102152-03-4Relevant articles and documents
HYDROXAMATE COMPOUNDS AS ANTAGONISTS OF THE ADENOSINE A2A RECEPTOR
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Paragraph 00520-00521, (2021/01/23)
The present invention relates to compounds of formula I shown below: (I) wherein R1, R2 and R3 are each as defined in the application. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or conditions in which adenosine A2a receptor activity is implicated, such as, for example, cancer.
OGA INHIBITOR COMPOUNDS
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, (2020/01/11)
The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors of formula (I). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.
Synthesis, structure-activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1
Sifferlen, Thierry,Koberstein, Ralf,Cottreel, Emmanuelle,Boller, Amandine,Weller, Thomas,Gatfield, John,Brisbare-Roch, Catherine,Jenck, Francois,Boss, Christoph
, p. 2212 - 2216 (2013/04/23)
A novel series of non-peptidic OX1R/OX2R orexin receptor antagonists was prepared by heterocyclic replacement of the dimethoxyphenyl moiety contained in the tetrahydroisoquinoline core skeleton of almorexant. Introduction of substituted imidazole moieties delivered potent dual orexin receptor antagonists with nanomolar potency for hOX1R and hOX2R suitable for further fine-tuning. The preparation of these novel orexin receptor antagonists and the outcome of preliminary structure-activity relationship studies are described in this communication.
SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ?-SECRETASE-INHIBITING ACTIVITY
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Page/Page column 74, (2011/04/25)
The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid β protein, for example,. a compound represented by the formula (I): wherein ruing A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES
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Page/Page column 68, (2008/12/06)
The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I),wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
Preparation of (fluoromethyl)- and (difluoromethyl)imidazoles
Dolensky, Bohumil,Kirk, Kenneth L.
, p. 1335 - 1344 (2007/10/03)
2-(Fluoromethyl)- and 2-(difluoromethyl)imidazoles, and 4-(fluoromethyl)- and 4-(difluoromethyl)imidazoles have been prepared by deoxyfluorination of (hydroxymethyl)imidazole or formylimidazole precursors.
Condensed thiazole derivative, production process thereof and pharmaceutical composition thereof
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, (2008/06/13)
Condensed thiazole derivatives useful as 5-HT3 receptor agonists are provided and can be represented by the following formula (I) or a pharmaceutically acceptable salt thereof, a process for the production thereof and a pharmaceutical composition thereof: STR1 wherein R, A, L1, L2, L, and R1 -R6 are defined herein and Im represents a group of the formula: STR2
Novel substituted imidazoles, their preparation and use
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, (2008/06/13)
Novel substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit cardioselective β-adrenergic blocking activity, and are useful as antihypertensive agents, cardioprotective agents, antiarrythmic agen
β1-Selective Adrenoceptor Antagonists: Examples of the 2-phenyl>imidazole Class. 2
Baldwin, John J.,Christy, Marcia E.,Denny, George H.,Habecker, Charles N.,Freedman, Mark B.,et al.
, p. 1065 - 1080 (2007/10/02)
An attempt to develop a highly cardioselective β-adrenoceptor antagonist devoid of intrinsic sympathomimetic activity (ISA) focused on exploring structure-activity relationships around (S)--amino>-2-hydroxypropoxy>phen
