Pharmaceutical compositions for the sublingual or buccal administration of therapeutic agents (particularly polypeptides) which are normally degraded upon oral administration comprise such a therapeutic agent, a solvent, optionally a cosolvent and/or hydrogel, and an oral mucosal membrane transport enhancing agent which is selected from the group consisting of essential and volatile oils and inorganic and organic acids.

Compositions and methods for the sublingual or buccal administration of therapeutic agents

4-methyloxybenzyloxycarbonyl (Moz) is used to protect the alpha amino groups of the amino acids used in solid-phase synthesis of thymosin α 1 . It was found that the Moz group can be removed rapidly and completely with 5-10% trifluoroacetic acid in CH 2 Cl 2 . Some advantages of utilizing Moz-amino acids over Boc-amino acids in solid-phase peptide synthesis are higher yields and purities with reduced consumption of trifluoroacetic acid during the acidolytic cleavage of the N.sup.α -Moz groups. Further improvements with respect to the recovery and recycling of the used solvent are obtained by using tributylamine in place of triethylamine as the neutralization agent making it possible to distill methylene chloride from the liquid waste without contamination by the lower boiling triethylamine. Methylbenzhydrylamine resin is the preferred resin support. Cleavage from the resin support and deprotection of the protected side groups of the protected thymosin α 1 can be accomplished using either HBr or trifluoromethane sulfonic acid in trifluoroacetic acid with anisole and thioanisole as scavengers.

A solid phase process for synthesizing Thymosin alpha 1

The invention relates to new gonadoliberin derivatives of the formula (I) Glp-His-Trp-Ser-Tyr-X-Leu-Arg-Pro-Y, (I) wherein Y 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.

Gonadoliberin derivatives process for the preparation and pharmaceutical compositions thereof

The present invention provides for a method for inducing sterility in fish by administering at least one compound that disrupts the establishment of the gonadotropin-releasing hormone system during early development thereby inhibiting sexual maturity in the treated fish. Effective compounds include GABA, GABA receptor agonists, or GABA receptor antagonists.

Inducing sterility in fish by disrupting the development of the GnRH system

Peptides which include unnatural amino acids and which either promote or inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such peptides that are GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads and may be used to treat steroid-dependent tumors. The agonists can be used for control of reproduction processes, to treat precocious puberty, endometriosis, and the like. The peptides are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions. Unnatural amino acids having the following formula are incorporated in a preferred group of synthesized peptides:

Peptide intermediates for making GnRH antagonists

The peptide having the following formula has a potent effect on the reproduction processes of fish and is termed Fish GnRH: pGlu-His-Trp-Ser-Tyr-Gly-Trp-Leu-Pro-Gly-NH2. Spawning of teleostei fish can be promoted by administration of effective amounts of the peptide.

Peptides affecting gonadal function

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Peptides affecting gonadal function