- 3-OXO-1,4-DIAZEPINYLE COMPOUNDS AS NRF2 ACTIVATORS
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The present invention relates to bisaryl lactam compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators. In particular, the compounds of this invention include a compound of Formula (I):
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Page/Page column 64
(2018/07/05)
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- Csp3-H bond activation with triel metals: Indium and gallium zwitterions through internal hydride abstraction in rigid salan ligands
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The hydropyrimidine salan (salan=N,N'-dimethyl-N,N'-bis[(2-hydroxyphenyl) methylene]-1,2-diaminoethane) proteo-ligands with a rigid backbone {ON^(CH 2)^NO}H2 react with M(CH2SiMe3) 3 (M=Ga, In) to yie
- Maudoux, Nicolas,Fang, Jian,Roisnel, Thierry,Dorcet, Vincent,Maron, Laurent,Carpentier, Jean-Francois,Sarazin, Yann
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supporting information
p. 7706 - 7717
(2014/07/07)
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- Compositions Comprising Enzyme-Cleavable Oxycodone Prodrug
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The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino)-2,2-dimethyl-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
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Page/Page column 27
(2012/07/27)
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- 5-Substituted isoquinoline derivatives
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A compound represented by the following formula (1) or a salt thereof: wherein R1 represents hydrogen atom, a halogen atom and the like; R2 represents hydrogen atom, a halogen atom, a C1-6 alkyl group and the like; and R3 represents —O—X—C(A1)(A11)—C(A2)(A2l)—N(A3l)(A3)(X represents propylene group etc., A11 and A21 represent hydrogen atom, or a C1-6 alkyl group, A31 represents a C1-6 alkyl group substituted with hydroxyl group, or hydrogen atom, and A1, A2, and A3 represent hydrogen atom, a C1-6 alkyl group and the like) and the like, which has an inhibitory activity on the phosphorylation of myosin regulatory light chain, and is useful for treatment of diseases relating to contraction of various cells and the like.
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- AMINE COMPOUNDS AND USE THEREOF
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It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1):In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(=O) or NR11; and D is a group represented by the following general formula (4) or (6).-Q-Y-BIn the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26. In the above formulae, R1 to R26 each represents hydrogen, alkyl, alkenyl or alkynyl.
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Page/Page column 46
(2010/02/12)
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- Solution parallel synthesis of cyclic guanidines
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An efficient method for the solution phase synthesis of cyclic guanidines is presented. A variety of 2-substituted monoprotected propanediamines react with a set of 5-substituted 2-methylthio-3,4,5,6- tetrahydropyrimidines under Rathke conditions for the construction of a potential library of 81 cyclic guanidines.
- Marmillon, Christelle,Bompart, Jacques,Calas, Michèle,Escale, Roger,Bonnet, Pierre-Antoine
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p. 1317 - 1328
(2007/10/03)
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- Design and synthesis of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)- en-2-yl)-ethyl]phosphonic acid (EAA-090), a potent N-methyl-D-asparate antagonist, via the use of 3-cyclobutene-1,2-dione as an achiral α-amino acid bioisostere
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The diazabicyclic amino acid phosphonate 15, [2-(8,9-dioxo-2,6- diazabicyclo[5.2.0]non-1(7)-en-2-yl)ethyl]phosponic acid, was identified as a potent NMDA antagonist. It contains the α-amino acid bioisostere 3,4- diamino-3-cyclobutene-1,2-dione and an addi
- Kinney, William A.,Abou-Gharbia, Magid,Garrison, Deanna T.,Schmid, Jean,Kowal, Dianne M.,Bramlett, Donna R.,Miller, Tracy L.,Tasse, Rene P.,Zaleska, Margaret M.,Moyer, John A.
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p. 236 - 246
(2007/10/03)
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