Patent ID: 7579435
Filing Date: 2009-08-25
Classification: A61K,A61P,C07D,C07K

Abstract:
1. A somatostatin-dopamine chimeric compound of the formula (I), wherein: X is H, Cl, Br, I, F, —CN, or C R1 is H, C R2 and R3, each are, independently H or absent, provided that R2 and R3 are not both absent; R4 is H or —CH Y is —O—, —C(O)—, —S—, —S—(CH R5, R6, R7 and R8 each is, independently, H or C m is 0 or 1; n is 0-10; L is —(CH L is —C(O)—(CR7R8)q-C(O)—, when Y is —N(R6)-, —O—, or —S—; L is -(Doc)t-, when Y is —C(O)—, SC(O)—, —OC(O)—, —S—(CH p is 1-10; q is 2-4; s is 1-10; t is 1-10; wherein said dopamine moiety binds to a dopamine D2 receptor; and Z is an SSTR-2 peptide somatostatin analog selected from the group consisting of; D-Nal-cyclo[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH D-Phe-cyclo[Cys-Tyr-D-Trp-Lys-Thr-Cys]-Nal-NH D-Phe-cyclo[Cys-Tyr-D-Trp-Lys-Abu-Cys]-Thr-NH D-Phe-cyclo[Cys-(3-Bromo-Tyr)-D-Trp-Lys-Thr-Cys]-Thr-NH D-Ser-cyclo[Cys-Phe-D-Trp-Lys-Thr-Cys]-Thr-NH D-Ser-cyclo[Cys-Phe-D-Trp-Lys-Thr-Cys]-Thr-ol; D-Tyr-cyclo[Cys-Phe-D-Trp-Lys-Thr-Cys]-Thr-NH D-Tyr-cyclo[Cys-Phe-D-Trp-Lys-Thr-Cys]-Thr-ol; D-Phe-cyclo[Cys-Phe-D-Trp-Lys-Thr-Cys]-Thr-ol; D-Phe-cyclo[Cys-Tyr-D-Trp-Lys-Val-Cys]-Trp-NH D-Ser-cyclo[Cys-Tyr-D-Trp-Lys-Val-Cys]-Trp-NH D-Tyr-cyclo[Cys-Tyr-D-Trp-Lys-Val-Cys]-Trp-NH D-Phe-cyclo[D-Cys-Pal-D-Trp-Lys-D-Cys]-Thr-(Bzl)-Tyr-NH cyclo[Cys-Phe-Phe-D-Trp-Lys-Thr-Phe-Cys]-NH D-Tyr-cyclo[Cys-Phe-Phe-D-Trp-Lys-Thx-Phe-Cys]-NH cyclo[Cys-Phe-Tyr-D-Trp-Lys-Thr-Phe-Cys]-NH D-Tyr-cyclo[Cys-Phe-Tyr-D-Trp-Lys-Thr-Phe-Cys]-NH Ser-cyclo[Cys-Phe-Phe-D-Trp-Lys-Thr-Phe-Cys]-NH D-Phe-cyclo[Cys-Phe-D-Trp-Lys-Val-Cys]-Thr-NH D-Tyr-cyclo[Cys-Phe-D-Trp-Lys-Val-Cys]-Thr-NH D-Tyr-cyclo[Cys-Tyr-D-Trp-Lys-Abu-Cys]-Thr-NH D-Phe-cyclo[Cys-(3-Iodo-Tyr)-D-Trp-Lys-Val-Cys]-Thr-NH or a pharmaceutically acceptable salt thereof.