发明名称 ALIPHATIC PROPARGYLAMINES AS SELECTIVE MAO-B INHIBITORS AND AS NEUROPROTECTIVE AGENTS
摘要 PCT No. PCT/CA92/00090 Sec. 371 Date Dec. 23, 1993 Sec. 102(e) Date Dec. 23, 1993 PCT Filed Feb. 28, 1992 PCT Pub. No. WO92/15551 PCT Pub. Date Sep. 17, 1992.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.
申请公布号 AU1323692(A) 申请公布日期 1992.10.06
申请号 AU19920013236 申请日期 1992.02.28
申请人 UNIVERSITY OF SASKATCHEWAN 发明人 PETER H YU;BRUCE A DAVIS;ALAN A BOULTON
分类号 A61K31/13;A61K31/185;A61P25/00;A61P25/24;A61P25/26;A61P25/28;A61P43/00;C07C211/21;C07C211/23;C07C211/24;C07C211/27;C07C215/08;C07C229/12;C07C317/28;C07C323/25;C07C323/65;C12N9/99 主分类号 A61K31/13
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