- BIS AROMATIC COMPOUNDS FOR USE IN THE TREATMENT OF INFLAMMATION
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There is provided compounds of formula (I), wherein ring A, D1, D2a, D2b, D3, Y, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
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Page/Page column 75
(2010/04/06)
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- BIS-AROMATIC COMPOUNDS USEFUL IN THE TREATMENT OF INFLAMMATION
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There is provided compounds of formula (I): wherein Y, ring A, D1, D2, D3, L1, Y1, L2, Y2, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
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Page/Page column 22
(2010/12/29)
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- HOMOGENEOUS TIME RESOLVED FLUORESCENCE BASED TEST SYSTEM
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The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the HIV gp41 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN36 (SEQ ID NO:1); a second helical polypeptide consisting essentially of the sequence of C34 (SEQ ID NO: 2) wherein said IQN36 is labeled with a light emitting fluorophore and said C34 is labeled with an ultra-violet excitable fluorophore.
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Page/Page column 25
(2010/12/29)
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- NEW METHYLENEBISPHENYL COMPOUNDS USEFUL IN THE TREATMENT OF INFLAMMATION
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There is provided compounds of formula (I), wherein Rx, Ry, X1, X2, L1, L2, Y1 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
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Page/Page column 54
(2008/12/07)
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- Discovering novel chemical inhibitors of human cyclophilin A: Virtual screening, synthesis, and bioassay
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Cyclophilin A (CypA) is a member of cyclophilins, a family of the highly homologous peptidyl prolyl cis-trans isomerases (PPIases), which can bind to cyclosporin A (CsA). CypA plays critical roles in various biological processes, including protein folding, assembly, transportation, regulation of neuron growth, and HIV replication. The discovery of CypA inhibitor is now of a great special interest in the treatment of immunological disorders. In this study, a series of novel small molecular CypA inhibitors have been discovered by using structure-based virtual screening in conjunction with chemical synthesis and bioassay. The SPECS_1 database containing 85,000 small molecular compounds was searched by virtual screening against the crystal structure of human CypA. After SPR-based binding affinity assay, 15 compounds were found to show binding affinities to CypA at submicro-molar or micro-molar level (compounds 1-15). Seven compounds were selected as the starting point for the further structure modification in considering binding activity, synthesis difficulty, and structure similarity. We thus synthesized 40 new small molecular compounds (1-6, 15, 16a-q, 17a-d, and 18a-l), and four of which (compounds 16b, 16h, 16k, and 18g) showed high CypA PPIase inhibition activities with IC50s of 2.5-6.2 μM. Pharmacological assay indicated that these four compounds demonstrated somewhat inhibition activities against the proliferation of spleen cells.
- Li, Jian,Chen, Jing,Gui, Chunshan,Zhang, Li,Qin, Yu,Xu, Qiang,Zhang, Jian,Liu, Hong,Shen, Xu,Jiang, Hualiang
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p. 2209 - 2224
(2007/10/03)
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