Abstract: This invention concerns novel sustained release microcapsule compositions comprising water-soluble, hormonally active polypeptides and, optionally, a polymer hydrolysis modifying agent encapsulated in a biocompatible, biodegradable polymer.

Abstract: A method for treating anestrus in ewes and beef cattle by treating a ewe or a beef cow for 4 to 16 days with a gestagen having protracted action, followed by administering LH-RH or an analogous compound of at least the same efficiency for 2 to 6 days to bring about an LH plasma level sufficient to induce ovulation.

Abstract: A pharmaceutical composition containing a hydrophilic drug which is poorly absorbable through the gastrointestinal tract, and cyclodextrin, increases the absorbability of the drug into the mammalian body when administered by a non-oral or non-injection route.

Abstract: Synthetic nonpeptide and decapeptide LHRH antagonist analogs have a novel guanido-substituted, amidine, tertiary or quaternary amine water-soluble aminoacyl residue at position 6.

Abstract: Novel peptides of the formula: ##STR1## where R.sup.1 through R.sup.8 are various radicals derived from L- and D- amino acids; having LHRH antagonist activity; useful in reducing fertility.Pharmaceutical compositions and methods for use in reducing fertility.

Abstract: A method of treatment of prostate cancer in susceptible male animals including humans whose testicular hormonal secretions are blocked by surgical or chemical means, e.g., by use of an LH-RH agonist, e.g., [D-Trp.sup.6, des-Gly-NH.sub.2.sup.10 ]LH-RH ethylamide which comprises administering an antiandrogen, e.g., flutamide in association with at least one inhibitor of sex steroid biosynthesis, e.g., aminoglutethimide and/or ketoconazole. Pharmaceutical compositions useful for such treatment and three, four and five component kits containing such compositions are also disclosed.

Abstract: A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.

Abstract: Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The peptides have the structure: X-R.sub.1 -R.sub.2 -R.sub.3 -Ser-Tyr-R.sub.6 -R.sub.7 -Arg-Pro-R.sub.10 wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R.sub.1 is dehydro-Pro or .beta.-D-NAL; R.sub.2 is Cl-D-Phe, F-D-Phe, NO.sub.2 -D-Phe, C.sup..alpha. Me-4-Cl-D-Phe, Cl.sub.2 -D-Phe or Br-D-Phe; R.sub.3 is D-Trp, substituted D-Trp, .beta.-D-NAL, or D-PAL; R.sub.6 is a D-isomer of a lipophilic amino acid or is 4-NH.sub.2 -D-Phe, D-Lys, D-Orn, D-Har, D-His, 4-gua-D-Phe, D-PAL or D-Arg; R.sub.7 is Nle, Phe, Met, Tyr, Nva, Trp, Cys, PAL or 4F-D-Phe; and R.sub.10 is Gly-NH.sub.2 or D-Ala-NH.sub.2 ; provided however that when R.sub.1 is .beta.-D-NAL, then R.sub.6 is 4-NH.sub.2 -D-Phe, D-Lys, D-Orn, D-Har, D-His, 4-gua-D-Phe, D-PAL or D-Arg.

Abstract: The invention relates to gonadoliberin derivatives of the general formula (I)Glp--His--Trp--Ser--Tyr--X.sub.1 --X.sub.2 --X.sub.3 --Pro--X.sub.4whereinX.sub.1 is a glycyl group or a D-isomer of any natural or synthetic amino acid group,X.sub.2 represents an L-amino acid group having 1 to 4 carbon atoms in the side chain, L-phenyl-alanyl or L-tryptophyl group,X.sub.3 represents an L-amino acid group having a C.sub.1-4 alkyl or C.sub.2-4 alkanoyl-amide side chain, andX.sub.4 is a glycine amide or a C.sub.1-4 alkyl amide group,with the proviso that if X.sub.1 stands for a group other than glycyl and X.sub.2 is a tryptophyl group then X.sub.3 may not be leucyl, and the addition salts formed with therapeutically useable acids and complexes thereof. Furthermore the invention relates to a process for preparing these compounds.The new gonadoliberin derivatives can be effectively used for the reproduction process of fish, birds and mammals.

Abstract: The invention relates to a process for obtaining ready-for-fertilization sexual products from sexually mature fish in a period independent of their natural spawning season, in which actual stage of ripening is determined by probing of sexual products [sperm or eggs], fish not yet ripe for ovulation are separated from ripe fish, compounds of hormonal effect are administered to fish, and after the ovulation sexual products are obtained from the fish or from their environment.In the process according to the invention a nonapeptide-C.sub.1-4 -alkyl-amide or a decapeptide amide of the general formula (I),Glp-His-Trp-Ser-Tyr-X.sub.1 -X.sub.2 -X.sub.3 -Pro-X.sub.4 (I)whereinX.sub.1 is a glycyl group or a D-isomer of any natural or synthetic amino acid group,X.sub.2 represents an L-amino acid group having 1 to 4 carbon atoms in the side chain, L-phenyl-alanyl or L-tryptophyl group,X.sub.3 represents an L-amino acid group having a C.sub.1-4 alkyl or C.sub.2-4 alkyl-amide side chain,X.sub.4 is a glycine-amide or a C.

Abstract: A compound having the formula K-His-Trp-Ser-Tyr-M-Q-Arg-Pro-T, wherein K is N-Acetyl-Sarconsine or pGlu; is D-Phe, D-Trp, D-.beta.-Naphthylalanine, or D-4-X-Phe, wherein X is OH, F, Cl, Br, or Me; Q is Leu, Phe, 4-X-Phe, Trp, or .beta.-Naphthylamine (wherein X is OH, F, Cl, Br, or Me), or an N-Me-derivative thereof; and T is Gly-NH.sub.2, NHCH.sub.3, NHCH.sub.2 CH.sub.3, or NHCH.sub.2 CH.sub.2 CH.sub.3 ; provided that, when Q is Leu or N-Me-Leu, K cannot be pGlu; or a pharmaceutically acceptable salt thereof.

Abstract: Therapeutically useful pseudopeptides characterized by the replacement of at least one peptide group, both in a naturally occurring peptide or protein by a thiomethylene group are useful in the treatment of various metabolic malfunctions.

Abstract: The invention relates to novel peptides and peptide derivatives which act as antagonists of natural LH-RH and have the general formula:X-R.sup.1 -R.sup.2 -R.sup.3 -Ser-Tyr-R.sup.4 -R.sup.5 -R.sup.6 -R.sup.7 -R.sup.8 -NH.sub.2whereinX represents hydrogen or a lower acyl(1-6 C) group,R.sup.1 and R.sup.2 represent either the same or different groups selected from D-Bal(2), D-Bal(3), D-Nal(1), D-Nal(2), D-Phe or D-Phe substituted at the phenyl moiety by one or more halogen, alkyl(1-4 C), alkoxy (1-4 C) or nitro groups;R.sup.3 represents D-Trp, D-Bal(2), D-Bal(3), D-Nal(1), D-Nal(2) or D-Pal, with the proviso that at least one of the symbols R.sup.1 and R.sup.3 represents a D-Bal(2) or D-Bal(3) group;R.sup.4 represents D-Arg, D-Lys, D-homo Arg or D-dialkyl (1-4 C)-homo Arg;R.sup.5 represents L-Leu, L-Met or the alkyl(1-4C) or phenylalkyl(7-10C) ether of L-Cys, L-Ser or L-homo Ser;R.sup.6 represents L-Lys or L-Arg;R.sup.7 represents L-Pro or L-thiaprolyl, andR.sup.8 represents D-Ala or Gly.

Abstract: Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The peptides have the structure:X-R.sub.1 -R.sub.2 -D-Trp-Ser-R.sub.5 -R.sub.6 -Leu-Arg-Pro-R.sub.10wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R.sub.1 is dehydro-Pro, D-pGlu, D-Phe, D-Trp or .beta.-D-NAL; R.sub.2 is Cl-D-Phe, F-D-Phe, C.sup..alpha. Me-4-Cl-D-Phe, NO.sub.2 -D-Phe, Cl.sub.2 -D-Phe or Br-D-Phe; R.sub.5 is Tyr, I-Tyr, CH.sub.3 -Phe, F-Phe or Cl-Phe; R.sub.6 is a D-isomer of a lipophilic amino acid or is 4-NH.sub.2 -D-Phe, 4-gua-D-Phe, D-His, D-Lys, D-Orn, D-Har or D-Arg; and R.sub.10 is Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-Y, with Y being lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR1## where Q is H or lower alkyl. When R.sub.1 is .beta.-D-NAL, R.sub.6 is 4-NH.sub.

Abstract: A conjugate between a nona- or decapeptide of the formula (i) or (ii):Lys-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH.sub.2, (i)orCys-Lys-Trp-Ser-Try-Gly-Leu-Arg-Pro-Gly-NH.sub.2, (ii)or mixtures of peptides (i) and (ii).and a protein is provided which, when used per se or when mixed with a suitable adjuvant, yields a vaccine which acts as an immunogen for LHRH and induces a mammal to produce antibodies which react with LHRH. Immunization against the body's LRHR results in lowering of male and female sex hormones including luteinizing hormone so as to prevent conception. Other uses for materials which lessen the effect of LHRH in the body are known in the art.

Abstract: The invention relates to new gonadoliberin derivatives of the formula (I)Glp-His-Trp-Ser-Tyr-X-Leu-Arg-Pro-Y, (I)whereinY represents a glycine-amide group or an -NH-alkyl group having 1 to 4 carbon atoms in the alkyl moiety,X stands for a D-thyroxyl, D-thyronyl or D-4-chlorophenylalanyl group,and acid addition salts and metal complexes thereof.The new nona- and decapeptide derivatives have an excellent luteinizing and folliculus stimulating hormone releasing activity, and they can therefore be used as active ingredients in pharmaceutical compositions for human or veterinary application.

Abstract: Synthetic nonapeptide and decapeptide LHRH agonists analogs having a novel gaunadino-substituted, amidine, tertiary or quatrinary aminoacyl residue at position 6 are disclosed herein.