- Double-target inhibitor targeting FGFR (fibroblast growth factor receptor) and HDAC (histone deacetylase) as well as preparation method and application thereof, pharmaceutical composition and medicament
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The invention discloses a double-target inhibitor targeting FGFR (fibroblast growth factor receptor) and HDAC (histone deacetylase) as well as a preparation method and application thereof, a pharmaceutical composition and a medicament, and belongs to the
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Paragraph 0429-0431
(2021/06/09)
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- Structure-Based Design of Dual-Acting Compounds Targeting Adenosine A2AReceptor and Histone Deacetylase as Novel Tumor Immunotherapeutic Agents
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Adenosine is an immunosuppressive factor in the tumor microenvironment mainly through activation of the A2A adenosine receptor (A2AR), which is a mechanism hijacked by tumors to escape immune surveillance. Small-molecule A2AR antagonists are being evaluat
- Yan, Wenzhong,Ling, Lijun,Wu, Yiran,Yang, Kexin,Liu, Ruiquan,Zhang, Jinfeng,Zhao, Simeng,Zhong, Guisheng,Zhao, Suwen,Jiang, Hualiang,Xie, Chengying,Cheng, Jianjun
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p. 16573 - 16597
(2021/12/02)
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- Pyrene-containing water-soluble dye and preparation method thereof
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The invention discloses a pyrene-containing water-soluble dye. The general formula of the pyrene-containing water-soluble dye is shown as a formula I. The pyrene-containing water-soluble dye with thewidened fluorescence emission spectrum is reasonable in
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Paragraph 0058-0060
(2020/12/30)
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- INHIBITORS OF THE WNT/BETA-CATENIN PATHWAY
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The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.
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Page/Page column 78
(2019/08/26)
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- New rosiglitazone analogue, preparation method and applications thereof
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The invention relates to a rosiglitazone analogue, a preparation method and applications thereof, wherein the compound has a structure represented by the following formula (I), R1 represents C3-10 cycloalkyl unsubstituted or optionally substituted by the
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Paragraph 0098-0102
(2020/01/12)
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- Naphthylamine compound and biologically acceptable salt thereof as well as preparation method and application thereof
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Aiming at shortage of anti-cancer targeting medicines in the prior art, the invention provides a naphthylamine compound and a biologically acceptable salt thereof as well as a preparation method and application thereof. By adopting the naphthylamine compo
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Paragraph 0088; 0106; 0119-0121
(2019/12/15)
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- PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
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Page/Page column 174
(2020/01/11)
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- Discovery of Novel 2-(piperidin-4-yl)-1H-benzo[d]imidazole Derivatives as Potential Anti-Inflammatory Agents
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A novel 2-(piperidin-4-yl)-1H-benzo[d]imidazole derivative 5 with good anti-inflammatory activity was identified from our in-house library. Based on hit compound 5, two series of 2-(piperidin-4-yl)-1H-benzo[d]imidazole derivative 6a-g and 7a-h were designed and synthesized as novel anti-inflammatory agents. Most of synthesized compounds exhibited good inhibitory activity on NO and TNF-α production in LPS-stimulated RAW 264.7 macrophages, in which the compound 6e showed most potent inhibitory activity on NO (IC50 = 0.86 μm) and TNF-α (IC50 = 1.87 μm) production. Further evaluation revealed that compound 6e displayed more potent in vivo anti-inflammatory activity than ibuprofen did on xylene-induced ear oedema in mice. Additionally, Western blot analysis revealed that compound 6e could restore phosphorylation level of IκBα and protein expression of p65 NF-κB in LPS-stimulated RAW 264.7 macrophages.
- Li, Qing,Hu, Qinghua,Wang, Xinning,Zong, Yang,Zhao, Leilei,Xing, Junhao,Zhou, Jinpei,Zhang, Huibin
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p. 509 - 516
(2015/03/30)
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- Development of unsymmetrical dyads as potent noncarbohydrate-based inhibitors against human β-N-acetyl-D-hexosaminidase
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Human β-N-acetyl-D-hexosaminidase has gained much attention due to its roles in several pathological processes and been considered as potential targets for disease therapy. A novel and efficient skeleton, which was an unsymmetrical dyad containing naphthalimide and methoxyphenyl moieties with an alkylamine spacer linkage as a noncarbohydrate-based inhibitor, was synthesized, and the activities were valuated against human β-N-acetyl-D- hexosaminidase. The most potent inhibitor exhibits high inhibitory activity with Ki values of 0.63 μM. The straightforward synthetic manners of these unsymmetrical dyads and understanding of the binding model could be advantageous for further structure optimization and development of new therapeutic agents for Hex-related diseases.
- Guo, Peng,Chen, Qi,Liu, Tian,Xu, Lin,Yang, Qing,Qian, Xuhong
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p. 527 - 531
(2013/07/26)
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- METHODS OF USING SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
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Methods of using semi-synthetic glycopeptides of formula I-XIV having antibacterial activity are described.
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Page/Page column 98; 99
(2011/11/30)
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- TARTRATE SALTS OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives that are inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The tartrate salts may further act as HDAC inhibitors.
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Page/Page column 83
(2009/04/24)
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- FORMULATION OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to a composition comprising an inclusion complex of a cyclodextrin and quinazoline containing zinc-binding moiety based derivatives. The cyclodextrin is preferable a β-cyclodextrin or a derivative thereof. The quinazolines have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 81
(2009/05/29)
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- MULTI-FUNCTIONAL SMALL MOLECULES AS ANTI-PROLIFERATIVE AGENTS
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The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.
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Page/Page column 150
(2008/06/13)
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- Antithrombotic agents
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The invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts, as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.
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- Biphenyl derivatives and the use thereof as integrin inhibitors
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Novel biphenyl derivatives of the general formula (I), in which Y, R R1, R2, R3, R4, m, o and p are as defined in claim 1, and their physiologically acceptable salts and solvates are integrin inhibitors and can
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- INHIBITORS OF ADENOSINE MONOPHOSPHATE DEAMINASE
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Novel diazepine derivatives which selectively inhibit adenosine monophosphate deaminase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine
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- BETA-ADRENERGIC BLOCKING AGENTS IN THE 1,2,3-THIADIAZOLE SERIES
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Novel 4-2,3 or 4(3-amino-2-hydroxypropoxy) phenyl!-and 5-2, 3 or 4(3-amino-2-hydroxypropoxy) phenyl!-1,2,3-thiadiazole derivatives which may be further substituted at the C-5 or C-4 position of the thiadiazole ring, respectively, by a lower alkyl, phenyl, trifluoromethyl, carboxy, alkoxycarbonyl, cyano or an aminocarbonyl group, and the pharmaceutically acceptable acid addition salts thereof and processes for the production of such compounds; 4-4(3-t-butylamino-2-hydroxypropoxy) phenyl!-1,2,3-thiadiazole and 5-4(3-t-butylamino-2-hydroxypropoxy) phenyl!-1,2,3-thiadiazole are representative of the class. These compounds possess cardiovascular activity and are useful for the treatment of abnormal heart conditions in mammals.
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