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Machine translation
1. (WO1982000004) CONTRACEPTIVE TREATMENT OF MALE MAMMALS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1982/000004    International Application No.:    PCT/US1980/000818
Publication Date: 07.01.1982 International Filing Date: 26.06.1980
IPC:
C07K 7/23 (2006.01), A61K 38/00 (2006.01)
Applicants: THE SALK INSTITUTE FOR BIOLOGICAL STUDIES
Inventors:
Priority Data:
Title (EN) CONTRACEPTIVE TREATMENT OF MALE MAMMALS
(FR) TRAITEMENT CONTRACEPTIF DES MAMMIFERES MALES
Abstract: front page image
(EN)Peptides which are LRF analogs that inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads can be effective contraceptives when administered to male mammals. The peptides are LRF antagonists having a binding affinity at least about 15 times that exhibited by LRF and which have an ICR50 of less than 1/1. Examples of peptides which may be used are those having the structure: R1-R2-R3-D-Trp-Ser-Tyr-R4-Leu-Arg-Pro-Gly-NH2 wherein R1 is selected from the group consisting of hydrogen, formyl, acetyl, acrylyl, benzoyl and allyl; R2 is selected from the group consisting of dehydro Pro, dehydro D-Pro, Thz and D-Thz; R3 is selected from the group consisting of pCl-D-Phe, pF-D-Phe, pNO2-D-Phe and 3, 4 Cl-D-Phe; R4 is selected from the group consisting of D-Trp and (imBzl) D-His; and Leu may be substituted by N(Alpha)MeLeu.
(FR)Des peptides, qui sont des analogues LRF qui inhibent la secretion des gonadotropines par la glande pituitaire et inhibent la liberation de steroides par les gonades, peuvent etre des contraceptifs efficaces lorsqu'ils sont administres a des mammiferes males. Les peptides sont des antagonistes de LRF ayant une affinite de liaison au moins quinze fois environ superieure a celles du LRF et ont un ICR50 inferieur a 1/1. Des exemples de peptides qui peuvent etre utilises sont ceux qui possedent la structure suivante: R1-R2-R3-D-Trp-Ser-Tyr-R4-Leu-Arg-Pro-Gly-NH2 ou R1 est selectionne parmi le groupe constitue de l'hydrogene, le formyle, l'acetyle, l'acrylile, le benzoyle, et l'allyle; R2 est selectionne parmi le groupe constitue de dehydro Pro, dehydro D-Pro, Thz et D-Thz; R3 est selectionne parmi le groupe constitue de pCl-D-Phe, pF-D-Phe, pXNO2-OD-Phe et Cl-D-Phe 3, 4; R4 est selectionne parmi le groupe constitue de D-Trp et (imBzl) D-His; et Leu peut etre substitue par N(Alpha)Ne- Leu.
Designated States:
Publication Language: English (EN)
Filing Language: English (EN)