3-Heterocyclic benzylamide derivatives as potassium channel openers
AssigneeBristol-Myers Squibb Company
InventorsYong-Jin Wu, Alexandre L'Heureux, Huan He
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Abstract
The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I 1 wherein R1, R2, R3, R4, R5, R6, A and Het 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 novel 3-heterocyclic benzylamides 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
- 81
- wherein
- R1 is selected from the group consisting of straight or branched chain C1-6 alkyl optionally substituted with amino, C1-4 alkylamino or di(C1-4 alkyl) amino, pyridinyl, pyrrodidinyl, piperidinyl, 2-thienyl, furanyl, imidazolyl, indenyl, benzofuran, C3-6 cycloalkyl and phenyl optionally substituted with substituent independently selected from the group consisting of halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, and trifluoromethoxy;
- A is —CH═CH—, 1,1-cyclopropyl, or 13 (CH2)n—;
- R2 is C1-4 alkyl, CF3 or hydroxymethyl;
- R3, R4, R5 and R6 each are independently hydrogen or fluoro;
- n is an integer of 0 to 4, inclusive;
- Het is selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, thiazolyl, imidazolyl, isoxazolyl, oxazolyl, pyrazolyl and triazolyl optionally substituted with substituents independently selected from the group consisting of C1-4 alkyl, halogen, amino and dimethylaminomethyl;
- provided that when Het is pyridinyl, pyrimidinyl or pyrazinyl, then A is not —CH═CH—.
Dependencies are inferred from the claim text.