- Synthesis of 4-(3-oxo-3-phenylpropyl)morpholin-4-ium chloride analogues and their inhibitory activities of nitric oxide production in lipopolysaccharide-induced BV2 cells
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Based on our previous report that 3-morpholino-1-phenylpropan-1-one 2, one of the fluoxetine's simplified morpholino analogue, inhibited nitric oxide (NO) production, in this paper, various substituted benzene analogues with morpholine hydrochloride of 2 were synthesized and their inhibitory effects on NO production in lipopolysaccharide (LPS)-induced BV2 cells were tested. Among the synthesized compounds, 2-trifluoromethyl analogue 16n (IC50 = 8.6 μM) showed a significantly higher inhibitory activity than that of the parent compound 2a (IC50 > 50 μM) and suppressed NO production dose-dependently without cytotoxicity. Compound 16n also inhibited iNOS expression in LPS-induced BV2 cells at 2, 10 and 20 μM concentrations. These results suggest that compound 16n inhibited NO production by suppressing the expression of iNOS and can be used as a lead structure for developing new inhibitor of NO production.
- Yoon, Sung-Hwa,Lee, Eunhwa,Cho, Duk-Yeon,Ko, Hyun Myung,Baek, Ha Yeon,Choi, Dong-Kug,Kim, Eunha,Park, Ju-Young
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supporting information
(2021/02/02)
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- IMIDAZO[1,2-C]PYRIMIDINE DERIVATIVES AS PRC2 INHIBITORS FOR TREATING CANCER
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Disclosed are compounds that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, disclosed are compounds of Formula (I) and pharmaceutical compositions thereof, and methods of using the compounds and pharmaceutical compositions in, for example, methods of treating cancer.
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Paragraph 0403-0404
(2020/12/29)
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- SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES
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The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
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Page/Page column 14-15; 18; 68
(2019/11/12)
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- FUNGICIDAL OXIMES AND HYDRAZONES
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Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G, W2 and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for co
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Page/Page column 83
(2011/12/04)
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- FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY
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The present invention relates to certain certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the "Fused Tricyclic Compounds"), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.
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Page/Page column 48
(2011/06/16)
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- Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
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The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory- and immune-associ
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Page/Page column 35
(2008/06/13)
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- SUBSTITUTED THIAZOLE AND PYRIMIDINE DERIVATIVES AS MELANOCORTIN RECEPTOR MODULATORS
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The present invention provides substituted thiazole and pyrimidine derivatives of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I), and methods of use in treating human or animal disorders. The compounds of the invention can be useful as inhibitors of action of AgRP on a melanocortin receptor and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases which may be responsive to the modulation of melanocortin receptors including obesity-related disorders.
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Page/Page column 110
(2010/02/14)
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- Synthesis of (Imidazopyrimidin-2-yl)phenylmethanones and 6-Benzoylpyrrolopyrimidinones
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4-Pyrimidinamines have been reacted with 3-bromo-1-phenylpropane-1,2-dione to give a series of (imidazopyrimidin-2-yl)phenylmethanones.The dione also reacted with ethyl amidinoacetate to yield ethyl 2-amino-5-benzoylpyrrole-2-carboxylate which was used to prepare a series of 6-benzoylpyrrolopyrimidines.
- Danswan, Geoffrey,Kennewell, Peter D.,Tully, W. Roger
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p. 293 - 299
(2007/10/02)
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- 2-substituted imidazo[1,2-c]pyrimidines having anxiolytic properties
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Novel imidazo[1,2-c]pyrimidines of the formula STR1 wherein R is an aryl of 6 to 12 carbon atoms, R 1 is selected from the group consisting of hydrogen and alkyl, alkoxy and alkylthio of 1 to 5 carbon atoms when R 2 and R 3 together form a carbon-nitrogen bond or R 1 and R 2 together are 0 when R 3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and alkenyl of 2 to 5 carbon atoms, R 4 is selected from the group consisting of alkoxy and alkylthio of 1 to 5 carbon atoms, R 5 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anxiolytic properties.
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- Preparation and Photocyclisation of Bromomethyl 1,2-Diketones
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A simple preparative route to the title compounds is given involving bromine addition to α-ethoxyvinyl ketones and subsequent hydrolysis.These compounds undergo efficient photocyclisation with retention of the halogen to hydroxycyclobutanone and hydroxycy
- Hamer, Neil K.
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