- SPIRO-OXADIAZOLINE COMPOUNDS AS AGONISTS OF α-7-NICOTINIC ACETYLCHOLINE RECEPTORS
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The present invention relates to novel spiro-oxadiazoline compounds that are suitable as agonists or partial agonists of a7-nAChR, and pharmaceutical compositions of the same, methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering a spiro-oxadiazoline cx7-nAChR agonist or partial agonist, to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
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- Fragment based discovery of a novel and selective PI3 kinase inhibitor
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We report the use of fragment screening and fragment based drug design to develop a PI3c kinase fragment hit into a lead. Initial fragment hits were discovered by high concentration biochemical screening, followed by a round of virtual screening to identify additional ligand efficient fragments. These were developed into potent and ligand efficient lead compounds using structure guided fragment growing and merging strategies. This led to a potent, selective, and cell permeable PI3c kinase inhibitor with good metabolic stability that was useful as a preclinical tool compound.
- Hughes, Samantha J.,Millan, David S.,Kilty, Iain C.,Lewthwaite, Russell A.,Mathias, John P.,Reilly, Mark A.O.,Pannifer, Andrew,Phelan, Anne,Stühmeier, Frank,Baldock, Darren A.,Brown, David G.
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scheme or table
p. 6586 - 6590
(2011/12/04)
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- NOVEL FUSED IMIDAZOLE DERIVATIVE
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The present invention relates to a compound represented by the Formula [I]: Wherein: the A ring is a 5-membered aromatic heterocyclic group containing at least one hetero atom selected from a nitrogen atom, and the like; A1 and A2, are each a nitrogen atom, and the like; X2, X3, X4, and X5 are all carbon atoms, or alternatively any one of X2, X3, X4, and X5 is a nitrogen atom and the rest are all carbon atoms; R1 is a hydrogen atom, or the like; R2, R3, R4, and R5, are each a hydrogen atom, or the like; R6 and R6', are each a hydrogen atom, and the like; R7 is an aryl group and the like; and R8 is an amino group or a hydroxy group, or a pharmaceutically acceptable salt or ester thereof.
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Page/Page column 80
(2010/11/28)
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- Heterocyclization of functionalized vinylic derivatives of imidazo[1,2-α]pyridines
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Heterocyclization of functionalized vinylic derivatives of imidazo[1,2-α]pyridines was explored experimentally and theoretically using semiempirical AM1 and ab initio methods. A range of functionalized vinylic derivatives (azido, amino, and carbodiimide groups) were prepared for conversion into pyrroloazaindoles 19-22, imidazo[1,x]-; (x=5, 6, 7, 8), [2,6]-, and [2,7]naphthyridines 28-30, 35-38 by thermal reaction. In the case of vinylic groups in the 5 position, peri annulation also was observed. The experimental and theoretical data are compared and discussed.
- Chezal,Moreau,Delmas,Gueiffier,Blache,Grassy,Lartigue,Chavignon,Teulade
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p. 6576 - 6584
(2007/10/03)
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- Thioformamide derivatives
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The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: [Figure] wherein Y represents [Figure] or the like [wherein R7 represents benzyloxy or the like; R11 and R12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, [Figure] (wherein R14 and R15 each represent hydrogen, benzyl or the like) or the like]; Z represents --CH2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R1 and R2 each represent hydrogen, lower alkyl or the like; and R3 and R4 each represent hydrogen, lower alkyl or the like.
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- The photosolvolysis of N-arylmethyladenines. Photoremovable N-arylmethyl protective groups for N-containing compounds
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N-arylmethyladenines are photolyzed in water, giving adenine and the corresponding arylmethanols.The reaction is not only observed when the arylmethyl group is a metasubstituted benzyl, but also with more complex substituents like imidazopyridin-6-ylmethyl.Meta-substituted arylmethyl groups are proposed as photoremovable N-protective groups in adenine chemistry.
- Er-Rhaimini, A.,Mohsinaly, N.,Mornet, R.
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p. 5757 - 5760
(2007/10/02)
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