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    • 50. 发明公开
    • Therapeutic decapeptides
    • 治疗脱卡肽
    • EP0225746A2
    • 1987-06-16
    • EP86308905.8
    • 1986-11-14
    • The Administrators of The Tulane Educational Fund
    • Coy, David H.Moreau, Jacques-Pierre
    • C07K7/06C07K7/20A61K37/02
    • C07K7/23A61K38/00
    • A decapeptide of the formula:
      A 9 , wherein each A 1 , A2, and A3, independently, is D-β-Nal, D-p-X-Phe (where X is halogen, H, NH 2 , NO 2 , OH, or C 1-3 alkyl), D-Trp, D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A4 is p-X-Phe (where X is halogen, H, NH 2 , N0 2 , or C 1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A 5 is D-Lys, D-Tyr, D-Arg, D-Phe, D-β-Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH 2 , N0 2 , or C 1-3 alkyl), or D-Lys-ε-NH-R (where R is H, a branched or straight chain C 1 -C 10 akyl group, or an aryl group); A 6 is Leu, β-Nal, p-X-Phe (where X is halogen, H, NH 2 , N0 2 , OH, C 2 F 5 , C 1-3 alkyl), or Trp; A 7 is Arg, Lys, or Lys-e-NH-R (where R is H, a branched or straight chain C 1 -C 6 alkyl group, or an aryl group); As is Pro; and A 9 is D-Ala, D-Ala-NH 2 , Ala-NH 2 , aminoisobutyric acid amide, or Gly-NH 2 ; provided that at least one of A 2 or A3 must be D-Phe or D-Tyr, and provided further that when A4 is Lys or Arg, A 5 must not be D-Arg, D-Lys, D-homo-Arg, D-diethyl-homo-Arg, or D-Lys-ε-NH-R, or a pharmaceutically acceptable salt thereof, can be used to inhibit the release of sex hormones in the treatment or prophylaxis of various sex hormone-released conditions. They may also be used as female contraceptives.
    • 下式的十肽:N-Ac-A 1 -A 2 -A 3 -Ser-A 4 -A 5 -A 6 -7 -A -A 8 > -A <9>,其中每个A 1,A 2和A 3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-Trp,D-苯并噻吩基(2)-Ala或D-苯并噻吩基(1)-Ala; A 4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; A 5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是H,支链或直链C 1 -C 10烷基或芳基)。 A 6是Leu,β-Nal,p-X-Phe(其中X是卤素,H,NH 2,NO 2,OH,C 2 F 5,C 1-3烷基)或Trp; A 7是Arg,Lys或Lys-ε--NH-R(其中R是H,支链或直链的C 1 -C 6烷基或芳基); A <8>是Pro A 9为D-Ala,D-Ala-NH 2,Ala-NH 2,氨基异丁酸酰胺或Gly-NH 2; 条件是A 2或A 3中的至少一个必须是D-Phe或D-Tyr,并且进一步提供当A 4为Lys或Arg时,A 5不得为D-Arg, D-Lys,D-homo-Arg,D-二乙基高-Arg或D-Lys-ε--NH-R或其药学上可接受的盐可用于抑制性激素在治疗或预防中的释放 各种性激素释放条件。 它们也可以用作女性避孕药。