2140264-81-7Relevant academic research and scientific papers
AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Paragraph 0190, (2021/08/05)
The present invention relates to new compounds that show pharmacological activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the μ-opiod receptor (MOR or mu-opioid). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.
COMPOUNDS AS MODULATORS OF ROR GAMMA
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Page/Page column 42, (2018/07/05)
The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
Process for the preparation of enantiomerically enriched cyclic beta-aryl or heteroaryl carbocyclic acids
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Page/Page column 23, (2008/06/13)
The present invention relates to a process for the preparation of cis substituted cyclic β-aryl or heteroaryl carboxylic acid derivatives in high diastereo- and enantioselectivity by enantioselective hydrogenation in accordance with the following scheme w
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists
Young, Jonathan R.,Eid, Ronsar,Turner, Cherilyn,DeVita, Robert J.,Kurtz, Marc M.,Tsao, Kwei-Lan C.,Chicchi, Gary G.,Wheeldon, Alan,Carlson, Emma,Mills, Sander G.
, p. 5310 - 5315 (2008/03/11)
The preparation and structure-activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK1 antagonists in vitro and efficacious in vivo with minimal interactions with P450 liver enzymes. Oxadiazole analog 22 was determined to have excellent hNK1 binding affinity, functional activity, and a good PD response in vivo.
