FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel derivatives of 1-[2-(substituted vinyl)]-5H-2,3-benzodiazepine, method of their synthesis, pharmaceutical composition, method of its preparing and method of treatment of patients with diseases of the central nervous system. Compounds have the general formula (I) where A and B in common form the group of the formula =C=N or =CH-NH-; R1 means phenyl that can has from 2 to 3 hydroxyl groups or from 1 to 3 similar or different substituents taken among the group including halogen atom, trifluoromethyl-, nitro-, cyano-, amino-group, (C1-3alkyl)amino-, C1-4alkanoylamino-, C1-4alkyl, C1-4-alkoxy-group, carboxyl, (C1-4-alkoxy)-carbonyl, methylenedioxyl-group, naphthyl that can has substituent as hydroxyl, furyl, thienyl or indolyl; R2 means hydrogen atom or C1-4alkyl; R3 and R4 each means C1-4alkoxy-group bound at position 7 or 8 of benzodiazepine ring, or R3 and R4 in common form 7,8- or 8,9-methylenedioxyl group, and their pharmaceutically acceptable acid addition salts. Compounds show significant activity with respect to the central nervous system. EFFECT: new compounds indicated above, improved method of synthesis, valuable medicinal properties. 9 cl, 10 tbl, 98 ex
Title | Year | Author | Number |
---|---|---|---|
DERIVATIVES OF 1-[2-(SUBSTITUTED VINYL)]-3,4-DIHYDRO-5H-2,3-BENZODIAZEPINE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF PREPARING PHARMACEUTICAL COMPOSITION AND METHOD OF SUPPRESSION OF CONVULSIONS | 1996 |
|
RU2155757C2 |
DERIVATIVES OF 2,3-BENZODIAZEPINE, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD FOR TREATMENT | 2000 |
|
RU2243228C2 |
3-SUBSTITUTED DERIVATIVES OF 3H-2,3-BENZODIAZEPINE, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION | 1995 |
|
RU2146678C1 |
DERIVATIVES OF 1,3-DIOXOL[4,5-H][2,3]BENZODIAZEPINE AS INHIBITORS OF AMPA/KAINATE RECEPTOR, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD OF TREATMENT | 1998 |
|
RU2208014C2 |
METHOD OF PRODUCING DERIVATIVES OF 1-(HYDROXYSTYRIL)-5N-2,3-BENZODIAZEPINE | 0 |
|
SU1503681A3 |
DERIVATIVES OF N-ACYL-2,3-BENZODIAZEPINE, OR THEIR STEREOISOMERS, OR ACID ADDITIVE SALTS HAVING BIOLOGICAL ACTIVITY CONNECTED WITH AFFECTION UPON CENTRAL NERVOUS SYSTEM AND PHARMACOLOGICAL ACTIVE COMPOSITION ON THEIR BASE | 1991 |
|
RU2102387C1 |
DERIVATIVES OF 8-SUBSTITUTED=9H-1,3-DIOXOL[4,5-H][2,3]- BENZODIAZEPINE AS INHIBITORS OF AMPA/KAINATE RECEPTOR, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD OF TREATMENT | 1998 |
|
RU2208013C2 |
DERIVATIVES OF 2,3-BENZODIAZEPINE, INTERMEDIATE COMPOUNDS FOR THEIR SYNTHESIS AND AGENT ELICITING INHIBITORY ACTIVITY WITH RESPECT TO AMPA-RECEPTORS | 1997 |
|
RU2179557C2 |
DERIVATIVES OF PIPERAZINYLALKYLTHIOPYRIMIDINE, PHARMACEUTICAL COMPOSITION CONTAINING THEREOF AND METHOD FOR PREPARING | 2000 |
|
RU2245334C2 |
DERIVATIVES OF 2-(1,2,4-TRIAZOLE-1-YL)-1,3,4-THIADIAZOLE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND INTERMEDIATE COMPOUND | 1998 |
|
RU2180903C2 |
Authors
Dates
2001-01-10—Published
1996-02-08—Filed