ACID 5,6,7-TRIHYDROXIHEPTANOIC AND ANALOGS FOR THE TREATMENT OF EYE DISEASES AND DISEASES ASSOCIATED WITH THE ANGIOGENIC AND HYPERPROLIFERATIVE RESPONSES.

摘要

Use in the preparation of a medicament for the treatment of people suffering from a posterior segment eye disease or a hyperproliferative cell disorder, of one or more compounds of formula I: ** (See formula) ** in which R1 is C2H5, CO2R, CONR2R3, CH2OR4 or CH2NR5R6; R is H, branched or straight chain C1-C6 alkyl, or branched or straight chain C3-C6 alkenyl, branched or straight chain C3-C6 alkynyl, C3-C6 cycloalkyl, or phenyl; or R1 is a carboxylate salt of formula CO2-R +, in which R + is Li +, Na +, K +, or an ammonium moiety of formula + NR10R11R12R13, in which R10, R11, R12 and R13 are independently H or C1- alkyl C6 branched or straight chain, each alkyl group optionally presenting an OH or OCH3 substituent; R2, R3 are independently H, branched or straight chain C1-C6 alkyl, branched or straight chain C3-C6 alkenyl, branched or straight chain C3-C6 alkynyl, C3-C6 cycloalkyl, benzyl, phenyl, OH, OCH3, or OC2H5, provided that at most only one of R2, R3 is OH, OCH3, or OC2H5; R4 is H, C (O) R14, branched or straight chain C1-C6 alkyl, branched or straight chain C3-C6 alkenyl, branched or straight chain C3-C6 alkynyl, C3-C6 cycloalkylbenzyl, or phenyl; R5, R6 are independently H, C (O) R14 branched or straight chain C1-C6 alkyl, branched or straight chain C3-C6 alkenyl, branched or straight chain C3-C6 alkynyl, C3-C6 cycloalkyl, benzyl, phenyl , OH, OCH3, or OC2H5, provided that, at most, only one of R5, R6 is OH, OCH3 or OC2H5; X is O, CH2 or S; R7, R8 and R9 are independently H, CH3, C2H5, C (O) R14, C (O) NR14R15 or CO2R15; or R7 and R8 or R8 and R9 together constitute a carbonyl group (C = O), thus forming a cyclic carbonate; or OR8R1 together form a cyclic ester (a lactone); R14 and R15 are H, branched or straight chain C1-C8 alkyl, branched or straight chain C3-C6 alkenyl, branched or straight chain C3-C6 alkynyl, C3-C6 cycloalkyl, benzyl, or phenyl; and ** (See formula) ** indicates that the OR9 substituent can be arranged to provide the absolute R or S configuration at that position: ** (See formula) **