872001-95-1Relevant academic research and scientific papers
ARYLSULFONAMIDE DERIVATIVES AS MGLUR4 NEGATIVE ALLOSTERIC MODULATORS
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Page/Page column 55, (2021/02/19)
The present invention provides new arylsulfonamide compounds having the general formula (I), wherein L, R1, R2, R3 and R4are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as mGLUR4 negative allosteric modulators.
(AZA)INDAZOLYL-ARYL SULFONAMIDE AND RELATED COMPOUNDS AND THEIR USE IN TREATING MEDICAL CONDITIONS
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, (2020/10/21)
The invention provides (aza)indazolyl-aryl sulfonamide and related compounds, pharmaceutical compositions, and their use in the treatment of medical conditions, such as cancer, and in inhibiting GCN2 activity.
Exploration of pyrrole derivatives to find an effective potassium-competitive acid blocker with moderately long-lasting suppression of gastric acid secretion
Nishida, Haruyuki,Fujimori, Ikuo,Arikawa, Yasuyoshi,Hirase, Keizo,Ono, Koji,Nakai, Kazuo,Inatomi, Nobuhiro,Hori, Yasunobu,Matsukawa, Jun,Fujioka, Yasushi,Imanishi, Akio,Fukui, Hideo,Itoh, Fumio
, p. 3447 - 3460 (2017/05/29)
With the aim to discover a novel excellent potassium-competitive acid blocker (P-CAB) that could perfectly overcome the limitations of proton pump inhibitors (PPIs), we tested various approaches based on pyrrole derivative 1 as a lead compound. As part of a comprehensive approach to identify a new effective drug, we tried to optimize the duration of action of the pyrrole derivative. Among the compounds synthesized, fluoropyrrole derivative 20j, which has a 2-F-3-Py group at position 5, fluorine atom at position 4, and a 4-Me-2-Py sulfonyl group at the first position of the pyrrole ring, showed potent gastric acid-suppressive action and moderate duration of action in animal models. On the basis of structural properties including a slightly larger C?log?P value (1.95), larger log?D value (0.48) at pH 7.4, and fairly similar pKa value (8.73) compared to those of the previously optimized compound 2a, compound 20j was assumed to undergo rapid transfer to the stomach and have a moderate retention time there after single administration. Therefore, compound 20j was selected as a new promising P-CAB with moderately long duration of action.
HETEROCYCLIC ANTIVIRAL COMPOUNDS
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, (2010/02/15)
Chemokine receptor antagonists, in particular, 3,7-diazabicyclo [3.3.0] octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are allieviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula (I).
