Imidazole therapeutic agents
AssigneePfizer Inc.
InventorsPeter E. Cross, Roger P. Dickinson
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Abstract
A series of 2-(imidazol-1-ylmethyl)pyridines and 2-(imidazol-1-ylmethyl)quinolines has been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy for the treatment of ischaemic heart disease, migraine, transient ischaemic attack and stroke. Preferred member compounds include 2-(imidazol-1-ylmethyl)-3-methoxypyridine, 2-(imidazol-1-ylmethyl)-3-methoxy-6-methylpyridine and 2-(imidazol-1-ylmethyl)-3-benzyloxypyridine, respectively. Alternate methods of preparation are provided and the principal synthetic routes leading to the preferred compounds are described in some detail.
Claims14
A compound of the formula:
- ##STR8## and the pharmaceutically acceptable acid addition salts thereof, wherein R is 2-quinolyl or a pyridyl moiety of the formula:
- ##STR9## wherein R.sup.1 is hydrogen, halogen or alkyl of 1-4 carbon atoms;
- and R.sup.2 is alkyl of 1-4 carbon atoms, or a group of the formula --OR.sup.3 wherein R.sup.3 is hydrogen, alkyl of 1-4 carbon atoms, allyl, prop-2-ynyl, cycloalkylmethyl having 3-6 carbon atoms in the cycloalkyl group, or benzyl in which the phenyl moiety is unsubstituted on the ring or is monosubstituted with halogen, alkyl of 1-4 carbon atoms or alkoxy of 1-4 carbon atoms;
- with the proviso that said --OR.sup.3 is always a group located at the 3- or 5-positions of the pyridine ring.
2-(Imidazol-1-ylmethyl)-3-methoxypyridine.
2-(Imidazol-1-ylmethyl)-3-benzyloxypyridine.
2-(Imidazol-1-ylmethyl)-3-methoxy-6-methylpyridine.
Dependencies are inferred from the claim text.