57260-67-0Relevant articles and documents
MONOACYLGLYCEROL LIPASE INHIBITORS
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Paragraph 0111-0112; 0141; 0153-0154; 0208-0209, (2021/09/09)
Provided are compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof: Also provided are compositions comprising compounds of formula (I). The compounds and compositions are also provided for use as medicaments, for example as medicaments useful in the treatment of a condition modulated by monoacylglycerol lipase (MAGL). Also provided are the use of compounds and compositions for the inhibition of monoacylglycerol lipase (MAGL).
Discovery of imidazole carboxamides as potent and selective CCK1R agonists
Zhu, Cheng,Hansen, Alexa R.,Bateman, Thomas,Chen, Zhesheng,Holt, Tom G.,Hubert, James A.,Karanam, Bindhu V.,Lee, Susan J.,Pan, Jie,Qian, Su,Reddy, Vijay B.G.,Reitman, Marc L.,Strack, Alison M.,Tong, Vincent,Weingarth, Drew T.,Wolff, Michael S.,MacNeil, Doug J.,Weber, Ann E.,Duffy, Joseph L.,Edmondson, Scott D.
scheme or table, p. 4393 - 4396 (2009/04/06)
High-throughput screening revealed diaryl pyrazole 3 as a selective albeit modest cholecystokinin 1 receptor (CCK1R) agonist. SAR studies led to the discovery and optimization of a novel class of 1,2-diaryl imidazole carboxamides. Compound 44, which was profiled extensively, showed good in vivo mouse gallbladder emptying (mGBE) and lean mouse overnight food intake (ONFI) reduction activities.
Pharmaceutically active pyrrolidine derivatives as bax inhibitors
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, (2008/06/13)
The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating-up to an inhibitory-activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c). The present invention is furthermore related to novel pharmaceutically activity substituted pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of O, S, CRR, NOR, NNRR; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO2-, —SO2NH—; —CH2-; B is either a group —(C═O)—NRR or represents a heterocyclic residue having the formula (II) wherein Q is NR, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.