| 摘要 |
<p>The invention relates to novel peptides and peptide derivatives which act as antagonists of natural LH-RH and have the general formula:
<UnorderedLists id="ula01" listStyle="none"><ListItem>X-R<Sup>1</Sup>-R<Sup>2</Sup>-R<Sup>3</Sup>-Ser-Tyr-R<Sup>4</Sup>-R<Sup>5</Sup>-R<Sup>6</Sup>-R<Sup>7</Sup>-R<Sup>8</Sup>-NH<Sub>2</Sub> wherein</ListItem><ListItem>X represents hydrogen or a lower acyl (1-6 C) group,</ListItem><ListItem>R' and R<Sup>2</Sup> represent either the same or different groups selected from D-Bal (2), D-Bal (3), D-Nal (1), D-Nal (2), D-Phe or D-Phe substituted at the phenyl moiety by one or more halogen, alkyl (1-4 C), alkoxy (1- 4 C) or nitro groups; R' represents D-Trp, D-Bal (2), D-Bal (3), D-Nal (1), D- Nal (2) or D-Pal, with the proviso that at least one of the symbols R' or R<Sup>3</Sup> represents a D-Bal (2) or D-Bal (3) group;</ListItem><ListItem>R<Sup>4</Sup> represents D-Arg, D-Lys, D-homo Arg or D-dialkyl (1-4 C)-homo Arg;</ListItem><ListItem>R<Sup>5</Sup> represents L-Leu, L-Met or the alkyl (1-4C) or phenylalkyl</ListItem><ListItem>(7-10C) ether of L-Cys, L-Ser or L-homo Ser;</ListItem><ListItem>R<Sup>6</Sup> represents L-Lys or L-Arg;</ListItem><ListItem>R<Sup>7</Sup> represents L-Pro or L-thiaprolyl, and</ListItem><ListItem>R<Sup>8</Sup> represents D-Ala or Gly.</ListItem></UnorderedLists></p><p>The invention also includes the acid addition salts of the above defined peptides.</p> |
