- P300/CBP HAT INHIBITORS
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Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).
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Paragraph 00110; 00215-00216
(2019/09/04)
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- Rapid access to spirocyclic oxindole alkaloids: Application of the asymmetric palladium-catalyzed [3 + 2] trimethylenemethane cycloaddition
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The marcfortines are complex secondary metabolites that show potent anthelmintic activity and are characterized by the presence of a bicyclo[2.2.2]diazaoctane fused to a spirooxindole. Herein, we report the synthesis of two members of this family. The syn
- Trost, Barry M.,Bringley, Dustin A.,Zhang, Ting,Cramer, Nicolai
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supporting information
p. 16720 - 16735
(2013/12/04)
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- Indolyne experimental and computational studies: Synthetic applications and origins of selectivities of nucleophilic additions
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Efficient syntheses of 4,5-, 5,6-, and 6,7-indolyne precursors beginning from commercially available hydroxyindole derivatives are reported. The synthetic routes are versatile and allow access to indolyne precursors that remain unsubstituted on the pyrrole ring. Indolynes can be generated under mild fluoride-mediated conditions, trapped by a variety of nucleophilic reagents, and used to access a number of novel substituted indoles. Nucleophilic addition reactions to indolynes proceed with varying degrees of regioselectivity; distortion energies control regioselectivity and provide a simple model to predict the regioselectivity in the nucleophilic additions to indolynes and other unsymmetrical arynes. This model has led to the design of a substituted 4,5-indolyne that exhibits enhanced nucleophilic regioselectivity.
- Im, G-Yoon J.,Bronner, Sarah M.,Goetz, Adam E.,Paton, Robert S.,Cheong, Paul H.-Y.,Houk,Garg, Neil K.
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supporting information; experimental part
p. 17933 - 17944
(2011/02/26)
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- HETEROARYLAMIDE LOWER CARBOXYLIC ACID DERIVATIVE
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To provide a novel compound which has S1P receptor agonistic activity, exhibits excellent immunosuppressing effect, gives less adverse side effects, and can be orally administered. The invention provides a compound represented by general formula (I) (wherein A is a single bond, -O-, or - CH2-; R1 represents a hydrogen atom or a C1-C6 alkyl group, and V represents any one group selected from among the following groups (1) to (3) : (1) -G1-, (2) -G2-N(R2) -G3-, and (3) a group represented by formula 2, wherein each of Z1 and Z2 represents a hydrogen atom or a C1-C6 alkyl group, Z3 represents a hydrogen or the like, Q represents -CH2-O- or the like, and Y represents a group represented by foumula 3, a salt thereof, or a solvate thereof.
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Page/Page column 69
(2009/02/10)
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- Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides
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(4-Benzylpiperidine-1-yl)-(6-hydroxy-1H-indole-2-yl)-methanone (6a) derived from (E)-1 -(4-benzylpiperidin-1-yl)-3-(4-hydroxy-phenyl)-propenone (5) was identified as a potent NR2B subunit-selective antagonist of the NMDA receptor. To establish the structu
- Borza, István,Bozó, éva,Barta-Szalai, Gizella,Kiss, Csilla,Tárkányi, Gábor,Demeter, ádám,Gáti, Tamás,Háda, Viktor,Kolok, Sándor,Gere, Anikó,Fodor, László,Nagy, József,Galgóczy, Kornél,Magdó, Ildikó,ágai, Béla,Fetter, József,Bertha, Ferenc,Keserü, Gy?rgy M.,Horváth, Csilla,Farkas, Sándor,Greiner, István,Domány, Gy?rgy
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p. 901 - 914
(2008/02/03)
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- Concise, asymmetric, stereocontrolled total synthesis of stephacidins A, B and notoamide B
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Concise asymmetric total syntheses of the fungal metabolites (-)-stephacidin A, (+)-stephacidin B, and (+)-notoamide B are described. Key features of these total syntheses include (1) a facile synthesis of (R)-allyl proline methyl ester, (2) a revised rou
- Artman III, Gerald D.,Grubbs, Alan W.,Williams, Robert M.
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p. 6336 - 6342
(2008/02/03)
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- Concise syntheses of the 1,7-dihydropyrano[2,3-g]indole ring system of the stephacidins, aspergamides and norgeamides
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Three approaches towards the synthesis of the 1,7-dihydropyrano[2,3-g] indole ring system of the stephacidins, paraherquamides and norgeamides have been investigated. The first involves a tandem nitrene insertion/aromatic Claisen rearrangement. The second
- Grubbs, Alan W.,Artman III, Gerald D.,Williams, Robert M.
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p. 9013 - 9016
(2007/10/03)
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