The present invention relates to an improved process for the preparation of Cetrorelix acetate (1). More particularly, the present invention relates to the purification of Cetrorelix acetate (1) by simple method. ##STR00001##

The present invention relates to an improved process for the preparation of Cetrorelix acetate (1). More particularly, the present invention relates to the purification of Cetrorelix acetate (1) by simple method. ##STR00001##

The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.

The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.

The present invention provides immune stimulating peptides (immunorhelins) capable of stimulating GnRH receptors when dosed to human patients or cells. These immunorhelins have utility in treating viral diseases and cancer.

The present invention provides immune stimulating peptides (immunorhelins) capable of stimulating GnRH receptors when dosed to human patients or cells. These immunorhelins have utility in treating viral diseases and cancer.

Provided herein are luteinizing hormone-releasing hormone (LHRH) peptide derivatives that target the LHRH receptor. LHRH peptide derivatives, LHRH peptide-drug conjugates (LHRH-PDCs) and methods of using the derivatives and/or conjugates thereof to treat a LHRH receptor expressing cancer are described.

The invention relates to a compound or a salt thereof, a method for preparation thereof, and use thereof, wherein the compound has the structure of Formula (1):

##STR00001## the substituents in Formula (1) are as defined in the specification. The compound of Formula (1) or a salt thereof can be attached to a solid-phase resin, on which solid-phase synthesis may be performed.

The invention relates to a compound or a salt thereof, a method for preparation thereof, and use thereof, wherein the compound has the structure of Formula (1):

##STR00001## the substituents in Formula (1) are as defined in the specification. The compound of Formula (1) or a salt thereof can be attached to a solid-phase resin, on which solid-phase synthesis may be performed.

The present invention relates to a novel long-acting palmitic acid-conjugated gonadotrophin-releasing hormone (GnRH) derivative and a pharmaceutical composition containing the same. A GnRH derivative of the present invention is expected to greatly contribute, through excellent bioavailability and increased half-life in blood, to the reduction in drug dosing frequency and dosage and the like in the treatment of sex hormone-dependent diseases. Particularly, the GnRH derivative can overcome the disadvantages of existing GnRH sustained-release preparations, which have the side effects of residual feeling and pain at the injection site.