Abstract: The present invention relates to adenosine A3 receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containings them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and (III) and to the preparation thereof.

Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.

Abstract: The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).

Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (I), within those preferably to the antagonists, including a salt, solvate or isomer (tautomer, desmotrop, and optically active isomer) thereof, to a pharmaceutical composition containing the ligand, to the use of the ligand, to its preparation, and intermediates of the ligand of the general formula (II?), (III?), (IV?), (V?), (VI?), (VII?), (VIII?) and (XIII?) and their preparation.

Abstract: Compounds of general formula (I), wherein R4 and R5 stand for hydrogen atom or form together an 1,3-butadienyl group, optionally substituted by a methylenedioxy group or one or more straight or branched C1-4 alkyl group, straight or branched C1-4 alkoxy group, hydroxy group or halogen atom; are strong adenosine A3 receptor ligands preferably antagonists.

Abstract: This invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Z, m, n, o, p and r are as defined herein, its preparation, pharmaceutical composition and use as an adenosine A3 receptor ligand preferably an antagonist.

Abstract: Heterocyclic amides useful as inhibitors of dipeptylpeptidase-IV (DPP-IV) enzyme, process for the preparation thereof and intermediates therefore.

Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.

Abstract: The present invention relates to adenosine A-3? receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and theirs salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and to the preparation thereof.

Abstract: The present invention relates to adenosine A3 receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containings them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and (heir salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and (III) and to the preparation thereof.

Abstract: Compounds of general formula (I), wherein R4 and R5 stand for hydrogen atom or form together an 1,3-butadienyl group, optionally substituted by a methylenedioxy group or one or more straight or branched C1-4 alkyl group, straight or branched C1-4 alkoxy group, hydroxy group or halogen atom; are strong adenosine A3 receptor ligands preferably antagonists.

Abstract: Orally active compounds of general formula (I) wherein R1 is methyl, ethyl or 2-morpholino-ethyl group, R2 is piperidino, morpholino or 4-methyl-piperazinyl group, n is 2 or 3 and their salts, solvates and hydrates.

Abstract: The present invention relates to new prolylendopeptidase inhibitors of general formula (I).

Abstract: A process for the preparation of condensed as-triazinium derivatives of the formula I ##STR1## and isomers thereof, wherein R.sub.1 inter alia is an alkyl group, R.sub.2 inter alia is hydrogen or an alkyl group and R.sub.3 is hydrogen and where Z is a group of the formula a or b ##STR2## which comprises reacting a compound of the formula II ##STR3## where Y is a group of the formula c or d ##STR4## with a compound of the formula IIaNH.sub.2 --CO--R.sub.2 (IIa)in the presence of a dehydrating agent. The advantage of the process is that it consists of fewer reaction steps and provides higher yields than the known methods. The compounds of formula I are pharmaceutically active known derivatives.

Abstract: The invention relates to new compounds of the general Formula I ##STR1## and isomers thereof wherein R.sub.1 is C.sub.1-10 alkyl, C.sub.3-6 cycloalkyl or phenyl, naphthyl or phenyl-(C.sub.1-4 alkyl), wherein the aryl ring of the three latter groups may optionally bear one or more halogen, nitro, trifluoromethyl, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s);R.sub.2 stands for hydrogen, halogen, hydroxy, oxo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or naphthyl, wherein the two latter groups may optionally bear one or more halogen, nitro, trifluoromethyl, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s);R.sub.3 represents hydrogen, hydroxy or C.sub.1-4 alkoxy;Z is buta-1,3-dienyl or a group of the general Formula (a) ##STR2## or (b) ##STR3## and X is hydrogen or halogen.The compounds of the general Formula I possess useful pharmacological properties, particularly antidepressant and antiarrhythmial effect.

Abstract: A one step process for the preparation of compounds having antidepressant activity of the formula I ##STR1## and isomers thereof, wherein R.sub.1, R.sub.2, Z and A.sup.- have the meanings indicated in the claims, which process comprises: heating a compound of the formula II ##STR2## wherein Z, A.sup.-, R.sub.1 and R.sub.2 have the meanings set out in the claims and R.sub.3 stands for hydrogen or C.sub.1-4 alkyl, in the presence of a dehydrating agent to split off a compound of the formula R.sub.3 OH. The invention is also directed to compounds of the formula I, wherein R.sub.2 is halogen and to compositions containing a compound of the formula I which exhibit antidepressant activity.

Abstract: The invention relates to new condensed as-triazine derivatives of the general Formula I ##STR1## and isomers thereof (wherein R.sub.1 stands for C.sub.1-10 alkyl or phenyl or naphthyl, wherein the two latter groups may be optionally substituted by one or more halogen, nitro, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s);R.sub.2 is hydrogen, C.sub.1-4 alkyl, hydroxy, halogen or phenyl or naphthyl, wherein the two latter groups may be optionally substituted by one or more halogen, nitro, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s);R.sub.3 represents hydrogen or C.sub.1-4 alkyl;Z is buta-1,3-dienyl or a group of the Formula (a) ##STR2## and A.sup.- is an anion).The compounds of the general Formula I possess useful pharmacological properties, particularly antiarrhythmial and antidepressant effect.

Abstract: The invention relates to new condensed as-triazine derivatives of the general formula (I) ##STR1## wherein Z represents a buta-1,3-dienyl group or a group of the formula (a), (b), (c) or (d) ##STR2## R.sub.1 denotes a C.sub.1-10 alkyl group, an oxo group or a C.sub.6-10 aryl or C.sub.6-10 aryl-(C.sub.1-3 alkyl) group optionally substituted by one or more identical or different substituents selected from the group consisting of amino, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy and halogen,R.sub.2 stands for hydrogen, C.sub.1-10 alkyl or amino,R.sub.3 represents hydrogen, C.sub.1-10 alkyl or C.sub.6-10 aryl or C.sub.6-10 aryl-(C.sub.1-3 alkyl) optionally substituted by one or more identical or different substituents selected from the group consisting of nitro, amino, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy and halogen,X.sup.- denotes an anion, andn is 0 or 1,with the proviso that if n is O, R.sub.1 is other than an oxo group and R.sub.1 ' and R.sub.

Abstract: The invention relates to new pyrido[3,2-e]-as-triazine derivatives of the formula I and pharmaceutically acceptable acid addition salts thereof, ##STR1## wherein R.sub.1 stands for a C.sub.1-20 alkyl-carbonyl group, halogen-C.sub.1-4 alkyl-carbonyl, benzoyl, phenyl-C.sub.1-4 alkyl-carbonyl, or pyridyl-carbonyl group;R.sub.2 is a hydrogen atom or a C.sub.1-4 alkyl-carbonyl group; or R.sub.1 and R.sub.2 form together with the adjacent nitrogen atoms a pyrazole-2,4-dione ring which carries a C.sub.1-6 alkyl substituent in position 3;R.sub.3 is a hydrogen atom, a C.sub.1-20 alkyl, phenyl, phenyl-C.sub.1-3 alkyl, furyl or pyridyl group or a phenyl group optionally substituted by one to three C.sub.1-4 alkoxy-groups.The compounds of the formula I are prepared by acylating the respective 1,2-un-substituted 1,2-dihydropyrido [3,2-e]-as-triazine derivatives. The new compounds exert valuable effects on the central nervous system and possess analgesic, antiphlogistic effects, and can be applied to advantage in therapy.