Luteinizing and follicle-stimulating hormones releasing...

C - Chemistry – Metallurgy – 07 – K

Patent

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530/7.2

C07K 7/23 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1206959

ABSTRACT OF THE DISCLOSURE: The present invention relates to new, biologically active nonapeptides of the general formula (I) 1 2 3 4 5 6 7 9 pGlu-His-Trp-Ser-Tyr-D-Tle-Leu- Image -Pro-NH-Et (I) wherein X represents a hydrogen atom or a protective group, preferably a p-toluenesulfonyl (tosyl) radical. These new substances are synthetic analogs of the luteinizing and follicle-stimulating hormones releasing factor and have high gonadotropic activity. The substances are expected to find use in human and veterinary medicine, especially for the control of the estral cycle, for the treatment of estral disturbances or as a nonsteroidal contraceptive. The nona- peptide compounds of the formula (I) can be prepared by processes which comprise reactions of combining the respec- tive amino acid or lower peptide radicals with the use of preparative methods of the peptide chemistry. Preferable original methods for the elimination of the protective tosyl group in the position 8 and for the isolation and purifica- tion of the successive products are described.

434011

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