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US 4,791,103 AGranted
2,N.sup.6 -disubstituted adenosines, derivatives and methods of use
AssigneeWarner-Lambert Company
InventorsBharat K. Trivedi, Walter Moos, Harriet W. Hamilton, William C. Patt
Life of this patent
Estimating the term…
Abstract
Novel N.sup.6 -substituted adenosines having desirable ratio of affinities at A1 or A2 receptors and highly desirable central nervous system and cardiovascular activities, such as analgesic, antipsychotic, sedative, or antihypertensive as well as immunoinflammatory activity.
Claims48
A compound of the formula
- wherein R.sub.1 is of the formula ##STR3## wherein n is one to four;
- Y is hydrogen, lower alkyl, or OR where R is hydrogen, lower alkyl or lower alkanoyl;
- A is a bond or a straight or branched alkylene of one to four carbon atoms, inclusive with the proviso that A cannot be a bond when R.sub.1 is of Formula II and n is one;
- X and X' are each independently hydrogen, lower alkyl, lower alkoxy, hydroxy, lower alkanoyl, nitro, trifluoromethyl, halogen, amino, monoloweralkyl or diloweralkylamino, or when taken together a methylenedioxy group;
- R.sub.2 is (a) hydrogen, (b) halogen, (c) NR'R" where R' and R" are independently hydrogen, lower alkyl, phenyl, or phenyl substituted by lower alkyl, lower alkoxy, halogen, or trifluoromethyl, (d) SR'" where R'" is hydrogen, lower alkyl, lower alkanoyl, benzoyl, or phenyl;
- R'.sub.2, R'.sub.3, and R'.sub.5 are each independently hydrogen, alkanoyl having two to twelve carbon atoms, inclusive, in a straight or branched alkyl chain, benzoyl, or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or R'.sub.2 and R'.sub.3 taken together are a five-membered ring having a total of up to twenty carbons;
- or R'.sub.5 is independently a phosphate, hydrogen, or dihydrogen phosphate, or an alkali metal or ammonium, or dialkali or diammonium salt thereof;
- its diastereomer;
- or a pharmaceutically acceptable acid addition salt thereof;
- with the proviso that overall when R.sub.1 is II and X, X', Y, and Z are hydrogen, or lower alkyl then n cannot be two.
7 more elements
Dependencies are inferred from the claim text.