Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.

Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions comprising the same, and the use thereof in the preparation of pharmaceutical compositions for the treatment of vascular diseases.

Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.

Abstract: The invention relates to carboxamidine derivatives to pharmaceutical compositions containing the same and the use thereof in the preparation of pharmaceutical compositions for the treatment of vascular diseases.

Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.

Abstract: 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.

Abstract: Peptides are disclosed which inhibit the immune system. The peptides are selected from the group consisting of:Arg-Lys(Chc)-Asp-ValArg-Lys(Chc)-AspArg-Sar-Asp-ValArg-Sar-AspOrn-Lys-Asp-ValOrn-Lys-AspArg-Lys-Aad-ValArg-Lys-Aad[Arg-Lys-Asp-NH-CH.sub.2 -].sub.2 ##STR1##Lys-Ser-Lys-LeuSer-Lys-LeuSer-Ser-Ser-ThrLys-Glu-ThrLys-Thr-Glu-ThrPro-Lys-Leu-ThrLys-Lys-Thr-Glu andLys-His-Leu-NH.sub.2,and pharmaceutically acceptable acid addition salts thereof.

Abstract: The new peptides of the Formulae(1) Glp-Lys-NH.sub.2(2) Glp-Glu-Lys-NH.sub.2(3) Arg-Lys-Glu-NH.sub.2(4) Arg-lys-Asp-NH.sub.2(5) Arg-Lys-Glu-OH(6) Arg-Lys-Gln-OH(7) Leu-Val-Ala-OH(8) Arg-Orn-Asp-Val-NH.sub.2(9) Arg-Orn-Asp-Val-OH(10) Lys-Glu-Lys-Lys-OH(11) Lys-Leu-Lys-Lys-OH(12) Lys-Asp-Leu-Lys-OH(13) Glu-Leu-Val-Ala-OH and(14) Leu-Pro-Ala-Gly-OHand acid addition salts thereof inhibit the proliferation of leukaemic cells and exhibit immunostimulant effect.

Abstract: The invention relates to novel peptides and their acid addition salts, suppressing the function of the immune system, pharmaceutical compositions containing these peptides as well as to a process for preparing these peptides and compositions. The peptides are represented by formulae (1) to (16): ##STR1## The novel peptides are useful for the therapy of diseases where a decrease in the activity of the immune system is desirable.

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: Peptides affecting the immune regulation selected from the following group:Arg-Lys-AspArg-Lys-Asp-ValArg-Lys-Asn-ValArg-Lys-Asu-ValArg-Lys-Ala-ValArg-Lys-Asp-AlaArg-Lys-Asp-IleArg-Lys-Glu-ValArg-Ala-Asp-ValArg-Asp-Lys-ValAla-Lys-Asp-ValLys-Arg-Asp-ValGlp-Arg-Lys-AspGlp-Arg-Lys-Asp-ValGlp-Arg-Lys-Asp-Val-Tyr and salts, amides lower alkyl esters and protected derivatives thereof.