Imidazole derivatives of formula I ##STR1##wherein n is 0 or 1, R.sub.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sub.2 is hydrogen or R.sub.2 and R.sub.3 together form a double bond, R.sub.3 is hydrogen or C.sub.1 -C.sub.4 -alkyl or R.sub.2 and R.sub.3 together form a double bond, R.sub.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, hydroxy or C.sub.1 -C.sub.4 -alkoxy, R.sub.5 is hydrogen or C.sub.1 -C.sub.4 -alkyl or R.sub.4 and R.sub.5 together with the carbon atom to which they are attached form a carbonyl group, R.sub.6, R.sub.7 and R.sub.8 are each the same or different and are independently hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.2 -C.sub.4 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -hydroxyalkyl, thiol, C.sub.1-4 -alkylthio, C.sub.1-4 -alkylthiol, halogen, trifluoromethyl, nitro or optionally substituted amino, X is --CHR.sub.9 --(CHR.sub.10).sub.m --, m is 0 or 1, and R.sub.9 and R.sub.10 are each the same or different and are independently hydrogen or C.sub.1 -C.sub.4 -alkyl; or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described. The compounds have affinity for alpha2 receptors and are useful e.g. in the treatment of hypertension, glaucoma, chronic or acute pain, migraine, diarrhea, common cold, ischemia, addiction to chemical substances, anxiety, especially preoperative anxiety and different neurological, musculoskeletal, psychiatric and cognition disorders or as adjuncts to anesthesia.

Orion Corporation

Imidazole derivatives having affinity for .alpha.2 receptors

Imidazole derivatives of formula (I) ##STR1##wherein n is 0 or 1, R.sub.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sub.2 is hydrogen or R.sub.2 and R.sub.3 together form a double bond, R.sub.3 is hydrogen or C.sub.1 -C.sub.4 -alkyl or R.sub.2 and R.sub.3 together form a double bond, R.sub.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, hydroxy or C.sub.1 -C.sub.4 -alkoxy, R.sub.5 is hydrogen or C.sub.1 -C.sub.4 -alkyl or R.sub.4 and R.sub.5 together with the carbon atom to which they are attached form a carbonyl group, R.sub.6, R.sub.7 and R.sub.8 are each the same or different and are independently hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.2 -C.sub.4 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -hydroxyalkyl, thiol, C.sub.1-4 -alkylthio, C.sub.1-4 -alkylthiol, halogen, trifluoromethyl, nitro or optionally substituted amino, X is --CHR.sub.9 --(CHR.sub.10).sub.m --, m is 0 or 1, and R.sub.9 and R.sub.10 are each the same or different and are independently hydrogen or C.sub.1 -C.sub.4 -alkyl; or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described. The compounds have affinity for alpha2 receptors and are useful e.g. in the treatment of hypertension, glaucoma, chronic or acute pain, migraine, diarrhea, common cold, ischemia, addiction to chemical substances, anxiety, especially preoperative anxiety and different neurological, musculoskeletal, psychiatric and cognition disorders or as adjuncts to anesthesia.

common cold/diarree

Imidazole derivatives having affinity for .alpha.2 receptors

Imidazole derivatives having affinity for alpha2 receptors

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