摘要:
Novel acrylic acid salts of formula ##STR1## wherein R represents a hydrogen or a halogen atom, a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group,M represents a cation derived from bismuth, zinc or a pharmaceutically acceptable organic base,X represents an inorganic anion,n is an integer of from 0 to 2,m is an integer of from 1 to 3,p is 0 or 1, andr is an integer of from 0 to 6having cytoprotective and antiulcer activities are provided. A process is also described for the preparation of said compounds.
摘要:
The present invention relates to a method of treating a gastric ulcer by administering a 2-thia-zolone of the formula (I), ##STR1## wherein X stands for --CN, --CONH.sub.2, --CO.sub.2 H or --CO.sub.2 R group, wherein R is a C.sub.1-5 alkyl group; andn is 0, 1 or 2, with the proviso, that when X stands for CO.sub.2 H, CO.sub.2 R, n is other than 0.
摘要:
The invention relates to new 1,2,3,4,6,7,12,12b-octahydroindolo[2,3,-a]quinolizin-1-yl-alkanecarboxylic acid amides of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 stand independently for a hydrogen or halogen atom, or a hydroxyl, nitro or C.sub.1-4 alkoxy group;R.sub.3 and R.sub.4 stand independently for a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.5 and R.sub.6 stand independently for a hydrogen atom, C.sub.1-8 alkyl group, C.sub.3-8 alkenyl or cycloalkyl group, aryl or aralkyl group, heteroaryl or heteroaralkyl group containing oxygen, nitrogen or sulphur atom, all these groups being optionally substituted; orR.sub.5 and R.sub.6 together form an optionally substituted C.sub.2-8 .alpha.,.omega.-alkylene group, wherein one carbon atom may optionally be replaced by an oxygen or nitrogen atom; andG means a C.sub.1-4 straight chained alkylene group, as well as to their therapeutically suitable acid addition salts and pharmaceutical compositions containing these compounds. The compounds of the formula (I) have valuable therapeutic properties, namely vasodilatory, spasmolytic, antiarrhythmic and gastrocytoprotective effects. The gastrocytoprotective effect is particularly important.
摘要:
The invention relates to new 1-[6-(2'-substituted-5', 6', 7', 8'-tetrahydro-4'-oxo-quinazolino)]-3,4-dihydro-6,7-disubstituted-isoquinoline 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.
摘要:
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. Processes for the preparation of these compounds and pharmaceutical compositions are also within the scope of the invention.
摘要:
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.
摘要:
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.
摘要:
A compound of the following formula: ##STR1## wherein X.sub.1 is hydrogen or mercapto;X.sub.2 is mercapto or acetylthio;X.sub.3 is hydrogen or acetylthio; andX.sub.4 is hydrogen, acetylthio or X.sub.3 and X.sub.4 together form a valence bond, but if X.sub.3 and X.sub.4 form a valence bond X.sub.2 is mercapto. The compounds are useful in the treatment of heavy-metal poisoning.
摘要:
The present invention relates to a process for the preparation of high purity crystalline peptides Arg Lys Asp hydrate acetate and Arg Lys Asp Val from crude, amorphous peptides Arg Lys Asp and Arg Lys Asp Val hydrate acetate.The process is characterized in thatthe crude, amorphous peptide Arg Lys Asp or Arg Lys Asp Val is let stand at room temperature in 5 to 20 unit volume of ethanol containing 0.5 to 4.0% by volume of acetic acid and 5 to 25% by volume of water, wherein the volume unit is calculated for the mass unit of the material and mass unit relates to volume unit as g relates to ml,then the crystallized peptide is separated from the crystalline suspension, preferably after cooling.
摘要:
Novel acrylic amide derivatives of the Formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom or a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group.n is an integer of 0 to 2,A represents an amino acid residue derived from a naturally occurring amino acid or an antipode thereof which is bonded to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid, bonded to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C.sub.1-4 alkyl group or is amidated; or A represents a group of the formula ##STR2## wherein R.sub.2 is a hydrogen atom or a phenyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxycarbonyl group,and their salts which have cytoprotective and antiulcer to activities. A process is also described for the preparation of said compounds.