- Rhein specific group modified organic compound, aryl metal complex, preparation method and application thereof
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The invention discloses a rhein specific group modified organic compound, an aryl metal complex, a preparation method and application thereof. Compared with rhein molecules, the organic compound and metal complex have better antitumor and antibacterial activity, and the metal complex also can induce nucleic acid configuration transformation. Specifically, the aryl metal dimer and the above-mentioned metal complex both have good FTO (fat mass and obesity associated) inhibitory activity, and are good FTO inhibitors. The invention also discloses a synthesis method of the organic compound and themetal complex thereof, and the method has the characteristics of simple technological process, easy operation, and high yield. Finally, the invention discloses application of the rhein group-containing organic compound, the metal complex and aromatic metal dimer thereof in preparation of FTO inhibitor drugs, FTO inhibitor drug components, weight-reducing drugs, weight-reducing drug components, anticancer drugs, anticancer drug components, antibacterial drugs and antibacterial drug components.
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Paragraph 0102; 0105-0108
(2018/10/11)
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- CINNAMIC ACID AMIDE DERIVATIVE
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The present invention provides a cinnamic acid amide derivative having an excellent analgesic action. The cinnamic acid amide derivative of the present invention is a compound showing excellent analgesic actions to not only a nociceptive pain model animal but also a neuropathic pain model animal, which is very useful as an agent for treating various pain diseases showing acute or chronic pains or neuropathic pains.
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Paragraph 0028; 0057
(2015/11/24)
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- Synthesis and characterization of N-substitutional ethylenediamine derivatives
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N-Substituted and N,N-disubstituted ethylenediamine derivatives were prepared rapidly in aqueous conditions from 30 to 76 % yields, respectively, on a multi-gram scale starting from inexpensive and commercially available starting materials. The steps involved Michael addition, hydrazinolysis and Curtius rearrangements. The highlight of this method lies on its convenience and economy in accessing these intermediates.
- Yao, Ri-Sheng,Jiang, Lai-En,Wu, Sheng-Hua,Deng, Sheng-Song,Yang, Yang
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p. 3792 - 3794
(2012/01/05)
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- Carbamate-appended N-alkylsulfonamides as inhibitors of γ-secretase
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The synthesis and γ-secretase inhibition data for a series of carbamate-appended N-alkylsulfonamides are described. Carbamate 54 was found to significantly reduce brain Aβ in transgenic mice. 54 was also found to possess markedly improved brain levels in transgenic mice compared to previously disclosed 1 and 2.
- Bergstrom, Carl P.,Sloan, Charles P.,Lau, Wai-Yu,Smith, David W.,Zheng, Ming,Hansel, Steven B.,Polson, Craig T.,Corsa, Jason A.,Barten, Donna M.,Felsenstein, Kevin M.,Roberts, Susan B.
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p. 464 - 468
(2008/12/21)
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- CHEMICAL COMPOUNDS
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The present invention provides novel compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind specifically to the chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 and/or CCR5 of a target cell.
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Page/Page column 154
(2010/10/20)
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- The first potent inhibitors for human glutaminyl cyclase: Synthesis and structure-activity relationship
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The first effective inhibitors for human glutaminyl cyclase (QC) are described. The structures are developed by applying a ligand-based optimization approach starting from imidazole. Screening of derivatives of that heterocycle led to compounds of the imidazol-1-yl-alkyl thiourea type as a lead scaffold. A library of thiourea derivatives was synthesized, resulting in an inhibitory improvement by 2 orders of magnitude, leading to 1-(3-(1H-imidazol-1-yl)propyl)- 3-(3,4-dimethoxyphenyl)thiourea as a potent inhibitor. Systematic exploitation of the scaffold revealed a strong impact on the inhibitory efficacy and resulted in the development of imidazole-propyl-thioamides as another new class of potent inhibitors. A flexible alignment of the most potent compounds of the thioamide and thiourea class and a QC substrate revealed a good match of characteristic features of the molecules, which suggests a similar binding mode of both inhibitors and the substrate to the active site of QC.
- Buchholz, Mirko,Heiser, Ulrich,Schilling, Stephan,Niestroj, André J.,Zunkel, Katrin,Demuth, Hans-Ulrich
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p. 664 - 677
(2007/10/03)
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- ORGANIC COMPOUNDS
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Compounds of Formula (I); in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
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Page/Page column 41
(2008/06/13)
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- Chemokine receptor binding heterocyclic compounds with enhanced efficacy
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The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
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Page/Page column 17-19
(2010/02/03)
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- Epoxysuccinamide derivative or salt thereof
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PCT No. PCT/JP98/01778 Sec. 371 Date Dec. 17, 1998 Sec. 102(e) Date Dec. 17, 1998 PCT Filed Apr. 17, 1998 PCT Pub. No. WO98/47887 PCT Pub. Date Oct. 29, 1998The invention relates an epoxysuccinamide derivative represented by a formula (I): wherein R1 represents a hydrogen atom, an alkyl or aminoalkyl group, R2 represents an aminoalkyl group which May be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an aralkyl group which may be substituted, or an alkyl group substituted by a heterocyclic ring which may be substituted, or R1 and R2 may form a nitrogen-containing heterocyclic ring, which may be substituted, together with the adjacent nitrogen atoms, and R3 and R4 are the same or different from each other and independently represent a hydrogen atom, or an alkyl or aralkyl group, or a salt thereof, a preparation process thereof, and a medicine comprising such a derivative or salt as an active ingredient. This compound has a specific inhibitory activity for cathepsin L and family enzymes thereof, and is useful as an agent for preventing and treating metabolic osteopathy such as osteoporosis and hypercalcemia.
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- Method for inhibiting advanced glycosylation of proteins using aminosubstituted imidazoles
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The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging), Accordingly, a composition is disclosed which comprises 2-aminoimidazoles capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation, The method comprises contacting the target protein with the composition, Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
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- Hypoxia-selective antitumor agents. 8. Bis(nitroimidazolyl)alkanecarboxamides: A new class of hypoxia-selective cytotoxins and hypoxic cell radiosensitisers
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A series of novel bis(nitroimidazolyl)alkanecarboxamides has been prepared and evaluated for hypoxia-selective cytotoxicity and hypoxic cell radiosensitisation in vitro and in vivo. The compounds were prepared by direct coupling of preformed side chain acid and amine components, using diethyl phosphorocyanidate at room temperature. Although designed to be bis- bioreductive prodrugs of DNA cross-linking agents, none of the compounds showed evidence of DNA cross-linking activity, being equally potent against cell lines deficient and proficient in repair of cross-links. However, one of these compounds, N-[2-(2-methyl-5-nitro-1H-imidazolyl)ethyl]-4-(2-nitro-1H- imidazolyl)butanamide (10; SN 24699), showed high hypoxic selectivity as a cytotoxin (rising to 200-fold after exposure to the drug for several hours) in the repair-proficient Chinese hamster cell line AA8. This selectivity was greater than observed for the alkylating 2-nitroimidazole (4; RB 6145) (40- fold) or simple mononitroimidazoles (5-25-fold). Investigation of structure- activity relationships for hypoxic selectivity of bis(nitroimidzoles) was restricted by their low aqueous solubility, but a certain minimum separation of the two nitroimidazole units (by more than five atoms) appears desirable. All the compounds radiosensitized hypoxic cells in vitro but were little more potent as radiosensitizers than the corresponding monomeric nitroimidazoles. Compound 10 caused additional cell killing in the KHT tumor when multiple drug doses were administered in combination with a single dose of radiation. It is not yet clear whether this activity reflects hypoxic cell radiosensitization or cytotoxicity toward hypoxic cells, but this new class of bis-bioreductive agent clearly warrants further investigation.
- Hay,Wilson,Moselen,Palmer,Denny
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p. 381 - 391
(2007/10/02)
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