- AZEPANE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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PROBLEM TO BE SOLVED: To provide a compound that has 5-HT2C receptor agonist activity and is useful as a therapeutic agent or a preventive agent for stress urinary incontinence. SOLUTION: The present invention provides an azepane derivative represented by the following formula or a pharmaceutically acceptable acid addition salt thereof. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPO&INPIT
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- SYNTHESIS OF TRICYCLIC BENZAZEPINES AND THEIR DOPAMINE D1- AND D2-AFFINITY
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A new group of angular 8,9-annelated 3-benzazepines has been found to be potent and selective dopamine D1-receptor antagonists of interest as possible pharmaceuticals in the treatment of schizophrenia.The synthesis of three new conformationally constrained representatives of this group of benzazepines is described and their affinity to the D1-receptor evaluated.Although none of these proved superior to the previously examined compounds, useful information on the receptor binding site was obtained.
- Horn Jensen, Eva,Nielsen, Per Halfdan
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p. 2441 - 2458
(2007/10/03)
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- Chemistry of the podocarpaceae LXXI. Preparation, structure, and reactions of some (arene)tricarbonylchromium(0) complexes. Crystal structure of α-tricarbonylchromium(0)
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Tricarbonylchromium(0) (7), tricarbonylchromium(0) (11) and (benzene)tricarbonylchromium(0) (10) were prepared and examined.Complex 7 was obtained as a mixture of diastereomers, an X-ray structural determination showing that the α-isomer possesses a near eclipsed conformation, in agreement with the conformation in solution deduced from 400 MHz 1H NMR analysis.Carbanions derived from 1,3-dithiane, 2-methyl-1,3-dithiane and 2-(2,2-dimethoxyethyl)-1,3-dithiane (24), and the dianion derived from 2,2'-methylenebis-1,3-dithiane (27) were prepared and brought into reaction with the complexes.Compounds 23 and 33 resulted from regioselective attack on 7 at the site predicted.Treatment with methyl electrophiles of the dithianyl η5-intermediate leading to 22 did not give products of acetyl incorporation.Arene lithiation-electrophilic quenching of 7 gave a mixture of compound 6 and its C(14) regioisomer along with the novel ketone 39 and its C(14) regioisomer.
- Cambie, Richard C.,Clark, George R.,Gallagher, Stewart R.,Rutledge, Peter S.,Stone, Martin J.,Woodgate, Paul D.
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p. 315 - 338
(2007/10/02)
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