- Benzo[b]thiophene derivatives. XXVIII. 5-Bromo-3-benzo[b]thienylalanine and derivatives
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A potential inhibitor of gelation of sickle hemoglobin, 5-bromo-3-benzo[b]thienylalanine, has been synthesized along with several derivatives. Several hydrolytic pathways from the intermediate ethyl 5-bromo-3-benzo[b]thienylformamidomalonate have been exa
- Campaigne,Kim
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- 5-Halobenzothiophene analogues of melatonin: Synthesis and affinity for mt1 and MT2 receptors in man
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A novel series of melatonin analogues based on the benzothiophene nucleus is described. In these compounds the methoxy group was replaced by electron-attracting groups such halogens (Br and Cl) with the aim of supplementing structure-affinity relationship
- Leclerc,Beaurain,Depreux,Bennejean,Delagrange,Boutin,Lesieur
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- GEMINAL SUBSTITUTED QUINUCLIDINE AMIDE COMPOUNDS AS AGONISTS OF ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTORS
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The present invention relates to novel geminal substituted quinuclidine amide compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7- nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
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- NEW COMPOUNDS
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A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.
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- 17α-HYDROXYLASE/C17,20-LYASE INHIBITORS
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The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds of the present invention have been found to be useful as 17α-hydroxylase/C17,20-lyase inhibitors.
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- Preparation and pharmacological evaluation of a novel series of 2-(phenylthio)benzo[b]thiophenes as selective MT2 receptor ligands
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A series of N-(2-(5-fluoro-2-(4-fluorophenylthio)benzo[b]thiophen-3-yl) ethyl)acylamides was synthesized and evaluated for binding affinity and intrinsic activity at melatonin receptors. The affinity of each compound for the melatonin receptors was determined by binding studies on cloned human MT 1 and MT2 receptors expressed in CHO cells. Agonist and antagonist potency was measured on the [35S]GTPγS binding assay for the most interesting compounds. The new derivatives 8-14 showed modest to high selectivity (between 4 and 220) for MT2 receptors. The most selective compound, N-(2-(5-fluoro-2-(4-fluorophenylthio)benzo[b]thiophen-3-yl) ethyl)but-3-enamide (14), an MT2 ligand with affinity for the MT 2 receptor similar to that of melatonin and a 220-fold preference over MT1 receptors, acts as a partial agonist. In addition, N-(2-(5-fluoro-2-(4-fluorophenylthio)benzo[b]thiophen-3-yl)ethyl)propionamide (9), a nanomolar MT2 ligand with a good selectivity ratio (MT 1/MT2 = 51) shows antagonist activity on both melatonin receptors.
- Mésangeau, Christophe,Fraise, Mika?l,Delagrange, Philippe,Caignard, Daniel Henri,Boutin, Jean Albert,Berthelot, Pascal,Yous, Sa?d
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p. 1835 - 1840
(2011/05/06)
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- Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma
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We identified a new benzothiophene containing Rho kinase inhibitor scaffold in an ultra high-throughput enzymatic activity screen. SAR studies, driven by a novel label-free cellular impedance assay, were used to derive 39, which substantially reduced intr
- Davis, Robert L.,Kahraman, Mehmet,Prins, Thomas J.,Beaver, Yan,Cook, Travis G.,Cramp, Jessica,Cayanan, Charmagne S.,Gardiner, Elisabeth M.M.,McLaughlin, Marsha A.,Clark, Abbot F.,Hellberg, Mark R.,Shiau, Andrew K.,Noble, Stewart A.,Borchardt, Allen J.
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scheme or table
p. 3361 - 3366
(2010/08/07)
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- Indole derivatives for the treatment of depression and anxiety
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The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.
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Page/Page column 17
(2010/02/05)
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- New serotonin 5-HT1F agonists
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This invention provides novel 5-HT1Fagonists of formula where X, Y, Z,and R are defined in the specification, which are useful for the prevention and treatment of migraine and associated disorders.
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- Triazole containing indole derivatives
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A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT 1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
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- Synthesis of Substituted Benzothiophenes by Acid-Catalyzed Cyclization of Thiophenylacetals and Ketones
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Benzothiophenes substituted at the 3 position with methyl or carboxymethyl and at the 5 position with methyl, methoxy, chloro, bromo and nitro were prepared by cyclization of thiophenyl-acetals and ketones using a suspension of polyphosphoric acid in refluxing chlorobenzene.The overall efficiency of this method is superior to literature procedures because of the lower temperature and the limited amount of PPA used.
- Ple, Patrick A.,Marnett, Lawrence J.
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p. 1271 - 1272
(2007/10/02)
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