Abstract: Peptide components of formula 1, pharmaceutically acceptable base salts thereof, pharmaceutical compositions and their use as antiinfective agents ##STR1## where R.sub.1 is alkyl, cycloalkyl or cycloalkylmethyl; R.sub.2 is hydrogen or alkyl and R.sub.3 is hydroxy or an amino acid residu of the formula ##STR2## where X is hydrogen, alkyl or hydroxymethyl and n is an integer of 0 to 4 and R.sub.4 and R.sub.5 are alkyl, hydrogen, benzyl or cyclohexylmethyl.

Abstract: New peptides of the formula IX--Z--W--E--W'--Y Iwherein X, Z, W, E, W' and Y are as defined herein and their salts inhibit the activity of human plasma renin.

Abstract: Compounds of the formula ##STR1## are disclosed. These compounds intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as antihypertensive agents.

Abstract: The invention relates to novel peptides of enhanced pharmacological activity of the formula: ##STR1## wherein R.sup.1 is hydroxyalkanoyl,R.sup.2 and R.sup.q are each hydrogen, carboxy, protected carboxy, or a group of the formula: ##STR2## wherein R.sub.a.sup.2 is mono- or di-carboxy (or protected carboxy) lower alkyl or ar(carboxy or protected carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy, R.sup. 2 is hydrogen or lower alkyl; R.sup.p is hydrogen, carboxy, protected carboxy, with proviso that when one of R.sup.2 and R.sup.q is hydrogen, then the other is carboxy or protected carboxy or a group of the formula: ##STR3## wherein R.sub.a.sup.2 and R.sub.b.sup.2 are each as defined above; R.sup.r is hydrogen or amino protective group; m is an integer 1 to 3;or its pharmaceutically acceptable salt.

Abstract: New diamino acid derivatives of the formula IX--Z--NH--CH(CH.sub.2 R.sup.1)--CH(NH.sub.2)--CH.sub.2 --CO--E--G--Y IwhereinX is H, R.sup.2 --O--C.sub.n H.sub.2n --CO--, R.sup.2 --C.sub.n H.sub.2n --O--CO--, R.sup.2 --C.sub.n H.sub.2n --CO--, R.sup.2 --SO.sub.2, (R.sup.2 --C.sub.n H.sub.2n)--L(R.sup.2 --C.sub.r H.sub.2r)--C.sub.t H.sub.2t --CO--, H--(NHCH.sub.2 CH.sub.2).sub.n --NH--CH.sub.2 CO-- or 9-fluorenyl--C.sub.n H.sub.2n --O--CO--,Z is 0 to 4 amino acid radicals, bonded to one another in a peptide-like manner, selected from the group consisting of Abu, Ada, Ala, Arg, Dab, Gly, His, Ile, Leu, tert.-Leu, Lys, Met, Nbg, Nle, N-Me-His, N-Me-Phe, Orn, Phe, Pro, Ser, Thr, Tic, Trp, Tyr and Val,R.sup.1 is H, A, cycloalkyl with 3-7 C atoms, Ar or C.sub.p H.sub.2p --W,E is absent or is Ala, Gly, Ile, Leu, tert.-Leu, Met, Ser, Thr or Val,G is absent or is His, Phe, Trp, Tyr or --NH--CH(CH.sub.2 R.sup.1)--CH(NH.sub.2)--CH.sub.2 CO--,Y is --O--C.sub.m H.sub.2m --R.sup.3, --NH--C.sub.m H.sub.2m --R.sup.3, --NH--C.

Abstract: The invention relates to peptide derivatives modeled on the basis of pepstatin.These derivatives inhibit renin and acid proteases.

Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension and for treating hyperaldosteronism. Novel intermediates, processes for preparing both the intermediates and the novel peptides, pharmaceutical compositions, and methods of treatment are included.

Abstract: Antitumor amino acid and peptide derivatives of 1,4-bis[(aminoalkyl and hydroxyaminoalkyl)amino]-5,8-dihydroxyanthraquinones.

Abstract: A series of novel polypeptide derivatives, containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues, which are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin. Particularly valuable precursors for many of these compounds are certain other 5-amino-2,5-disubstituted-4-hydroxypentanoic acid derivatives.

Abstract: Retro-inverted peptides, analogues of Bradykinin Potentiator Pentapeptide (BPP.sub.5a), definable by the general formula (I) ##STR1## useful as antihypertensives and diagnostics.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, A represents an optionally N-alkylated .alpha.-amino acid residue which is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl having 2 or more carbon atoms, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy or optionally substituted mercapto and R.sub.

Abstract: The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is an N-protecting group; R.sub.1, R.sub.2 and R.sub.3 are independently selected from loweralkyl or lipophilic or aromatic amino acid side chains; and R.sub.4 is --CHO, --CO.sub.2 H, halomethyl or alkanoyl; and R.sub.5 is hydrogen or loweralkyl.

Abstract: A high-cysteine polypeptide having an amino acid sequence of the formula:-(.gamma.-Glu-Cys).sub.n -Glyin which,n is an integer from 4 to 7,.gamma.-Glu represents .gamma.-glutamic acid,Cys represents cysteine, andGly represents glycine,for use in pharmaceutical preparations for treating acute and chronic heavy metal poisoning. Alternatively, the polypeptides may be employed in the treatment of metal deficiency phenomena or for maintaining the homeostasis in physiological systems with respect to such metals as iron or zinc. Processes for producing the polypeptides of the invention are also disclosed.

Abstract: New peptide compounds having a lactone or cycloamide structure and containing a saturated bicyclic structure, pharmaceutically-acceptable acid addition salts thereof, method for the preparation thereof, pharmaceutical compositions containing the same, and use thereof for the stimulation of cyclic AMP in the cerebral tissue and consequently increasing the metabolic capacities of the brain, thereby making them of interest in the treatment of diseases of the central nervous system or disorders approximating normal or pathological aging, are disclosed.

Abstract: The invention relates to pepstatin analogs which inhibit renin and acid proteases.These analogs are particularly suitable for the treatment of arterial tension.

Abstract: The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is an N-protecting group; R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are independently selected from loweralkyl or lipophilic or aromatic amino acid side chains; and R.sub.4 is hydrogen, loweralkyl, loweralkylmercapto or loweralkylsulfonyl.

Abstract: New amino acid derivatives of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CHR.sup.4 --(CHR.sup.5).sub.n CO--B--D Iin which X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, B, D and n have the meanings defined herein, and their salts inhibit the activity of human plasma renin.

Abstract: Aminopeptidase inhibitory activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo-substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl or heteroaryl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, (heteroaryl)alkyl, ##STR2## R.sub.4 and R.sub.5 are each independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, or (heteroaryl)alkyl;A is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, valyl, aspartyl, prolyl, norleucyl, or norvalyl; andn is an integer of 1 to 6.

Abstract: Peptido-mimetic compounds of hypotensive action definable by the general formula: ##STR1## in which: X represents the pyroglutamic acid residue or a ##STR2## residue where R.sub.2 represents a hydrogen atom, an alkyloxycarbonyl, an arylalkyloxycarbonyl or an acyl group with from 1 to 7 carbon atoms in the linear chain,R.sub.1 represents the aromatic residue of L-phenylalanine, L-tyrosine or L-tryptophan, andZ represents a hydroxyl, hydroxyalkyl, amino or alkylamino group, and their salts and alkyl amides or esters.

Abstract: Novel peptides of the formula: ##STR1## wherein R is hydrogen or a lower alkyl group, or a pharmaceutically acceptable salt thereof, and processes for preparing the same are disclosed. The peptides and pharmaceutically acceptable salts thereof are useful for the treatment of central nervous system disorders.

Abstract: New peptides of the formula IX--Z--NH--CHR--CHOH--CH.sub.2 --CO--NH--CHR.sup.1 --CH.sub.2 --NH--CHY--C.sub.n H.sub.2n --R.sup.2 Iin whichX is H, R.sup.3 --O--CH.sub.2 --CO--, R.sup.3 --O--CO--, R.sup.3 --CH.sub.2 --O--CO-- or R.sup.3 --C.sub.m H.sub.2m --CO--,Z is 1 to 4 aminoacid residues which are bonded together in the manner of peptides and are selected from the group comprising Abu, Ala, Arg, Asn, Dab, Gln, Gly, His, Ile, Leu, Lys, Met, NLeu, Orn, Phe, Pro, Trp, Tyr and Val,is A, Ar-alkyl (in which the group -alkyl contains 1-4 C atoms) or cycloalkyl-alkyl having 4-11 C atoms,R.sup.1 is H or A,Y is H, A, --C.sub.p H.sub.2p --OR.sup.4, --C.sub.p H.sub.2p --NHR.sup.4, --COOR.sup.4, --CONHR.sup.4 or --CONA.sub.2,R.sup.2 is A, cycloalkyl having 3-7 C atoms, Ar, pyridyl, indolyl, imidazolyl, piperidyl, N-benzylpiperidyl or piperazinyl,R.sup.3 is A, cycloalkyl having 3-7 C atoms or Ar,R.sup.

Abstract: Sulfates of glutathione monoalkyl esters (alkyl.gamma.-L-glutamyl-L-cysteinylglycinates) are new and can be prepared by reaction of glutathione with an alcohol in the presence of sulfuric acid. This process forms virtually no diesters, which are toxic compounds and must be completely removed when the sulfates are used as medicine. In addition, since pure glutathione monoester sulfates can be isolated from reaction mixture, high-purity free glutathione monoesters, which have importance as therapeutical and preventive medicines, can be obtained by treatment with a neutralizer or by mere desalting.

Abstract: The present invention provides novel renin-inhibiting peptides of the formula X-A.sub.6 -B.sub.7 -C.sub.8 -D.sub.9 -E.sub.10 -F.sub.11 -G.sub.12 -H.sub.13 -I.sub.14 -Z, having a lactam pseudo-dipeptide at C.sub.8 -D.sub.9 positions, X and Z are terminal groups, and the remaining variables are absent or are amino acid residues. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension.

Abstract: This invention relates to a process for converting a teicoplanin-like compound into antibiotic L 17046 characterized in that a teicoplanin-like compound selected from teicoplanin complex, any further purified preparation thereof, teicoplanin factor A.sub.2, teicoplanin factor A.sub.3, each of the main components of teicoplanin factor A.sub.2, antibiotic L 17054 and a mixture of two or more of the above substances in any proportion is submitted to hydrolysis with a strong acid in the presence of a polar aprotic organic solvent selected from ethers, ketones and mixtures thereof that a room temperature are liquid.

Abstract: Certain functionalized cogeners of 1,3-dialkylxanthine exhibit high potency and selectivity as antagonists for A.sub.1 - and A.sub.2 -adenosine receptors and are suitable for attachment to probes, drug carriers, or solid supports. These derivatives are characterized by the presence of a phenyl at the 8 position para-substituted with a functionalized chain to provide high water solubility and high receptor affinity. Some of these analogs, containing a distal amino- or carboxylic-functionalized chain, are suitable for synthesis of amino acid conjugates. The compounds of this invention are suitable for use as antiallergenic, antiasthmatic, or cardiotonic drugs, central nervous system stimulants, and diuretics.

Abstract: The invention relates to the peptides of the formula: ##STR1## in which: R.sub.1 represents hydrogen or a protecting group for the amine group, such as t-butoxycarbonyl, benzyloxycarbonyl or lower alkanoyl groups;X represents beta-alanine glycine or a direct bond between R.sub.1 and the amine group; andR.sub.2 represents a group chosen from: ##STR2## corresponding to the side chains of the natural amino acid leucine, methionine and norleucine.These peptides inhibit gastric secretion.

Abstract: Analogs of substance P and eledoisin which are conformationally constrained by the presence of a lactam in the peptide chain demonstrate greater selectivity and increased protease stability and are useful as analgesic, anti-inflammatory, antihypertensive, central nervous system agents, and stimulants of lachrymal secretion. The compounds are prepared by standard peptide synthetic procedures.

Abstract: New diamino acid derivatives of the formula IX--Z--NH--CH(CH.sub.2 R.sup.1)--CH(NH.sub.2)--CH.sub.2 --CO--E--G--Y IwhereinX is H, R.sup.2 --O--C.sub.n H.sub.2n --CO--, R.sup.2 --C.sub.n H.sub.2n --O--CO--, R.sup.2 --C.sub.2n --CO--, R.sup.2 --SO.sub.2, (R.sup.2 --C.sub.n H.sub.2n)--L(R.sup.2 --C.sub.r H.sub.2r)--C.sub.t H.sub.2t --CO--, H--(NHCH.sub.2 CH.sub.2).sub.n --NH--CH.sub.2 CO-- or 9-fluorenyl--C.sub.n H.sub.2n --O--CO--,Z is 0 to 4 amino acid radicals, bonded to one another in a peptide-like manner, selected from the group consisting of Abu, Ada, Ala, Arg, Dab, Gly, His, Ile, Leu, tert.-Leu, Lys, Met, Nbg, Nle, N--Me--His, N--Me--Phe, Orn, Phe, Pro, Ser, Thr, Tic, Trp, Tyr and Val,R.sup.1 is H, A, cycloalkyl with 3-7 C atoms, Ar or C.sub.p H.sub.2p --W,E is absent or is Ala, Gly, Ile, Leu, tert.-Leu, Met, Ser, Thr or Val,G is absent or is His, Phe, Trp, Tyr or --NH--CH(CH.sub.2 R.sup.1)--CH(NH.sub.2)--CH.sub.2 CO--,Y is --O--C.sub.m H.sub.2m --R.sup.3, --NH--C.sub.m H.sub.2m --R.sup.3, --NH--C.sub.

Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.

Abstract: A compound of the formula: ##STR1## wherein R.sub.1 is alkoxy containing one to six carbon atoms or lower alkyl containing one to six carbon atoms; R.sub.2 is benzyl or napthylmethyl, R.sub.3 is lower alkyl containing one to six carbon atoms or imidazolemethyl; R.sub.4 is benzyl, R.sub.5 is hydrogen or lower alkyl and n is 0 or 1. These compounds are useful as renin inhibitors.

Abstract: New retro-inverso peptides and peptide derivatives in the form of analogues of C-terminal hexapeptide fragments of Substance P, which are pharmacologically active, possess prolonged action with time, and are of general formula (I): ##STR1## they being useful as vasedilators.

Abstract: Peptides wherein an amide bond is replaced by nonhydrolyzable isosteric linkage are disclosed as thrombogenic inhibitors.

Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.

Abstract: Peptide-substituted heterocyclic compounds having the formula below, pharmaceutically acceptable salts thereof and intermediates therefor; processes for their preparation and use as immunostimulant and antiinfective agents. ##STR1## wherein R is a 5- or 6-membered N-containing heterocyclyl moiety which can have an additional hetero atom selected from N, S or O; R.sup.1 is hydrogen or (C.sub.1-4)alkyl; x is 0 or an integer from 1 to 5; and y is 0 or 1; provided that when y is 0, said N-containing heterocyclyl moiety is linked to the ##STR2## group at its N atom.

Abstract: The present invention is directed to a chemical process for preparing the antibiotic substance denominated antibiotic L 17054 and its pharmaceutically acceptable salts by selectively hydrolyzing teicoplanin or a factor or component thereof with a concentrated strong organic acid.

Abstract: An enkephalin-degrading aminopentidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15; A.sub.2, A.sub.3, A.sub.4 and A.sub.