公开(公告)号：EP0738154A1

公开(公告)日：1996-10-23

申请号：EP94924100.0

申请日：1994-07-29

Applicant: Abbott Laboratories

Inventor： HAVIV, Fortuna ,  FITZPATRICK, Timothy D. ,  SWENSON, Rolf E. ,  NICHOLS, Charles, J. ,  MORT, Nicholas A.

IPC: A61K38 ,  A61P5 ,  A61P13 ,  A61P15 ,  A61P25 ,  A61P35 ,  C07K7

CPC classification number: C07K7/23 ,  A61K38/00

Abstract: Decapeptide and undecapeptides substituted on the N-terminal nitrogen atom by acyl groups which include furo-2-yl, isonicotinyl, nicotinyl, 2-, 3-, and 4-quinolinecarbonyl, shikimyl, dihydroshikimyl, and tetrahydrofur-2-oyl are potent antagonists of LHRH and are useful for hormones the levels of sex hormones in mammals.

Abstract translation: 在N-末端氮原子上被包括呋喃-2-基，异烟碱基，烟酰基，2-，3-和4-喹啉羰基，莽草酰基，二氢麝香基和四氢呋喃-2-酰基的酰基取代的十肽和十一肽是有效的拮抗剂 的LHRH，并且可用于激素水平的哺乳动物性激素水平。

公开(公告)号：EP0673254A1

公开(公告)日：1995-09-27

申请号：EP94903367.0

申请日：1993-11-30

Applicant: ABBOTT LABORATORIES

Inventor： GREER, Jonathan ,  HAVIV, Fortuna ,  FITZPATRICK, Timothy D. ,  SWENSON, Rolf E. ,  NICHOLS, Charles J. ,  MORT, Nicholas A.

IPC: A61K38 ,  A61P5 ,  C07K7

CPC classification number: C07K7/23 ,  A61K38/00

Abstract: The present invention provides a class of decapeptide compounds which are potent antagonists of LHRH activity and which have the structure A?1-D2-E3-G4-J5-L6-M7-Q8-R9-T10¿. The compounds of the percent invention are characterized by having an Φ-amino-functionalized side chain on the D-aminoacyl residue at position 6. The Φ-amino group of this side chain is further derivatized by the attachment of an extending group which likewise has a terminal amino group which is capped by an acyl group.