- Fast and calibration free determination of first order reaction kinetics in API synthesis using in-situ ATR-FTIR
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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
- Rehbein, Moritz C.,Husmann, Sascha,Lechner, Christian,Kunick, Conrad,Scholl, Stephan
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- PLANT GROWTH REGULATION
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The present invention relates to a new class of plant growth regulators. In particular, the invention relates to fused azepinone derivative of general formula (I) or an agriculturally acceptable salt thereof wherein X is CO2R2 or H;
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Page/Page column 27
(2008/06/13)
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- N-CARBAMOYL NITROGEN-CONTAINING FUSED RING COMPOUNDS AND DRUGS CONTAINING THESE COMPOUNDS AS THE ACTIVE INGREDIENT
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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.
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- TUMOUR-INHIBITING ANNELLATED AZEPINONE DERIVATIVES
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The invention relates to annellated azepinone derivatives, to a method for the production thereof, to metal complexes of the annellated azepinone derivatives, and to the use of the same for treating tumour diseases.
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Page/Page column 17
(2010/02/07)
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- Substituted imidazo [1,5-a] pyrimido [5,4-d] [1] benzazepine derivatives
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The present invention is a compound of formula wherein R1 is halogen or lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, —(CH2)m-phenyl, wherein the phenyl ring may be substituted by lower alkoxy, or is —(CH2)m-indolyl; R3 is —C(O)O-lower alkyl, —C(O)OH, or a five membered heteroaromatic group, which rings may be substituted by lower alkyl or cycloalkyl; n is 0, 1 or 2; m is 0, 1 or 2; or a pharmaceutically acceptable acid addition salt thereof. Compound I shows high affinity and selectivity for GALA A α5 receptor binding sites.
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- Design and synthesis of 1,5- and 2,5-substituted tetrahydrobenzazepinones as novel potent and selective integrin αVβ3 antagonists
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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.
- Kling, Andreas,Backfisch, Gisela,Delzer, Juergen,Geneste, Herve,Graef, Claudia,Hornberger, Wilfried,Lange, Udo E. W.,Lauterbach, Arnulf,Seitz, Werner,Subkowski, Thomas
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p. 1319 - 1341
(2007/10/03)
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