Abstract: The present invention is directed to hydrazono compounds that function as inhibitors of copper-containg amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-1 (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases.

Abstract: The present invention is directed to hydrazino compounds that function as inhibitors of copper-containing amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-1 (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases. The compounds have the general formula: or a pharmaceutically acceptable solvate, hydrate, or salt thereof, wherein R1 to R8 and X are as defined herein.

Abstract: The present invention is directed to hydrazono compounds that function as inhibitors of copper-containg amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-1 (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases.

Abstract: New compounds with the ability to inhibit calcium uptake in the brains of mammals are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.4 alkyl;one of R.sup.2 and R.sup.3 is C.sub.1 to C.sub.4 alkoxy and the other one is phenyl-C.sub.1 to C.sub.4 alkoxy optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus; andR.sup.4 is phenyl optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus, or their solvates, individual optically active and geometric isomers, mixtures of such isomers, as well as pharmaceutically acceptable acid addition salts thereof. The compounds of the Formula (I) are capable of inhibiting calcium uptake to brain cells and have a protective effect on hypobaric hypoxia.

Abstract: The invention relates to new 1-[6-(2'-substituted-5', 6', 7', 8'-tetrahydro-4'-oxo-quinazolino)]-3,4-dihydro-6,7-disubstituted-isoquinol ine derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hdyroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is alky having from 1 to 6 carbon atoms, optionally substituted phenyl, optionally substituted alkylphenyl having from 1 to 4 carbon atoms in the alkyl moiety or an optionally substiutted heterocyclic group,and acid addition and quaternary salts thereof.Compounds of the formula (I) are pharmaceutically active, in particular show spasmolytic, analgesic, antipyretic activity and have a protecting effect in acute alcoholic intoxication.

Abstract: The invention relates to new N-substituted bis(hydroxymethyl)-methyl-isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,the dotted line is an optional double bond in the 1,2-position,R.sup.3 is alkyl having from 1 to 6 carbon atoms or aralkyl containing from 1 to 4 carbon atoms in the alkyl moiety, or--if there is a single bond in the 1,2-position--represents a group of the formula ##STR2## in which X is oxygen ifR.sup.4 is alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 4 carbon atoms, hydroxyl, phenyl or substituted phenyl; orX is oxygen or sulfur ifR.sup.4 is an --NH.sub.2, --NH--C.sub.1-4 -alkyl, --NH--C.sub.3-6 -cycloalkyl, --NH-phenyl or --NH--C.sub.1-4 -alkyl-phenyl group; andR.sup.5 and R.sup.6 independently stand for hydrogen, alkyl having from 1 to 4 carbon atoms or phenyl, with the proviso that at least one of them is other than phenyl,and salts thereof.

Abstract: The invention relates to new 1-[bis(hydroxymethyl)-methyl]-3,4-dihydro- or -1,2,3,4-tetrahydroisoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen or a single electron pair,and the dotted line represents an optional double bond,and salts thereof.The new compounds are useful intermediates in the preparation of other, pharmaceutically active isoquinoline derivatives or are pharmaceutically active themselves.

Abstract: The invention relates to new bis(substituted methyl)-methyl-isoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or a ##STR2## group, in which R.sup.4 is alkyl having from 1 to 5 carbon atoms, phenyl, substituted phenyl or --NH--phenyl,X is oxygen or sulfur,R.sup.7 is hydroxyl, halogen or an ##STR3## group, R.sup.8 is halogen, alkoxy from 1 to 4 carbon atoms or an ##STR4## group, in which X has the same meaning as defined above, andR.sup.9 independently from R.sup.4 may have the same meanings as defined for R.sup.4, or is an --NH(C.sub.1-4 -alkyl) or C.sub.3-6 -cycloalkyl group,and salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds and pharmaceutical compositions containing them.

Abstract: The invention relates to new [1,3]oxazino[4,3-a]-isoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen, alkyl having from 1 to 8 carbon atoms, cycloakyl or cycloalkenyl having from 3 to 6 carbon atoms, optionally substituted phenyl, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or heteroaryl,R.sup.4 is hydrogen or alkyl having from 1 to 4 carbon atoms, orR.sup.3 and R.sup.4 together form a --(CH.sub.2).sub.n -- group, in which n is an integer from 3 to 7,R.sup.5 is hydroxyl, halogen or an ##STR2## group, in which R.sup.6 is optionally substituted phenyl,X is oxygen or sulfur,and salts thereof.According to another aspect of the invention there is provided a process for the preparation of these compounds. Compounds of formula (I) are pharmaceutically active. Pharmaceutical compositions containing them are also within the scope of the invention.

Abstract: The invention relates to new 1-cyclohexyl-3,4-dihydroisoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hydrogen, hydroxyl or alkoxy having from 1 to 6 carbon atoms,X is oxygen andZ is a .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is hydrogen or alkyl having from 1 to 6 carbon atoms; orX represents an .dbd.NR.sup.4 group, in which R.sup.4 is hydrogen or hydroxyl, andZ is a .dbd.CH--CN, .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is as defined above,and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular show antispasm, analgesic, gastric acid secretion inhibiting, sedative and hypnotic activity and effectively reduce the alcoholic narcosis time. According to a further aspect of the invention there is provided a process for the preparation of these compounds. The invention further relates to pharmaceutical compositions containing them as active ingredient.

Abstract: The invention relates to new 2H-azeto[2,1-a]isoquinoline derivatives of formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydroxyl, halogen or an ##STR2## group, whereinX is oxygen or sulfur,R.sup.4 is optionally substituted phenyl,and acid addition, metal and quaternary salts thereof.According to the invention the new compounds are prepared by cyclization of the corresponding compounds of formula (II), ##STR3## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, and Hal is halogen.Compounds of formula (I) are pharmaceutically active, in particular are potent analgesic and antipyretic agents.

Abstract: The invention relates to 1-(hydroxymethyl)-1,6,7,11b-tetrahydro-2H,4H-[1,3]oxazino- or -thiazino-[4,3-a]isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are alkoxy having from 1 to 6 carbon atoms,X is oxygen or sulfur,Y is .dbd.O, .dbd.S or an .dbd.NR.sup.3 group, whereinR.sup.3 is hydrogen, alkyl having from 1 to 6 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms or optionally substituted phenyl,and acid addition and quaternary salts thereof.

Abstract: Compounds of the formula ##STR1## or pharmaceutically acceptable acid-addition or quaternart ammonium salts thereofwhereinR is hydroxy, carboxy, lower alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl, carbamoyl, N-loweralkyl-carbamoyl, N,N-dilower-alkyl-carbamoyl, carboazido, carbohydrazido or cyano;R.sup.2 is C.sub.1 to C.sub.6 alkyl;R.sup.3 is C.sub.1 to C.sub.6 alkyl or benzyl; andR.sup.4 is a single electron pair, hydrogen or lower alkyl; and the dotted lines represent saturated or unsaturated bonds, are disclosed with analgesic properties.

Abstract: Pharmaceutical intermediates, morphine potentiators and other compounds have the formula ##STR1## wherein R is hydrogen, halogen, C.sub.1-4 alkyl, hydroxy, nitro, amino, carboxy or a carboxylic acid derivate radical, R.sup.1 is hydrogen or a C.sub.1-4 alkyl, R.sup.2 is hydrogen or C.sub.1-4 alkyl, R.sup.3 is hydrogen, R.sup.4 is hydrogen or C.sub.1-4 alkyl, R.sup.5 is hydrogen R.sup.6 is hydrogen or R.sup.3 and R.sup.4 and/or R.sup.5 and R.sup.6 form a chemical bond, X is oxygen or imino, m is 1, 2, 3 or 4, n is 0, 1, 2 or 3, and if n is 1, then the dotted lines can stand for bonds, with the proviso that if m=1 and n=1 and if in the 2,3-, 6,7-, 8,9- and 1,10-positions double bonds are present, and R.sup.1 and R.sup.2 are hydrogen, then R is other than 9-hydroxy or 9-methyl; if m=2 and n=1 and R.sup.2 is hydrogen, then at least one of R and R.sup.1 is other than hydrogen; and if m=2 and n=2 and R.sup.2 is hydrogen and the molecule is a 2,3,4,6,7,8,9,10-octahydro derivative, then at least one of R and R.sup.

Abstract: Compounds of the formula: ##STR1## or pharmaceutically acceptable acid addition or quaternary ammonium salts thereofwhereinR.sup.2 is C.sub.1 to C.sub.6 alkyl:R.sup.3 is C.sub.1 to C.sub.6 alkyl;R.sup.4 is a single electron pair, hydrogen or lower alkyl; and the dotted lines indicate saturated or unsaturated bonds, are disclosed with analgesic properties.

Abstract: A compound of the formula ##STR1## or a pharmaceutically effective salt thereof in which R.sup.1 and R.sup.2 are hydrogen or lower alkyl and R.sup.3 is halogenoalkenyl or propinyl. The compounds have pharmacological effects similar to those of phenylethylamine but are free from the amphetamine effect with an excellent therapeutic index and selectivity especially with respect to inhibition of monoaminooxidase.

Abstract: An antiedema compound of the formula: ##STR1## in which R.sup.1 is methyl, ethyl, cyclohexyl, phenyl, m-tolyl, p-tolyl, p-tert-butylphenyl, m-trifluoromethylphenyl, m-fluorophenyl, p-fluorophenyl, m-chlorophenyl, p-chlorophenyl, m-bromophenyl, p-bromophenyl, o-hydroxyphenyl, p-methoxyphenyl, p-nitrophenyl, benzyl, p-chlorobenzyl, m,p-dimethoxybenzyl, and o-pyridyl;R.sup.2 is hydrogen, p-tolyl, p-ethoxyphenyl, m-pyridyl, methyl or phenyl; andn is 1, 2 or 3And a process for the preparation thereof are disclosed.