- BENZOFURAN AMIDES AND HETEROAROMATIC ANALOGUES THEREOF FOR USE IN THERAPY
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The present invention relatesto a pharmaceutical composition comprising acompound of the formula Ias described belowor a tautomeror a pharmaceutically acceptable salt thereof; to the compound of the formula Ias described below or a tautomer or a phar- mac
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- Novel 3beta-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
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The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3- thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4 alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.
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Page/Page column 6
(2010/02/11)
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- SPIROFUROPYRIDINE ARYL DERIVATIVES
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Compounds of formula (I): and pharmaceutically-acceptable salts thereof, wherein: Ar is a moiety of formula (II) or (III): and A, B, and R1 are as defined in the specification, compositions containing such compounds and the use of such compounds and compositions for use in therapy.
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Page/Page column 15; 16
(2008/06/13)
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- Furopyridines.III.A New Synthesis of Furopyridine
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A convenient synthesis of furopyridine and its 2- and 3-methyl derivatives from ethyl 3-hydroxypicolinate (1) is described.The hydroxy ester 1 was O-alkylated with ethyl bromoacetate or ethyl 2-bromopropionate to give the diester 2a or 2b.Cyclization of compound 2a afforded ethyl 3-hydroxyfuropyridine-2-carboxylate (3) which in turn was hydrolyzed and decarboxylated to give furopyridin-3-(2H)-one (4a).Cyclization of 2b gave the 2-methyl derivative 4b.Reduction of 4a and 4b with sodium borohydride yielded the corresponding hydroxy derivative 5a and 5b respectively, which were dehydrated with phosphoric acid to give furopyridine (6a) and its 2-methyl derivative (6b). 2-Acetylpyridin-3-ol (8) was converted to the ethoxycarbonylmethyl ether (9) by O-alkylation with ethyl bromoacetate, which was cyclized to give 3-methylfuropyridine-2-carboxylic acid (10).Decarboxylation of 10 afforded 3-methylfuropyridine (11).
- Shiotani, Shunsaku,Morita, Hiroyuki
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p. 665 - 668
(2007/10/02)
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