159847-83-3Relevant articles and documents
FUROISOQUINOLINE DERIVATIVE AND USE THEREOF
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Page/Page column 39, (2010/02/11)
The present invention provides a compound represented by the formula ???wherein A represents (1) a bond, (2) a group represented by the formula -CRa=CRb- (Ra and Rb each represent a hydrogen atom or C1-6 alkyl) and the like; R1 represents (1) cyano or (2) an optionally esterified or amidated carboxyl group; R2 represents(1) a hydrogen atom, (2) an optionally substituted hydroxy group,(3) an optionally substituted amino group and the like; R3 and R4 each represent a hydrogen atom and the like; R5 represents a hydrogen atom and the like; R6 represents an optionally substituted hydroxy group and the like; R7and R8 each represent an optionally substituted hydrocarbon group and the like; R9 and R10 each represent (1) a hydrogen atom and the like; Y represents an optionally substituted methylene group; and n represents 0 or 1, or a salt thereof, which has an excellent phosphodiesterase IV inhibiting action.
1,3-BENZOTHIAZINONE DERIVATIVES, PROCESS FOR PRODUCING THE SAME AND USE THEREOF
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Page/Page column 25, (2010/02/13)
As prophylactic and/or therapeutic agents for cardiovascular diseases, bone or joint diseases, infectious diseases, inflammatory diseases, kidney diseases, etc. having safe and excellent effects of cell death inhibition, MIF binding, etc., there are provi
Quinoxaline compounds
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Page/Page column 29, (2008/06/13)
Certain amidophenyl-sulfonylamino-quinoxaline compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
Regioselective Hydrolysis of Aromatic Dinitriles Using a Whole Cell Catalyst
Crosby, John,Moilliet, Jock,Parratt, Julian S.,Turner, Nicolas J.
, p. 1679 - 1688 (2007/10/02)
A series of aromatic dinitriles have been examined as substrates for an immobilised whole cell Rhodococcus sp. that catalyses the hydrolysis of nitriles to amides and/or carboxylic acids.The fluorinated aromatic dinitriles 48 and 49 were regioselectively hydrolysed to the corresponding cyano amides 48a and 49a whereas the non-fluorinated analogues 41-44 were converted to cyano acids but with poorer regioselectivity.
3-Acyl-4-hydroxyquinolin-2(1H)-ones. Systemically Active Anticonvulsants Acting by Antagonism at the Glycine Site of the N-Methyl-D-Aspartate Receptor Complex
Rowley, Michael,Leeson, Paul D.,Stevenson, Graeme I.,Moseley, Angela M.,Stansfield, Ian,et al.
, p. 3386 - 3396 (2007/10/02)
Most full antagonists at the glycine site of the NMDA receptor contain a carboxylic acid, which we believe to be detrimental to penetration of the blood-brain barrier.By consideration of a pharmacophore, novel antagonists at this site have been designed in which the anionic functionality is a vinylogous acid, in the form of a 4-hydroxyquinolin-2(1H)-one.In this series, a 3-substituent is necessary for binding, and correct manipulation of this group leads to compounds such as the 3-(3-hydroxyphenyl)propargyl ester 24 (L-701,273), with an IC50 for displacement of -L-689,560 binding of 0.17 μM and Kb against NMDA in the cortical slice of 1.39 μM.Compounds were tested for their ability to prevent audiogenic seizure in DBA/2 mice; the most potent compound in this series is the cyclopropyl ketone 42 (L-701,252), with an ED50 of 4.1 mg/kg ip.A model is proposed for binding to the glycine site, in which an important interaction is of a putative receptor cation with the ?-system of the 3-substituent.