166883-00-7Relevant articles and documents
6-MEMBERED CYCLIC AMINES OR LACTAMES SUBSTITUTED WITH UREA AND PHENYL
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Paragraph 0377; 0379, (2018/04/13)
The present invention relates to a compound according to general formula (I) which acts as a modulator of FPR2 and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by FPR2.
Palladium nanoparticles supported on a titanium dioxide cellulose composite (PdNPs@TiO2-Cell) for ligand-free carbon-carbon cross coupling reactions
Jadhav, Sanjay,Jagdale, Ashutosh,Kamble, Santosh,Kumbhar, Arjun,Salunkhe, Rajshri
, p. 3406 - 3420 (2016/01/25)
Well-dispersed non-spherical PdNPs with a diameter of 39-45 nm supported on a TiO2-cellulose composite (PdNPs@TiO2-Cell) can be synthesized by a simple and clean route. The catalyst was well characterized by XRD, FE-SEM, EDS, and TEM techniques. The PdNPs have good dispersity on the TiO2-Cell support. This results in excellent catalytic activities for the synthesis of biphenyls, acrylates, acetylenes and prochiral ketones using low Pd loading (1 mol%) at comparatively low temperature. The effects of the nature and amount of bases, nature of solvents, amount of catalyst and the reaction temperature on the activity of PdNPs@TiO2-Cell were thoroughly investigated. The catalyst showed at least four times reusability without decrease in catalytic activity.
NRF2 REGULATORS
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Page/Page column 314; 315, (2017/01/02)
Provided are aryl analogs,pharmaceutical compositions containing them and their use as NRF2 regulators.
NRF2 REGULATORS
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Page/Page column 566, (2015/07/07)
The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans
Lansdell, Mark I.,Hepworth, David,Calabrese, Andrew,Brown, Alan D.,Blagg, Julian,Burring, Denise J.,Wilson, Peter,Fradet, David,Brown, T. Bruce,Quinton, Faye,Mistry, Neela,Tang, Kim,Mount, Natalie,Stacey, Peter,Edmunds, Nick,Adams, Cathryn,Gaboardi, Samantha,Neal-Morgan, Stevie,Wayman, Chris,Cole, Susan,Phipps, Joanne,Lewis, Mark,Verrier, Hugh,Gillon, Val,Feeder, Neil,Heatherington, Anne,Sultana, Stefan,Haughie, Scott,Martin, Steven W.,Sudworth, Maria,Tweedy, Sarah
scheme or table, p. 3183 - 3197 (2010/09/15)
The relevance of the melanocortin system to sexual activity is well established, and nonselective peptide agonists of the melanocortin receptors have shown evidence of efficacy in human sexual dysfunction. The role of the MC4 receptor subtype has received particular scrutiny, but the sufficiency of its selective activation in potentiating sexual response has remained uncertain owing to conflicting data from studies in preclinical species. We describe here the discovery of a novel series of small-molecule MC4 receptor agonists derived from library hit 2. The addition of methyl substituents at C3 and C5 of the 4-phenylpiperidin-4-ol ring was found to be markedly potency-enhancing, enabling the combination of low nanomolar potencies with full rule-of-five compliance. In general, the series shows only micromolar activity at other melanocortin receptors. Our preferred compound 40a provided significant systemic exposure in humans on both sublingual and oral administration and was safe and well tolerated up to the maximum tested dose. In a pilot clinical study of male erectile dysfunction, the highest dose of 40a tested (200 mg) provided a similar level of efficacy to sildenafil.
Pharmaceutically active compounds
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Page/Page column 65, (2010/02/13)
The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein and especially to selective MCR4 agonist compounds, to
ETHER DERIVATIVES HAVING 5-LIPOXYGENASE INHIBITORY ACTIVITY
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, (2008/06/13)
The invention concerns ether derivatives of the formula I Q1?X?Ar?Q2 wherein Q1 is an optionally substituted 9-, 10- or 11-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur; X is oxy, thio, sulphinyl or sulphonyl; Ar is optionally substituted phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazoiediyl, thiadiazoiediyl or oxadiazolediyl; and Q2 is selected from the groups of the formulae II and III: wherein R1 is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl; R2 is (l-4C)alkyl; and R3 is hydrogen or (l-4C)alkyl; or R2 and R3 are linked to form a methylene, vinylene, ethylene or trimethylene group; or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.