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53 条记录 (耗时 0.024 秒)

    An octapeptide bombesin analog
    2.
    发明授权
    An octapeptide bombesin analog 失效
    十字路口BOMBESIN模拟

    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 。

    Imidazole compounds which reduce gastric acid secretion
    7.
    发明授权
    Imidazole compounds which reduce gastric acid secretion 失效
    减少胃酸分泌的咪唑化合物

    公开(公告)号：US4495193A

    公开(公告)日：1985-01-22

    申请号：US454733

    申请日：1982-12-30

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

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

    IPC分类号： C07D209/46 ,  C07D403/06 ,  C07D403/12 ,  A61K31/415

    CPC分类号： C07D403/06 ,  C07D209/46 ,  C07D403/12

    摘要： A compound having gastric acid secretion reducing activity and having the formula ##STR1## wherein each V and W, independently, is H, --CH.sub.2 COOR.sup.4 where R.sup.4 is H or lower alkyl, --CH.sub.2 CN, or ##STR2## or V and W together represent .dbd.CHCOOR.sup.4 or .dbd.CHCN; A is ##STR3## R.sup.1 is H or CH.sub.3 ; L is CH.sub.2 S; Q is O or CH.sub.2 S; n is 0 or 1; 2 m 4; each R.sup.2 and R.sup.3, independently, is hydrogen, lower alkyl, lower cycloalkyl, or lower aralkyl; or R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, form a 4, 5, or 6 membered heterocyclic ring containing 0, 1, or 2 oxygen atoms and 1, 2, or 3 nitrogen atoms and being unsubstituted or lower alkyl substituted; and Ar is a single ring aromatic group selected from aryl, substituted aryl, fused aryl, or heteroaryl; or the pharmaceutically acceptable salt thereof.

    摘要翻译： 具有胃酸分泌降低活性并具有下式的化合物：其中每个V和W独立地是H，-CH 2 COOR 4，其中R 4是H或低级烷基，-CH 2 CN或V和W一起代表= CHCOOR4或= CHCN; A是 + TR R1是H或CH3; L是CH2S; Q是O或CH2S; n为0或1; 2 m 4; 每个R 2和R 3独立地是氢，低级烷基，低级环烷基或低级芳烷基; 或R 2和R 3与它们所连接的氮原子一起形成含有0,1或2个氧原子和1,2或3个氮原子的4,5或6元杂环，并且是未取代的或低级的 烷基取代; Ar为选自芳基，取代芳基，稠合芳基或杂芳基的单环芳基; 或其药学上可接受的盐。

    Pyrazolo[1,5-a]-1,3,5-triazines
    10.
    发明授权
    Pyrazolo[1,5-a]-1,3,5-triazines 失效
    吡唑并[1,5-a] -1,3,5-三嗪

    公开(公告)号：US4565815A

    公开(公告)日：1986-01-21

    申请号：US614454

    申请日：1984-05-25

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

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

    IPC分类号： A61K31/53 ,  A61P1/04 ,  C07D487/04 ,  A61K31/415 ,  C07D403/14 ,  C07D407/14

    CPC分类号： C07D487/04

    摘要： A compound having anti-ulcer activity and having the formula ##STR1## wherein D is H, SH, NH.sub.2, OH, R.sup.4 S where R.sup.4 is a lower alkyl group; E is OH or NH.sub.2 ; J is H or aryl; X is CH or N; Y is CH, N, or CT, wherein T is a halogen; Z is CH or N; A is ##STR2## and replaces a hydrogen of D, X, or E; R.sup.1 is H or CH.sub.3 ; L is CH.sub.2 S; Q is O or CH.sub.2 S; n is 0 or 1; 2 m 4; each R.sup.2 and R.sup.3, independently, is H, lower alkyl, cycloalkyl, or arylalkyl; or R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, form a 4, 5, or 6 membered heterocyclic ring containing 0, 1, or 2 oxygen atoms and 1, 2, or 3 nitrogen atoms and being unsubstituted or lower alkyl substituted; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 具有抗溃疡活性并具有下式的化合物：其中D是H，SH，NH 2，OH，R 4，其中R 4是低级烷基; E是OH或NH 2; J为H或芳基; X是CH或N; Y是CH，N或CT，其中T是卤素; Z是CH或N; A是 + TR ，代替D，X或E的氢; R1是H或CH3; L是CH2S; Q是O或CH2S; n为0或1; 2 m 4; 每个R 2和R 3独立地是H，低级烷基，环烷基或芳基烷基; 或R 2和R 3与它们所连接的氮原子一起形成含有0,1或2个氧原子和1,2或3个氮原子的4,5或6元杂环，并且是未取代的或低级的 烷基取代; 或其药学上可接受的盐。