291289-21-9Relevant academic research and scientific papers
OXAZINE MONOACYLGLYCEROL LIPASE (MAGL) INHIBITORS
-
Page/Page column 214, (2019/10/15)
The invention provides new heterocyclic compounds having the general formula (Ic) wherein A, L, X, m, n and R20 to R23 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
-
, (2008/06/13)
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4fare defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
Novel piperidine σ receptor ligands as potential antipsychotic drugs
Gilligan,Cain,Christos,Cook,Drummond,Johnson,Kergaye,McElroy,Rohrbach,Schmidt,Tam
, p. 4344 - 4361 (2007/10/02)
σ receptor ligands represent a new class of potential antipsychotic drugs. This paper presents the structure-activity relationships leading to novel disubstituted piperidine σ ligands, which have little or no affinity for dopamine D2 receptors. Selectivity for σ sites over dopamine D2 or serotonin 5-HT2 receptors appears to be governed by the chemical nature of the piperidine nitrogen substituent, its distance from the basic nitrogen, and its orientation relative to the other piperidine substituent. Several of these compounds have good oral potency in some animal models used to evaluate potential antipsychotic drugs. The N-cyclopropylmethyl ketones and ethers (e.g. 6i (DuP 734), 6q, 18a, and 18n) have the best in vivo potency. Compounds 6i (DuP 734) and 6q did not cause catalepsy in the rat, even at very high doses. On the basis of the pharmacology profiles of these σ ligands, we propose these compounds may be effective antipsychotic drugs, which do not induce extrapyramidal side effects or tardive dyskinesia.
1,4-Disubstituted-piperidinyl compounds useful as analgesics and muscle relaxants
-
, (2008/06/13)
The present invention relates to 1,4-disubstituted-piperidinyl compounds and their use as analgesic agents and as muscle relaxants.
