80452-55-7Relevant academic research and scientific papers
A facile synthesis of 1,3,4,6-tetrahydro-1,6-benzodiazocine-2,5-diones
Jarikote,Pawar,Bhusare,Hangarge,Vibhute,Pawar
, p. 575 - 577 (2004)
1,3,4,6-Tetrahydro-1,6-benzodiazocine-2,5-diones were synthesized from 3,4-dihydro-1H-benzaze-pine-2,5-diones through the corresponding oximes using simple reagents and procedures.
LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
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Page/Page column 310, (2008/06/13)
The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
Substituted imidazo [1,5-a] pyrimido [5,4-d] [1] benzazepine derivatives
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, (2008/06/13)
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.
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.
Synthesis of 7-phenylpyrimido[5,4-d][1]benzazepin-2-ones
Chen,Gilman
, p. 663 - 666 (2007/10/02)
The syntheses of the 7-phenylpyrimido[5,4-d][1]benzazepin-2-ones 3, 4, and 5 are described. The 7-phenyl group was introduced by phenylation of the lactam nitrogen in 10, 13 and 16 respectively. One of these compounds, 5, showed moderate activity as a CNS agent.
BENZOCONDENSED HEPTAATOMIC HETEROCYCLES AND THEIR DERIVATIVES. VII. SYNTHESIS OF BENZAZEPINES AND BENZAZEPINONES ANALOGUES OF KNOWN ANXIOLYTIC DRUGS
Rossi, Silvano,Micheli, Marcello,Giannotti, Michele,Salvatori, Americo,Peruzzi, Guidubaldo
, p. 365 - 370 (2007/10/02)
Two syntheses are described for a series of benzazepines structurally similar to known anxiolytic drugs.Some of the new molecules are active in the barbiturates-induced sleep potentiation test and possess a negligible acute toxicity.
