162744-47-0Relevant academic research and scientific papers
BENZOTHIOPHENE DERIVATIVE
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, (2016/02/18)
[Problem to be Solved] It is intended to provide a compound having PDE10A inhibitory activity and having a novel structure, or an isotope thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. [Solution] The present invention provides a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof.
GEMINAL SUBSTITUTED QUINUCLIDINE AMIDE COMPOUNDS AS AGONISTS OF ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTORS
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Paragraph 00677-00678, (2016/07/05)
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.
Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases
Crosignani, Stefano,Prêtre, Adeline,Jorand-Lebrun, Catherine,Fraboulet, Ga?le,Seenisamy, Jeyaprakashnarayanan,Augustine, John Kallikat,Missotten, Marc,Humbert, Yves,Cleva, Christophe,Abla, Nada,Daff, Hamina,Schott, Olivier,Schneider, Manfred,Burgat-Charvillon, Fabienne,Rivron, Delphine,Hamernig, Ingrid,Arrighi, Jean-Fran?ois,Gaudet, Marilène,Zimmerli, Simone C.,Juillard, Pierre,Johnson, Zoe
, p. 7299 - 7317 (2011/12/15)
New phenoxyacetic acid antagonists of CRTH2 are described. Following the discovery of a hit compound by a focused screening, high protein binding was identified as its main weakness. Optimization aimed at reducing serum protein binding led to the identification of several compounds that showed not only excellent affinities for the receptor (41 compounds with Ki 50 100 nM; PGD2-induced eosinophil shape change). Additional optimization of the PK characteristics led to the identification of several compounds suitable for in vivo testing. Of these, 19k and 19s were tested in two different pharmacological models (acute FITC-mediated contact hypersensitivity and ovalbumin-induced eosinophilia models) and found to be active after oral dosing (10 and 30 mg/kg).
PHENOXY ACETIC ACID DERIVATIVES
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Page/Page column 72-73, (2010/09/03)
The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
