Egis Gyogyszergyar Rt.

Geza Szabo

Gyula Simig

Gabor Gigler

Jozsef Barkoczy

Gabor Blasko

Andras Egyed

Istvan Ling

Karoly Tihanyi

Szabolcs Kertesz

Laszlo Gabor Harsing

Zoltan Ratkai

Gyula Szücs

Bernadett Martonné Marko

György Levay

Annamaria Simo

The invention relates to new 8-chloro-2,3-benzodiazepine derivatives of the general formula (I), wherein R stands for a lower alkyl group or a group of the general formula &#x2014;NH&#x2014;R', wherein R&#x2032; stands for a lower alkyl or a lower cycloalkyl group), and pharmaceutically acceptable acid addition salts thereof. The invention also encompasses a process for the preparation of said compounds, pharmaceutical compositions containing them and new intermediates useful for the preparation of the new 8-chloro-2,3-benzodiazepine derivatives. The compounds according to the invention possess AMPA/kainate receptor inhibiting activity. 

8-chloro-2,3-benzodiazepine derivatives

The invention relates to new 2,3-benzodiazepine derivatives of general Formula (I), (wherein Rstands for methyl, formyl, carboxy, cyano, &#x2014;CH&#x2550;NOH, &#x2014;CH&#x2550;NNHCONHor &#x2014;NRR, wherein Rand Rindependently from each other represent hydrogen or lower alkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); Ris nitro or amino; Rstands for hydrogen, lower alkanoyl or CO&#x2014;NRR, wherein Rand Rindependently from each other stand for hydrogen, lower alkoxy, lower alkyl or lower cycloalkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); Ris hydrogen or lower alkyl; the dotted lines have the following meaning: if Rand Rare not present, the bond between positions Cand Cis a single bond and the bond between positions Cand Nis a double bond; if Rand Rare present, the bonds between positions Cand Cand between position Cand Nare single bonds; and if Ris present and Ris missing, the bond between positions Cand Cis a double bond and the bond between positions Cand Nis a single bond) and salts thereof. The invention compounds have neuroprotective effect.

2,3-benzodiazepine derivatives

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Budapest, Hungary

Geza Szabo