2, (SEQ ID No. 1), wherein A1 is (D)Leu or Leu, B2 is (D)Gln, Gln, (D)Trp, or Trp, C3 is (D)Arg, Arg, (D)Ile, or Ile, D4 is (D)Ile, Ile, (D)His, or His, E5 is (D)Leu, Leu, (D)His, or His, and F6 is (D)Trp, Trp, (D)Arg, or Arg. The novel peptides can be used to inhibit the activity of calmodulin. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a calmodulin-inhibitor peptide. These compositions can be used to treat calmodulin related disorders.
摘要翻译： 本发明涉及抑制钙调蛋白并具有通用结构Ac-A1-B2-C3-D4-E5-F6-NH2（SEQ ID No.1）的新型家族，其中A1是（D）Leu或 Leu，B2是（D）Gln，Gln，（D）Trp或Trp，C3是（D）Arg，Arg，（D）Ile或Ile，D4是（D）Ile，Ile，（D） 或His，E5为（D）Leu，Leu，（D）His或His，F6为（D）Trp，Trp，（D）Arg或Arg。 新型肽可用于抑制钙调蛋白的活性。 此外，本发明涉及包含药学上可接受的载体和钙调蛋白抑制剂肽的药物组合物。 这些组合物可用于治疗钙调蛋白相关疾病。
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公开(公告)号：US5440016A
公开(公告)日：1995-08-08
申请号：US79445
申请日：1993-06-18
CPC分类号： C07K7/06 , C07K5/0215 , C07K5/1019
摘要： Peptides having Anti-microbial activity and having the formula (KFmoc)ZZZ-NH.sub.2, wherein Z is an amino acid are disclosed. Also disclosed are peptides having anti-trypsin activity and having the formula Ac-rypwz-NH.sub.2, wherein z is a D-amino acid. Also disclosed are compositions containing these peptides and methods of using them.
摘要翻译： 公开了具有抗微生物活性并具有式（KFmoc）ZZZ-NH 2的肽，其中Z是氨基酸。 还公开了具有抗胰蛋白酶活性并具有式Ac-rypwz-NH 2的肽，其中z是D-氨基酸。 还公开了含有这些肽的组合物和使用它们的方法。
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公开(公告)号：US5698673A
公开(公告)日：1997-12-16
申请号：US434761
申请日：1995-05-04
CPC分类号： C07K7/06 , C07K5/0215 , C07K5/1019
摘要： Disclosed are peptides having anti-mellitin activity and having the formulae AC-IVILZZ-NH.sub.2, wherein Z is an amino acid. Also disclosed are compositions containing these peptides and methods of using them.
摘要翻译： 公开了具有抗梅毒素活性并具有式AC-IVILZZ-NH 2的肽，其中Z是氨基酸。 还公开了含有这些肽的组合物和使用它们的方法。
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公开(公告)号：US07022882B2
公开(公告)日：2006-04-04
申请号：US10381956
申请日：2001-10-05
IPC分类号： C07C211/13 , C07C211/27 , C07C215/52 , A61K31/135
CPC分类号： C07C215/54 , A61K31/00 , A61K31/137 , C07B2200/07 , C07C211/27 , C40B40/00
摘要： Neuroprotectant agents are provided which do not contain peptides and axe protected from the degradation that limits the use of peptide-based drugs in systemic circulation. With great selectivity for NMDA receptors, the agents exert an open channel block on NMDA receptors, and protect neuronal cells containing such receptors from excitatoxic cell death.
摘要翻译： 提供的神经保护剂不含有限制肽系药物在体循环中使用的降解的肽和斧头。 对NMDA受体具有很好的选择性，该试剂在NMDA受体上发挥开放通道阻断，并保护含有此类受体的神经元细胞免于兴奋性细胞死亡。
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公开(公告)号：US5624902A
公开(公告)日：1997-04-29
申请号：US485396
申请日：1995-06-07
摘要： The present invention relates to novel family of peptides which inhibit calmodulin and which have the general structure Ac-(D)Leu-A1-B2-C3-D4-E5-NH.sub.2, wherein A1 is (D)Gln or (D)Trp, B2 is (D)Arg or (D)Ile, C3 is (D)Ile or (D)His, D4 is (D)Leu or (D)His and E5 is (D)Trp or (D)Arg. The novel peptides can be used to inhibit the activity of calmodulin. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a calmodulin-inhibitor peptide. These compositions can be used to treat calmodulin related disorders.
摘要翻译： 本发明涉及抑制钙调蛋白并具有通式结构Ac-（D）Leu-A1-B2-C3-D4-E5-NH2的新型家族，其中A1为（D）Gln或（D）Trp， B2是（D）Arg或（D）Ile，C3是（D）Ile或（D）His，D4是（D）Leu或（D）His和E5是（D）Trp或（D）Arg。 新型肽可用于抑制钙调蛋白的活性。 此外，本发明涉及包含药学上可接受的载体和钙调蛋白抑制剂肽的药物组合物。 这些组合物可用于治疗钙调蛋白相关疾病。
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6.发明授权公开(公告)号：US06359144B1
公开(公告)日：2002-03-19
申请号：US09018173
申请日：1998-02-03
申请人： John M. Ostresh , Jean-Philippe Meyer , Colette T. Dooley , Sylvie E. Blondelle , Christa C. Schoner , Richard A. Houghten
发明人： John M. Ostresh , Jean-Philippe Meyer , Colette T. Dooley , Sylvie E. Blondelle , Christa C. Schoner , Richard A. Houghten
IPC分类号： C07D40302
CPC分类号： C07D487/04 , C40B40/04
摘要： The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.
摘要翻译： 本发明提供了组合合成和筛选双环胍化合物组合文库的快速方法。 本发明还提供了通过组合合成制备的化合物及其使用方法。
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公开(公告)号：US5235038A
公开(公告)日：1993-08-10
申请号：US643343
申请日：1991-01-22
IPC分类号： A61K38/00 , C07K14/435
CPC分类号： C07K14/43572 , A61K38/00 , Y10S530/858
摘要： A compound comprising an analogue of the melittin peptide having the following structural formula: ##STR1## wherein at least one and no more than four amino acid residues are omitted from the peptide, or at least one of amino acid residues 1-6, 8-18, or 20-26 in the peptide is substituted with a hydrophobic residue, provided that no more than two of amino acid residues 21-26 is substituted with a hydrophobic residue. Such deletion and substitution analogues are useful as antibiotics, antimicrobial agents, antifungal agents, anti-tumor agents, antiviral agents, or agents which stimulate wound healing.
摘要翻译： 包含具有以下结构式的蜂毒肽的类似物的化合物：其中从肽中除去至少一个不超过四个氨基酸残基，或至少一个氨基酸（SEQ ID NO： 肽中的残基1-6,8-18或20-26被疏水残基取代，条件是不超过两个氨基酸残基21-26被疏水残基取代。 这种缺失和取代类似物可用作抗生素，抗微生物剂，抗真菌剂，抗肿瘤剂，抗病毒剂或刺激伤口愈合的药剂。
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公开(公告)号：US08372848B2
公开(公告)日：2013-02-12
申请号：US10593941
申请日：2005-03-23
申请人： Richard A. Houghten , Colette Dooley , Adel Nefzi , Zhiwei Wang , Oliver Civelli , Hiroshi Nagasaki
发明人： Richard A. Houghten , Colette Dooley , Adel Nefzi , Zhiwei Wang , Oliver Civelli , Hiroshi Nagasaki
IPC分类号： A61K31/495 , A61K31/4166 , A61K31/4168 , C07D233/12 , C07D239/10 , C07D239/12
CPC分类号： A61K31/4015 , C07D233/42
摘要： This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).
摘要翻译： 本发明一般涉及N-苄基氨基环硫脲，含有它们的药物组合物及其作为黑色素浓缩激素受体（MCH受体）拮抗剂的用途。
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公开(公告)号：US07067623B2
公开(公告)日：2006-06-27
申请号：US10286670
申请日：2002-11-01
IPC分类号： C07K1/04
摘要： A solid phase synthetic method is disclosed in which the usual solid phase synthetic steps are carried out and the spent solid phase support is reacted to form a volatilizable compound upon cleavage of the reaction product from the solid phase support. The cleaved product is then separated from the volatile compound by volatilization of that compound. Exemplary solid supports that form a volatilizable compound are also disclosed.
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![Synthesis of [3,5,7]-1H-imidazo [1,5-a]imidazol-2 (3H)- one compounds](/abs-image/US/2003/12/16/US06664282B2/abs.jpg.150x150.jpg)
10.发明授权Synthesis of [3,5,7]-1H-imidazo [1,5-a]imidazol-2 (3H)- one compounds 失效[3,5,7] -1H-咪唑并[1,5-a]咪唑-2（3H） - 酮化合物的合成公开(公告)号：US06664282B2
公开(公告)日：2003-12-16
申请号：US10141439
申请日：2002-05-08
IPC分类号： A61K31415
CPC分类号： C07D487/04 , C40B40/00
摘要： Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
摘要翻译： 公开了单独取代的[3,5,7] -1H-咪唑并[1,5-a]咪唑-2（3H） - 酮化合物及其药学上可接受的盐，以及这些化合物的文库。 还公开了制备和使用化合物文库以及文库的单独化合物的方法。
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