259543-70-9Relevant academic research and scientific papers
Conformationally rigid derivatives of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin-1a receptors
Jorgensen, William T.,Gulliver, Damien W.,Katte, Timothy A.,Werry, Eryn L.,Reekie, Tristan A.,Connor, Mark,Kassiou, Michael
, p. 1644 - 1656 (2018)
WAY-267,464 (1) and twelve conformationally rigid analogues (3a-f–4a-f) were synthesised, characterised and evaluated in cellular assays with the aim of systematically exploring interactions with the oxytocin receptor (OTR). Each analogue was evaluated in
COMPOUNDS FOR MODULATING FXR
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Paragraph 000326; 000328; 000329; 000335; 000337; 000338, (2020/12/30)
Provided herein are compounds of Formula (I), a stereoisomer, enantiomer or a pharmaceutically acceptable salt thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).
POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES
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Paragraph 2088; 2089, (2020/03/29)
The present disclosure relates to bifunctional compounds, ULM— L—PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
RORGAMMA MODULATORS AND USES THEREOF
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Page/Page column 36; 37, (2018/09/02)
The present invention provides novel compounds of formula (la) that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, metabolic diseases, fibrotic diseases, or cholestatic diseases. (formula Ia)
Isoxazolinone antibacterial agents
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, (2008/06/13)
This invention describes isoxazolinone compounds which possess antibacterial activity and are useful in the treatment of bacterial diseases. More particularly, isoxazolinones are provided having the formula
