- NLRP3 INHIBITORS
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The present application relates to compounds with NLRP3inhibitory activity and to associated salts, solvates, prodrugs and pharmaceutical compositions. The present application further relates to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3inhibition.
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Page/Page column 125
(2020/06/10)
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- NOVEL COMPOUNDS
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The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
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Page/Page column 104; 105
(2019/04/27)
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- NOVEL COMPOUNDS
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The present invention relates to substituted 5-membered nitrogen containing heteroaryl compounds, such as sulfonyl triazoles, where the heteroaryl ring is further substituted, optionally via a linking group such as -NH-, with a cyclic group which in turn is substituted at the α-position. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.
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Page/Page column 191
(2019/11/19)
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- Novel sulfamoyl benzamides as selective CB2 agonists with improved in vitro metabolic stability
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A lead optimization campaign in our previously reported sulfamoyl benzamide class of CB2 agonists was conducted to improve the in vitro metabolic stability profile in this series while retaining high potency and selectivity for the CB2 receptor. From this study, compound 14, N-(3,4-dimethyl-5-(morpholinosulfonyl)phenyl)-2,2-dimethylbutanamide, was identified as a potent and selective CB2 agonist exhibiting moderate in vitro metabolic stability and oral bioavailability. Compound 14 demonstrated in vivo efficacy in a rat model of post-surgical pain.
- Sellitto, Ian,Bourdonnec, Bertrand Le,Worm, Karin,Goodman, Allan,Savolainen, Markku A.,Chu, Guo-Hua,Ajello, Christopher W.,Saeui, Christopher T.,Leister, Lara K.,Cassel, Joel A.,DeHaven, Robert N.,LaBuda, Christopher J.,Koblish, Michael,Little, Patrick J.,Brogdon, Bernice L.,Smith, Steven A.,Dolle, Roland E.
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scheme or table
p. 387 - 391
(2010/04/06)
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- 2,4-DI(AMINOPHENYL) PYRIMIDINES AS PLK INHIBITORS
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The invention relates to compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1, and R3 are defined as indicated in claim 1. Said compounds are used for the treatment of diseases characterized by excessive or anomalous cell proliferation. Also disclosed is the use of the inventive compounds for producing a medicament having said properties.
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Page/Page column 35
(2008/06/13)
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- 4-and 5-nitroindane
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Mononitration of indane produces a mixture of 4- and 5- nitroindanes. Crystallization from mixtures occurs after distillation improves composition of a major component to above 80%. 4-Nitroindane: triclinic, space group P1 (#2), a = 7.332(4) A, b = 8.304(4) A, c = 8.358(4) A, α = 61.43(4)°, β = 67.60(4)°, γ = 70.15(4)°, V = 405.4(4) A3, Z = 2. Non-H-atoms are nearly planar, aliphatic H's are eclipsed. 5-Nitroindane: monoclinic, space group P21/c (#14), a = 10.946(8) A, b = 15.643(10) A, c = 9.415(6) A, β = 92.34(5)°, V = 1611(2) A3, Z = 8. Non-H-atoms in the two molecules differ in torsion of the nitro group with respect to indane and fold of the nonbenzylic methylene group. Semiempirical calculations (PM3) suggest that distorsion from planarity may be associated with the two lowest energy vibrational modes. Uv, ir, ms, proton, and 13C-nmr spectra are correlated with the solid state structures.
- Fuller, Jason F.,Valente, Edward J.
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p. 815 - 821
(2007/10/03)
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