A compound of formula (I) wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, —CO2R7, CONR4R5 or halo; R3 is H, NR4R5, NC(O)R8, halo, trifluoromethyl, alkyl, nitrile or alkoxy; R4 and R5 may be the same or different, and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R4 and R5 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; X is O, S or NR6; R6 is H or alkyl; R7 is hydrogen, methyl or ethyl; R8 is methyl or ethyl; L is (CH2)n, where n is 1, 2 or 3; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; together with pharmaceutically acceptable salts thereof. The use of these compounds as potassium channel inhibitors is also described.

Furanopyrimidine compounds as potassium ion channel inhibitors

This invention relates to novel compound of formula (I) 
or pharmaceutically acceptable salts thereof. The invention is also directed to the uses of compounds having formula (I) in the treatment or prevention of diseases or disorders which requires potassium channel inhibition to an animal, mammal or human in need thereof. The invention is also directed to the use of compounds having formula (I) in the treatment or prevention of arrhythmia to an animal, mammal or human in need thereof.

Substituted thieno[2,3-d]pyrimidines as potassium channel inhibitors

The invention provides compounds of the formula: wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, CO2R7, CONR5R6 or halo; R3 and R4 are H, NR5R6, NC(O)R7, halo, trifluromethyl, alkyl, CONR5R6, CO2R7, nitrile or alkoxy; R5 and R6 may be the same or different and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R5 and R6 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; R7 is H or alkyl; A is H, halo, or a group of formula X-L-Y; X is O, S or NR8; R8 is H or alkyl; L is (CH2)n, where n is 0, 1, 2, 3 or 4; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; the products of mono- and di-oxidation of sulphur and/or mono-oxidation of nitrogen moieties in compounds of formula I; or a pharmaceutically acceptable salt thereof. These compounds find use as inhibitors of potassium ion channels and thus are useful in the treatment of various conditions including arrhythmia and type-2 diabetes mellitus.

Thieno[2 3-b]pyridines as potassium channel inhibitors

The present invention provides thienopyridine compounds which are potassium channel inhibitors. In another embodiment, the invention provides pharmaceutical compositions comprising thienopyridines. In another embodiment, the invention provides methods of using thienopyridines in the treatment or prevention of cancer, arrhythmias, autoimmune diseases and inflammatory diseases, including gastric cancer, atrial fibrillation, type-2 diabetes mellitus, rheumatoid arthritis, type-1 diabetes, inflammatory bowel disorder and demyelinating disorders such as multiple sclerosis.

Thieno[3,2-c]pyridine potassium channel inhibitors

2-Amino-5-methyl-4-(2,2,2-trichloroethyl)-3-furonitrile was synthesized from 3,5,5,5-tetrachloropentan-2-one, a product of the radical addition of CCl4 to methyl vinyl ketone, according to a scheme known for α-haloketones. The product was converted via the corresponding imino-ether into N2-substituted N1 [5-methyl-4-(2,2,2-trichloroethyl)-3-cyano-2-furyl]formamidines. Cyclization of these formamidines gave 2-methyl-3-(2,2,2-trichloroethyl)-5-R-4-imino-4,5-dihydrofuro[2,3-d]pyrimidines, which readily regroup according to Dimroth into 2-methyl-3-(2,2,2-trichloroethyl)-4-R-aminofuro[2,3-d]pyrimidines.

Synthesis of heterocyclic compounds from the products of addition of polyhaloalkanes to unsaturated systems 4. Synthesis of substituted furo[2,3-d]pyrimidines

E. D. Lubuzh

Papers

Synthesis of heterocyclic compounds from the products of addition of polyhaloalkanes to unsaturated systems 4. Synthesis of substituted furo[2,3-d]pyrimidines