Non-acidic cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives as therapeutic agents
AssigneeAllergan, Inc.
InventorsDavid F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
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AssigneeAllergan, Inc.
InventorsDavid F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
Estimating the term…
The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives, substituted in the 1-position with halo, methyl, hydroxyl, nitro, amino, amido, azido, oxime, cyano, thiol, either or thioether groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) derivatives. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) derivatives of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) derivatives of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.
A method of treating ocular hypertension which comprises applying to the eye an amount sufficient to treat ocular hypertension of a compound of formula I ##STR11## wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to six carbon atoms, which radical may substituted with one or more hydroxy, oxo, alkyloxy or akylcarboxy groups, B is a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of phenyl, thienyl, furanyl and pyridyl;
A method of treating ocular hypertension which comprises applying to the eye an amount sufficient to treat ocular hypertension of a compound is a compound of formula II ##STR12## wherein y is 0 or 1 and either the .alpha. or .omega. chain may be unsaturated, Y is a radical selected from the group consisting of halo, nitro, amino, thiol, hydroxy, alkyloxy and alkylcarboxy, n is 0 or an integer of from 1 to 3 R.sub.3 and is .dbd.O,--OH or --O(CO)R.sub.6.
Dependencies are inferred from the claim text.