USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CESKE REPUBLIKY
发明人:
HOLY, ANTONIN,DE CLERCQ, ERIK DESIRE ALICE
申请号：
ES96909007
公开号：
ES2392840T3
申请日:
1996.04.19
申请国别(地区):
ES
年份:
2012
代理人:
摘要：
A compound having the structure (2) wherein: Y is, independently, -OH, -OR 3, -OCH (R16) OC (O) R3, a monophosphate, a diphosphate, an amidate amino acid 10 of an amidate polypeptide, -NHR 3, or -N (R3) 2 R3 is independently C1-C15 alkyl, aryl, C2-C15 alkenyl, C2-C15 alkynyl, alkaryl, alkynylaryl or alkenylaryl said unsubstituted or substituted with C1-C6 alkoxy, C1-C6 carboxilalquil ester, halo, carboxy, hydroxy, cyano, nitro, N-morpholino, or amino groups being and / or said groups having -CH 2 substituted by NH, S, or O R2 and R2 are independently halo, NH2, X or H, but at least one of R2 and R2 is X R16 is R3 Ho and X is - (CH2) m (O) n (CH2) mN (R10) 2 wherein m is 0-2, n is 0-1 it, and R10 is independently: - H, or - cyclopropyl, alkenyl C2- C15, C2-C15, or C1-C6 alkylamino- C1-C6 alkyl, or - C2-C15 alkyl, C3-C15 alkynyl, C3-C15, C1-C6 alkylamino- C1-C6 heteroalkyl, C6- C15, heterocycloalkyl or C3-C6, where the methylene in the alkyl moiety not adjacent to N6 has been replaced by -O-, optionally one of the above groups R10 is substituted with 1 to 3 halo, CN or N3 but at least one group R10 is not H and Z is N or CH, with the condition that the core varies heteríclico purine by no more than one Z E is - (CH2) 2-, -CH (CH3) CH2-, -CH (CH2F) CH2-, -CH (CH2O) CH2-, -CH (CH> = CH2) CH2-, -CH (C> = CH) CH2-, -CH (CH2N3) CH2-, -CH (R6) OCH (R6 ) -, -CH (R9) CH2O- or -CH (R8) O-, wherein the right hand bond is linked the 9 position of the purine, monoazapurina or monodesazapurina heterocycle and wherein Y and the hydroxyl group of -CH (CH2OH) CH2-, or a hydroxyl group present in R6, R8, or R9 are joined to form a ring 6 members R6 and R6 are independently H, C1-C6 alkyl, C1-C6 hydroxyalkyl, or C2-C7 alkanoyl R8 is H, C1-C6 alkyl, hydroxyalkyl or C1-C6 C1-C6 haloalkyl and R9 is H, hydroxymethyl or acyloxymethyl and therapeutically acceptable salts thereof with the proviso that when E is -CH (CH3) CH2- and R2 is NH2, then X is not cyclopropylamino.Un compuesto que tien
