120572-43-2Relevant academic research and scientific papers
Fast and calibration free determination of first order reaction kinetics in API synthesis using in-situ ATR-FTIR
Rehbein, Moritz C.,Husmann, Sascha,Lechner, Christian,Kunick, Conrad,Scholl, Stephan
, p. 95 - 100 (2017/10/23)
In early stages of drug development only sparse amounts of the key substances are available, which is problematic for the determination of important process data like reaction kinetics. Therefore, it is important to perform experiments as economically as
BIARYL-CONTAINING COMPOUNDS AS INVERSE AGONISTS OF ROR-GAMMA RECEPTORS
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Paragraph 00319-00320, (2014/01/18)
The present invention relates to biaryl-containing inverse agonists of ROR-gamma receptors. The invention also provides pharmaceutical compositions comprising these biaryl- containing inverse agonists, and methods of modulating ROR-gamma receptors using these inverse agonists. Also provided are methods of using biaryl-containing inverse agonists to treat ROR-gamma mediated diseases.
N-CARBAMOYL NITROGEN-CONTAINING FUSED RING COMPOUNDS AND DRUGS CONTAINING THESE COMPOUNDS AS THE ACTIVE INGREDIENT
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Page 42, (2008/06/13)
The present invention relates to the compound presented by formula (I) (wherein all symbols in formula (I) are the same mean as the description shown in the specification.), mitocondorial benzogeazepin receptor (MBR) antagonist comprising the compound, the preventive and/or treatment medicine against diseases caused by stress of which an active ingredient is the compound. Since the compound represented by formula (I) has MBR antagonistic activity, and controls the production of neurosteroid, it is useful as the preventive and/or treatment medicine against diseases caused by stress.
Design and synthesis of 1,5- and 2,5-substituted tetrahydrobenzazepinones as novel potent and selective integrin αVβ3 antagonists
Kling, Andreas,Backfisch, Gisela,Delzer, Juergen,Geneste, Herve,Graef, Claudia,Hornberger, Wilfried,Lange, Udo E. W.,Lauterbach, Arnulf,Seitz, Werner,Subkowski, Thomas
, p. 1319 - 1341 (2007/10/03)
The design and synthesis of novel integrin αVβ3 antagonists based on a 1,5- or 2,5-substituted tetrahydrobenzaezpinone core is described. In vitro activity of respective compounds was determined via αVβ3 binding assay, and selected derivatives were submitted to further characterization in functional cellular assays. SAR was obtained by modification of the benzazepinone core, variation of the spacer linking guanidine moiety and core, and modification of the guanidine mimetic. These efforts led to the identification of novel αVβ3 inhibitors displaying potency in the subnanomolar range, selectivity versus αIIbβ3 and functional efficacy in relevant cellular assays. A method for the preparation of enantiomerically pure derivatives was developed, and respective enantiomers evaluated in vitro. Compounds 31 and 37 were assessed for metabolic stability, resorption in the Caco-2 assay and pharmacokinetics.
Reactions of Cyclic Anhydrides: Part XIII - Facile Synthesis of 1,2,3,4-Tetrahydro-10H-pyridazinoquinazoline-2,10-diones
Balasubramaniyan, V.,Argade, N. P.
, p. 906 - 908 (2007/10/02)
1,2,3,4-Tetrahydro-10H-pyridazinoquinazoline-2,10-diones have been prepared by hydrazinolysis of o-alkoxycarbonylsuccinanilic acids (IIIa-d), alkyl o-alkoxycarbonylsuccinanilates (IVa-f) or alkyl β-(4-oxo-3,1-benzoxazin-2-yl)propionates (Va,b) via
