Patent ID: 6566327
Filing Date: 2003-05-20
Classification: A61K,C07K

Abstract:
A compound of Formula I: whereinR1 represents hydrogen, alkyl, alkenyl, alkynyl, â€”(CH2)nâ€”NH2, â€”(CH2)nâ€”NHâ€”C(&boxH;NH)NH2, or â€ƒwherein â€œnâ€  is an integer from 0 to 10; R2 represents â€”(CH2)nCONH2, wherein â€œnâ€  represents an integer from 0 to 10; R3 represents hydrogen, alkyl, alkenyl, alkynyl, the radical of formula: or the radical of formula: â€ƒwherein â€œnâ€  represents an integer from 0 to 10; and R11, R12 and R13 may be the same or different and represent hydrogen, alkyl, alkenyl, alkynyl, â€”I, â€”F, â€”Br, â€”Cl, or â€”OH; and R4 represents â€”(CH2)nNH2, â€”(CH2)nNHC(&boxH;NH)NH2, or â€ƒwherein â€œnâ€  represents an integer from 0 to 10; R5 and R9 may be the same or different and represent hydrogen, alkyl, alkenyl, alkynyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, dialkylamino, or â€”(CH2)naryl, wherein â€œnâ€  is an integer from 1 to 10; R6, R7, and R8 may be the same or different and represent hydrogen, alkyl, alkenyl, or alkynyl; R10 represents hydroxy, alkoxy, alkenyloxy, alkynyloxy, amino, alkylamino, dialkylamino, alkylaryl, arylalkoxy, aryloxy, alkoxyaryl, A1, A1-A2, A1-A2-A3, A1-A2-A3-A4, or, A1-A2-A3-A4-A5, â€ƒwherein A1 represents threonine or serine; A2 represents leucine, glycine, alanine, valine, or isoleucine; A3 represents tyrosine, phenylalanine, or tryptophan; A4 represents glycine, alanine, leucine, isoleucine, or valine; and A5 represents phenylalanine, tyrosine, or tryptophan; or pseudopeptide analogues thereof wherein one or more of the carbonyl groups of the peptide linkage is replaced by â€”C(&boxH;S)â€” or by â€”CH2â€”, and/or wherein one or more of the amide bonds, â€”C(O)â€”NHâ€”, is replaced by the retro-inverso form, â€”NHâ€”C(O)â€”, thereof; and pharmaceutically acceptable salts and esters thereof, with the proviso that the compound is not selected from the group consisting of: H-glycine-glutamine-glycine-arginine-threonine-leucine-tyrosine-glycine-phenylalanine (SEQ ID NO: 16); H-valine-glutamine-tryptophan-lysine (SEQ ID NO: 18); H-histidine-asparagine-leucine-lysine (SEQ ID NO: 19); H-leucine-glutamine-&PSgr;(CSâ€”NH)leucine-lysine (SEQ ID NO: 20); H-lysine-glutamine-phenylalanine-lysine (SEQ ID NO: 21); and H-glycine-glutamine-leucine-lysine (SEQ ID NO: 22).