Patent ID: 6511961
Filing Date: 2003-01-28
Classification: A61K,C07K

Abstract:
A cyclic peptide represented by formula (I) where, in formula (I),A and F may be the same or different, and are both selected from the group consisting of L- or D-form Cys, homo-Cys, Pen and Mpr, B is selected from the group consisting of L- or D-form Ala, Ala(t-Bu), Val, Leu, Ile, aIle, Abu, Nle, Nva, Tle, Cha, Chg, Phe, Phg, Trp, Ala(3-Bzt), Ala(1-Naph), Ala(2-Naph), Ala(2-Pyr), Ala(2-Qui), His, Thi, Ala(4-Thz), 2-Abz, Pro, homo-Pro and Tic, C is selected from the group consisting of L-form Asp analogues, Glu analogues, Aad analogues, Asn analogues, Gln analogues, Ser, Ser(OMe), homo-Ser, Dpr, Dab, Orn, Met, Met(O), Met(O2), aIle, Nle, Nva, Chg, Phg, Tyr and Tle and, when C is selected from the group consisting of the L-form Asp analogues, Glu analogues and Aad analogues, then C is of formula (II) n=1 Asp n=2 Glu n=3 Aad where R3 may be hydrogen or a C1 to C6 straight chain or branched alkyl group, provided that when C is an Asn analogue or a Gln analogue, then C is of formula (III) n=1 Asn n=2 Gln where R4 and R5 may be the same or different, and may respectively be hydrogen or a C1 to C6 straight chain or branched alkyl group, D is selected from the group consisting of L- or D-form Tyr, Ser, homo-Ser, Leu, Ile, aIle, Nle, Nva, Chg, Cha, Val, Ala(t-Bu), Abu, Tle, Ala, Phg, homo-Phe, Phe, Ala(2-Naph), Ala(2-Pyr), Ala(3-Bzt), Ala(1-Naph), Ala(2-Qui), Thi, Ala(4-Thz), 2-Abz, Trp and His, E is selected from the group consisting of L- or D-form Leu, Ile, aIle, Nle, Nva, Chg, Cha, Tle, Phg, homo-Phe, Ala(2-Naph), Ala(2-Pyr), Ala(3-Bzt), Ala(1-Naph), Ala(2-Qui), Thi, Ala(4-Thz), 2-Abz and His, G represents a disulphide bond, R1 may be hydrogen or an acyl group, and in the case where R1 is an acyl group, then R1 is of formula (IV) where R6 is selected from the group consisting of a C1 to C6 straight chain or branched alkyl group, a C4 to C8 cycloalkyl group, a C5 to C11 alkylcycloalkyl group, a C6 to C14 aryl group or a C7 to C11 aralkyl group, and R2 may be hydrogen or a C1 to C6 straight chain alkyl or branched alkyl group, or salts thereof.