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105 条记录 (耗时 0.041 秒)

    Hydrophilic somatostatin analogs
    71.
    发明授权
    Hydrophilic somatostatin analogs 失效
    亲水性生长抑素类似物

    公开(公告)号：US06465613B1

    公开(公告)日：2002-10-15

    申请号：US09196259

    申请日：1998-11-19

    申请人： David H. Coy ,  William A. Murphy ,  Eugene A. Woltering ,  Joseph A. Fuselier ,  George Drouant

    发明人： David H. Coy ,  William A. Murphy ,  Eugene A. Woltering ,  Joseph A. Fuselier ,  George Drouant

    IPC分类号： A61K3816

    CPC分类号： C07K14/655 ,  A61K38/00 ,  A61K2123/00

    摘要： The invention features novel somatostatin analogs that may be readily labeled with toxic or non-toxic detectable labels. These unlabeled and labeled analogs are useful for specifically targeting somatostatin receptor bearing cells, in particular neoplastic cells. Labeled analogs are useful, for example, for tumor localization and detection. Where labeled with a toxic label (e.g., radioactivity), the analogs are useful for the targeted delivery of toxicity to somatostatin receptor-bearing cells, in particular neoplastic cells. Also disclosed are methods for treating and detecting neoplasms, and methods for imaging somatostatin receptor-bearing cells.

    摘要翻译： 本发明的特征在于可以容易地用有毒或无毒的可检测标记标记生物素抑制素类似物。 这些未标记和标记的类似物对于特异性靶向生长抑素受体的细胞，特别是肿瘤细胞是有用的。 标记的类似物可用于例如肿瘤定位和检测。 当标记有毒性标签（例如放射性）时，类似物可用于靶向产生生长抑素受体的细胞，特别是肿瘤细胞的毒性递送。还公开了治疗和检测肿瘤的方法，以及用于成像生长抑素受体的方法 细胞。

    Octapeptide bombesin analogs
    72.
    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 。

    Method for synthesizing a peptide containing a non-peptide
    75.
    发明授权
    Method for synthesizing a peptide containing a non-peptide 失效
    合成含有非肽的肽的方法

    公开(公告)号：US4803261A

    公开(公告)日：1989-02-07

    申请号：US879348

    申请日：1986-06-27

    申请人： David H. Coy ,  Simon J. Hocart

    发明人： David H. Coy ,  Simon J. Hocart

    IPC分类号： C07K1/04 ,  C07K1/10 ,  C07K1/113 ,  C07K7/02 ,  C07K7/06 ,  C07K7/23 ,  C07K14/575 ,  C07K14/655 ,  A61K37/02

    CPC分类号： C07K7/23 ,  C07K1/10 ,  C07K7/02

    摘要： This invention features a method for the solid phase synthesis of non-peptide bonds (CH.sub.2 --NH) in polypeptide chains. These polypeptides are synthesized by standard procedures and the non-peptide bond synthesized by reacting an amino aldehyde and an amino acid in the presence of NaCNBH.sub.3.This invention also features somatostatin analogs with non-peptide bonds.This invention further features a solid phase method of chemically modifying a peptide. The method involves synthesizing .alpha.-N-R and side group N-R analogs of peptides, where R is an alkyl or aryl group, by reacting a carbonyl-containing compound and an amino acid in the presence of NaCNBH.sub.3.

    摘要翻译： 本发明的特征在于在多肽链中固相合成非肽键（CH 2 -NH）的方法。 这些多肽通过标准方法合成，通过氨基醛和氨基酸在NaCNBH3存在下反应合成的非肽键。 本发明还涉及具有非肽键的生长抑素类似物。 本发明还涉及化学修饰肽的固相方法。 该方法涉及通过在NaCNBH 3存在下使含羰基的化合物与氨基酸反应来合成肽的α-N-R和侧基N-R类似物，其中R是烷基或芳基。

    Novel nonapeptides, intermediates therefor, and compositions and methods employing said nonapeptides
    77.
    发明授权
    Novel nonapeptides, intermediates therefor, and compositions and methods employing said nonapeptides 失效
    新颖的肽，其中间体，以及使用所述非肽的组合物和方法

    公开(公告)号：US4139504A

    公开(公告)日：1979-02-13

    申请号：US807134

    申请日：1977-06-16

    申请人： David H. Coy ,  Abba J. Kastin

    发明人： David H. Coy ,  Abba J. Kastin

    IPC分类号： A61K38/00 ,  C07K14/67 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K14/672 ,  A61K38/00 ,  Y10S514/809 ,  Y10S930/12

    摘要： Novel nonapeptides having the following amino acid sequence:H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ywherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-proline D-aspartic acid, D-asparagine, D-lysine, D-arginine and D-histidine; and Y is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and lower alkoxy; and the pharmaceutically acceptable salts thereof; intermediates useful in making the novel compounds; and pharmaceutical compositions and methods employing the novel compounds.

    摘要翻译： 具有以下氨基酸序列的新型肽：

    Novel pentacosapeptides, intermediates therefor and pharmaceutical compositions and methods employing said pentacosapeptides
    79.
    发明授权
    Novel pentacosapeptides, intermediates therefor and pharmaceutical compositions and methods employing said pentacosapeptides 失效
    新戊五肽，其中间体以及使用所述五十肽的药物组合物和方法

    公开(公告)号：US4127538A

    公开(公告)日：1978-11-28

    申请号：US807213

    申请日：1977-06-16

    申请人： David H. Coy ,  Abba J. Kastin

    发明人： David H. Coy ,  Abba J. Kastin

    IPC分类号： A61K38/00 ,  C07K14/675 ,  C08L37/00 ,  C07C103/52

    CPC分类号： C07K14/6755 ,  A61K38/00 ,  Y10S514/809 ,  Y10S930/12 ,  Y10S930/28

    摘要： Novel pentacosapeptides having the following amino acid sequenceH-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Phe-Lys-Asn-Ala-Ile-Ile-Lys-Asn-Ywherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-proline D-aspartic acid, D-asparagine, D-lysine, D-arginine and D-histidine; and Y is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and lower alkoxy; and the pharmaceutically acceptable salts thereof; intermediates useful in making the novel compounds; and pharmaceutical compositions and methods employing the novel compounds.

    摘要翻译： 具有以下氨基酸序列H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Ph e-Lys-Asn的新型五肽 -Ala-Ile-Ile-Lys-Asn-Y其中：X是D-氨基酸的手性残基，其选自D-丙氨酸，D-亮氨酸，D-异亮氨酸，D-缬氨酸，D-苯丙氨酸 ，D-酪氨酸，D-色氨酸，D-丝氨酸，D-苏氨酸，D-甲硫氨酸，D-谷氨酸，D-谷氨酰胺，D-脯氨酸D-天冬氨酸，D-天冬酰胺，D-赖氨酸，D-精氨酸和 D-组氨酸 Y选自羟基，氨基，低级烷基氨基，二低级烷基氨基和低级烷氧基; 及其药学上可接受的盐; 用于制备新型化合物的中间体; 以及使用该新化合物的药物组合物和方法。