C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
260/314, 260/519
C07F 7/10 (2006.01) C07D 233/54 (2006.01) C07D 233/64 (2006.01) C07F 7/08 (2006.01)
Patent
CA 1104141
ABSTRACT Novel compounds of the formula Image wherein R4 is hydrogen or a straight chain alkyl group of from 1 to 4 carbon atoms; R5 is hydrogen or -COOR1 wherein R1 is a straight chain alkyl group of from 1 to 4 carbon atoms; R6 is hydrogen or -Si(R8)3 wherein R8 is methyl, ethyl, n-propyl or n-butyl and each R8 is the same or two of the R8 groups are methyl and the other R8 group is tert-butyl; and Z is 3,4-dihydroxybenzyl, 1,3-dioxolan-2- yl-ethyl, 3-oxopropyl, 3-aminopropyl, 4-aminobutyl, 2- propenyl, 2-carboxyvinyl, carboxyalkyl wherein the alkyl moiety has from 1 to 3 carbon atoms and is straight chained or 5-imidazolylmethyl with the proviso that when Z is 3-oxopropyl or 2-propenyl neither of R4, R5 or R6 is hydrogen and when Z is other than 3-oxopropyl and 2-pro- penyl each of R4, R5 and R6 is hydrogen, and the prepara- tion thereof. The compounds are irreversible inhibitors of aromatic amino acid decarboxylase and they are useful in the treatment of various pathophysiological conditions, for example, Parkinsonism, depressive syndromes and action myoclonus, rheumatoid arthritis and carcinoid syndrome.
304971
Casara Patrick J.
Jung Michel
Metcalf Brian W.
Merrell Toraude Et Compagnie
Osler Hoskin & Harcourt Llp
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