20265-37-6Relevant articles and documents
Peptide thioacylation with high stereochemical preservation
Hoeg-Jensen, Thomas,Holm, Arne,Sorensen, Hilmer
, p. 383 - 387 (1996)
A dipeptide thioamide model system, Boc-Leu-ψ[CSNH]-Met-OMe, was used for evaluating the preservation of amino acid stereochemistry during thioacylation utilizing amino monothio acids. The LL and DL peptide diastereomers were separated by use of high performance capillary electrophoresis (micellar electrokinetic capillary chromatography). The described thioacylation method combines monothio acids with coupling reagents of the PyBOP-family for generating active thiono esters with low-levels of enantiomerisation ( 2%). The best results in terms of stereochemical preservation and yield were obtained with PyNOP, a 6-nitro analog of PyBOP. The successful activation of thiobenzoic acid with all four coupling reagents extended the scope of the method to include aryl monothio acids.
NOVEL COMPOUNDS FOR MODULATION OF ROR-GAMMA ACTIVITY
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Paragraph 00586, (2014/03/22)
The present invention relates to aryl sulfones and related compounds that are modulators of ROR-gamma receptors. The invention also provides pharmaceutical compositions comprising these modulators, and methods of modulating ROR-gamma receptors using them. Also provided are methods of using aryl sulfones and related compounds as modulators of ROR-gamma to treat ROR-gamma mediated diseases
THIENOPYRIMIDINE COMPOUNDS AND USE THEREOF
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Page/Page column 27, (2010/02/14)
The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1') a halogen, (2') a hydroxy group, (3') a C1-4 alkyl and (4') a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1') a halogen, (2') a C1-4 alkoxy-C1-4 alkyl, (3') a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4') a C1-4 alkoxy and (5') a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.