- Development of an efficient large-scale synthesis for a 4 H-imidazo[5,1- c ][1,4]benzoxazine-3-carboxamide derivative for depression and anxiety
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The development and scale-up of an optimized synthesis for a novel drug candidate for depression and anxiety is presented. The updated synthesis represents a convergent and efficient four-stage approach to the API, overcoming high cost of goods (COG), gen
- Giubellina, Nicola,Stabile, Paolo,Laval, Gilles,Perboni, Alcide D.,Cimarosti, Zadeo,Westerduin, Pieter,Cooke, Jason W. B.
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experimental part
p. 859 - 867
(2011/03/20)
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- Design and synthesis of novel tricyclic benzoxazines as potent 5-HT 1A/B/D receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4 h-imidazo[5,1-c][1,4] benzoxazine-3-carboxamide (GSK588045)
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Bioisoteric replacement of the metabolically labile N-methyl amide group of a series of benzoxazinones with small heterocyclic rings has led to novel series of fused tricyclic benzoxazines which are potent 5-HT1A/B/D receptor antagonists with a
- Bromidge, Steven M.,Arban, Roberto,Bertani, Barbara,Bison, Silvia,Borriello, Manuela,Cavanni, Paolo,Dal Forno, Giovanna,Di-Fabio, Romano,Donati, Daniele,Fontana, Stefano,Gianotti, Massimo,Gordon, Laurie J.,Granci, Enrica,Leslie, Colin P.,Moccia, Luca,Pasquarello, Alessandra,Sartori, Ilaria,Sava, Anna,Watson, Jeannette M.,Worby, Angela,Zonzini, Laura,Zucchelli, Valeria
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experimental part
p. 5827 - 5843
(2010/11/04)
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- FUSED TRICYCLIC DERIVATIVES FOR THE TREATMENT OF PSYCHOTIC DISORDERS
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Compounds of formula (I) wherein R1, R2, X, A, Y, B, Z1, Q, p, r and s are defined in the specification for treating inter alia psychotic disorders, depressive disorders, anxiety disorders and sexual dysfunctions.
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Page/Page column 122
(2010/10/20)
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