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2024年3月10日发(作者：int是多少位的)

专利内容由知识产权出版社提供

专利名称：Polypeptides

发明人：BOISSONNAS ROGER,GUTTMANN STEPHAN

申请号：US3546060

申请日：19600613

公开号：US3232923A

公开日：19660201

摘要：The invention comprises the cyclic polypeptide of the formula p I, and the

nonapeptide of the formula II, in which R and R1 each represents a protective group for

the sulphhydryl group, with the proviso that R and R1 need not be dissimilar, and R11 and

R111 each represents a protective group for the amino group with the proviso that R11

and R111 need not be dissimilar and with the further proviso that all of R, R1, R11 and

R111 may represent hydrogen atoms and pharmaceutical compositions containing the

polypeptide. The groups R and R1 are particularly benzyl groups, R11 a carbobenzoxy

group and R111 a p-toluenesulphonyl group. The compounds of the invention may be

prepared by condensing the hexapeptide VIII, after splitting off the carbobenzoxy group,

with the azide of the tripeptide VIII, to give the nonapeptide II, treating this with an alkali

metal in liquid ammonia to yield the free nonapeptide and oxidising this to the cyclic

polypeptide I by air or hydrogen peroxide. The hexapeptide VIII is prepared by

condensing N-carbobenzoxy-L-glutaminyl-L-asparaginyl- S-benzyl- L-cysteinyl -azide with

L-propyl-e -N-p-toluenesulphonyl- L-lysylgylcinamide prepared by hydrolysis of N-

carbobenzoxy-L -prolyl-e -N- p-toluenesulphonyl-L-lysylglycinamide with hydrobromic

acid. The tripeptide azide VIII is prepared by condensing N-carbobenzoxy- S-benzyl-L-

cysteinyl-L-phenyl-alanine with L-phenylalanine methyl ester and converting the

tripeptide ester in the azide with hydrazine. Pharmaceutical compositions comprise the

cyclic polypeptide in addition to an inert carrier. The compositions may be formulated as

solutions for injection or as nasal sprays. The peptide may be stored in the dry state

when mixed with a water soluble carrier, e.g. sodium chloride, to increase its stability. The

compositions have vasopressor activity.

申请人：SANDOZ A.G.

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