Imidazole compounds and their use
AssigneeNeuroSearch A/S
InventorsOskar Axelsson, Mikkel Thaning, Peter Moldt
Life of this patent
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Abstract
The application discloses benzimidazole derivatives, pharmaceutical preparations comprised the compounds, their preparation and use in the treatment of disorders of the Central Nervous System such as ischemia, migraine, epilepsia, psychosis, Parkinsonism and depression.
Claims10
A method of treating a disorder of a mammal, including a human, which is responsive to the blockade of N-type and/or L-type of calcium channels, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound having the formula:
- ##STR13## wherein R' and R" independently are hydrogen or C.sub.1-4 -alkyl which may be straight or branched, or R' and R" together form an alkylene chain of 2-6 carbon atoms;
- R.sup.4, R.sup.5, R.sup.6, R.sup.7 independently of each other are hydrogen, halogen, CF.sub.3, or CN;
- R.sup.11 is hydrogen, halogen, CF.sub.3, hydroxy or OR.sup.I wherein R.sup.I is C.sub.1-4 -alkyl which may be straight or branched;
- R.sup.12, R.sup.13 and R.sup.14 independently are hydrogen, halogen, CF.sub.3, C.sub.1-4 -alkyl which may be straight or branched, OH, OR.sup.16 wherein R.sup.16 is C.sub.1-4 -alkyl which may be straight or branched, phenyl, piperidyl, pyrrolidyl, or phenyl which may be substituted one or more times with halogen, CF.sub.3, CN, C.sub.1-4 -alkyl which may be straight or branched, OH, NO.sub.2, CO.sub.2 H, NH.sub.2, OR.sup.II wherein R.sup.II is C.sub.1-4 -alkyl which may be straight or branched, CO.sub.2 R.sup.III wherein R.sup.III is C.sub.1-4 -alkyl which may be straight or branched, NR.sup.IV R.sup.V wherein R.sup.IV and R.sup.V independently are hydrogen, C.sub.1-6 -alkyl which may be straight or branched, acyl, or wherein R.sup.IV and R.sup.V together form an alkylene chain of 2-6 carbon atoms;
- R.sup.15 is hydrogen or together with R.sup.14 form an extra benzo ring;
- or a pharmaceutically acceptable addition salt thereof.
A compound having the formula ##STR14## wherein R' and R" independently are hydrogen or C.sub.1-4 -alkyl which may be straight or branched, or R' and R" together form an alkylene chain of 2-6 carbon atoms;
- R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of each other are hydrogen, halogen, CF.sub.3 or CN;
- R.sup.11 is hydrogen, halogen, CF.sub.3, hydroxy or OR.sup.I wherein R.sup.I is C.sub.1-4 -alkyl which may be straight or branched;
- two of R.sup.12, R.sup.13 and R.sup.14 independently are hydrogen, halogen, CF.sub.3, C.sub.1-4 -alkyl which may be straight or branched, OH, OR.sup.16 wherein R.sup.16 is C.sub.1-4 alkyl which may be straight or branched, or phenyl and the last of R.sup.12, R.sup.13 and R.sup.14 is pyrrolidyl, piperidyl, or phenyl which may be substituted one or more times with halogen, CF.sub.3, CN, C.sub.1-4 -alkyl which may be straight or branched, OH, NO.sub.2, CO.sub.2 H, NH.sub.2, OR.sup.II wherein R.sup.II is C.sub.1-4 -alkyl which may be straight or branched, CO.sub.2 R.sup.III wherein R.sup.III is C.sub.1-4 -alkyl which may be straight or branched, NR.sup.IV R.sup.V wherein R.sup.IV and R.sup.V independently are hydrogen, C.sub.1-6 -alkyl which may be straight or branched, acyl, or wherein R.sup.IV and R.sup.V together form an alkylene chain of 2-6 carbon atoms;
- R.sup.15 is hydrogen or together with R.sup.14 form an extra benzo ring;
- or a pharmaceutically acceptable addition salt thereof.
Dependencies are inferred from the claim text.