Patent RU-2245883-C2 (RU)
Inventor: LIBERATOR ANN-MARI
IPC: A61K31/55
Filed: 2000-04-07
Granted: 2005-02-10
Abstract: FIELD: organic chemistry, chemical technology, pharmacy. 
     SUBSTANCE: invention relates to new biologically active derivatives of pyridothienodiazepine. Invention describes derivatives of pyridothienodiazepine of the general formula (I): 
        as a racemate or in form of enantiomers or diastereomers, or their mixture wherein R 1  represents hydrogen atom or radical of the formula: R' 1 -NH-C(Y)- wherein R' represents phenyl radical optionally substituted with one or more similar or different substitutes taken among lower alkyl, lower alkoxy-group, lower alkylthio-group, lower alkoxycarbonyl, lower alkylsulfonyl, halogen atom, trifluoromethyl, trifluoromethyloxy-group, hydroxy-, nitro-, cyano-group, phenyl, phenoxy-group, cycloalkyl or heterocycloalkyl; R 2  represents lower alkyl, trifluoromethyl or phenyl radical optionally substituted with one or more similar or different substitutes taken among hydroxy-group, halogen atom, lower alkyl or lower alkoxy-group; X and Y represent independently oxygen (O) or sulfur (S) atom; R 3a  represents hydrogen atom, lower alkyl, hydroxy-group or radical of the formula -OC(O)R' 3a  wherein R' 3a  represents alkyl radical comprising from 1 to 10 carbon atoms optionally substituted with radical of the formula: NR'' 3a R''' 3a  wherein NR'' 3a  and R''' 3a  represent independently hydrogen atom, lower alkyl, phenyl, lower phenylalkyl, alkylcarbonyl or alkoxycarbonyl; R 3b  represents hydrogen atom or lower alkyl radical; R 4  represents radical of the formula: -(CH 2 ) n -CHR' 4 R'' 4  wherein n represents a whole number 0, 1, 2, 3, 4, 5 or 6; R' 4  and R'' 4  represent independently hydrogen atom, lower alkyl, cycloalkyl, lower cycloalkylalkyl, phenyl, pyridyl, phenylcarbonyl or adamantyl wherein indicated radicals are substituted optionally with one or more similar or different substitutes taken among hydroxy-group, halogen atom, trifluoromethyl, lower alkyl or lower alkoxy-group; A----B represents -C=N- or -C-N(R 5 )- wherein R 5  represents hydrogen atom, amino-radical, lower alkylamino-group, di-(lower alkyl)-amino-group, cycloalkyl, heterocycloalkyl, guanidyl optionally substituted with nitro- or cyano-group, phenyl optionally substituted with one or more similar or different substitutes taken among alkyl or alkoxyalkyl wherein indicated alkyl or alkoxyalkyl are substituted optionally with oxy- or amino-group; indolyl or radical of the formula: -NH-C(O)-(CH 2 ) c -NH-C(O)(CH 2 ) d -NH 2 ; p represents a whole number 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; c and d represent independently a whole number 0, 1, 2 or 3; or salts of these compounds. Also, invention describes methods for preparing compounds of the general formula (I), pharmaceutical composition based on compounds of the general formula (I) eliciting activity to inhibit binding somatostatin-14 and an intermediate compound of the formula (2) given in the invention description. Invention provides preparing new compounds eliciting useful biological properties. 
     EFFECT: improved preparing method, valuable medicinal properties of compounds. 
     17 cl, 70 ex