American Home Products Corporation

Ayerst, Mckenna & Harrison, Inc.

Hans U Immer

Manfred K Gotz

Amedeo Failli

Verner R Nelson

Kazimir Sestanj

Nedumparambil A Abraham

Francesco Bellini

Jean-Marie Ferland

Menfred K Gotz

Nedumparampil A Abraham

Marvin M Kobric

The N-substituted dimeric cyclopeptide derivatives of formula ##STR1## in which A is a peptide residue having one to four amino acid residues; R.sup.1 is lower alkyl, phenyl or phenyl(lower)alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; and R.sup.3 is a neutral amino acid side chain and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful for treating microbial infections. Pharmaceutical compositions also are disclosed.

N-Substituted dimeric cyclopeptide derivatives

The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed.

N-Substituted cyclopeptide derivatives

Herein is described a process for preparing the decapeptide Pry-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2 ([D-Trp.sup.6 ]-LH-RH) by coupling Pyr-His-Trp-NHNH.sub.2 with H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2. [D-Trp.sup.6 ]-LH-RH had been established to be an efficient agent for causing release of lutenizing hormone and follicle-stimulating hormone in mammals.

Preparation of (D-Trp .sup.6)-LH-RH via the heptapeptide

The N-substituted dimeric cyclopeptide derivatives of formula ##STR1## in which A is a peptide residue having one to four amino acid residues; R.sup.1 is lower alkyl, phenyl or pheny(lower) alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; R.sup.3 is a neutral amino acid side chain and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful for treating microbial infections. Pharmaceutical compositions also are disclosed.

N-substituted dimeric cyclopeptide derivatives and preparation thereof

Peptides of formula I ##STR1## in which X is (CH.sub.2).sub.2, S--CH.sub.2 or CH.sub.2 --S or a therapeutically acceptable acid addition salt thereof are disclosed. The peptides of formula I are useful as agents for the treatment of acromegaly and the management of diabetes in a mammal. Compositions and methods for the preparation of the peptides of formula I are also disclosed.

Carba decapeptide derivatives of [TYR.sup.6 ]-somatostatin

N-substituted cyclopeptide derivatives and preparation thereof

Compounds of the formula HSCH.sub.2 CHR.sup.1 CO--Pro--R.sup.2 --R.sup.3 --OH in which R.sup.1 is hydrogen or lower alkyl, R.sup.2 is an amino acid residue exclusive of prolyl and R.sup.3 is an amino acid residue exclusive of glutamyl are useful for alleviating angiotensin related hypertension.

Tripeptide angiotensin converting enzyme inhibitors

N-[N-[N-[N-[N-(5-Oxo-L-prolyl)-L-histidyl]-L-tryptophyl]-L-seryl]-L-tyrosyl ]glycine hydrazide trifluoroacetate is converted to N-[N-[N-[N-[N-(5-oxo-L-prolyl)-L-histidyl]-L-tryptophy]-L-seryl]-L-tyrosyl ]glycine azide, a useful intermediate for preparing LH and FSH releasing hormone.

N-[N-[N-[

A process for preparing the LH- and FSH-releasing hormone of the formula I

Process for preparing the releasing hormone of luteinizing hormone (LH)

Compounds of the formula 1 or 1a ##STR1##

Decapeptide analogs of somatostatin

Dipeptide derivatives with central nervous system activity and

A new process for preparing the cyclic dodecapeptide triglycyl-lysine vasopressin of the formula ##STR1## which comprises the preparation of a first hexapeptide of formula Boc--Gly--Gly--Gly--Cys(Trt)--Tyr--Phe--NHNH.sub.2 and a second hexapeptide of formula H--Gln(Mbh)--Asn(Mbh)--Cys(Trt)--Pro--Lys(Boc)--Gly--NH.sub.2 by a series of condensations involving the reaction of an appropriately protected peptide unit having an activated carboxyl with an appropriately protected peptide having a free amino group. Subsequently, the first and second hexapeptides are condensed according to the azide coupling method to obtain the linear protected dodecapeptide of formula Boc--Gly--Gly--Gly--Cys(Trt)--Tyr--Phe--Gln(Mbh)--Asn(Mbh)--Cys(Trt)--Pro- -Lys(Boc)--Gly--NH.sub.2 ; thereafter the linear protected dodecapeptide is transformed into the desired cyclic dodecapeptide, triglycyllysine vasopressin, by oxidizing and deprotecting processes.

Process for producing triglycyl-lysine vasopressin and intermediates

Compounds of the formula 1 or 1a ##STR1## wherein R.sup.1 is H--, H--Gly or H--Leu and R.sup.2 is H or COOH and pharmaceutically acceptable salts thereof, are disclosed. The compounds of formulae 1 and 1a are useful for the management of diabetes and the treatment of acromegaly. Methods for their use are also disclosed.

Extended chain derivatives of somatostatin

Pyridylmethyl esters of N-(phenoxyalkanoyl)peptide derivatives are disclosed. The derivatives are characterized by having a phenoxyalkanoyl group and a pyridylmethyloxy group-joined together by a peptide group. They possess antihyperlipoproteinemic activity. In addition, methods for their preparation and use are disclosed.

Growing community of inventors

Mount Royal, Canada

Hans U Immer