TRIAZOLO (4,3-a) 1,4 BENZO DIAZEPINES AND THRENO (3,2 Russian patent published in 1997 - IPC

f) (1,2,4) TRIAZOLO (4.3-a) DIAZEPINES IN CASE OF PRESENCE OF AT LEAST ONE ASYMMETRIC CENTER, ENANTIOMERS, RACEMATES AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, METHOD OF PREPARATION THEREON, AND PHARMACEUTICAL COMPOSITION INHIBITING THROMBOCYTE ACTIVATION FACTOR. FIELD: pharmaceutical industry. SUBSTANCE: present invention describes new triazolo [4,3- a] [1,4] benzodiazepines or thieno [3,2-f] [1,2,4] triazolo [4,3-a] diazepines of general formula I: wherein X is -CH=CH- or S; R₁ is lower alkyl or trifluoromethyl; R₂ is theorine or fluorine; R₃ is radical of formula: R₄-(CH₂)_n-C≡C- or R₅-O-CH₂-C≡C- in which n is integer of 0.1 or 2; s is 0 or 1; R₄ is phenyl or mono-, di- or tricyclic 5-6 membered heterocyclic radical containing O or S as heteroatoms and/or nitrogen atoms unsubstituted or substituted by lower alkoxy, oxo, oxy group or chlorine; R₅ is phenyl or pyridyl provided that when is 0, R₄ should be attached to carbon bond through carbon and R₅ is always attached to oxygen bond through carbon and if at least one ASYMMETRIC center is present, said radical is attached to enantiomers, racemates and pharmaceutically acceptable acid addition salts thereof which exhibit properties of thrombocyte activation factor antagonists and respectively having antiprotector, immunological and antishock properties as well as properties that inhibit/of the organs to be transplanted, and pharmcompositions based thereon. Present invention also describes compounds of formula I in which R₃ C=CH. Compounds of formula I or pharmaceutically acceptable acid addition salts thereof are prepared by reaction of compound of formula II with compound of formula: C≡CH. is which R₄-Y is as defined in claim 1, and Y is bromine or iodine, and optionally for preparation compound of formula I in which s is 1 and R₄ is other than residue containing main nitrogen atom, the compound of formula I in which s is O and R₄ is other than residue containing main nitrogen atom, peracid and/or the resulting compound of formula I is optionally transformed into pharmaceutically acceptable acid addition salt thereof. EFFECT: improved properties of the title compounds. 18 cl, 7 tbl