C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/240.1
C07D 243/16 (2006.01) A61K 31/395 (2006.01) C07D 245/06 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 491/04 (2006.01)
Patent
CA 1169425
ABSTRACT OF THE DISCLOSURE Novel 2-acylaminomethyl-1H-2,3-dihydro-1,4- benzodiazepine derivatives are disclosed which possess the Formula I Image (I) wherein R1 represents hydrogen, lower alkyl, lower alkenyl or cyclopropylmethyl, R2 represents hydrogen, lower alkyl or lower alkenyl; R3 represents a group of the formula a, b, c or d: Image or Image a b c d wherein R is hydrogen or C1-C3- alkyl; R4 is hydrogen, lower alkyl, lower alkoxy, nitro or halogen, and R4' is hydrogen or C1-C4-alkyl and the aromatic groups A and B may be unsubstituted or substituted by 1 to 3 substituents such as halogen, lower alkylthio, lower alkoxy, lower alkyl, hydroxy, nitro, trifluoromethyl or methylenedioxy or ethylenedioxy and optical isomers and acid addition salts of the compounds. In addition to psycho pharmacological, diuretic and antiarrhythmic properties, the novel compounds of Formula I possess primarily out- standing analgesic activities and are low in toxicity. The compounds are prepared by acylating 2-aminomethyl- 1,4-benzodiazepine derivatives with corresponding carbonic acid derivatives. Furthermore, 2-azidomethyl- 1,4-benzodiazepine derivatives are disclosed which provide valuable intermediates for the preparation of the compounds of Formula I yet also possess them- selves pharmacological activities.
367417
Liepmann Hans
Milkowski Wolfgang
Roemer Dietmar
Zeugner Horst
Solvay Pharmaceuticals Gmbh
Swabey Ogilvy Renault
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