- ARBOVIRUS INHIBITORS AND USES THEREOF
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The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of arboviruses.
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Page/Page column 70
(2012/10/08)
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- AMINOMETHYL SUBSTITUTED BICYCLIC AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
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The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula (I) wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring mem
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Page/Page column 106
(2010/11/08)
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- QUINOLINE-2-ONE-DERIVATIVES FOR THE TREATMENT OF AIRWAYS DISEASES
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Compounds of formula (I) in free or salt form, wherein -C-Y-, R1 and R2 are G have the meanings as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the (β2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
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Page/Page column 40
(2008/06/13)
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- Diaminoindanes as microsomal triglyceride transfer protein inhibitors
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The synthesis and biological activities of biarylamide-substituted diaminoindanes as microsomal triglyceride transfer protein (MTP) inhibitors are described. One of the more potent compounds, 8aR, inhibited both the secretion of apoB from Hep G2 cells and the MTP-mediated transfer of triglycerides between synthetic acceptor and donor liposomes with IC50 values of 0.7 and 70 nM, respectively. In normolipidemic rats and dogs, oral administration of 8aR dose-dependently reduced both plasma triglycerides and total cholesterol. Moreover, in rats and dogs, 8aR also prevented the postprandial rise in plasma triglycerides following a bolus administration of a fat load. Because MTP inhibitors decrease very low density lipoprotein assembly in the liver, the potential for hepatic lipid accumulation was evaluated. In normolipidemic rats, hepatic cholesterol and triglyceride contents were dose-dependently increased by 8aR. However, hepatic lipid accumulation resulted in negligible change in total liver weight and was reversible after withdrawal of the compound.
- Ksander,DeJesus,Yuan,Fink,Moskal,Carlson,Kukkola,Bilci,Wallace,Neubert,Feldman,Mogelesky,Poirier,Jeune,Steele,Wasvery,Stephan,Cahill,Webb,Navarrete,Lee,Gibson,Alexander,Sharif,Hospattankar
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p. 4677 - 4687
(2007/10/03)
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- Synthesis and thromboxane A2 antagonistic activity activity of indane derivatives.
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A new series of indane derivatives were prepared and evaluated for their thromboxane A2 (TXA2, 1) antagonistic activity. Among these compounds, 24a (Z-335) was found to be a potent TXA2 antagonist in oral administration.
- Shinozaki,Sato,Iwakuma,Sato,Kurimoto,Yoshida
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p. 401 - 406
(2007/10/03)
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- Cyclic imino derivatives and pharmaceutical compositions containing them
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The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.
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