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公开(公告)号：US08349797B2
公开(公告)日：2013-01-08
申请号：US11988468
申请日：2006-07-10
IPC分类号： A61K38/12 , A61K38/16 , A61K38/22 , C07K14/575 , C07K14/665
CPC分类号： C07K14/685 , A61K38/00 , C07K14/69 , C07K14/695
摘要： The present invention is directed to a compound according to formula, (R2R3)-B1-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-A11-A12-A13-B2-B3-R1, that act as ligands for one or more of the melanocortin receptors, the pharmaceutically-acceptable salts thereof, to methods of using such peptides to treat mammals and to pharmaceutical compositions useful therefore comprising said peptides.
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公开(公告)号：US08039435B2
公开(公告)日：2011-10-18
申请号：US11988533
申请日：2006-07-10
IPC分类号： A61K38/00
CPC分类号： C07K7/06 , A61K38/00 , C07K7/08 , C07K14/665
摘要： The present invention is directed to compounds according to formula, (R2R3)-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-R1, and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.
摘要翻译： 本发明涉及下式的化合物：（R2R3）-A1-c（A2-A3-A4-A5-A6-A7-A8-A9）-A10-R1及其药物上可接受的盐作为配体 对于一种或多种黑皮质素受体，使用这些化合物治疗哺乳动物的方法和包含所述化合物的药物组合物。
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公开(公告)号：US20090232838A1
公开(公告)日：2009-09-17
申请号：US11988468
申请日：2006-07-10
CPC分类号： C07K14/685 , A61K38/00 , C07K14/69 , C07K14/695
摘要： The present invention is directed to a compound according to formula, (R2R3)-B1-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-A11-A12-A13-B2-B3-R1, that act as ligands for one or more of the melanocortin receptors, the pharmaceutically-acceptable salts thereof, to methods of using such peptides to treat mammals and to pharmaceutical compositions useful therefore comprising said peptides.
摘要翻译： 本发明涉及下式化合物：（R2R3）-B1-A1-c（A2-A3-A4-A5-A6-A7-A8-A9）-A10-A11-A12-A13-B2-B3 -R1，其用作一种或多种黑皮质素受体的配体，其药学上可接受的盐，使用这些肽来治疗哺乳动物的方法和用于因此包含所述肽的药物组合物。
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公开(公告)号：US20060211607A1
公开(公告)日：2006-09-21
申请号：US11434273
申请日：2006-05-15
申请人： Michael Culler , Zheng Dong , Sun Kim , Jacques-Pierre Moreau
发明人： Michael Culler , Zheng Dong , Sun Kim , Jacques-Pierre Moreau
IPC分类号： A61K38/31 , C07K14/655
CPC分类号： C07D471/04 , A61K38/00 , C07D471/06 , C07K14/6555
摘要： Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8β-ergolinglmethylthioacetyl-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2
摘要翻译： 公开了一系列在体内保持生长抑素和多巴胺活性的生长抑素 - 多巴胺嵌合类似物。 一个例子是：6-正丙基-8β-麦角酰甲基硫代乙酰基-D-Phe-c（Cys-Tyr-D-Trp-Lys-Abu-Cys）-Thr-NH 2
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公开(公告)号：US20050026827A1
公开(公告)日：2005-02-03
申请号：US10788563
申请日：2004-02-27
申请人： David Coy , Jacques-Pierre Moreau , Sun Kim
发明人： David Coy , Jacques-Pierre Moreau , Sun Kim
IPC分类号： A61K38/00 , C07K7/02 , C07K7/08 , C07K7/18 , C07K14/575 , C07K14/685 , A61K38/17
CPC分类号： C07K7/086 , A61K38/00 , C07K7/02 , C07K7/18 , C07K14/57572 , C07K14/685
摘要： A linear (i.e., non-cyclic) analog of biologically active amphibian bombesin, mammalian gastrin-releasing peptide (GRP), or mammalian growth hormone releasing factor (GRF), having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell. Cleavage of a peptide bond in the active site of naturally occurring bombesin, GRP, or GRF is unnecessary for in vivo biological activity. The analog has one of the following modifications: (a) a deletion of an amino acid residue within the active site and a modification of an amino acid residue outside of the active site, (b) a replacement of two amino acid residues within the active site with a synthetic amino acid, a β-amino acid, or a γ-amino acid residue, or (c) a non-peptide bond. instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue.
摘要翻译： 具有活性位点和负责肽结合的结合位点的生物活性水陆两栖铃蟾肽，哺乳动物胃泌素释放肽（GRP）或哺乳动物生长激素释放因子（GRF）的线性（即非循环）类似物 到目标细胞上的受体。 在天然存在的铃蟾肽，GRP或GRF的活性位点中肽键的切割对于体内生物活性是不必要的。 类似物具有以下修饰之一：（a）活性位点内的氨基酸残基的缺失和活性位点之外的氨基酸残基的修饰，（b）在活性位点内置换两个氨基酸残基 具有合成氨基酸，β-氨基酸或γ-氨基酸残基的位点，或（c）非肽键。 而不是活性位点的氨基酸残基与相邻氨基酸残基之间的肽键。
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36.发明授权Ionic molecular conjugates of N-acylated derivatives of poly(2-amino-2-deoxy-D-glucose) and polypeptides 失效聚（2-氨基-2-脱氧-D-葡萄糖）N-酰化衍生物和多肽的离子分子共轭物公开(公告)号：US06794364B2
公开(公告)日：2004-09-21
申请号：US10251018
申请日：2002-09-20
申请人： Shalaby W. Shalaby , Steven A. Jackson , Francis X. Ignatious , Jacques-Pierre Moreau , Ruth M. Russell
发明人： Shalaby W. Shalaby , Steven A. Jackson , Francis X. Ignatious , Jacques-Pierre Moreau , Ruth M. Russell
IPC分类号： A61K3800
CPC分类号： C08B37/003 , A61K38/31 , A61K47/61 , C08L5/08 , C08L2666/02
摘要： A copolymer comprising an N-acylated derivative, and a composition comprising said copolymer and a polypeptide, said polypeptide comprising at least one effective ionogenic amine, wherein at least 50 percent, by weight, of said polypeptide present in said composition is ionically bound to said polymer.
摘要翻译： 包含N-酰化衍生物的共聚物和包含所述共聚物和多肽的组合物，所述多肽包含至少一种有效的离子型胺，其中存在于所述组合物中的所述多肽的至少50重量％离子地结合到所述 聚合物。
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公开(公告)号：US5736517A
公开(公告)日：1998-04-07
申请号：US73771
申请日：1993-06-08
CPC分类号： A61K38/105 , A61K38/22 , A61K38/31
摘要： A method of treating cancer in a human patient, the method involving administering to the patient a cancer cell inhibiting amount of an analog of a naturally occurring biologically active peptide or a fragment thereof, the peptide being one of mammalian gastrin-releasing peptide, neuromedin B, neuromedin C, amphibian bombesin, or litorin.
摘要翻译： 一种在人类患者中治疗癌症的方法，所述方法包括向患者施用癌细胞抑制量的天然存在的生物活性肽或其片段的类似物，所述肽是哺乳动物胃泌素释放肽，神经介肽B之一 ，神经介肽C，两栖动物铃蟾肽，或丁酸。
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公开(公告)号：US5663295A
公开(公告)日：1997-09-02
申请号：US352391
申请日：1994-12-08
IPC分类号： A61K38/00 , A61P25/00 , C07K5/02 , C07K5/027 , C07K5/065 , C07K5/087 , C07K5/107 , C07K7/06 , C07K14/575 , C07K14/655 , C07K7/00
CPC分类号： C07K7/06 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/0812 , C07K5/1016 , A61K38/00
摘要： Opioid peptides including those of the formula ##STR1## in which A.sub.1 is the identifying group of an amino acid selected from 3,4-dihydroxyphenylalanine, 3,4-dimethoxyphenylalanine, azatyrosine, and 2,6-dimethyltyrosine; A.sub.2 is the identifying group of an amino acid selected from D-Ala and D-Arg; A.sub.3 is H, or the identifying group of an amino acid selected from of 3,4-dihydroxyphenylalanine and 3,4-dimethoxyphenylalanine, A.sub.4 is H, cyclohexylmethyl, the identifying group of an amino acid selected from 3,4-dihydroxyphenylalanine, 3,4-dimethoxyphenylalanine, Phe, and substituted Phe with its benzene ring substituted by halogen, NO.sub.2, OH, or CH.sub.3 ; A.sub.5 is the identifying group of a D- or L-amino acid selected from Leu, Nle, Lys, Met and Met(O), or is deleted together with R.sub.4 --CH attached thereto; each R.sub.1 and R.sub.2 is --H, --C(NH.sub.2).dbd.NH, or C.sub.1-12 alkyl; R.sub.3 is ##STR2## R.sub.4 is ##STR3## and R.sub.5 is --(CH.sub.2).sub.n+1 OH, ##STR4## wherein m is 0-6, n is 0-6, and X is H, C.sub.1-12 alkyl, C.sub.6-12 aryl, C.sub.7-18 aralkyl, C.sub.7-18 alkaryl, C.sub.7-18 alkayl, C.sub.6-17 pyridylalkyl, or C.sub.6-17 alkylpyridyl; provided that when one of R.sub.1 and R.sub.2 is --C(NH.sub.2).dbd.NH, the other must be H; or a pharmaceutically acceptable salt thereof.
摘要翻译： 阿片样肽包括式“IMAGE”的那些，其中A1是选自3,4-二羟基苯丙氨酸，3,4-二甲氧基苯丙氨酸，氨甲酰酪氨酸和2,6-二甲基酪氨酸的氨基酸的鉴定基团; A2是选自D-Ala和D-Arg的氨基酸的鉴定基团; A3是H，或选自3,4-二羟基苯丙氨酸和3,4-二甲氧基苯丙氨酸的氨基酸的鉴定基团，A4是H，环己基甲基，选自3,4-二羟基苯丙氨酸， 4-二甲氧基苯丙氨酸，Phe和取代的Phe，其苯环被卤素，NO 2，OH或CH 3取代; A5是选自Leu，Nle，Lys，Met和Met（O）的D-或L-氨基酸的鉴定基团，或与其连接的R4-CH一起缺失; 每个R 1和R 2是-H，-C（NH 2）= NH或C 1-12烷基; R3是
，R4是 ，R5是 - （CH2）n + 1OH，其中m是0-6，n是0-6，X是H，C1-12烷基，C6-12 芳基，C7-18芳烷基，C7-18烷芳基，C7-18烷基，C6-17吡啶基烷基或C6-17烷基吡啶基; 条件是当R 1和R 2中的一个是-C（NH 2）= NH时，另一个必须是H; 或其药学上可接受的盐。 -
公开(公告)号：US5410019A
公开(公告)日：1995-04-25
申请号：US860675
申请日：1992-03-30
IPC分类号： A61K38/00 , C07K7/02 , C07K7/08 , C07K7/18 , C07K7/22 , C07K14/575 , C07K14/685 , C07K7/06
CPC分类号： C07K7/22 , C07K14/57572 , C07K14/685 , C07K7/02 , C07K7/086 , C07K7/18 , A61K38/00
摘要： A linear peptide which is an analog of naturally occurring, biologically active substance P having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell. The analog has a non-peptide bond instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue, or a synthetic, a .beta.-amino acid, or a .alpha.-amino acid residue replacing two amino acid residues of the active site.
摘要翻译： 线性肽，其是具有活性位点的天然存在的生物活性物质P的类似物，以及负责将肽与靶细胞上的受体结合的结合位点。 该类似物具有非肽键而不是活性位点的氨基酸残基与相邻氨基酸残基之间的肽键，或者合成的β-氨基酸或取代两个氨基酸的α-氨基酸残基 活性位点的残基。
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40.发明授权
公开(公告)号：US5084443A
公开(公告)日：1992-01-28
申请号：US444999
申请日：1989-12-04
IPC分类号： A61K38/09
CPC分类号： A61K38/09
摘要： A method for promoting regrowth of damaged nerve tissue in a mammal, the method comprising administering to the mammal a nerve tissue regrowth promoting amount of an LHRH antagonist namely, N-Acetyl -D-Naphthylalanine-D-para-Cl-Phe-D-Phe-Ser-Tyr-D-Arg-Phe-Arg-Pro-D-Ala-NH.sub.2.
摘要翻译： 一种用于促进哺乳动物损伤的神经组织的再生长的方法，所述方法包括向哺乳动物施用促进神经组织的促生长量的LHRH拮抗剂，即N-乙酰-D-萘基丙氨酸-D-对-C1-Phe-D- Phe-Ser-Tyr-D-Arg-Phe-Arg-Pro-D-Ala -NH 2。
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