Patent ID: 6344477
Filing Date: 2002-02-05
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 an EP4 receptor agonist according to formula I: wherein:R1=CO2R, CONR4R5, or CH2OR6, where: R=H or pharmaceutically acceptable cationic salt moiety, or CO2R=pharmaceutically acceptable ester moiety; R4, R5=same or different=H or alkyl, and R6=H, acyl, or alkyl; n=0 or 2; one of R9a, R9b=H and the other=OR7, where R7=H, alkyl, or acyl; or, R9bR9a taken together=O as a carbonyl; X=H, Cl, F, or OR8 in either configuration, where R8=H, alkyl, or acyl; B=O, or H and OR10 in either configuration, where R10=H, alkyl, or acyl; - - - -=single or double bond; R2, R3=same or different=H or alkyl, or R2, R3 may be combined to form a C3-C7 cycloalkyl; A=H, C2-C6 alkyl, C3-C7 cycloalkyl, (CH2)nâ€²â€²D, (CH2)nâ€²OD, where: nâ€²=1-4; and D=â€ƒwherein: nâ€³=0-3; Z=H, halogen, C1-C4 alkyl, C1-C4 alkoxy, or CF3; and Yâ€²=CH&boxH;CH, O, or S; with the proviso that when R2-R3 form a cycloalkyl, then A=H;with the further provisos that:when R9aR9b=O as a carbonyl, then X=H or OR8 in either configuration and Aâ‰ (CH2)nâ€²D or (CH2)nâ€²OD; when one of R9a, R9b=H and the other=OR7, then R2=R3=H and A=(CH2)nâ€²D or (CH2)nâ€²OD; and PGE1 and PGE2 are excluded.