C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 211/00 (2006.01) A01N 33/02 (2006.01) A01N 47/10 (2006.01) A61K 31/135 (2006.01) A61K 31/27 (2006.01) C07C 215/64 (2006.01) C07C 219/26 (2006.01) C07C 261/00 (2006.01) C07C 269/00 (2006.01) C07C 271/00 (2006.01) C07D 265/12 (2006.01)
Patent
CA 2477218
The subject invention provides derivatives of propargylamino indan (PAI) and propargylamino tetralin that selectively inhibit monoamine oxidase (MAO) in the brain, having the structure:, wherein R1 is OC (O) R9 and R2 is H, wherein R9 i s branched or unbranched C1 to C6 alkyl, aryl, or aralkyl, or R1 is OC (O) R4 and R2 is OC (O) R4, wherein R4 is branched or unbranched C1 to C6 alkyl, aryl, aralkyl or NR5R6, wherein R5 and R6 are each independently H, C1 to C8 alkyl, C6 to C12 aryl, C6 to C12 aralkyl or C6 to C12 cycloalkyl, each optionally substituted; wherein R3 is H or C1 to C6 alkyl; wherein n is 0 or 1; and wherein m is 1 or 2, or a pharmaceutically acceptable salt thereof. Additionally, the subject invention provides methods of treating neurological disorders using these compounds, uses of these compounds for the manufacture of medicaments for treating neurological disorders and processes for synthesis of these compounds.
La présente invention concerne des dérivés de propargylaminoindane (PAI) et de propargylaminotétraline inhibant sélectivement la monoamine oxydase (MAO) dans le cerveau et présentant la structure (I), ou un sel pharmaceutiquement acceptable correspondant. Dans cette structure, R¿1? est OC(O)R¿9? et R¿2? est H, R¿9? étant alkyle C¿1?-C¿6? ramifié ou non ramifié, aryle ou aralkyle, ou R¿1? est OC(O)R¿4? et R¿2? est OC(O)R¿4?, R¿4? étant alkyle C¿1?-C¿6? ramifié ou non ramifié, aryle, aralkyle ou NR¿5?R¿6?, R¿5? et R¿6? étant chacun indépendamment H, alkyle C¿1?-C¿8?, aryle C¿6?-C¿12?, aralkyle C¿6?-C¿12? ou cycloalkyle C¿6?-C¿12?, chacun d'eux étant éventuellement substitué, R¿3? est H ou alkyle C¿1?-C¿6?, n vaut 0 ou 1 et m vaut 1 ou 2. En outre, la présente invention concerne des méthodes de traitement de troubles neurologiques au moyen de ces composés, des utilisations de ces composés dans la fabrication de médicaments destinés à traiter des troubles neurologiques, ainsi que des procédés de synthèse desdits composés.
Blaugrund Eran
Herzig Yaacov
Sterling Jeffrey
Heenan Blaikie Llp
Teva Pharmaceutical Industries Ltd.
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