Abstract: The invention relates to the crystalline and amorphous forms of the desmotrope of general formula IB and its salts and solvates, and their preparation.

Abstract: Process for the preparation of a compound of the general formula (I) and pharmaceutically acceptable salts and solvates thereof, (I) characterised by reacting an N-(amino-tioxo-methyl)-1H-indole-2-carboxamide of the general formula (II), with an &agr;-halogen-ketone of the general formula (III), wherein X stands for halogen.

Abstract: New salts of the general formula (I), their solvates, polymorphs and pseudo polymorphs wherein X stands for ethanolamine, diethanolamine or diethylamine.

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

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 invention relates to a new process for the preparation of antibacterial compounds of the Formula I ##STR1## wherein R.sup.1 stands for phenyl substituted by 1 or 2 halogen atoms;R.sup.2 stands for piperazinyl or 4-methyl-piperazinyl;and pharmaceutically acceptable salts thereof which comprises using a compound of the Formula II ##STR2## wherein R stands for halogen or an aliphatic acyloxy group containing 2 to 6 carbon atoms or an aromatic acyloxy group containing 7 to 11 carbon atoms andR.sup.4 stands for fluorine or chlorine as a starting material.

Abstract: The invention relates to a new process for the preparation of compounds of the general Formula I ##STR1## wherein R stands for piperazinyl, 4-methyl-piperazinyl or 4-ethyl-piperazinyl group and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II ##STR2## wherein R.sup.1 and R.sup.2 stand for halogen, for an aliphatic acyloxy group containing 2 to 6 carbon atoms and optionally substituted by halogen, or for an aromatic acyloxy group containing 7 to 11 carbon atoms with a piperazine derivative of the general Formula III ##STR3## wherein R.sup.3 stands for hydrogen, methyl or ethyl or a salt thereof and subjecting the compound of the general Formula IV ##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 general Formula I thus obtained into a salt thereof or setting free the same from its salt.

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 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 general Formula I ##STR1## /wherein R stands for piperazinyl, 4-methyl-piperazinyl or 4-ethyl-piperazinyl group/ and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II ##STR2## /wherein R.sup.1 and R.sup.2 stand for halogen, for an aliphatic acyloxy group containing 2 to 6 carbon atoms and optionally substituted by halogen, or for an aromatic acyloxy group containing 7 to 11 carbon atoms/ with a piperazine derivative of the general Formula ##STR3## /wherein R.sup.3 stands for hydrogen, methyl or ethyl/ or a salt thereof and subjecting the compound of the general Formula IV ##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 general Formula I thus obtained into a salt thereof or setting free the same from its salt.

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: The invention relates to new quinoline-3-carboxylic acid anhydride intermediates of the Formula I ##STR1## wherein R stands for cyclopropyl, a group of the Formula --CH.sub.2 CR.sup.5 R.sup.6 R.sup.7 wherein R.sup.5, R.sup.6 and R.sup.7 stand for hydrogen or halogen, or phenyl optionally substituted by 1 or 2 halogen,R.sup.1 and R.sup.2 stand for halogen, or an aliphatic acyloxy group containing 2 to 6 carbon atoms optionally substituted by halogen, or an aromatic acyloxy group containing 7 to 11 carbon atoms,R.sup.3 stands for chlorine or fluorine andR.sup.4 stands for hydrogen or fluorine. The compounds of the Formula I are new intermediates for the preparation of known quinoline-3-carbocxylic acids showing antibacterial activity.

Abstract: The present invention relates to a process for the preparation of compounds of the general Formula I ##STR1## and pharmaceutically acceptable salts thereof (wherein R stands for piperazinyl or 4-methyl-piperazinyl) which comprises reacting a compound of the general Formula II ##STR2## (wherein R.sup.1 and R.sup.2 stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms) with a piperazine of the general Formula III ##STR3## (wherein R.sup.3 represent hydrogen or methyl) or a salt thereof, hydrolysing the compound of the general Formula IV ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) without or after hydrolysis and if desired converting the compound of the general Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the general Formula I are known antibacterial agents.

Abstract: The invention relates to new 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid/boric acid anhydrides of the general Formula I ##STR1## (wherein R and R.sup.1 stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms).The new compounds of the general Formula I are valuable intermediates useful in the preparation of the antibacterial agent 6-fluoro-1-methylamino-7-(4-methyl-piperazino)-4-oxo-1,4-dihydro-quinoline -3- carboxylic acid.The new compounds of the general Formula I may be prepared by reacting a compound of the Formula II ##STR2## or a compound of the general Formula III ##STR3## (wherein R.sup.2 stands for alkyl comprising 1-4 carbon atoms) with hydrogen fluoro borate of the Formula IVHBF.sub.4 /IV/or a borone trihalide of the general Formula VBX.sub.

Abstract: The invention relates to a process for the preparation of compounds of the Formula I ##STR1## (wherein R and R.sup.1 stand for an aliphatic acyloxy group comprising 2-5 carbon atoms and optionally substituted by halogen or for an aromatic acyloxy group comprising 7-11 carbon atoms), which comprises reacting a compound of the general Formula II ##STR2## (wherein R.sup.2 stands for hydrogen or alkyl comprising 1-4 carbon atoms) with a boron derivative of the Formula III ##STR3## (wherein R.sup.3, R.sup.4 and R.sup.5 stand for an alkyl group comprising 1-4 carbon atoms and optionally substituted by halogen or for an aryl group comprising 6-10 carbon atoms).The new compounds of the general Formula I are useful pharmaceutical intermediates.