FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of imidazo[1,2a] thieno[2,3-d] -azepines of the formula (I) or their pharmaceutically acceptable addition salt or stereochemical isomer where each of dotted line means independently a possible (complementary) bond; R1 means hydrogen atom, C1-4-alkyl; R2 means hydrogen atom, C1-4-alkyl, C1-4-alkyl substituted with hydroxycarbonyl or C1-4-alkylhydroxycarbonyl; R3 means hydrogen atom, C1-4-alkyl; X means S-atom; L means hydrogen atom, C1-6-alkyl, C1-6-alkyl containing a substituent taken from a group including hydroxy-group, C1-4-alkylhydroxy-group, hydroxycarbonyl, C1-4-alkylhydroxycarbonyl, C1-4-alkylaminocarbonyl, C1-4-alkyl-hydroxycarbonylamino-group, C1-4-alkylhydroxycarbonyl-C1-4-alkylhydroxy-group, hydroxycarbonyl-C1-4-alkylhydroxy-group, C1-4-alkylaminocarbonylamino-group, C1-4-alkylaminocarbonyl- -amino-group, C1-4-alkylaminothiocarbonylamino-group, aryl and arylhydroxy-group; C3-6-alkenyl substituted with aryl where each aryl is phenyl or phenyl substituted with halogen atom, hydroxy-group, C1-4-alkylhydroxy-group or L means a radical of the formula -Alk-Y-Het1, -Alk-NH-CO-Het2 or -Alk-Het3 where Alk means C1-4-alkanediyl; Y means O-atom or NH; Het1 means pyrimidinyl; Het2 - furanyl; Het3 - pyrrolyl substituted with C1-4-alkylhydroxycarbonyl, pyridinyl, 4,5-dihydro-5-oxo-1H-tetrazolyl substituted with C1-4-alkyl, 2-oxo-3-oxazolidinyl, 2,3-dihydro-2-oxo-1H-benzimidazol-1-yl or radical of the formula (II) where A-Z means a group S-CH=CH, S-CH2-CH2, S-CH2-CH2-CH2, CH= CH-CH=CH. Compounds show an antiallergic activity. Invention describes also a method of synthesis of the above indicated compounds, pharmaceutical composition based on said and a method of preparing the composition for treatment of patients with allergic diseases. EFFECT: improved method of synthesis, antiallergic effect. 14 cl, 90 ex
Title |
Year |
Author |
Number |
IMIDAZOAZEPINE DERIVATIVE, PHARMACEUTICAL COMPOSITION, METHOD OF ITS PREPARING, METHOD OF SYNTHESIS OF IMIDAZOAZEPINE DERIVATIVE |
1994 |
- Frans Ehduard Zhansens
- Jozef Ehlizabet Lehnarts
|
RU2133249C1 |
DERIVATIVES OF TRIAZOLEBENZAZEPINE, METHODS OF THEIR SYNTHESIS, INTERMEDIATE COMPOUND FOR THEIR SYNTHESIS, PHARMACEUTICAL ANTIHISTAMINIC COMPOSITION AND METHOD OF ITS PREPARING |
1993 |
- Frans Ehduard Zhansen
- Zhan Fernan Arman Lakranpe
- Izabell' Noehll' Konstans Pilat
|
RU2126802C1 |
DERIVATIVES OF TRIAZOLO-(PYRROLO-, THIENO- OR FURANO)-AZEPINE ELICITING ANTIALLERGIC ACTIVITY, METHOD OF THEIR SYNTHESIS, INTERMEDIATE COMPOUND FOR THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND METHOD OF ITS PREPARING |
1993 |
- Frans Ehduard Zhansen
- Zhan Fernan Arman Lakranpe
- Izabell' Noehll' Konstans Pilat
|
RU2127737C1 |
DERIVATIVES OF PYRROLEQUINOLINONE, METHOD OF THEIR SYNTHESIS, INTERMEDIATE COMPOUNDS FOR THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND METHOD OF ITS PREPARING |
1994 |
- Ehddi Zhan Ehdgar Frejn
- Al'Fons German Margarita Rajmakers
|
RU2129554C1 |
N-SUBSTITUTED PIPERIDINYLBENZOATES, THEIR N-OXIDE FORMS, PHARMACEUTICALLY ACCEPTABLE SALTS OF ADDITIVE ACID SALTS AND STEREOCHEMICALLY ISOMERIC FORMS, METHODS OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND INTERMEDIATE SUBSTANCE |
1995 |
- Zhorzh Ehnri Pol' Van Dal'
- Zhan-Pol' Rene Mari Andre Bosmans
- Frans Marija Al'Fons Van Den Kejbus
|
RU2154064C2 |
ESTER DERIVATIVES OF 9-HYDROXY-PYRIDO[1,2-A]PYRIMIDINE-4-ONE, A METHOD OF THEIR SYNTHESIS, A COMPOSITION SHOWING ANTIPSYCHOTIC ACTIVITY AND A METHOD OF ITS PREPARING |
1994 |
- Jan Vandenberk
- Ljudo Ehdmon Zhozefin Kenni
|
RU2126406C1 |
METHOD OF SYNTHESIS OF DERIVATIVES OF N-(3-HYDROXY-4-PIPERIDINYL)-(DIHYDROBENZOFURAN, DIHYDRO-2H-BENZOPYRAN OR DIHYDROBENZODIOXINE)-CARBOXAMIDE, OR THEIR SALTS, OR THEIR STEREOCHEMICALLY ISOMERIC FORM |
1990 |
- Zhorzh Anri Pol' Van Del'[Be]
- Frans Marija Al'Fons Van Den Kejbus[Be]
|
RU2037492C1 |
DERIVATIVES OF SUBSTITUTED TETRACYCLIC AZEPINE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, INTERMEDIATE SUBSTANCE AND METHOD OF ITS SYNTHESIS |
1995 |
- Viktor Karel Sipido
- Frantsisko Khav'Er Fernandes-Gadea
- Khose Ignasio Andres-Khil
- Teo Frans Mert
- Pilar Khillopetegi
|
RU2163240C2 |
DERIVATIVES OF PHENYLOXOALKYL-(4-PIPERIDINYL)-BENZOATE, METHODS OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD OF ITS PREPARING AND INTERMEDIATE COMPOUND |
1995 |
- Zhorzh Ehnri Pol' Van Dal'
- Zhan-Pol' Rene Mari Andre Bosmans
- Mark Gustaf Selin Verdonk
|
RU2154634C2 |
DIMETHYLBENZOFURANS AND DIMETHYLBENZOPYRANES, THEIR USE AS 5-HT-ANTAGONISTS, METHODS OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION |
1993 |
- Zhorzh-Anri Pol' Van Dael'
- Zhan-Pol' Rene Mari Andre Bosman
- Uilli Dzhouns Karolus Van Laerovan
|
RU2116072C1 |