Metastin derivatives and use thereof

摘要

The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotropic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids, the metastin derivatives of the present invention achieve more improved blood stability, solubility, etc., reduced gelation tendency, improved pharmacokinetics, as well as exhibit an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity. The metastin derivatives of the present invention also have a gonadotropic hormone secretion suppressing activity, sex hormone secretion suppressing activity, etc.

主权项

1. A compound represented by the formula below, or a salt thereof,
XX0-XX2-XX3-XX4-XX5-T-XX9-XX10-NH2 wherein: XX0 represents C1-12 alkanoyl; XX2 represents D-Tyr; XX3 represents Hyp or Pro(4F); XX4 represents Asn or 2-amino-3-ureidopropionic acid; XX5 represents Thr; T represents a group represented by formula II: Z4 represents O, R2 represents a linear C1-10 alkyl group, which may optionally be substituted with a C3-8 cycloalkyl group; Q1 represents a C1-4 alkyl group, which may optionally be substituted with an optionally substituted non-aromatic cyclic hydrocarbon group having carbon atoms not greater than 7; A represents a carbon atom substituted with hydrogen atom; A′ represents a carbon atom substituted with hydrogen atom or O; Q2 represents CH2; Y represents —CONH—; XX9 represents Arg or Arg(Me); and, XX10 represents Trp.