Benzimidazoles as NMDA glycine-site antagonists: Study on the structural requirements in 2-position of the ligand
A series of different substituted benzimidazole derivatives has been synthesized and evaluated for the ability to displace [3H]MDL-105,519 to rat cortical membranes. Two benzimidazole-2-carboxylic acids 9 b and 9 c, in this substitution pattern not yet described as glycine antagonists, showed IC50 values of 0.89 μM (9 b) and 38.0 μM (9 c). Replacement of the carboxylate function in 2-position by a sulfonic acid moiety appreciably increased solubility, but decreased the affinity giving evidence for the strong need of the carboxylate group within the ligand. Further structure-activity studies using benzimidazol-2-one derivatives with an acetic acid moiety adjacent to a ring nitrogen revealed new insights into the importance of amide functionalities within the heterocycle for the affinity of antagonist glycine-site ligands.
Cascade coupling/cyclization process to N-substituted 1,3- dihydrobenzimidazol-2-ones
Assembly of N-substituted 1,3-dihydrobenzimidazol-2-ones is achieved starting from methyl o-haloarylcarbamates via a Cul/amino acid catalyzed coupling with amines and subsequent condensative cyclization. A number of functional groups are tolerated by thes
The corresponding N-mono and N,N'-dicarboxyalkylbenzimidazolin-2-ones were prepared by the reaction of the sodium salts of benzimidazolin-2-one and its 1,5,6-substituted derivatives with chloroacetic acid, acrylonitrile. and γ-butyrolactone.
Khalikov, S. S.,Kadyrov, Ch. Sh.,Ayupova, A. T.,Molchanov, L. V.
COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS
Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I'" or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
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(2017/03/14)
THIAZOLE DERIVATIVES AS CXCR3 RECEPTOR MODULATORS
The invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, which are antagonist of the CXCR3 chemokine receptor useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
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Page/Page column 116
(2008/06/13)
2-ARYLTHIAZOLE DERIVATIVES AS CXCR3 RECEPTOR MODULATORS
The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
Novel ramoplanin derivatives are disclosed. These ramoplanin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against gram positive bacteria, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.
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Page/Page column 67
(2010/11/23)
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists
A rapid analogue approach to identification of spirohydantoin-based CGRP antagonists provided novel, low molecular weight leads. Modification of these leads afforded a series of nanomolar benzimidazolinone-based CGRP receptor antagonists. The oral bioavai
Bell, Ian M.,Bednar, Rodney A.,Fay, John F.,Gallicchio, Steven N.,Hochman, Jerome H.,McMasters, Daniel R.,Miller-Stein, Cynthia,Moore, Eric L.,Mosser, Scott D.,Pudvah, Nicole T.,Quigley, Amy G.,Salvatore, Christopher A.,Stump, Craig A.,Theberge, Cory R.,Wong, Bradley K.,Zartman, C. Blair,Zhang, Xu-Fang,Kane, Stefanie A.,Graham, Samuel L.,Vacca, Joseph P.,Williams, Theresa M.
p. 6165 - 6169
(2007/10/03)
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