发明授权
- 专利标题： CHRH antagonists with low histamine release
- 专利标题（中）： 低组胺释放的CHRH拮抗剂
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申请号： US371552申请日： 1989-06-26
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公开(公告)号： US5470947A公开(公告)日： 1995-11-28
- 发明人: Karl A. Folkers , Anders Ljungqvist , Dong-Mei Feng , Minoru Kubota , Pui-Fun L. Tang , Cyril Y. Bowers
- 申请人： Karl A. Folkers , Anders Ljungqvist , Dong-Mei Feng , Minoru Kubota , Pui-Fun L. Tang , Cyril Y. Bowers
- 申请人地址： TX Austin LA New Orleans
- 专利权人： Board of Regents, The University of Texas System,The Administrators of the Tulane Educational Fund
- 当前专利权人： Board of Regents, The University of Texas System,The Administrators of the Tulane Educational Fund
- 当前专利权人地址： TX Austin LA New Orleans
- 主分类号： A61K38/04
- IPC分类号： A61K38/04 ; A61K38/00 ; A61P15/00 ; C07K7/06 ; C07K7/23
摘要：
Antide is the decapeptide, N--Ac--D--2--Nal,D--pClPhe, D--3--Pal, Ser,NicLys, D--NicLys, Leu, ILys, Pro, D--Ala,NH.sub.2 which is an antagonist of luteinizing hormone releasing hormone (LHRH). This decapeptide, like others of the present invention, has high antiovulatory activity (AOA) and releases negligible histamine. Antide is scheduled for scale-up, safety testing and evaluation in the experimental primate and in clinical medicine. Numerous other peptides having structures related to Antide were prepared and tested. These peptides had variations primarily in positions 5, 6, 7, and 8. Of these, N--Ac--D--2--Nal, D--pClPhe,D--3--Pal,Ser,PicLys,cis--DpzACAla, Leu,ILys,pro,D--Ala--NH.sub.2 was one of the most potent and had higher antiovulatory activity than Antide, i.e. 73%/0.25 ug and 100%/0.5 ug vs. 36%/0.5 ug and 100%/1.0 ug. Antide showed significant, (p
公开/授权文献
- US5674821A Detergent compositions 公开/授权日：1997-10-07
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