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US 5,686,463 AGranted
Oxadiazoles useful in the treatment of senile dementia
AssigneeMerck Sharp & Dohme Corp.
InventorsRaymond Baker, Kevin John Merchant, Angus Murray MacLeod, John Saunders
Life of this patent
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Abstract
A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring, and substituted on the other ring carbon atom with a substituent of low lipophilicity; are potent muscarinic agonists, and have good CNS penetrability. The compounds are therefore useful in the treatment of neurological and mental illnesses.
Claims24
A compound of the formula (I):
- ##STR11## or a salt thereof;
- wherein one of X, Y or Z is an oxygen atom and the other two are nitrogen atoms, and the dotted circle represents aromaticity (two double bonds) thus forming a 1,3,4-oxadiazole or 1,2,4-oxadiazole nucleus;
- R.sup.1 represents a non-aromatic azacyclic or azabicyclic ring system;
- and R.sup.2 represents a substituent of low lipophilicity having a Rekker f value of not greater than 1.5.
1 more element
A compound according to claim 11 wherein R.sup.1 is a 1-azabicyclo2.2.1!heptane ring.
A 1,2,4-oxadiazole having the formula (II):
- ##STR14## or a pharmaceutically acceptable salt thereof;
- wherein R.sup.1 represents a non-aromatic azacyclic or azabicyclic ring system;
- and R.sup.2 represents a low-lipophilic substituent with a Rekker E value .ltoreq.1.5.
A compound of the formula:
- ##STR15## or a pharmaceutically acceptable salt thereof:
- wherein R.sup.1 represents a non-aromatic azabicyclic ring system;
- and R.sup.2 represents a C.sub.1-2 alkyl group.
Dependencies are inferred from the claim text.