Novel GnRH analogues with antitumour effects and pharmaceutical compositions thereof

A pharmacologically active compound of formula (I)

• Y(Wu,Vz,Xr,Ak) (I)
• wherein
• Y represents the molecular moiety of formula (Ia),
• wherein n is an integer from 10 to 400;
• one of R1 and R2 represents hydrogen atom whereas the other one represents a group of formula (B);
• R3 represents a polymerization-initiating group;
• W represents a hydroxyl group, optionally as a salt formed with an alkali metal ion;
• V represents a C1-8 alkylamino group bonded through its amino group or a valence bond;
• X is a “spacer” group being an amino acid group or an oligopeptide group of at most six members wherein the amino acid or oligopeptide group is coupled through its N-terminal to the Y group and is optionally bearing a hydroxyl group or a valence bond on its C-terminal, wherein the amino acids are Gly, Ala, Leu, Ile, Val, Phe, Tyr, Ahx, Pro, Arg, or His;
• A is present and represents a pharmacologically active polypeptide hormone group containing an amino group and directly coupled therethrough to the Y group when r is 0;
• or coupled to the C-terminal of the X group, respectively, when r is larger than 0;
• r is an integer from 0 to 0.2 n;
• k is an integer being at most equal to r;
• z is an integer from 0 to (n-r);
• and
• u is an integer from n to 2n-r-z, as well as the salts and complexes of these compounds.

A compound containing an activated ester group of formula (Ic),

• Y[Wu,V′z,(XOQ)r] (Ic)
• wherein Y represents the molecular moiety of formula (Ia), wherein n is an integer from 10 to 400;
• one of R1 and R2 represents hydrogen atom whereas the other one represents a group of formula (B);
• R3 represents a polymerization-initiating group;
• W represents a hydroxyl group, optionally as a salt formed with an alkali metal ion;
• V′ represents a C1-8, alkylamino group bonded through its amino group;
• X represents an amino acid group or an oligopeptide group of at most six members coupled through its N-terminal to the Y group;
• OQ represents an activated ester group on C-terminal of the X group;
• r is an integer from 0 to 0.2 n;
• z is an integer from 0 to (n-r);
• and u is an integer from n to (2n-r-z), as well as the salts of these compounds.