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10 条记录 (耗时 0.03 秒)

    Opioid peptides
    4.
    发明授权
    Opioid peptides 失效
    阿片类肽

    公开(公告)号：US5663295A

    公开(公告)日：1997-09-02

    申请号：US352391

    申请日：1994-12-08

    申请人： Jacques-Pierre Moreau ,  Sun Hyuk Kim ,  John E. Taylor

    发明人： Jacques-Pierre Moreau ,  Sun Hyuk Kim ,  John E. Taylor

    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。

    Octapeptide bombesin analogs
    6.
    发明授权
    Octapeptide bombesin analogs 失效
    八肽铃蟾肽类似物

    公开(公告)号：US5877277A

    公开(公告)日：1999-03-02

    申请号：US337127

    申请日：1994-11-10

    申请人： David H. Coy ,  Jacques-Pierre Moreau ,  Sun Hyuk Kim

    发明人： David H. Coy ,  Jacques-Pierre Moreau ,  Sun Hyuk Kim

    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 。

    Bradykinin analogs with non-peptide bond
    7.
    发明授权
    Bradykinin analogs with non-peptide bond 失效
    具有非肽键的缓激肽类似物

    公开(公告)号：US5750646A

    公开(公告)日：1998-05-12

    申请号：US408197

    申请日：1995-03-22

    申请人： David H. Coy ,  Jacques-Pierre Moreau ,  John E. Taylor ,  Sun Hyuk Kim

    发明人： David H. Coy ,  Jacques-Pierre Moreau ,  John E. Taylor ,  Sun Hyuk Kim

    IPC分类号： A61K38/00 ,  C07K7/18 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

    CPC分类号： C07K7/18 ,  A61K38/00

    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。

    Octapeptide bombesin analogs
    8.
    发明授权
    Octapeptide bombesin analogs 失效
    八肽铃蟾肽类似物

    公开(公告)号：US06307017B1

    公开(公告)日：2001-10-23

    申请号：US09260846

    申请日：1999-03-02

    申请人： David H. Coy ,  Jacques-Pierre Moreau ,  Sun Hyuk Kim

    发明人： David H. Coy ,  Jacques-Pierre Moreau ,  Sun Hyuk Kim

    IPC分类号： A61K3800

    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 &bgr;-amino acid, or a &ggr;-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 。

    Linear therapeutic peptides
    9.
    发明授权
    Linear therapeutic peptides 失效
    线性治疗肽

    公开(公告)号：US5767236A

    公开(公告)日：1998-06-16

    申请号：US387634

    申请日：1995-02-13

    申请人： Sun Hyuk Kim ,  Jacques-Pierre Moreau

    发明人： Sun Hyuk Kim ,  Jacques-Pierre Moreau

    IPC分类号： A61K38/00 ,  C07K7/08 ,  C07K5/00 ,  C07K7/00 ,  C07K15/00

    CPC分类号： C07K7/086 ,  A61K38/00

    摘要： The invention features linear therapeutic peptides of the following formula: ##STR1## in which A.sup.1 is a D-.alpha.-aromatic amino acid or a D-.alpha.-tethered amino acid; A.sup.2 is Gln, His, 1-methyl-His, or 3-methyl-His; A.sup.3 is the D- or L-isomer selected from Nal, Trp, Phe, and p-X-Phe, where X is F, Cl, Br, NO.sub.2, OH or CH.sub.3 ; A.sup.4 is Ala, Val, Leu, Ile, Nle, or .alpha.-aminobutyric acid; A.sup.5 is Val, Ala, Leu, Ile, Nle, Thr, or .alpha.-aminobutyric acid; A.sup.6 is Gly, Sar, .beta.-Ala, or the D-isomer selected from Ala, N-methyl-Ala, Trp, and Nal; A.sup.7 is His, 1-methyl-His, 3-methyl-His, Lys, or .epsilon.-alkyl-Lys; A.sup.8 is Leu, Ile, Val, Nle, .alpha.-aminobutyric acid, Trp, Pro, Nal, Chx-Ala, Phe, or p-X-Phe, where X is F, Cl, Br, NO.sub.2, OH or CH.sub.3 ; A.sup.9 is Met, Met-oxide, Leu, Ile, Nle, .alpha.-aminobutyric acid, or Cys; each R.sub.1 and R.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, or COE.sub.1, where E.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkynyl, phenyl, 3,4-dihydroxyphenylalkyl, naphthyl, or C.sub.7-10 phenylalkyl; provided that when either R.sub.1 or R.sub.2 is COE.sub.1, the other must be H; and R.sub.3 is OH, NH.sub.2, C.sub.1-12 alkoxy, C.sub.7-10 phenylalkoxy, C.sub.11-20 naphthylalkoxy, C.sub.1-12 alkylamino, C.sub.7-10 phenylalkylamino, C.sub.11-20 naphthylalkylamino; or a pharmaceutically acceptable salt of such peptides.

    摘要翻译： 本发明的特征在于线性治疗肽，其具有以下结构式：其中A1是D-α-芳香族氨基酸或D-α-被束缚氨基酸的 A2是Gln，His，1-甲基-He或3-甲基-He; A3是选自Nal，Trp，Phe和p-X-Phe的D-或L-异构体，其中X是F，Cl，Br，NO 2，OH或CH 3; A4是Ala，Val，Leu，Ile，Nle或α-氨基丁酸; A5是Val，Ala，Leu，Ile，Nle，Thr或α-氨基丁酸; A6是Gly，Sar，β-Ala或选自Ala，N-甲基-Ala，Trp和Nal的D-异构体; A7是His，1-甲基-He，3-甲基-His，Lys或ε-烷基-Ilu; A8是Leu，Ile，Val，Nle，α-氨基丁酸，Trp，Pro，Nal，Chx-Ala，Phe或p-X-Phe，其中X是F，Cl，Br，NO 2，OH或CH 3; A9是Met，Met-氧化物，Leu，Ile，Nle，α-氨基丁酸或Cys; 每个R1和R2独立地是H，C1-12烷基，C7-10苯基烷基或COE1，其中E1是C1-20烷基，C3-20烯基，C3-20炔基，苯基，3,4-二羟基苯基烷基，萘基 或C7-10苯基烷基; 条件是当R1或R2是COE1时，另一个必须是H; 并且R 3是OH，NH 2，C 1-12烷氧基，C 7-10苯基烷氧基，C 11-20萘基烷氧基，C 1-12烷基氨基，C 7-10苯基烷基氨基，C 11-20萘基烷基氨基; 或这些肽的药学上可接受的盐。