1-aryl-2-hydroxyethyl amides as potassium channel openers
AssigneeBristol-Myers Squibb Company
InventorsYong-Jin Wu, Li-Qiang Sun, Huan He, Alexandre L'Heureux
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Abstract
The present invention provides novel aryl hydroxyethyl amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, R7 and A are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said aryl hydroxyethyl amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.
Claims8
A compound of Formula I or a pharmaceutically acceptable salt thereof
- wherein
- R1 is selected from the group consisting of pyridinyl, 3-quinolinyl, 2-thienyl, furanyl, C3-6 cycloalkyl and phenyl optionally substituted with substituent independently selected from the group consisting of halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy and nitro;
- A is —CH═CH— or —(CH2)n—;
- R2 is hydrogen or hydroxymethyl;
- n is an integer of 0, 1 or 2;
- R4 is selected from the group consisting of di(C1-4 alkyl)amino, trifluoromethoxy and optionally substituted morpholin-4-yl, morpholin-4-ylmethyl, pyridinyl, pyrimidinyl, piperazinyl, and pyrazinyl with one or two substituents in which said substituent is independently selected from the group consisting of C1-4 alkyl, aminomethyl, hydroxymethyl, chloro or fluoro;
- R5 is hydrogen or fluoro;
- or R4 and R5 taken together is —CH═CH—CH═CH— optionally substituted with a substituent independently selected from the group consisting of C1-4 alkyl, C1-4 alkoxy, trifluoromethyl and trifluoromethoxy;
- and
- R3, R6, and R7 are each independently hydrogen or fluoro.
Dependencies are inferred from the claim text.