1026689-58-6Relevant articles and documents
COMPOUNDS AND PROBES FOR IMAGING HUNTINGTIN PROTEIN
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Paragraph 0335; 0336, (2021/06/26)
Provided herein are certain compounds of formula (I) and imaging agents useful for detecting a condition or disorder associated with protein aggregation, compositions thereof, and methods of their use.
UR-DEBa176: A 2,4-Diaminopyrimidine-Type Radioligand Enabling Binding Studies at the Human, Mouse, and Rat Histamine H4 Receptors
Bartole, Edith,Littmann, Timo,Tanaka, Miho,Ozawa, Takeaki,Buschauer, Armin,Bernhardt, Günther
supporting information, p. 8338 - 8356 (2019/10/11)
Differences in sequence homology between human (h), mouse (m), and rat (r) histamine H4 receptors (H4R) cause discrepancies regarding affinities, potencies, and/or efficacies of ligands and therefore compromise translational animal models and the applicability of radioligands. Aiming at a radioligand enabling robust and comparative binding studies at the h/m/rH4Rs, 2,4-diaminopyrimidines were synthesized and pharmacologically investigated. The most notable compounds identified were two (partial) agonists with comparable potencies at the h/m/rH4Rs: UR-DEBa148 (N-neopentyl-4-(1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl)pyrimidin-2-amine bis(2,2,2-trifluoroacetate), 43), the most potent [pEC50 (reporter gene assay) = 9.9/9.6/10.3] compound in the series being slightly G-protein biased and UR-DEBa176 [(R)-4-[3-(dimethylamino)pyrrolidin-1-yl]-N-neopentylpyrimidin-2-amine bis(2,2,2-trifluoroacetate), 46, pEC50 (reporter gene assay) = 8.7/9.0/9.2], a potential "cold" form of a tritiated H4R ligand. After radiolabeling, binding studies with [3H]UR-DEBa176 ([3H]46) at the h/m/rH4Rs revealed comparable Kd values (41/17/22 nM), low nonspecific binding (11-17%, aKd), and fast associations/dissociations (25-30 min) and disclosed [3H]UR-DEBa176 as useful molecular tool to determine h/m/rH4R binding affinities for H4R ligands.
DERIVATIVES OF N- [(1H-PYRAZOL-1-YL) ARYL] - 1H - INDOLE OR 1H - INDAZOLE - 3 - CARBOXAMIDE, THEIR PREPARATION AND THEIR USE AS P2Y12 ANTAGONISTS
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Page/Page column 75, (2012/11/13)
The present invention relates to compounds corresponding to formula (I) and their use as P2Y12 antagonists for the treatment of cardiovascular diseases.
Anti-ulcer and antisecretory activity of selected imidazopiperidines
Arcari,Bernardi,Cimaschi,Falconi,Luini,Scarponi
, p. 1467 - 1471 (2007/10/02)
New thioureas and ureas with an interesting anti-ulcer and antisecretory activity are presented. The chemical synthesis, determination of the structure, and structure-activity relationships of the compounds are discussed.