Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.

Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.

Abstract: The invention relates to pharmaceutical compositions for the treatment or prevention of lesions of gastrointestinal mucous membranes and having secretion inhibiting, cytoprotective activities. The compositions contain in a biologically effective quantity a triazole-group-substituted quinoline derivative of general formula (I)R.sup.1 stands for a 1-triazolyl-group in position 2 or 4 ora 3-triazolyl-thio ora 5-/C.sub.1-4 -alkyl/-3-triazolyl-thio-group,R.sup.2 stands for a hydrogen atom in position 3 or optionally in position 2, or for a C.sub.1-4 -alkyl-group,R.sup.3 stands for a hydrogen atom or for a C.sub.1-4 -alkyl-group,X stands for a hydrogen or halogen-atom or for a C.sub.1-4 -alkyl-group or its salts. The invention includes processes for the preparation of the above compositions, and methods for treatment of patients in need of such treatment by administering the substance or the composition. The prefered substance of formula (IV) is also subject of the invention.

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 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.