- Synthesis and structure-activity relationships of 4-oxo-1-phenyl- 3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: Novel PDE4 inhibitors
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A novel series of benzodiazepine derivatives have been discovered as inhibitors of PDE4 enzymes. We have found that our compounds are selective versus other PDE enzymes, and that the activity can be modulated by specific structural modifications. One compound exhibited a strong eosinophilic infiltration inhibiting action on sensitized Brown-Norway rats (compound 9, 5.1 mg/kg p.o.), moreover this compound is not emetic at 3 mg/kg i.v.
- Pascal, Yves,Andrianjara, Charles R.,Auclair, Eric,Avenel, Nadine,Bertin, Bernadette,Calvet, Alain,Feru, Frederic,Lardon, Sophie,Moodley, Indres,Ouagued, Malika,Payne, Adrian,Pruniaux, Marie-Pierre,Szilagyi, Corinne
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- Benzodiazepines, process and intermediates for the preparation thereof and their application in therapy
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Benzodiazepines of formula STR1 in which R1 is H of halogen, R2 is H or halogen, Ar is indolyl, phenyl, naphthyl, indolyl monosubstituted with a halogen or with a methoxy or phenyl mono-, di- or trisubstituted with a halogen or with
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