Abstract: The present invention deals with LHRH antagonists which possess improved water solubility and while having the high antagonist potency of the basic peptides, are free of the edematogenic effects. These compounds are highly potent in inhibiting the release of gonadotropins from the pituitary gland in mammals, including humans.The compounds of this invention are represented by the formulaX-R.sup.1 -R.sup.2 -R.sup.3 -Ser-Tyr-R.sup.6 -Leu-Arg-Pro-R.sup.10 -NH.sub.2whereinX is an acyl group derived from straight or branched chain aliphatic or alicyclic carboxylic acids having from 1 to 7 carbon atoms,R.sup.1 is D- or L-Pro, D- or L- .DELTA. .sup.3 -Pro, D-Phe, D-Phe(4-H1), D-Ser, D-Thr, D-Ala, D-Nal (1) or D-Nal (2),R.sup.2 is D-Phe or D-Phe(4-H1)R.sup.3 is D-Trp, D-Phe, D-Pal, D-Nal(1) or D-Nal (2),R.sup.6 is D-Cit, D-Hci, D-Cit(Q) or D-Hci(Q) andR.sup.

Abstract: Novel compositions of the formula ##STR1## wherein A represents an L, D or DL amino-acid selected from the group consisting of Ala, Val, Phe, p-Cl-Phe, Trp, Pro, Ser, Thr, Glu, Gly, Beta Ala, Abu, N-Me Ala, 5-F-Trp, 5-Br-Trp, 5-Cl-Trp, their acetylated derivatives or a pharmaceutically acceptable acid addition salt thereof;B represents an L, D or DL amino acid amide selected from the group consisting of Thr NH.sub.2, Val NH.sub.2, Pro NH.sub.2, HO-Pro NH.sub.2, Ser NH.sub.2, Tyr NH.sub.2, Trp NH.sub.2, 5-F-Trp NH.sub.2, For-Trp NH.sub.2, Ala NH.sub.2, Gly NH.sub.2, Me Ala NH.sub.2 ;X represents L-Phe or L-Tyr,Y represents L-Thr or L-Val;Z is L, D or DL-5-F-Trp, 5-Br-Trp, 5-Cl-Trp, 5-I-Trp or D-Trp; andC" and C' represent L or D Cys, Abu, Asp or Lys; and the pharmaceutically acceptable acid addition salts thereof; are useful as agents for inhibiting the release of growth hormone, for the treatment of gastrointestinal disorders and for therapy of certain cancers and the management of diabetes.

Abstract: Novel compositions of the formula ##STR1## wherein A represents an L, D or DL amino-acid selected from the group consisting of Ala, Val, Phe, p-Cl-Phe, Trp, Pro, Ser, Thr, Glu, Gly, Beta Ala, Abu, N-Me Ala, 5-F-Trp, 5-Br-Trp, 5-Cl-Trp, their acetylated derivatives or a pharmaceutically acceptable acid addition salt thereof;B represents an L, D or DL amino acid amide selected from the group consisting of Thr NH.sub.2, Val NH.sub.2, Pro NH.sub.2, HO-Pro NH.sub.2, Ser NH.sub.2, Tyr NH.sub.2, Trp NH.sub.2, 5-F-Trp NH.sub.2, For-Trp NH.sub.2, Ala NH.sub.2, Gly NH.sub.2, Me Ala NH.sub.2 ;X represents L-Phe or L-Tyr,Y represents L-Thr or L-Val;Z is L, D or DL-5-F-Trp, 5-Br-Trp, 5-Cl-Trp, 5-I-Trp or D-Trp; andC" and C' represent L or D Cys, Abu, Asp or Lys; and the pharmaceutically acceptable acid addition salts thereof; are useful as agents for inhibiting the release of growth hormone, for the treatment of gastrointestinal disorders and for therapy of certain cancers and the management of diabetes.

Abstract: There are disclosed peptides of the formula A-B-C and pharmaceutically acceptable salts thereof, in which A is selected from the group consisting of L-pyroglutamyl, D-pyroglutamyl, and L-homo-pyroglutamyl; B is selected from the group consisting of L-histidyl, L-3'-methylhistidyl, D-histidyl, L-phenylalanyl, L-p-aminophenylalanyl, and L-.beta.-(pyrazolyl-1)alanyl; and C is selected from the group consisting of glycine and lower alkyl esters thereof, glycinamide and lower alkyl amides thereof, 2-amino-1-hydroxyethyl, D-alanine, L-.beta.-(2-thienyl)-alanine, and NHR.sup.1 in which R.sup.1 is lower alkyl, with the proviso that C may not be glycine or glycinamide when A is L-pyroglutamyl and B is L-histidyl.The compounds have anorexigenic properties, inhibit excessive gastric and pancreatic secretion, and cause activation in the CNS. Methods for their preparation and use are also disclosed.

Abstract: Disclosed herein are peptide analogs of the luteinizing hormone releasing hormone (LH-RH) which are potent antagonist of LHRH. The analogs differ in structure from LH-RH by having different amino acid residues at positions 1, 2 and 6, and optionally at positions 3 and 10. Methods for preparing and using these analogs are described.

Abstract: Tetradecapeptides of the formula ##STR1## in which A represents L, D or DL 5- or 6- fluoro-, bromo-,chloro- or iodotryptophyl, or a therapeutically acceptable acid addition salt thereof, their preparation and intermediates for their preparation are disclosed. The tetradecapeptides are useful for inhibiting the release of growth hormone. Compositions and methods for their use also are disclosed.

Abstract: [D-Ser.sup.4,D-Leu.sup.6,desGly-NH.sub.2.sup.10 ]-LH-RH (lower alkyl)amides, salts thereof, and intermediates used for the synthesis thereof are disclosed. The compounds have potent LH- and FSH-releasing hormone properties.

Abstract: The decapeptide [D-Trp.sup.6 ]-LH-RH, salts thereof, and intermediates used for the synthesis thereof are disclosed. The decapeptide has potent LH- and FSH-releasing hormone properties.