Abstract: The present invention relates to novel peptides of formulaeXaa Glu Asp Cys Lys (SEQ I.D. No: 1),andGlu Asp Cys Lys (SEQ I.D. No: 2)wherein the Cys sulfur is bonded to an acetamidomethyl group, and Xaa is pyro-Glu, the acid addition salts thereof, the pharmaceutical compositions comprising the same and a process for the preparation of the novel peptides and compositions.The novel peptides selectively inhibit the proliferation of hemopoietic cells.The invention also covers the treatment of mammals (including human beings) with the said peptides and compositions for selectively inhibiting the proliferation of hemopoietic cells.The advantage of the novel compounds is that they are almost completely harmless, they do not have any side-effect in therapeutic dose-range, in addition they significantly inhibit the damaging effects of drugs and radiation used for the therapy of tumorous diseases or the dose of drug or radiation can be increased when they are administered.

Abstract: The present invention relates to novel pentapeptide of formulaXaa Glu Asp Ser Gly (SEQ ID NO: 1)wherein Xaa is pyro-alpha-aminoadipic acid, having specific inhibiting effect on epidermal cell proliferation, salts thereof, pharmaceutical compositions comprising the same and a method for the treatment of mammals for inhibiting the epidermal cell proliferation by administering the novel pentapeptide. The invention also covers a process for the preparation of both the pentapeptide and the pharmaceutical composition.

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 present invention relates to novel optically active or racemic tetrahydro-1,2,4-oxadiazine-5-thione derivatives of the formula ##STR1## methods for their preparation, pharmaceutical compositions comprising the said compounds as active ingredients and a method for the anticonvulsive treatment of mammals, especially human beings.The compounds of the formula I have as good activity as diphenyl hydantoine but their toxicity is much lower.

Abstract: The invention relates to octapeptides of the formulaX-Arg-Val-Tyr-Y-His-Pro-W (I)whereinX is a sarcosyl, lactoyl or hydroxyacetyl radical,Y is cyclopentylglycyl or cyclohexylglycyl, andW is an alanine radical or lactic acid radicalhaving angiotensine-II antagonistic activity.

Abstract: The invention relates to new, pharmaceutically active copolymers with heparin-like activity, pharmaceutically acceptable salts thereof and a process for their preparation.

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.

Abstract: A tranquillo-sedative substituted 1,3,4,5-tetrahydro-2H-1,4-benzodiazepine-2-one of the formula (I), ##STR1## wherein R.sub.1 is halogen or nitro,R.sub.2 is hydrogen or methyl,R.sub.3 is --CONH.sub.2 or --CONHCH.sub.3, andR.sub.6 is phenyl or halophenyl.

Abstract: New octapeptides of the general formula (I),X--Arg--Val--Tyr--Ile--His--Pro--Y--OA (I)whereinX stands for the acyl group of an N-methylamino acid or the acyl group of an aliphatic .alpha.-hydroxy- or .alpha.-aminooxycarboxylic acid,Y is the residue of an aliphatic amino acid, andA is a C.sub.1-5 alkyl group, are prepared so that the protecting groups of a protected octapeptide derivative of the general formula (II),B--X--Arg(C)--Val--Tyr(D)--Ile--His(E)--Pro--Y--OA (II)whereinB is a group removable by acidolysis or catalytic hydrogenation,C is a group for the temporary protection of the guanidino group on the Arg moiety,D is a group for the temporary protection of the aromatic hydroxy group on the Tyr moiety,E is a group for the temporary protection of the imidazole group on the His moiety, andA, X and Y are as defined above,are removed either stepwise or in a single step. If desired, a compound of the general formula (I) is converted into its acid addition salt or pharmaceutically acceptable complex.

Abstract: The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I),X--Y--W--NH.sub.2 (I)whereinX is L-pyroglutamyl, D-pyroglutamyl, L-2-keto-imidazolidine-4-carbonyl, L-6-keto-pipecolyl, L-thiazolidine-4-carbonyl, L-prolyl or orotyl group,Y is L-leucyl, L-norvalyl or L-histidyl group, andW is L-prolyl, D-prolyl, L-thiazolidine-4-carbonyl, L-pipecolyl, L-homoprolyl, L-leucyl, L-isoleucyl, L-methionyl or D-pipecolyl group, orthe W-NH.sub.2 group stands for pyrrolidyl or piperidyl group, with the proviso that if X is L-pyroglutamyl and Y is L-histidyl group, W is other than L-prolyl group, and pharmaceutically acceptable complexes thereof.These compounds are prepared by methods commonly applied in the peptide chemistry.

Abstract: The invention relates to a process for the preparation of a biologically active substance, which can be isolated from normal white blood cells and is capable of inhibiting the proliferation of normal and leukemic myeloid cells selectively.The substance obtained is a peptide, which has an amino acid composition of Tau.sub.1, Asx.sub.1, Ser.sub.2, Thr.sub.1, Glx.sub.3, Gly.sub.2, Ala.sub.1, (PO.sub.4).sub.1.sup.2-, a negative charge at pH 6.5, an electrophoretic mobility of -0.55 to -0.65 related to aspartic acid, has no charge at pH 1.9, has a mobility of about 0.26 related to .epsilon.-DNP-lysine and gives a positive chloro-toluidine reaction.

Abstract: The invention relates to new tetrahydro-1,2,4-oxadiazin-5-one derivatives having a CNS activity. More particularly, the invention concerns new N.sup.4 -substituted tetrahydro-1,2,4-oxadiazin-5-ones of the formula (1) ##STR1## wherein R.sup.2 is benzyloxycarbonyl or alkylcarbonyl containing 1 to 4 carbon atoms in the alkyl moiety, preferably acetyl;R.sup.3 is phenyl optionally substituted with 1 to 3 lower alkoxy groups; andR.sup.4 is an aliphatic or cyclic alkyl group having 1 to 11 carbon atoms, hydroxymethyl, halomethyl or acyloxymethyl.According to another aspect of the invention there are provided processes for the preparation of compounds of formula (1). Still another aspect of the invention is a pharmaceutical composition which comprises as active ingredient a compound of formula (1).

Abstract: A tranquillo-sedative substituted 1,3,4,5-tetrahydro-2H-1,4-benzodiazepine-2-one of the formula (I), ##STR1## wherein R.sub.1 is halogen or nitro,R.sub.2 is hydrogen or C.sub.1 to C.sub.6 alkyl,R.sub.3 is --CONH.sub.2, andR.sub.6 is phenyl or halophenyl.

Abstract: New angiotensin-II analogues of the general formula (I),X-Arg-Val-Tyr-Ile-His-Pro-Y-OA (I)whereinX stands for the acyl group of an N-methylamino acid, or the acyl group of an aliphatic .alpha.-aminooxy- or .alpha.-hydroxycarboxylic acid,Y is the residue of an aliphatic .alpha.-hydroxycarboxylic acid, andA is hydrogen or a C.sub.

Abstract: The invention relates to new optically active or racemic 5-phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one derivatives of the general formula (I) ##STR1## wherein R.sup.1 stands for hydrogen, halogen, trifluoromethyl or a nitro group;R.sup.2 stands for hydrogen or alkyl having 1 to 6 carbon atoms;R.sup.3 represents a group conventionally attached to the --CH(NH.sub.2)--COOH group of the known optically active or racemic .alpha.-amino-acids, preferably an optionally substituted lower alkyl group;R.sup.4 is hydrogen, chlorocarbonyl or carbamoyl; andX is hydrogen, halogen or trifluoromethyl, with the proviso that if in the racemic compounds R.sup.4 stands for hydrogen R.sup.3 is other than alkyl having 1 to 6 carbon atoms, in which the centers of asymmetry in the 3- and 5-positions have the same absolute configuration, and pharmaceutically acceptable acid addition salts thereof, and a process for their preparation.

Abstract: The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I),Glp--X--Y--NH--A (I)whereinX is L-norleucyl, L-leucyl, L-norvalyl, D-leucyl, L-prolyl, L-2-aminobutyryl, L-valyl, L-threonyl, L-isoleucyl, L-2-aminodecanoyl, L-cyclohexylalanyl or L-tert.-butyl-seryl group andY is L-prolyl group, orX is L-histidyl group andY is L-homoprolyl or D-pipecolyl group, furthermoreA is hydrogen, a C.sub.1-10 alkyl group or a C.sub.1-3 alkyl group having a dimethylamino substituent,with the proviso that if X is L-leucyl group, A is other than hydrogen, and pharmaceutically acceptable complexes thereof.These compounds are prepared by methods commonly applied in the peptide chemistry.

Abstract: There are disclosed pharmaceutical compositions comprising at least one cytostatic agent and N.sup..epsilon. -trimethylthyllysin or a pharmaceutically acceptable salt thereof, optionally in association with conventional pharmaceutical carriers and other additives.The new compositions possess a reduced toxicity compared with the cytostatic agents administered alone.

Abstract: Novel Angiotensin II peptides of the formula:X-Arg-Val-Tyr-Ile-His-Pio-Ywhere X is hydroxyacetyl or .alpha.-hydroxypropyl and Y is leucyl, isoleucyl, alanyl or threonyl or an acid addition salt or a complex thereof are disclosed and a process for the preparation thereof are disclosed having the ability to lower renal hypertension.