885275-10-5Relevant articles and documents
COLLAGEN 1 TRANSLATION INHIBITORS AND METHODS OF USE THEREOF
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Paragraph 0078-0079; 00139-00140, (2021/10/30)
The present invention relates to novel Collagen 1 translation inhibitors, composition and methods of preparation thereof, and uses thereof for treating Fibrosis including lung, liver, kidney, cardiac and dermal fibrosis, IPF, wound healing, scarring and Gingival fibromatosis, Systemic Sclerosis, and alcoholic and non-alcoholic steatohepatitis (NASH).
SPIRO-OXADIAZOLINE COMPOUNDS AS AGONISTS OF α-7-NICOTINIC ACETYLCHOLINE RECEPTORS
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Paragraph 00286-00287, (2015/05/19)
The present invention relates to novel spiro-oxadiazoline compounds that are suitable as agonists or partial agonists of a7-nAChR, and pharmaceutical compositions of the same, 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 a spiro-oxadiazoline cx7-nAChR agonist or partial agonist, 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.
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: Discovery of an inverse agonist radioligand for PET
Prante, Olaf,Tietze, Rainer,Hocke, Carsten,L?ber, Stefan,Hübner, Harald,Kuwert, Torsten,Gmeiner, Peter
, p. 1800 - 1810 (2008/09/21)
A series of fluoro-substituted analogs structurally derived from the aminomethyl-substituted pyrazolo[1,5-a]pyridine lead compounds 9 (FAUC 113) and 10 (FAUC 213) were synthesized and evaluated as high-affinity D4 receptor (D4R) ligands (3a-3h, Ki = 1.3-28 nM). The para-fluoroethoxy-substituted derivatives 3f and 3h revealed an outstanding D4 subtype selectivity of more than 3 orders of magnitude over both congeners D2 and D3 combined with inverse agonism at D4R. The corresponding 18F-labeled radioligands revealed high serum stability in vitro and log P values of 2-3. In vitro rat brain autoradiography showed specific binding of [18F]3h in distinct brain regions, including the gyrus dentate of the hippocampus, that were inhibited by both eticlopride (65-80%) and the selective D4R antagonist 10 (78-93%). The observed binding pattern was mainly consistent with the known D4R distribution in the rat brain. Thus, [18F]3h (FAUC F41) represents a potential radioligand for studying the D4R in vivo by positron emission tomography (PET).