785032-26-0Relevant articles and documents
Design and synthesis of novel meta-linked phenylglycine macrocyclic FVIIa inhibitors
Richter, Jeremy M.,Cheney, Daniel L.,Bates, J. Alex,Wei, Anzhi,Luettgen, Joseph M.,Rendina, Alan R.,Harper, Timothy M.,Narayanan, Rangaraj,Wong, Pancras C.,Seiffert, Dietmar,Wexler, Ruth R.,Priestley, E. Scott
supporting information, p. 67 - 72 (2017/12/12)
Two novel series of meta-linked phenylglycine-based macrocyclic FVIIa inhibitors have been designed to improve the rodent metabolic stability and PK observed with the precursor para-linked phenylglycine macrocycles. Through iterative structure-based design and optimization, the TF/ FVIIa Ki was improved to subnanomolar levels with good clotting activity, metabolic stability, and permeability.
MACROCYCLIC FACTOR VIIA INHIBITORS
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Paragraph 00279, (2015/01/09)
The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments.
Synthesis and evaluation of [11C]Cimbi-806 as a potential PET ligand for 5-HT7 receptor imaging
Herth, Matthias M.,Hansen, Hanne D.,Ettrup, Anders,Dyssegaard, Agnete,Lehel, Szabolcs,Kristensen, Jesper,Knudsen, Gitte M.
experimental part, p. 4574 - 4581 (2012/09/07)
2-(2′,6′-Dimethoxy-[1,1′-biphenyl]-3-yl)-N, N-dimethylethanamine has been identified as a potent ligand for the serotonin 7 (5-HT7) receptor. In this study, we describe the synthesis, radiolabeling and in vivo evaluation of [11C]2-(2
COMPOUNDS, PREPARATIONS AND USES THEREOF
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Page/Page column 130-131, (2011/07/09)
The present invention provides novel compounds of the Formula (I), pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susc
Structure-activity correlations for β-phenethylamines at human trace amine receptor 1
Lewin, Anita H.,Navarro, Hernan A.,Wayne Mascarella
, p. 7415 - 7423 (2008/12/22)
A cell line in which RD-HGA16 cells were stably transfected with the hTAAR 1 receptor was created and utilized to carry out a systematic evaluation of a series of β-phenethylamines. Fair agreement was observed with data obtained for aryl and ethylene chain substituted analogs in an AV12-664 cell line in which hemagglutinin-tagged hTAAR 1 was stably co-expressed with rat Gαs. Analogs with multiple substituents as well as analogs with bulky groups were found to be partial agonists. Analogs in which the primary amino group was converted to a secondary or a tertiary amino group by N-methylation were also partial agonists. Comparative Molecular Field Analysis (CoMFA) using the potency data yielded a regression coefficient r2 of 0.824. The steric field contribution to the model was 61% with the balance (39%) contributed by the electrostatic field. The collective results suggest that increasing steric bulk both at the amino nitrogen, particularly by N-dimethylation, and at the 4-position of the aromatic ring leads to low efficacy ligands.
Heterocyclyl-substituted-ethylamino-phenyl derivatives, their preparation and use as medicaments
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Page/Page column 35; 36, (2008/12/06)
The present invention relates to heterocyclyl-substituted-ethylamino-phenyl compounds of general formula (I) wherein K-L-M-N, Z and R1, R2, R3, R4 are described in the claims, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatments of humans or animals.
Combination of a 5-HT7 receptor ligand and an opioid receptor ligand
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Page/Page column 28-29, (2009/01/20)
The present invention refers to a combination of a 5HT7 receptor ligand and an opioid recptor ligand, especially of a 5HT7 receptor agonist and an opioid recptor agonist, a medicament comprising this combination, or the use of this combination for the treatment of the symptoms of pain, the prevention or the prophylaxis of the symptoms of pain.
