Aliphatic propargylamines as selective mao-b inhibitors and...

C - Chemistry – Metallurgy – 07 – C

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C07C 211/23 (2006.01) A61K 31/13 (2006.01) A61K 31/195 (2006.01) A61K 31/22 (2006.01) A61K 31/33 (2006.01) C07C 215/08 (2006.01) C07C 217/08 (2006.01) C07C 223/02 (2006.01) C07C 225/06 (2006.01) C07C 229/12 (2006.01) C07C 317/28 (2006.01) C07C 323/25 (2006.01)

Patent

CA 2105171

2105171 9215551 PCTABS00016 The invention relates to a series of propargylamines, their salts and pharmaceutical compositions containing a compound of formula (III) wherein R1, R3 and R4 are the same or different and represent hydrogen or a straight chain or branched lower alkyl; y is an integer ranging from 0 to 5; z is an integer ranging from 0 to 5; and R2 is a straight chain or branched alkyl, alkenyl, alkynyl, alkoxy, alkylthio or alkyl sulphinyl group having from 3 to 11 carbon atoms, said group being unsubstituted or substituted with at least one of the substituents selected from hydroxy, aldehyde, oxo, loweracyloxy, halogen, thio, sulfoxide, sulfone, phenyl, halogen-substituted phenyl, hydroxy-substituted phenyl, cycloalkyl having from 3 to 6 carbon atoms and heterocyclic substituents having between 3 and 6 atoms, of which form 1 to 3 are heteroatoms selected from O, S and/or N, and pharmaceutically acceptable salts thereof, in admixture with a pharmaceutically acceptable carrier, excipient or adjuvant. The compounds are useful as selective monoamine oxidase B inhibitors and have demonstrated neuroprotective properties in human and veterinary medicine.

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