- 3-PHENYLSULPHONYL-QUINOLINE DERIVATIVES AS AGENTS FOR TREATING PATHOGENIC BLOOD VESSELS DISORDERS
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The disclosure provides compounds, and compositions, including pharmaceutical compositions, kits that include the compounds, and methods of using (or administering) and making the compounds. The disclosure further provides compounds or compositions thereof for use in a method of modulating PLXDC1 (TEM7) and/or PLXDC2 or killing pathogenic blood vessles. The disclosure further provides compounds or compositions thereof for use in a method of treating a disease, disorder, or condition that is mediated, at least in part, by PEDF receptors or by angiogenesis.
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Paragraph 0322
(2021/04/23)
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- The discovery of CCR3/H1 dual antagonists with reduced hERG risk
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A series of dual CCR3/H1 antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to del
- Barton, Patrick,Brough, Steven,Evans, Richard,Luckhurst, Christopher A.,Mochel, Tobias,Perry, Matthew W. D.,Rigby, Aaron,Sanganee, Hitesh,Sisson, Adam,Springthorpe, Brian,Bahl, Ash,Bowers, Keith,Riley, Robert J.
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p. 6688 - 6693,6
(2012/12/12)
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- TRPV4 ANTAGONISTS
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The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
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Page/Page column 38
(2011/10/13)
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- Chemical compounds
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The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
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