- S-triazine compounds as well as preparation method and application thereof
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The invention discloses s-triazine compounds and pharmaceutically acceptable salts thereof; experiments prove that the compounds can be used for treating or preventing diseases related to protein kinase activity, such as leukemia and lymphoma, by inhibiti
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Paragraph 0088-0090
(2020/05/05)
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- As tyrosine kinase inhibitors containing nitrogen and ring compound
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The invention belongs to the technical field of medicine, particularly relates to a heterocyclic nitrogen compound which acts as a tyrosine kinase inhibitor and is represented by a general formula (I) as well as a deuterated material, pharmaceutically acc
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Paragraph 0313; 0314; 0315; 0316
(2017/04/26)
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- ARYL SULFONAMIDE COMPOUNDS AS CARBONIC ANHYDRASE INHIBITORS AND THEIR THERAPEUTIC USE
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Disclosed herein are compounds having the following structure useful as inhibitors of carbonic anhydrase IX (CAIX) and XII, and particularly useful for reducing or eliminating metastases see Formula (I).
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Page/Page column 67
(2017/01/23)
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- 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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- 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; 00770
(2015/09/28)
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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; 00245
(2015/02/02)
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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; 00547
(2014/09/03)
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- ALKYLQUINOLINE AND ALKYLQUINAZOLINE KINASE MODULATORS
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The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula I: wherein R1, R2, R3, B, Z, G, Q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or c-kit and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or c-kit and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or c-kit and/or TrkB. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
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Page/Page column 72
(2010/11/25)
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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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- 6-Anilino-1,4,5-trihydroxyanthraquinones
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Blue anthraquinone dyestuffs are prepared from the reaction of 6-chloro-1,4,5-trihydroxyanthraquinone with an appropriate aniline reactant. The resultant blue dyestuffs are 6-anilino-1,4,5-trihydroxyanthraquinones which produce excellent blue dyeings on polyester fabrics, particularly polyethylene terephthalate.
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