Abstract: 4-oxo-4H-pyrido[1,2-a]-pyrimidines are disclosed of the formula ##STR1## wherein R is a C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-7 cycloalkyl, --(CH.sub.2).sub.n --COOR.sup.3 wherein R.sup.3 is C.sub.1 to C.sub.4 alkyl and n is 0 or 1 or a C.sub.7-8 aralkyl group, optionally substituted by one or more halogen atom(s), or by a nitro-group, R.sup.1 is a hydrogen atom or a C.sub.1-4 alkyl group, and salts thereof, as well as a process for their preparation, and pharmaceutical compositions containing them. These compounds are therapeutically useful as gastroprotectives in the treatment and prevention of ulcer.

Abstract: The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 represents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.

Abstract: The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 represents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.

Abstract: The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine -3-carbonamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## wherein: R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 repesents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.

Abstract: The invention relates to novel diphenylpropylamine derivatives of the general formula (I). ##STR1## R.sup.1 stands for hydrogen or a methyl group; R.sup.2 stands for hydrogen, a methyl or n-decyl group;Z means a phenyl group substituted by R.sup.3, R.sup.4 and R.sup.5, whereinR.sup.3 means hydrogen, fluorine, chlorine or bromine, or a nitro, C.sub.1-12 alkyl, C.sub.1-4 alkoxy, phenoxy or benzyloxy group;R.sup.4 and R.sup.5 represent hydrogen, chlorine or a hydroxy, alkoxy, benzyloxy, acetamino or carboxy group; orR.sup.4 and R.sup.5 together form a methylendioxy group;orZ may stand for a 4-methoxynaphtyl or 4-ethoxy-naphthyl group; andR.sup.6 stands for hydrogen or fluorine, with the proviso that each of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 cannot simultaneously stand for hydrogen, as well as their physiologically acceptable acid addition salts.The invention also relates to a process for the preparation of these compounds and to the pharmaceutical compositions containing these compounds.

Abstract: The invention relates to new oxidiazole-alkyl-purine-derivatives of the Formula I ##STR1## and pharmaceutically acceptable salts thereof wherein A stands for C.sub.1-4 alkylene andR.sup.1 represents C.sub.1-6 alkyl, hydroxyalkyl, halogenoalkyl, carboxyalkyl, C.sub.5-6 cycloalkyl or aminoalkyl of the Formula --(CH.sub.2).sub.n --NR.sup.2 R.sup.3 in which group n is an integer 1-3; R.sup.2 and R.sup.3 each stand for hydrogen or C.sub.1-4 alkyl or together with the adjacent nitrogen atom they are attached to form a 5- or 6-membered nitrogen containing heterocyclic ring which may optionally comprise a further nitrogen atom or an oxygen atom as heteroatom; orR.sup.1 stands for phenyl, hydroxyphenyl, carboxyphenyl, benzyl or dimethoxybenzylThe compounds of the Formula I can be prepared by methods known per se and can be used in therapy as antitussive agents.

Abstract: Pyridazinylhydrazones capable of lowering blood pressure have the formula ##STR1## wherein R.sup.1 is hydrogen, chlorine, alkyl having from 1 to 4 carbon atoms, methoxy, hydroxyl, carbamoyl or cyano;R.sup.2 is chloro; andK is a group having the formula ##STR2## wherein one of R.sup.3, R.sup.4, R.sup.5 or R.sup.6 is carboxyl or alkoxycarbonyl.

Abstract: The invention relates to new ergol-8-ene and ergoline derivatives of the general formula /I/ ##STR1## wherein x y stands for --CH.dbd.C.dbd. or --CH.sub.2 --CH.dbd. group,R stands for hydrogen atom or methyl group,R.sub.1 stands for hydrogen or halogen atom,R.sub.2 stands for lower alkylsulfonyloxy group, phenylsulfonyloxy group optionally substituted with a lower alkyl group, or azido group,R.sub.3 stands for lower alkylsulfonyloxy group or phenylsulfonyloxy group optionally substituted with a lower alkyl group, and acid addition salts thereof. These compounds can be prepared from compounds of the general formula II ##STR2## wherein x y and R are as defined above, by reacting at least two equivalents of a lower alkylsulfonic acid chloride or phenylsulfonic acid chloride substituted with lower alkyl group.

Abstract: A pharmaceutical compositions with hypotensive effects which comprise a compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof, ##STR1## wherein R.sup.1 is formula (II) ##STR2## wherein R.sup.4 and R.sup.5 each represent hydrogen, hydroxy, nitro at the same timeR.sup.2 and R.sup.3 are hydrogen, orR.sup.1 are 3-chloro-6-pyridazinylamino, 3-methyl-6-pyridazinylamino or 3-carbamoyl-6-pyridazinylamino, and at the same timeR.sup.2 and R.sup.3 form together formula (III), ##STR3## wherein R.sup.6 is C.sub.1-4 alkyl group,R.sup.7 is hydrogen or a C.sub.1-4 alkyl group, andn is an integer of 1 to 3, orR.sup.2 and R.sup.3 form together a group of the general formula (IV),=Q-R.sup.8 (IV)whereinQ is C.sub.5-7 cycloaliphatic, andR.sup.8 is hydrogen, a C.sub.1-4 alkoxycarbonyl or a C.sub.2-4 alkyl,and a compound of formula (V) or a pharmaceutically acceptable acid addition salt thereof, ##STR4## wherein R.sup.9 is naphthyl, 4-indolyl or 4-morpholino-1,2,5-thiadiazol-3-yl group or ##STR5## .

Abstract: Pyridazinylhydrazones capable of lowering blood pressure having the formula ##STR1## wherein R.sup.1 is hydrogen, chlorine, alkyl having from 1 to 4 carbon atoms, methoxy, hydroxyl, carbamoyl or cyano;R.sup.2 is morpholino; andK is a group having the formula ##STR2## wherein one of R.sup.3, R.sup.4, R.sup.5 or R.sup.6 is carboxyl or alkoxycarbonyl.

Abstract: 3-(1-Pyrazolyl)-pyridazine derivatives of the formula I, or pharmaceutically acceptable acid addition salts thereof, which decrease high blood pressure and inhibit catabolism or prostaglandins, ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl,R.sup.2 is hydrogen, cyano, carboxyl, carbamoyl, carbaxoyl or C.sub.1-4 alkoxycarbonyl,R.sup.3 is hydrogen or chlorine or --NR.sup.4 NHR.sup.5 or NR.sup.6 R.sup.7, wherein R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl, wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-5 alkyl, C.sub.1-5 hydroxyalkyl, C.sub.3-7 cycloalkyl, phenyl or benzyl, or benzyl or phenylethyl substituted with one or two chlorine atoms or methoxy groups, or a furylmethyl, pyridylmethyl, pyrrolidine or piperazine ring, or when R.sup.7 is hydrogen, R.sup.6 is --(CH.sub.2).sub.n --NR.sup.4 R.sup.5 wherein n is an integer from 1 to 3.

Abstract: The invention relates to new 8.beta.-hydrazinomethyl-ergoline derivatives of the general formula (I), ##STR1## wherein x y stands for a ##STR2## or ##STR3## group, R stands for hydrogen or methyl group, andR.sub.1 stands for hydrogen, a lower acyl group, a di-(lower-alkylaminocarbonyl group, a group of the general formula (VI), ##STR4## wherein Z.sub.1, Z.sub.2 and Z.sub.3 each represent hydrogen, halogen or a trifluoromethyl group, or a group of the general formula (VII), ##STR5## wherein Y represents a lower alkyl group, allyl group or phenyl group, and acid addition salts thereof. These compounds possess valuable antiserotonine, antidepressant and hypotensive effects, furthermore they can be applied as starting substances in the preparation of other biologically active ergoline derivatives.The new compounds of the general formula (I) are prepared according to the invention by reacting the respective 6-methyl-8.beta.-mesyloxymethyl or -tosyloxymethyl-ergoline derivatives with dry hydrazine.

Abstract: The invention relates to compounds of general formula ##STR1## wherein R.sup.1 stands for a hydrogen atom or a C.sub.1-6 alkyl-, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group,R.sup.2 stands for a hydrogen, fluorine, chlorine or bromine atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a nitro or an --NR.sup.5 R.sup.6 group, wherein R.sup.5 and R.sup.6 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl or a C.sub.2-4 hydroxyalkyl group,R.sup.3 stands for a hydrogen atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group, a chlorine atom or a hydroxyl, amino or methoxy group,R.sup.4 stands for a carbamoyl, a cyano or an --NR.sup.7 --NHR.sup.8 group, wherein R.sup.7 and R.sup.8 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.1-4 alkoxycarbonyl or an --NR.sup.9 R.sup.10 group, wherein R.sup.9 and R.sup.

Abstract: 9,10-Dihydrolysergic acid-(3'-/pyrrolid-2"-on-1'-yl/-propyl)-amide, 1-methyl-9,10-dihydrolysergic acid-(thiazoline-2'-yl)-amide and lysergic acid-(3'-allyloxy-2'-oxy-propyl)-amide and their pharmaceutically acceptable acid addition salts possess antihypertensive and antiserotonin effect and exert an action on the central nervous system.

Abstract: 1-Benzal-1,2,3,4-tetrahydro-isoquinolinium-theophylline-7-acetates are used in the manufacture of geriatric compositions.

Abstract: An anti-inflammatory analgesic pharmaceutical composition comprising as active ingredient a compound of the formula I ##SPC1##whereinR is a phenyl, chlorophenyl, naphthyl, pyrole, furane, furazole, thiazole, thiadiazole or pyridine group;R.sup.1 is hydrogen or alkyl having 1 to 7 carbon atoms;R.sup.2 is hydrogen, alkyl having 1 to 7 carbon atoms, alkoxy having 1 to 7 carbon atoms or dialkylamino having 1 to 7 carbon atoms per alkyl group in admixture with a pharmaceutical carrier.