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公开(公告)号：US5084555A
公开(公告)日：1992-01-28
申请号：US502438
申请日：1990-03-30
申请人： David H. Coy , Jacques-Pierre Moreau , Sun H. Kim
发明人： David H. Coy , Jacques-Pierre Moreau , Sun H. Kim
IPC分类号： A61K38/00 , A61K38/22 , A61P1/00 , A61P3/08 , A61P35/00 , C07K7/02 , C07K7/06 , C07K7/08 , C07K7/18 , C07K14/575
CPC分类号： C07K14/57572 , C07K7/02 , C07K7/086 , C07K7/18 , A61K38/00
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 .beta.-amino acid, or a .gamma.-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）非肽键代替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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公开(公告)号：US5462927A
公开(公告)日：1995-10-31
申请号：US990555
申请日：1992-12-14
IPC分类号： A61K38/00 , A61K38/08 , C07K14/685 , C07K14/695 , C07K7/00 , C07K7/06 , C07K14/68
CPC分类号： C07K14/685 , A61K38/08 , C07K14/6955
摘要： Biologically active peptides are disclosed of the formula: A.sup.1 --A.sup.2 --A.sup.3 --A.sup.4 --Phe--Arg--TrP--A.sup.5, or a pharmaceutically acceptable salt thereof; A.sup.1 is H or acetyl; A.sup.2 is Ala, or D--Ala; A.sup.3 is Glu or Gln; and A.sup.4 is His or Tyr; A.sup.5 is NH.sub.2, Gly--NH.sub.2, or D--Ala--NH.sub.2. Pharmaceutical compositions containing these peptides are capable of promoting nerve regeneration and increasing muscle mass or preventing muscle atrophy following an injury.
摘要翻译： 公开了具有下式的生物活性肽：A1-A2-A3-A4-Phe-Arg-TrP-A5或其药学上可接受的盐; A1是H或乙酰基; A2是Ala或D-Ala; A3是Glu或Gln; 而A4是His或Tyr; A5是NH2，Gly-NH2或D-Ala-NH2。 含有这些肽的药物组合物能够促进神经再生和增加肌肉量，或者在损伤后防止肌肉萎缩。
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公开(公告)号：US5162497A
公开(公告)日：1992-11-10
申请号：US282328
申请日：1988-12-09
IPC分类号： A61K38/00 , C07K7/02 , C07K7/08 , C07K7/18 , C07K14/575 , C07K14/685
CPC分类号： C07K7/086 , C07K14/57572 , C07K14/685 , C07K7/02 , C07K7/18 , A61K38/00 , Y10S514/803
摘要： A bradykinin analog which contains nine or ten amino acid residues and at least one [CH.sub.2 NH] pseudopeptide bond, the analog being useful as an antagonist or agonist of the naturally occuring bradykinin.
摘要翻译： 包含9或10个氨基酸残基和至少一个[CH 2 N H]假肽键的缓激肽类似物，该类似物可用作天然存在的缓激肽的拮抗剂或激动剂。
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公开(公告)号：US5073624A
公开(公告)日：1991-12-17
申请号：US352140
申请日：1989-05-15
CPC分类号： C07K7/06 , C07K7/23 , A61K38/00 , Y10S514/80
摘要： A decapeptide of the formula: N-AC-A.sup.1 -A.sup.2 -A.sup.3 -Ser-A-.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.8 -A.sup.9, wherein each A.sup.1, A.sup.2, and A.sup.3, independently, is D-.beta.-Nal, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, or C.sub.1-3 alkyl), D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A.sup.4 is p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A.sup.5 is D-Lys, D-Tyr, D-Arg, D-Phe, D-.beta.-Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), or D-Lys-.epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.10 alkyl group, or an aryl group); A.sub.6 is Leu, .beta.-Nal, p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, C.sub.2 F.sub.5, C.sub.1-3 alkyl), or Trp; A.sup.7 is Arg, Lys, or Lys .epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.6 alkyl group, or an aryl group); A.sub.8 is Pro; and A.sup.9 is D-Ala, D-Ala-NH.sub.2, Ala-NH.sub.2, aminoisobutyric acid amide, or Gly-NH.sub.2 ; provided that at least one of A.sup.2 or A.sup.3 must be D-Phe or D-Tyr, and provided further that when A.sup.4 is Lys or Arg, A.sup.5 must not be D-Arg, D-Lys, D-homo-Arg, D-diethyl-homo-Arg, or D-Lys-.epsilon.-NH-R, or a pharmaceutically acceptable salt thereof.The invention also features a method of treating T-cell-deficient patients, e.g., those suffering from Acquired Immune Dificiency Syndrome, by administering a therapeutically effective amount of an LH-RH antagonist.
摘要翻译： 下式的十肽：N-AC-A1-A2-A3-Ser-A-4-A5-A6-A7-A8-A9，其中每个A1，A2和A3独立地是D-β-Nal， DpX-Phe（其中X是卤素，H，NH 2，NO 2，OH或C 1-3烷基），D-苯并噻吩基（2）-Ala或D-苯并噻吩基（1）-Ala; A4是p-X-Phe（其中X是卤素，H，NH 2，NO 2或C 1-3烷基），Tyr，Lys，Arg，Leu，Trp或Nal; A5是D-Lys，D-Tyr，D-Arg，D-Phe，D-β-Nal，D-Trp，D-均一Arg，D-二乙基均一Arg，DpX-Phe（其中X是卤素 ，H，NH 2，NO 2或C 1-3烷基）或D-Lys-ε--NH-R（其中R为H，支链或直链C 1 -C 10烷基或芳基）; A6是Leu，β-Nal，p-X-Phe（其中X是卤素，H，NH2，NO2，OH，C2F5，C1-3烷基）或Trp; A7是Arg，Lys或Lysε--NH-R（其中R是H，支链或直链的C 1 -C 6烷基或芳基）; A8是Pro A9为D-Ala，D-Ala-NH2，Ala-NH2，氨基异丁酸酰胺或Gly-NH2; 条件是A2或A3中的至少一个必须是D-Phe或D-Tyr，并且进一步提供当A4是Lys或Arg时，A5不得是D-Arg，D-Lys，D-均聚-Gly，D- 二乙基均一Arg或D-Lys-ε--NH-R或其药学上可接受的盐。 本发明还涉及通过施用治疗有效量的LH-RH拮抗剂来治疗T细胞缺陷患者，例如患有获得性免疫性综合征的患者的方法。
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公开(公告)号：US4866160A
公开(公告)日：1989-09-12
申请号：US65765
申请日：1987-06-23
CPC分类号： C07K7/06 , C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： A decapeptide of the formula:N-Ac-A.sup.1 -A.sup.2 -A.sup.3 -Ser-A.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.8 -A.sup.9, wherein each A.sup.1, A.sup.2, and A.sup.3, independently, is D-.beta.-Nal, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, or C.sub.1-3 alkyl), D-Trp, D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A.sup.4 is p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A.sup.5 is D-Lys, D-Tyr, D-Arg, D-Phe, D-.beta.-Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), or D-Lys-.epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.10 alkyl group, or an aryl group); A.sub.6 is Leu, .beta.-Nal, p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, C.sub.2 F.sub.5, C.sub.1-3 alkyl), or Trp; A.sup.7 is Arg, Lys, or Lys .epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.6 alkyl group, or an aryl group); A.sub.8 is Pro; and A.sup.9 is D-Ala, D-Ala-NH.sub.2, Ala-NH.sub.2, aminoisobutyric acid amide, or Gly-NH.sub.2 ; provided that at least one of A.sup.2 or A.sup.3 must be D-Phe or D-Tyr, and provided further that when A.sup.4 is Lys or Arg, A.sup.5 must not be D-Arg, D-Lys, D-homo-Arg, D-diethyl-homo-Arg, or D-Lys-.epsilon.-NH-R, or a pharmaceutically acceptable salt thereof.The invention also features a method of treating T-cell-deficient patients, e.g., those suffering from Acquired Immune Deficiency Syndrome, by administering a therapeutically effective amount of an LH-RH antagonist.
摘要翻译： 下式的十肽：N-Ac-A1-A2-A3-Ser-A4-A5-A6-A7-A8-A9，其中每个A1，A2和A3独立地是D-β-Nal，DpX- Phe（其中X为卤素，H，NH2，NO2，OH或C1-3烷基），D-Trp，D-苯并噻吩基（2）-Ala或D-苯并噻吩基（1）-Ala; A4是p-X-Phe（其中X是卤素，H，NH 2，NO 2或C 1-3烷基），Tyr，Lys，Arg，Leu，Trp或Nal; A5是D-Lys，D-Tyr，D-Arg，D-Phe，D-β-Nal，D-Trp，D-均一Arg，D-二乙基均一Arg，DpX-Phe（其中X是卤素 ，H，NH 2，NO 2或C 1-3烷基）或D-Lys-ε--NH-R（其中R为H，支链或直链C 1 -C 10烷基或芳基）; A6是Leu，β-Nal，p-X-Phe（其中X是卤素，H，NH2，NO2，OH，C2F5，C1-3烷基）或Trp; A7是Arg，Lys或Lysε--NH-R（其中R是H，支链或直链的C 1 -C 6烷基或芳基）; A8是Pro A9为D-Ala，D-Ala-NH2，Ala-NH2，氨基异丁酸酰胺或Gly-NH2; 条件是A2或A3中的至少一个必须是D-Phe或D-Tyr，并且进一步提供当A4是Lys或Arg时，A5不得是D-Arg，D-Lys，D-均聚-Gly，D- 二乙基均一Arg或D-Lys-ε--NH-R或其药学上可接受的盐。 本发明还涉及通过施用治疗有效量的LH-RH拮抗剂来治疗T细胞缺陷患者，例如患有获得性免疫缺陷综合征的患者的方法。
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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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公开(公告)号：US4632979A
公开(公告)日：1986-12-30
申请号：US621673
申请日：1984-06-18
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： A compound having the formula K-His-Trp-Ser-Tyr-M-Q-Arg-Pro-T, wherein K is N-Acetyl-Sarconsine or pGlu; is D-Phe, D-Trp, D-.beta.-Naphthylalanine, or D-4-X-Phe, wherein X is OH, F, Cl, Br, or Me; Q is Leu, Phe, 4-X-Phe, Trp, or .beta.-Naphthylamine (wherein X is OH, F, Cl, Br, or Me), or an N-Me-derivative thereof; and T is Gly-NH.sub.2, NHCH.sub.3, NHCH.sub.2 CH.sub.3, or NHCH.sub.2 CH.sub.2 CH.sub.3 ; provided that, when Q is Leu or N-Me-Leu, K cannot be pGlu; or a pharmaceutically acceptable salt thereof.
摘要翻译： 具有式K-His-Trp-Ser-Tyr-M-Q-Arg-Pro-T的化合物，其中K是N-乙酰基 - 肉桂酸或pGlu; 是D-Phe，D-Trp，D-β-萘基丙氨酸或D-4-X-Phe，其中X是OH，F，Cl，Br或Me; Q是Leu，Phe，4-X-Phe，Trp或β-萘胺（其中X是OH，F，Cl，Br或Me）或其N-Me-衍生物; 和T是Gly-NH 2，NHCH 3，NHCH 2 CH 3或NHCH 2 CH 2 CH 3; 条件是当Q为Leu或N-Me-Leu时，K不能为pGlu; 或其药学上可接受的盐。
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公开(公告)号：US6083915A
公开(公告)日：2000-07-04
申请号：US698681
申请日：1991-05-10
IPC分类号： A61K38/00 , A61K38/04 , A61K38/10 , A61K38/22 , A61P1/16 , A61P35/00 , C07K7/06 , C07K7/08 , A61K38/08
CPC分类号： A61K38/105 , Y10S514/894 , Y10S530/828
摘要： A method of treating liver cancer involving administration to the subject a therapeutically effective amount of a bombesin analog.
摘要翻译： 一种治疗肝癌的方法，涉及向受试者施用治疗有效量的铃蟾肽类似物。
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公开(公告)号：US5877277A
公开(公告)日：1999-03-02
申请号：US337127
申请日：1994-11-10
IPC分类号： A61K38/00 , C07K7/02 , C07K7/08 , C07K7/18 , C07K14/575 , C07K14/685 , C07K5/00 , C07K7/00 , C07K7/06
CPC分类号： C07K7/086 , C07K14/57572 , C07K14/685 , C07K7/02 , C07K7/18 , A61K38/00
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 .beta.-amino acid, or a .gamma.-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）非肽键代替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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公开(公告)号：US5750646A
公开(公告)日：1998-05-12
申请号：US408197
申请日：1995-03-22
摘要： A linear peptide which is an analog of a naturally occurring, biologically active peptide 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 to the naturally occurring peptide being unnecessary for in vivo biological activity, the analog having a non-peptide bond instead of a peptide bond between an amino acid of the active site and an adjacent amino acid, and having the same binding site as the naturally occurring peptide, so that the analog is capable of acting as a competitive inhibitor of the naturally occurring peptide by binding to the receptor and, by virtue of the non-peptide bond, failing to exhibit the in vivo activity of the naturally occurring peptide.
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肽的类似物，以及负责肽与靶细胞上的受体结合的结合位点，将活性位点中的肽键切割成天然 发生的肽对于体内生物活性是不必要的，该类似物具有非肽键而不是活性位点的氨基酸与相邻氨基酸之间的肽键，并且具有与天然存在的肽相同的结合位点，因此 该类似物能够通过结合受体而作为天然存在的肽的竞争性抑制剂，并且由于非肽键，不能显示出天然存在的肽的体内活性。
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