Abstract: The invention relates to R-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazinone of formula (1), and to S-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazinone of formula (2), and to acid-addition salts thereof as well as pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for the preparation of the above compounds. The new starting compounds of formulae (4) and (5) are also involved in the scope of the invention. The compounds according to the invention possess &agr;1- and &agr;2-adrenoceptor antagonistic effects and urogenital selectivity. Thus, they are useful for the treatment of the benign prostate hyperplasia.

Abstract: The invention relates to R-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazionone of formula (1) and to S-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazionone of formula (2) and to acid-addition salts thereof as well as pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for the preparation of the above compounds. The new starting compounds of formula (4) and (5) are also involved in the scope of the invention. The compounds according to the invention possess &agr;1- and &agr;2-adrenoceptor antagonistic effects and urogenital selectivity. Thus, they are useful for the treatment of the benign prostate hyperplasia.

Abstract: The invention relates to novel 3(2H)-pyridazinone-derivatives of the general formula (I), pharmaceutical compositions containing them and process for their preparation. In the general formula (I) ##STR1## stands for an ethyl or propyl group substituted by a terminal halogen atom or a hydroxyl or NR.sup.1 R.sup.2 group, whereinR.sup.1 represents hydrogen atom or an unsubstituted or optionally substituted benzyl group;R.sup.2 represents hydrogen atom or an unsubstituted or optionally substituted benzo[1,4]dioxan-2-yl-methyl or -ethyl group or a (CH.sub.2).sub.n --R.sup.3 group, whereinn is 2 or 3; andR.sup.3 stands for an unsubstituted or optionally substituted phenoxy or phenylthio group; andX stands for a hydrogen or halogen atom or an unsubstituted or optionally substituted, saturated or unsaturated 5- or 6-membered heterocyclic group containing a nitrogen atom and optionally an additional heteroatom, e.g.

Abstract: The invention relates to novel pyrimido [5,4-b][1,4]oxazine derivatives of the formula (I), and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## wherein R.sup.1 stands for a C.sub.1-4 alkyl group;R.sup.2 stands for hydrogen or halogen or an azido group or an --NR.sup.5 R.sup.6 group, whereinR.sup.5 represents hydrogen or a benzyl group, or a C.sub.1-4 alkyl group unsubstituted or substituted by a hydroxyl group,R.sup.6 stands for hydrogen, an amino group, a C.sub.3-6 cycloalkyl group, a straight or branched-chain C.sub.1-4 alkyl group optionally substituted by a hydroxyl, mercapto, aminocarbonyl, furyl, 2-benzo[1,4]dioxanyl, di(C.sub.1-4 alkyl)amino group or by a phenyl or phenoxy group optionally mono- or polysubstituted by halogen or C.sub.1-4 alkoxy group (s) or by a 6-membered, saturated nitrogen-containing heterocycle optionally containing an additional nitrogen or oxygen atom and optionally substituted by a C.

Abstract: The invention relates to the new monohydrate of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidi ne (cimetidine), a histamine-H.sub.2 receptor antagonist which is called N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidi ne H (cimetidine H) as well as to a process for the preparation of same, which comprises pouring a hot, homogeneous aqueous solution of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidi ne, optionally containing also methylamine, onto ice and separating the N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidi ne monohydrate.

Abstract: The invention relates to a novel process for the preparation of 6-(substituted amino)-3-pyridazinylhydrazines having the general formula I ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.2 and R.sup.3 may be the same or different and stand for alkyl groups containing from 1 to 6 carbon atoms, alkenyl groups containing from 2 to 6 carbon atoms, hydroxyalkyl groups containing from 2 to 4 carbon atoms, cycloalkyl groups containing from 3 to 8 carbon atoms, phenyl or benzyl groups or phenyl, benzyl or phenylethyl groups containing one or two halogen atoms, nitro, methoxy or hydroxyl groups, and one of R.sup.2 and R.sup.3 may stand also for a hydrogen atom, or R.sup.2 and R.sup.3 together with the neighboring nitrogen atom may build up also a morpholino, pyrrolidino, piperidino, heptamethyleneimino or N-methylpiperazino group.

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: 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 novel sulfonamidobenzoic acid derivatives having the general formula ##STR1## wherein R.sup.1 denotes a C.sub.1-4 alkoxy group or a hydrazino group or an NR.sup.4 R.sup.5 group, wherein R.sup.4 and R.sup.5 denote each a hydrogen atom or an identical or different C.sub.1-4 alkyl group; furthermore R.sup.4 may denote an aralkyl or substituted aralkyl group provided that R.sup.5 denotes a hydrogen atom; furthermore NR.sup.4 R.sup.5 may denote a morpholine or piperazine ring;R.sup.2 and R.sup.3 may denote each a hydrogen atom or an identical or different C.sub.1-4 aliphatic group; furthermore R.sup.2 may denote a cycloaliphatic, aralkyl, substituted aralkyl or amino group provided that R.sup.3 denotes a hydrogen atom; furthermore R.sup.2 and R.sup.3 may denote together with the adjacent nitrogen atom a morpholino ring, an unsubstituted piperazine ring or a substituted piperazine ring,and to their pharmaceutically acceptable acid addition salts.

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: New acylated 2-aminothiazole derivatives of the general formula (I), ##SPC1##whereinR.sup.1 stands for phenyl group or a pyridyl group,R.sup.2 stands for hydrogen or lower alkyl,R.sup.3 stands for hydrogen, a lower alkyl group or benzyl group, andR.sup.4 and R.sup.5 each represent hydrogen, a C.sub.1-8 alkyl group, allyl group, a hydroxyalkyl group, a C.sub.3-6 cycloalkyl group, .beta.-dimethylaminoethyl group, .beta.-diethylaminoethyl group, benzyl group, 2-furylmethyl group, or a phenyl group having optionally a halogen, methyl, methoxy or trifluoromethyl substituent, orR.sup.4 and R.sup.5 may form, together with the adjacent nitrogen atom, a 5 to 8 membered polymethyleneimino group, morpholino group, piperazino group, N-methylpiperazino group or N-phenylpiperazino group, the compounds of formula I are anticholinergics.