- PROPENAMIDE THIOPHENE DERIVATIVES AS FLAVIVIRUS INHIBITORS AND THEIR USE
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The present invention deals with new flavivirus inhibitors, compositions comprising said inhibitors and methods for the treatment of disorders related to a viral infection, such as a disease due to a flavivirus infection, comprising administering said inhibitors.
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Page/Page column 24
(2017/07/06)
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- Eeyarestatin I derivatives with improved aqueous solubility
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Inhibition of p97 (also known as valosin-containing protein (VCP)), has been validated as a promising strategy for cancer therapy. Eeyarestatin I (EerI) blocks p97 through a novel mechanism of action and has favorable anti-cancer activities against cultured cancer cells. However, its poor aqueous solubility severely limits its in vivo applications. To circumvent this problem, we have identified EerI derivatives that possess improved aqueous solubility by introducing a single solubilizing group. These modified compounds preserved endoplasmic reticulum (ER) stress-inducing and antiproliferative activities as well as generally good in vitro metabolic properties, suggesting that these EerI derivatives could serve as candidates for further optimization.
- Ding, Rui,Zhang, Ting,Xie, Jiashu,Williams, Jessica,Ye, Yihong,Chen, Liqiang
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supporting information
p. 5177 - 5181
(2016/11/09)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.
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Paragraph 00243; 00244
(2015/02/02)
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- TYK2 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
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Paragraph 00768; 00769
(2015/09/28)
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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions th
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Paragraph 00544; 00546
(2014/09/03)
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- Chemokine receptor binding compounds
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The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds
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Page/Page column 17
(2008/06/13)
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- 1-benzenesulfonyl-1,3-dihydro-2H-benzimidazol-2-one derivatives
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The present invention relates to 1-benzenesulfonyl-1,3-dihydro-2H-benzimidazol-2-one derivatives of the formula: STR1 to their preparation and to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and oxytocin receptors.
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- Basic dyes
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Dyes of the general formula I STR1 where A? is an anion, B is methyl, ethyl, benzyl or β-hydroxyethyl, n is 1 or 2, R is alkyl of 1 to 4 carbon atoms, X is hydrogen, methoxy, ethoxy or chlorine and Z is STR2 The dyes of the formula I give very fast dyeings on anionically modified fibers.
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