Patent ID: 6462080
Filing Date: 2002-10-08
Classification: A61K,Y10S

Abstract:
A method for the treatment of dry eye in mammals comprising administering to an affected eye, a pharmaceutically effective amount of a compound of formula I: wherein:R1=(CH2)nCO2R, (CH2)nCONR4R5, (CH2)nCH2OR6, (CH2)nCH2NR7R8, where: R=H or pharmaceutically acceptable cationic salt moiety, or CO2R forms a pharmaceutically acceptable ester moiety; R4, R5=same or different=H, alkyl, or SO2CH3, with the proviso that if one of R4, R5=SO2CH3, then the other=H or alkyl; R6=H, acyl, or alkyl; R7, R8=same or different=H, acyl, or alkyl; with the proviso that if one of R7, R8=acyl, then the other=H or alkyl; n=0 or 2; ----=single or double bond, which may be cumulated to form an allene; R9b=Cl, and R9a=H, or R9bR9a taken together=O as a carbonyl; Y=CH2, O, or â€ƒwhere R11=H, alkyl, or acyl; A=O and B=CH2; or, Aâ€”B=CH2CH2 or cis-CH&boxH;CH; with the proviso that Aâ‰ O when Y=O. one of C, D=H, and the other=CH3 or OR2, where R2=H, acyl, or alkyl; or C=D=H; E and F=same or different=H or CH3; or one of E, F=CH3 and the other=OR2, where R2 is defined as above; with the proviso that exactly one of C, D, E, and F=OR2; X=O or direct bond; R20=C2-8 alkyl, C2-8 alkenyl, aryl, heteroaryl, aryloxy, or heteroaryloxy, optionally substituted with halo, trihalomethyl, OR3, NR3R21, wherein R3=H, alkyl, or acyl; and R21=H, alkyl, or acyl; with the proviso that if one of R3 and R21=acyl, then the other=H or alkyl; and wherein the C2-8 alkyl and C2-8 alkenyl may be optionally terminated by C3-8 cycloalkyl, C4-8 cycloalkenyl, aryl, heteroaryl, aryloxy, or heteroaryloxy, optionally substituted as described above; with the proviso that R20â‰ aryloxy or heteroaryloxy when X=O; with the proviso that the following compounds of formula I be excluded: those wherein all of the following limitations are satisfied: ----=a single bond between carbons 4 and 5 and a single or double bond between carbons 5 and 6; R9aR9b=O as a carbonyl; Y=CH2 or â€ƒwhere R11 as defined above; Aâ€”B=CH2CH2 or CH&boxH;CH; one of C, D=H and the other=OR2, where R2 is as defined above; and E and F=same or different=H or CH3.