- FLUORESCENT COMPOUND AND LABELING AGENT COMPRISING THE SAME
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A novel fluorescent compound having a high light fastness, high fluorescence quantum yield and sharp absorption spectrum, which emits fluorescence having a wavelength in long wavelength region, as well as its use as a labeling agent, is disclosed. In Form
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Page/Page column 18; 19
(2009/03/07)
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- FLUORO-SUBSTITUTED INHIBITORS OF D-AMINO ACID OXIDASE
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This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein A is NH or S. Q is a member selected from CR1 and N. X and Y are members independently selected from O, S, CR2, N and NH. R1, R2 and R4 are members independently selected from H and F, provided that at least one member selected from R1, R2 and R4 is F. R6 is a member selected from O?X+ and OH, wherein X+ is a positive ion, which is a member selected from inorganic positive ions and organic positive ions.
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Page/Page column 45
(2008/06/13)
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- The discovery of fused pyrrole carboxylic acids as novel, potent d-amino acid oxidase (DAO) inhibitors
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The 'NMDA hypofunction hypothesis of schizophrenia' can be tested in a number of ways. DAO is the enzyme primarily responsible for the metabolism of d-serine, a co-agonist for the NMDA receptor. We identified novel DAO inhibitors, in particular, acid 1, which demonstrated moderate potency for DAO in vitro and ex vivo, and raised plasma d-serine levels after dosing ip to rats. In parallel, analogues were prepared to survey the SARs of 1.
- Sparey, Tim,Abeywickrema, Pravien,Almond, Sarah,Brandon, Nick,Byrne, Noel,Campbell, Alister,Hutson, Pete H.,Jacobson, Marlene,Jones, Brian,Munshi, Sanjeev,Pascarella, Danette,Pike, Andrew,Prasad, G. Sridhar,Sachs, Nancy,Sakatis, Melanie,Sardana, Vinod,Venkatraman, Shankar,Young, Mary Beth
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scheme or table
p. 3386 - 3391
(2009/04/06)
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- USE OF FUSED PYRROLE CARBOXYLIC ACIDS FOR THE TREATMENT OF NEURODEGENERATIVE AND PSYCHIATRIC DISEASES AS D-AMINO ACID OXIDASE INHIBITORS
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The present invention provides the use of fused pyrrole carboxylic acids of formula (I) for the manufacture of a medicament to inhibit D-amino acid oxidase, particularly for the treatment of neurodegenerative and psychiatric disorders or diseases; certain
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Page/Page column 17
(2008/06/13)
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- Novel thienopyrrole glycogen phosphorylase inhibitors: Synthesis, in vitro SAR and crystallographic studies
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Two series of novel thienopyrrole inhibitors of recombinant human liver glycogen phosphorylase a (GPa) which are effective in reducing glucose output from rat hepatocytes are described. Representative compounds have been shown to bind at the dimer interface site of the rabbit muscle enzyme by X-ray crystallography.
- Whittamore, Paul R.O.,Addie, Matthew S.,Bennett, Stuart N.L.,Birch, Alan M.,Butters, Michael,Godfrey, Linda,Kenny, Peter W.,Morley, Andrew D.,Murray, Paul M.,Oikonomakos, Nikos G.,Otterbein, Ludovic R.,Pannifer, Andrew D.,Parker, Jeremy S.,Readman, Kristy,Siedlecki, Pawel S.,Schofield, Paul,Stocker, Andy,Taylor, Melvyn J.,Townsend, Linda A.,Whalley, David P.,Whitehouse, Jennifer
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p. 5567 - 5571
(2007/10/03)
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- Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: Potent human histamine H4 antagonists
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Three series of H4 receptor ligands,- derived from indoly-2-yl-(4-methyl-piperazin-1-yl)-methanones, have been synthesized and their structure-activity relationships evaluated for activity at the H 4 receptor in competitive binding and functional assays. In all cases, substitution of small lipophilic groups in the 4 and 5-positions led to increased activity in a [3H]histamine radiolabeled ligand competitive binding assay. In vitro metabolism and initial pharmacokinetic studies were performed on selected compounds leading to the identification of indole 8 and benzimidazole 40 as potent H4 antagonists with the potential for further development. In addition, both 8 and 40 demonstrated efficacy in in vitro mast cell and eosinophil chemotaxis assays.
- Venable, Jennifer D.,Cai, Hui,Chai, Wenying,Dvorak, Curt A.,Grice, Cheryl A.,Jablonowski, Jill A.,Shah, Chandra R.,Kwok, Annette K.,Ly, Kiev S.,Pio, Barbara,Wei, Jianmei,Desai, Pragnya J.,Jiang, Wen,Nguyen, Steven,Ling, Ping,Wilson, Sandy J.,Dunford, Paul J.,Thurmond, Robin L.,Lovenberg, Timothy W.,Karlsson, Lars,Carruthers, Nicholas I.,Edwards, James P.
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p. 8289 - 8298
(2007/10/03)
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- Heterocyclic compounds
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Certain thienopyrrolyl and furanopyrrolyl compounds are disclosed as useful to treat or prevent disorders and conditions mediated by the histamine H4 receptor, including allergic rhinitis.
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Page/Page column 9
(2010/02/05)
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