Ophthalmic formulations containing substituted gamma lactams and methods for use thereof

摘要

The invention provides ophthalmic formulations containing well-defined substituted gamma lactams. The formulations described herein are useful in treating a variety of ocular diseases related to ocular hypertension, such as for example, glaucoma.

主权项

1. An ophthalmic formulation comprising at least one therapeutically active agent at a concentration of from 0.01 to 0.12% (w/v) in an ophthalmically acceptable liquid vehicle, wherein the active agent has the structure: or a pharmaceutically acceptable salt thereof, wherein:
A is —(CH2)6—, cis-CH2CH═CH—(CH2)3—, or —CH2C≡C—(CH2)3—, wherein one or two CH2 moieties may be substituted with S or O; orA is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is from 1 to 4, and wherein one or two CH2 moieties are substituted with S or O;R1 is H or C1 to C6 alkyl; andB is optionally substituted aryl or optionally substituted heteroaryl.