首页> 外国专利> Analogifremgangsmaade for the preparation of LRF analogs nona- or decapeptidamider or non-toxic salts thereof and nona- or decapeptide derivatives for use as starting materials in the process

Analogifremgangsmaade for the preparation of LRF analogs nona- or decapeptidamider or non-toxic salts thereof and nona- or decapeptide derivatives for use as starting materials in the process

机译:用于制备LRF类似物九肽或十肽酰胺或其无毒盐以及九肽或十肽衍生物的类似物

摘要

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-R1-R2-R3-Ser-Tyr-R4-R5-Arg-Pro-R6 wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R1 is dehydro Pro, dehydro D-Pro, Thz or D-Thz; R2 is D-Phe, D-His, D-Trp, Trp, CI-D-Phe, dichloro-d-Phe, CF3-D-Phe, F-D-Phe, difluoro-D-Phe, AcNH-D-Phe, NO2-D-Phe, di-nitro-D-Phe, Br-D-Phe, dibromo-D-Phe, CH3S-D-Phe, OCH3-D-Phe or CH3-D-Phe; R3 is D-Trp, Trp, D-Phe or D-His; R4 is Gly or a D-isomer amino acid; R5 is Leu or N alpha Me-Leu; and R6 is Gly-NH2 or NHCH2CH3.
机译:抑制垂体分泌促性腺激素并抑制性腺释放类固醇的肽。给予有效量可防止雌性哺乳动物卵排卵和/或性腺释放类固醇。所述肽具有以下结构:X-R1-R2-R3-Ser-Tyr-R4-R5-Arg-Pro-R6,其中X是氢或碳原子数为7以下的酰基。 R1是脱氢Pro,脱氢D-Pro,Thz或D-Thz; R 2是D-Phe,D-His,D-Trp,Trp,CI-D-Phe,二氯-d-Phe,CF3-D-Phe,FD-Phe,二氟-D-Phe,AcNH-D-Phe, NO2-D-Phe,二硝基-D-Phe,Br-D-Phe,二溴-D-Phe,CH3S-D-Phe,OCH3-D-Phe或CH3-D-Phe; R3是D-Trp,Trp,D-Phe或D-His; R4是Gly或D-异构体氨基酸; R5是Leu或Nα-Me-Leu; R6为Gly-NH2或NHCH2CH3。

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