公开(公告)号：US4465625A

公开(公告)日：1984-08-14

申请号：US830831

申请日：1977-09-06

申请人： Sandor Bajusz ,  Andras Ronai ,  Jozsef Szekely ,  Laszlo Graf ,  Zsuzsa Mohai nee Nagy

发明人： Sandor Bajusz ,  Andras Ronai ,  Jozsef Szekely ,  Laszlo Graf ,  Zsuzsa Mohai nee Nagy

IPC分类号： C07K14/655 ,  A61K38/00 ,  A61K38/08 ,  A61P25/00 ,  A61P25/04 ,  C07K7/06 ,  C07K14/575 ,  C07K14/70 ,  C07C103/52

CPC分类号： C07K14/702 ,  A61K38/00

摘要： Analgesic compounds having the formula (I):Tyr-A-Gly-Phe-B-X-YwhereinA is a D-aminoacid group having a lower alkyl group or a lower thioalkyl group as a side chain,B is an aminoacid or a cyclic iminoacid group, either of which has a lower alkyl group as a side chain,X is an oxygen atom or an NH group, andY is a hydrogen atom or a lower alkyl group,or a pharmaceutically effective amide, ester or salt thereof.

摘要翻译： 具有式（I）的镇痛化合物：Tyr-A-Gly-Phe-BXY其中A是具有低级烷基或低级硫代烷基作为侧链的D-氨基酸，B是氨基酸或环状亚氨基酸 其中任一个具有低级烷基作为侧链，X是氧原子或NH基，Y是氢原子或低级烷基，或其药学上有效的酰胺，酯或盐。

公开(公告)号：US3953415A

公开(公告)日：1976-04-27

申请号：US360198

申请日：1973-05-14

申请人： Lajos Kisfaludy ,  Miklos Low ,  Istvan Schon ,  Tamas Szirtes ,  Maria Sz. Sarkozi ,  Sandor Bajusz ,  Andrae Turan ,  Rosa Beks ,  Attila Juhasz ,  Laszlo Graf ,  Kalman Medzihradszky ,  Laszlo Szporny

发明人： Lajos Kisfaludy ,  Miklos Low ,  Istvan Schon ,  Tamas Szirtes ,  Maria Sz. Sarkozi ,  Sandor Bajusz ,  Andrae Turan ,  Rosa Beks ,  Attila Juhasz ,  Laszlo Graf ,  Kalman Medzihradszky ,  Laszlo Szporny

IPC分类号： A61K38/00 ,  C07C67/00 ,  C07C231/00 ,  C07C231/12 ,  C07C271/22 ,  C07K1/06 ,  C07K1/08 ,  C07K7/08 ,  C07K14/575 ,  C07K14/695 ,  C07C103/52 ,  C07G7/00

CPC分类号： C07C271/22 ,  C07K1/066 ,  C07K1/088 ,  C07K14/695 ,  A61K38/00

摘要： The invention relates to the preparation of biologically active polypeptides containing the aspartyl group, particularly an aspartyl-glycine moiety, using the active-ester technique.According to the method of the invention, human adrenocorticotropic hormone and its fragments characteristic to the individual species, as well as the blocked derivatives of such compounds are prepared by the pentafluorophenol method, i.e., the carboxy group of the acylating component is activated by converting it into pentafluorophenyl ester in the coupling reaction carried out with blocked peptides containing the aspartyl group or an aspartylglycine moiety. The acylation is carried out preferably using equimolar quantities of the respective reactants. The free peptides obtained after removing the blocking groups can be converted into their acid addition salts or pharmaceutically acceptable complexes or condensates.Human adrenocorticotropic hormone and its derivatives are valuable substances of therapeutical activity.

摘要翻译： 本发明涉及使用活性酯技术制备含有天冬氨酰基，特别是天冬氨酰 - 甘氨酸部分的生物活性多肽。