58588-59-3Relevant academic research and scientific papers
MONOACYLGLYCEROL LIPASE INHIBITORS
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Paragraph 0352, (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).
Efficient three-component synthesis of diversely substituted tetrahydro-1H-cyclopenta[c]quinolines
Ni?o, Patricia,Caba, Marta,Aguilar, Nuria,Terricabras, Emma,Albericio, Fernando,Fernàndez, Joan-Carles
, p. 854 - 881 (2017/01/18)
The synthesis of highly functionalized substituted tetrahydro-1H-cyclopenta[c]quinoline (I) and its reduced derivatives hexahydro-1H-cyclopenta[c]quinolines (II) via Povarov reaction in high diastereoselectivity and high to moderate yields is described he
SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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Page/Page column 47; 48, (2013/10/22)
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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Page/Page column 48, (2013/10/22)
The present invention belongs to the field of EPl receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EPl receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EPl receptor as well as to pharmaceutical compositions comprising them.
Modeling, Synthesis and Biological Evaluation of Potential RetinoidX Receptor-Selective Agonists: Novel Halogenated Analogues of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene)
Furmick, Julie K.,Kaneko, Ichiro,Walsh, Angela N.,Yang, Joanna,Bhogal, Jaskaran S.,Gray, Geoffrey M.,Baso, Juan C.,Browder, Drew O.,Prentice, Jessica L.S.,Montano, Luis A.,Huynh, Chanh C.,Marcus, Lisa M.,Tsosie, Dorian G.,Kwon, Jungeun S.,Quezada, Alexis,Reyes, Nicole M.,Lemming, Brittney,Saini, Puneet,vanderVaart, Arjan,Groy, Thomas L.,Marshall, Pamela A.,Jurutka, Peter W.,Wagner, Carl E.
, p. 1551 - 1566 (2012/11/07)
The synthesis of halogenated analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (1), known commonly as bexarotene, and their evaluation for retinoidX receptor (RXR)-specific agonist performance is described. Compound 1 is FDA approved to treat cutaneous T-cell lymphoma (CTCL); however, bexarotene treatment can induce hypothyroidism and elevated triglyceride levels, presumably by disrupting RXR heterodimer pathways for other nuclear receptors. The novel halogenated analogues in this study were modeled and assessed for their ability to bind to RXR and stimulate RXR homodimerization in an RXRE-mediated transcriptional assay as well as an RXR mammalian-2-hybrid assay. In an array of eight novel compounds, four analogues were discovered to promote RXR-mediated transcription with EC50 values similar to that of 1 and are selective RXR agonists. Our approach also uncovered a periodic trend of increased binding and homodimerization of RXR when substituting a halogen atom for a proton ortho to the carboxylic acid on 1.
(Vinylaryloxy)acetic acids. A new class of diuretic agents. III. [(2 Nitro 1 alkenyl)aryloxy]acetic acids
Schultz,Bicking,Deana,Gould,Strobauge,Watson,Cragoe Jr.
, p. 783 - 787 (2007/10/12)
A series of [(2 nitro 1 alkenyl)aryloxy]acetic acids was synthesized and tested in dogs for saluretic and diuretic activity. A number of these compounds exhibit a high order of activity on iv or po administration; representative of these is (E) [2,3 dichl
