38239-45-1Relevant academic research and scientific papers
Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates
Cao, Xufeng,Xu, Yuanyuan,Cao, Yongbing,Wang, Ruilian,Zhou, Ran,Chu, Wenjing,Yang, Yushe
supporting information, p. 471 - 476 (2015/09/01)
In order to further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds (I), two series of novel azoles featuring thieno[2,3-c]pyrrolidone and thieno[3,2-c]pyrrolidone nuclei were designed and evaluated for their in vitro activity on the basis of the binding mode of albaconazole using molecular docking, along with SARs of antifungal triazoles. Most of target compounds exhibited excellent activity against Candida and Cryptococcus spp., with MIC values in the range of 0.0625 μg/ml to 0.0156 μg/ml. The thieno[3,2-c]pyrrolidone unit was more suited for improving activity against Aspergillus spp. The most potent compound, 18a, was selected for further development due to its significant in vitro activity against Aspergillus spp. (MIC Combining double low line 0.25 μg/ml), as well as its high metabolic stability in human liver microsomes.
OXAZOLE AND ISOXAZOLE CRAC MODULATORS
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Page/Page column 74, (2012/05/19)
The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).
PYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
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Page/Page column 98; 99, (2010/04/28)
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, Formula Ia, R4, R5, Formula Ib, R3, R3a, W, D, R2a, R2b and R2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.
2-SUBSTITUTED 5-MEMBERED HETEROCYCLES AS SCD INHIBITORS
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Page/Page column 78, (2008/12/06)
The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed
Novel thienopyridine compounds, and methods of use thereof
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Page/Page column 22, (2008/06/13)
The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).
Convergent processes for the synthesis of a GARFT inhibitor containing a methyl substituted thiophene core and intermediates therefor
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Page 13, (2010/02/10)
The invention relates to processes for the preparation of a GARFT inhibitor containing a methyl substituted thiophene core having the following structure: wherein each of R1 and R2 are independently a hydrogen atom or a moiety that together with the attached CO2 forms a readily hydrolyzable ester group; from an intermediate of the formula wherein R3 is a moiety that together with the attached CO2 forms a readily hydrolyzable ester group; Pg1 is an amino protecting group; R4 is H; or Pg1 can optionally be taken together with R4 and the nitrogen to which Pg1 and R4 are attached to form (i) an imine; or (ii) a fused or bridged bicyclic ring or a spirocyclic ring, wherein said ring is saturated and contains from 5 to 12 carbon atoms in which up to 2 carbon atoms are optionally replaced with a hetero moiety selected from O, S(O)j wherein j is an integer from 0 to 2, and —NR8—, provided that two O atoms, two S(O)j moieties, or an O atom and a S(O)j moiety are not attached directly to each other; R5 is selected from the group consisting of —C≡C— and —CH═CH—; and R8 is independently H or C1-C6 alkyl; to form the compound of the formula (I) that is optically pure; and to processes for preparing intermediates thereof.
