促生长素抑制素受体2拮抗剂

摘要

本发明公开了作为促生长素抑制素受体的受体拮抗剂的促生长素抑制素类似物，包括SSTR2-选择性拮抗剂。本发明还公开了相关的化合物、试剂盒和方法，包括与放射性核素络合或缀合的拮抗剂及其用途。本发明拮抗剂用于诊断和治疗赘生性和非赘生性哺乳动物疾病。

主权项

一种与SSTR2结合的促生长素抑制素拮抗剂，选自由下述组成的组：(i)DOTA‑pNO2Phe‑c[DCys‑Tyr‑DTrp‑Lys‑Thr‑Cys]‑DTyr‑NH2；(ii)H2N‑pNO2Phe‑c[DCys‑Tyr‑DAph(Cbm)‑Lys‑Thr‑Cys]‑2Nal‑NH2；(iii)H2N‑pNO2Phe‑c[DCys‑Aph(Hor)‑DAph(Cbm)‑Lys‑Thr‑Cys]‑2Nal‑NH2；(iv)H2N‑Cpa‑c[DCys‑L‑Agl(NMe.苯甲酰基)‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(v)H2N‑Cpa‑c[DCys‑D‑Agl(NMe.苯甲酰基)‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(vi)H2N‑Cpa‑c[DCys‑Leu‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(vii)H2N‑Cpa‑c[DCys‑Aph(Cbm)‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(viii)Cbm‑Cpa‑c[DCys‑Aph(Cbm)‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(ix)DOTA‑βAla‑Cpa‑c[DCys‑Aph(Cbm)‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(x)DOTA‑Peg‑Cpa‑c[DCys‑Aph(Cbm)‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(xi)H2N‑Cpa‑c[DCys‑Aph(Cbm)‑DTrp‑Lys‑Thr‑Cys]‑NH2；(xii)H2N‑Cpa‑c[DCys‑Aph(Cbm)‑DTrp‑Lys‑Thr‑Cys]‑Cha‑NH2；(xiii)H2N‑Cpa‑c[DCys‑Aph(Cbm)‑DTrp‑Lys‑Thr‑Cys]‑Aph(Hor)‑NH2；(xiv)H2N‑Cpa‑c[DCys‑Aph(Cbm)‑DTrp‑Lys‑Thr‑Cys]‑DAph(Cbm)‑NH2；(xv)H2N‑Cpa‑c[DCys‑Aph(Cbm)‑DTrp‑Lys‑Thr‑Cys]‑Aph(Cbm)‑NH2；(xvi)H2N‑Cpa‑c[DCys‑Aph(Cbm)‑DTrp‑Lys‑Thr‑Cys]‑DAph(Cbm)‑GlyOH；(xvii)H2N‑Cpa‑c[DCys‑Aph(CONH‑OCH3)‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(xviii)H2N‑Cpa‑c[DCys‑Aph(CONH‑OH)‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(xix)H2N‑Cpa‑c[DCys‑Aph(Cbm)‑5F‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(xx)H2N‑Cpa‑c[DCys‑Aph(Cbm)‑5F‑Trp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(xxi)H2N‑Cpa‑c[DCys‑Tyr‑DAph(Cbm)‑Lys‑Thr‑Cys]‑2Nal‑NH2；(xxii)H2N‑Cpa‑c[DCys‑Aph(Hor)‑DAph(Cbm)‑Lys‑Thr‑Cys]‑2Nal‑NH2；(xxiii)Ac‑pNO2Phe‑c[DCys‑Tyr‑DTrp‑Lys‑Thr‑Cys]‑DTyr‑NH2；(xxiv)H2N‑Cpa‑c[DCys‑Tyr‑DTrp‑Lys‑Thr‑Cys]‑2Nal‑NH2；(xxv)H2N‑Cpa‑c[DCys‑Tyr‑DTrp‑NMeLys‑Thr‑Cys]‑2Nal‑NH2；(xxvi)DOTA‑Cpa‑c[DCys‑Aph(Hor)‑Aph(Cbm)‑Lys‑Thr‑Cys]‑DTyr‑NH2；(xxvii)DOTA‑Cpa‑c[DCys‑Tyr‑DAph(Cbm)‑Lys‑Thr‑Cys]‑DTyr‑NH2；和(xxviii)DOTA‑Cpa‑[DCys‑Pal‑DAph(Cbm)‑Lys‑Thr‑Cys]DTyr‑NH2。