Polycyclic guanine derivatives
AssigneeSchering Corporation
InventorsBernard R. Neustadt, Neil A. Lindo, Brian A. Mc Kittrick
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AssigneeSchering Corporation
InventorsBernard R. Neustadt, Neil A. Lindo, Brian A. Mc Kittrick
Estimating the term…
Novel polycylic guanine derivatives of the formula: ##STR1## wherein J is oxygen or sulfur, R.sup.1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy; R.sup.2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino, monoalkyl amino or dialkylamino, or --(CH.sub.2).sub.m TCOR.sup.20 wherein m is an integer from 1 to 6, T is oxygen or --NH-- and R.sup.20 is hydrogen, aryl, heteroaryl, alkyl or alkyl substituted with aryl or heteroaryl; R.sup.3 is hydrogen, halo, trifluoromethyl, alkoxy, alkylthio, alkyl, cycloalkyl, aryl, aminosulfonyl, amino, monoalkylamino, dialkylamino, hydroxyalkylamino, aminoalkylamino, carboxy, alkoxycarbonyl or aminocarbonyl or alkyl substituted with awl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino; R.sup.a, R.sup.b, R.sup.c, and R.sup.d are defined in the specification; and n is zero or one. The compounds of formulas (I) and (I') are useful as antihypertensive, muscle relaxant and bronchodilating agents.
A compound of the formula:
A pharmaceutical composition comprising a compound of formula (I) or (I')in an amount effective to inhibit phosphodiesterase.
A pharmaceutical composition comprising a compound of formula (I) or (I') in an amount effective to relax smooth muscle.
A pharmaceutical composition comprising an anti-hypertensive or a bronchodilating effective amount of the compounds (I) or (I').
A method for treating hypertension or bronchoconstriction in a mammal comprising administering to a mammal in need of such treatment an amount of at least one of compounds (I) or (I') effective to treat any of the above diseases.
A method for maintaining or increasing guanosine 3':5'-cyclic monophosphate (cGMP) levels in a mammal by administering an amount of compounds (I) or (I') effective to maintain or increase cGMP.
Dependencies are inferred from the claim text.