Patent ID: 6429227
Filing Date: 2002-08-06
Classification: A61P,C07C,Y10S

Abstract:
In a pharmaceutical composition for treating dry eye and other disorders requiring the wetting of the eye comprising a HETE derivative according to formulas (I), (II) or (III): wherein:X is OR or NHRâ€²; R is H, a cationic pharmaceutically acceptable salt moiety, substituted or unsubstituted alkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, arylalkyl, wherein the substitution is made with a moiety selected from the group consisting of: alkyl, halogen, hydroxy and functionally modified hydroxy; Râ€² is H, substituted or unsubstituted alkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, arylalkyl, wherein the substitution is made with a moiety selected from the group consisting of: alkyl, halogen, hydroxy and functionally modified hydroxy; and Y is wherein Râ€³ is H or C(O)Râ€², the improvement wherein the HETE derivative is an improved stability HETE derivative having X is OR; R is a cationic pharmaceutically acceptable salt moiety, such that X is Oâˆ’M+; M+ is a pharmaceutically acceptable cation selected from the group consisting of: Na+, K+, Li+, Cs+, (A)4N+; and A is independently H, alkyl, cycloalkyl, (cycloalkyl)alkyl, alkyl(cycloalkyl), aryl, arylalkyl, heteroaryl, or (A)4N+ together form a heteroaryl, heterocycloalkenyl or heterocycloalkyl ring, and the composition further comprises ethanol.