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: A method of using a compound of the Formula (V) ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, wherein R.sup.1 and R.sup.2 are each C.sub.1 to C.sub.6 aliphatic acyloxy, unsubstituted or substituted by halogen, or are each C.sub.7 to C.sub.

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 a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.

Abstract: A new method of treatment is disclosed for a vascular obstructive lesion resulting from restricted blood circulation, characterized by an erythrocyte pathology, in an effected animal subject. The new method involves the administration of 1-(3',4'-diethoxybenzyl)-6,7-diethoxy-3,4-dihydroisoquinolinium-theophylli ne-7-acetat e, in a dosage and at a rate sufficient to maintain a blood concentration of at least 0.5 to at most 3 .gamma./ml, calculated on the basis of 1-(3',4'-diethoxybenzyl)-6,7-diethoxy-3,4-dihydroisoquinoline.

Abstract: N,N,N-trimethyl-2-hydroxyethyl-ammonium-[1-ethyl-6-fluoro-4-oxo-7-(1-pipera zinyl)-1,4-dihydro-quinolizine-3-carboxylate] of the formula I ##STR1## as a norfloxacin antimicrobial salt capable of enteral administration.

Abstract: The invention relates to a process for the restoration and prevention of gastrointestinal injuries, which comprises treating a patient with an effective dose of racemic or optically active 1,6-dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrimido[1,2-a]pyrimidine-3-c arboxamide.

Abstract: The invention relates to new azepino[1,2-a]pyrimidine derivatives--of the general formula ##STR1## wherein p=1, 2 and acid addition salts thereof which can be prepared by(a) reacting a compound of the formula ##STR2## with a compound of the general formula ##STR3## wherein p is as defined above and R.sup.7 is alkoxycarbonyl containing 2 to 5 carbon atoms or carboxamido or(b) reacting a compound of the general formula ##STR4## wherein R.sup.8 is alkyl containing 1 to 4 carbon atoms with a compound of the general formula ##STR5## wherein R.sup.7 is as defined above and if desired converting a compound of the general formula I to acid addition salt thereof or setting it free from the salt thereof.The new compounds show bronchodilatory activity.

Abstract: New 3-substituted-2-oxo-tetrahydro-pyrrolo[1,2-a]pyrimidines of the formula (II) ##STR1## or a pharmaceutically acceptable acid addition or quaternary ammonium salts thereof are disclosed, whereinR is hydrogen or lower alkyl;R.sup.1 is lower alkyl, phenyl, carboxyl, lower alkoxycarbonyl, nitrile, carbamoyl, or carbohydrazido; andR.sup.2 is hydrogen or lower alkyl. The compounds exert a positive inotropic activity on the heart and have digitalis-like activity.

Abstract: New Rutecarpine analogs are disclosed having Rutecarpine-like activity, especially diuretic activity. Also a novel process for the preparation of the Rutecarpine analogs is disclosed.

Abstract: Antiphlogistic and anticoagulant compounds of the formula: ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is C.sub.1 to C.sub.6 alkyl,R.sub.1 is hydrogen, or C.sub.1 to C.sub.6 alkyl,R.sub.2 is hydrogen, C.sub.1 to C.sub.6 alkyl, substituted or unsubstituted amino, substituted or unsubstituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sub.1 and R.sub.2 together form a --(CH.dbd.CH).sub.2 --group andR.sub.5 is 0 or imino or substituted imino.

Abstract: Compounds of the formula I ##STR1## or pharmaceutically acceptable salts, hydrates, stereoisomers, optically active isomers, geometrical isomers or tautomeric forms thereof are disclosedwhereinR is hydrogen or lower alkylR.sup.1 is hydrogen, lower alkyl, styryl, or a carboxylic acid; orR and R.sup.1 together form a group of the formula --(CH.dbd.CH).sub.2 -- and in this case the broken line represents a further C--C bond, while in all other cases there is a single bond between positions 6 and 7;R.sup.2 is hydrogen, lower alkyl or hydroxy;R.sup.3 is hydrogen, lower alkyl, aryl, lower alkanoyl, carboxyl or a carboxyl acid derivative or a group of the formula --(CH.sub.2)m--COOH or a derivative thereof formed in the carboxylic group;n=1-3;R.sup.4 is hydrogen, lower alkyl which can be substituted by hydroxy or carboxy; trifluoromethyl, substituted or unsubstituted aryl, phenyl-lower alkyl or substituted or an unsubstituted heterocyclic group;R.sup.

Abstract: New optionally racemic or optically active pyrimido(1,2a) heterocyclic compounds of the formula ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is an alkyl group containing one to six carbon atoms,R.sup.1 is hydrogen, alkyl containing one to six carbon atoms,R.sup.2 is hydrogen, alkyl containing one to six carbon atoms, optionally substituted amino, optionally substituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sup.1 and R.sup.2 together form a --(CH.dbd.CH).sub.2 -- group attached to the two adjacent carbon atoms of the ring A and the broken line represents a chemical bond,R.sup.3 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl or optionally substituted hydroxy,R.sup.

Abstract: A process for the preparation of nitrogen bridgehead condensed pyrimidine compounds of the general formula ##STR1## [wherein R represents hydrogen or lower alkyl;R.sup.1 represents hydrogen, lower alkyl, carboxy or a derivative thereof or styryl;R.sup.2 represents hydrogen or optionally substituted lower alkyl;R.sup.3 represents hydrogen, optionally substituted lower alkyl, aryl, aralkyl, halogen, carboxy or a derivative thereof, the group --(CH.sub.2).sub.m --COOH (in which m is the integer 1, 2 or 3) or a carboxy derivative thereof, formyl, lower alkanoyl or a condensed thereof;R.sup.4 represents hydrogen, optionally substituted alkyl, aryl optionally substituted by one or more substituents, optionally substituted aralkyl, a heterocyclic group optionally substituted by one or more substituents, the group (CH.sub.2).sub.m --Het (in which m is the integer 1, 2 or 3; Het is an optionally substituted heterocyclic group);R.sup.5 represents hydrogen, C.sub.

Abstract: A process is disclosed for the preparation of compounds of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or lower alkyl;R.sup.3 is carboxy, lower alkoxycarbonyl, carbamoyl, carbamoyl substituted by one or two lower alkyl groups, or cyano;R.sup.4 is hydrogen, lower alkyl, phenyl, naphthyl, phenyl or naphthyl substituted by at least one fluoro, chloro, bromo, iodo, lower alkyl, lower alkoxy, hydroxy, carboxy, or phenyl, pyridyl or tetrazolyl; andR.sup.5 is hydrogen or lower alkyl; or a pharmaceutically acceptable salt, hydrate, stereoisomer, optically active isomer, geometric isomer, or tautomer thereof, which comprises the step of aminating a racemic or optically active compound of the formula (II) ##STR2## wherein X is halogen with a compound of the formula (III) ##STR3## or a pharmaceutically acceptable acid addition salt thereof. The compound of formula (II) possess antiallergic, especially antiasthma, activity.

Abstract: 3 Substituted hexahydro-pyrimido[1, 2 a]azepines and quaternary derivatives, useful as antianginals are prepared. Specifically tested are 3 carboxylates and carbo hydrazides. 3 Cyano Carbamonyl and alkyl compounds are also disclosed.

Abstract: Intermediates useful in the preparation of Rutecarpine and Rutecarpine derivatives are disclosed as well as a process for the preparation of said intermediates having the following formula: ##STR1## wherein R, R.sup.1 and R.sup.2 are the same or different and stand for hydrogen, halogen, nitro, carboxy, nitrile, alkoxy containing 1 to 4 carbon atoms, alkoxycarbonyl containing 1 to 4 carbon atoms in the alkoxy group, alkyl containing 1 to 4 carbon atoms, amino or hydroxy or R and R.sup.1 together stand for methylenedioxy, R.sup.2 stands for hydrogen, R.sup.3 represents hydrogen or alkyl containing 1 to 4 carbon atoms, R.sup.

Abstract: Nitrogen bridgehead compounds (pyrido-[1,2-a]-pyrimidine derivatives) which are useful intermediates in the making of known compounds of this class and which themselves possess PG-antagonist, analgesic, antiartheriosclerotic, tranquilizing and like pharmaceutical activity.

Abstract: Compounds of the formula: ##STR1## or pharmaceutically acceptable salts thereof are disclosed wherein R is hydrogen or C.sub.1 to C.sub.6 alkyl;R.sup.2 and R.sup.3 are each hydrogen or together form a valency bond;R.sup.6 is carboxy or C.sub.1 to C.sub.6 alkoxycarbonyl;R.sup.7 and R.sup.8 are each hydrogen or together form a valency bond;R.sup.10 is carboxy or C.sub.1 to C.sub.6 alkoxycarbonyl and the dotted line represents two hydrogen atoms or a valency bond. The compounds are useful in the treatment of atherosclerosis.