954239-15-7Relevant academic research and scientific papers
PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
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, (2020/11/23)
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X-Y is -NHSO2- or -SO2NH-; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one ormore substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, C land alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl,Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl andhaloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl,SO2NR12R13, heteroaryl, CONR10R11 and alkyl, wherein said heteroaryl group is optionallysubstituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; and R9 is H, alkyl or halo; R10 and R11 are each independently H or alkyl; and R12 and R13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno- oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).
Synthesis of 2-Alkoxy/Thioalkoxy Benzo[d]imidazoles and 2-Thione Benzo[d]imidazoles via a Phase-Based, Chemoselective Reaction
Yoon, Hyo-Jeong,Yang, Seung-Ju,Gong, Young-Dae
supporting information, p. 738 - 747 (2017/12/18)
2-Alkoxy/thioalkoxy benzo-[d]-imidazole and 2-thione benzo-[d]-imidazole libraries were constructed in solution phase and on solid phase, respectively. The key step in this work is the phase-based chemoselective reaction of the 2-mercaptobenzo-[d]-imidazole intermediate with benzyl chloride (solution phase) and Merrifield resin (solid phase). In the solution-phase case, benzyl chloride reacted with the thiol group of 2-mercaptobenzo-[d]-imidazole, whereas in the solid-phase case, Merrifield resin was introduced at an internal amine group of benzo-[d]-imidazole. To afford the desired 2-alkoxy/thioalkoxy benzo-[d]-imidazole analogues, we used various alkyl halides, alcohols, and thiols in solution phase, and to obtain 2-thione benzo-[d]-imidazole derivatives on solid phase, we used diverse alkyl halides and boronic acids. Finally, to measure the drug potential to be orally active and the molecular diversity in three-dimensional (3D) space, we calculated physicochemical properties and displayed energy-minimized 3D structures. As a result, the libraries from solution phase and solid phase show distinct features in physicochemical properties and skeletal diversities in 3D space.
METABOTROPIC GLUTAMATE RECEPTOR NEGATIVE ALLOSTERIC MODULATORS (NAMS) AND USES THEREOF
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, (2016/01/01)
Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.
NOVEL BENZODIAZEPINONES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR FUNCTIONS AND NEUROLOGICAL USES THEREOF
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Paragraph 0133; 0134; 0135, (2013/03/28)
The present invention relates to novel benzodiazepinone compounds of Formulae (I) wherein R1, R2, R4, R6, R7, R8, R9, and R10 are as defined herein. The invention also
Synthesis, characterization and antibacterial evaluation of few 2, 3-substituted quinoxalines
Reddy, B. Jayachandra,Reddy, M.C. Somasekhara
, p. 483 - 485 (2011/12/02)
The quinoxaline derivatives (i-v) were synthesized through cyclization-oxidation of α- bromo carbonyl compounds with o-phenyl diamines (7a and 10a) and further coupling at 6-position via Suzuki reaction using PdCl2 (dppf).DCM, ter. BuNH2, Na2CO 3 in IPA, H2O refluxed for 16 h. As the results of antibacterial screening tests done by paper disc method, quinoxaline derivatives (i) and (v) revealed significant inhibition zone on Bacillus spericus and quinoxaline derivatives (iii) and (v) on Escherichia coli cultures.
Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides
Bressi, Jerome C.,Jennings, Andy J.,Skene, Robert,Wu, Yiqin,Melkus, Robert,Jong, Ron De,O'Connell, Shawn,Grimshaw, Charles E.,Navre, Marc,Gangloff, Anthony R.
scheme or table, p. 3142 - 3145 (2010/08/22)
A series of N-(2-amino-5-substituted phenyl)benzamides (3-21) were designed, synthesized and evaluated for their inhibition of HDAC2 and their cytotoxicity in HCT116 cancer cells. Multiple compounds from this series demonstrated time-dependent binding kin
BENZIMIDAZOLE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, THEIR USE AS FXR AGONISTS AND PHARMACEUTICAL PREPARATIONS CONTAINING THE SAME
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Page/Page column 119, (2008/06/13)
The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind
