Title:
【発明の名称】ペプチド、その製造法、該ペプチドを含有する、LHRH拮抗剤
Document Type and Number:
Japanese Patent JP2944669
Kind Code:
B2
Abstract:
The present invention deals with LHRH antagonists which possess improved water solubility and while having the high antagonist potency of the basic peptides, are free of the edematogenic effects. These compounds are highly potent in inhibiting the release of gonadotropins from the pituitary gland in mammals, including humans. The compounds of this invention are represented by the formula X-R1-R2-R3-Ser-Tyr-R6-Leu-Arg-Pro-R10-NH2 wherein X is an acyl group derived from straight or branched chain aliphatic or alicyclic carboxylic acids having from 1 to 7 carbon atoms, or H2N-CO, R1 is D- or L-Pro, D- or L- DELTA 3-Pro, D-Phe, D-Phe(4-H1), D-Ser, D-Thr, D-Ala, D-Nal(1) or D-Nal (2), R2 is D-Phe or D-Phe(4-C1) R3 is D-Trp, D-Phe, D-Pal(3), D-Nal(1) or D-Nal(2), R6 is D-Cit, D-Hci, D-Cit(Q) or D-Hci(Q) and R10 is Gly or D-Ala where Q is lower alkyl of 1-3 carbon atoms and H1 is fluoro, chloro or bromo, and the pharmaceutically acceptable acid addition salts thereof and methods of use pertaining to these compounds.
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Inventors:
ANDORUU BUI SHARII
SANDAA BAJAZU
SANDAA BAJAZU
Application Number:
JP17728888A
Publication Date:
September 06, 1999
Filing Date:
July 18, 1988
Export Citation:
Assignee:
ASUTA MEDEIKA AG
International Classes:
A61K31/00; A61P15/00; A61P15/18; C07K1/02; C07K1/04; A61K38/04; C07K1/113; C07K7/23; C07K14/59; A61K38/00; (IPC1-7): C07K7/23; A61K31/00; A61K38/04; C07K1/02; C07K1/04; C07K14/59
Domestic Patent References:
| JP61122297A |
Other References:
ＦＯＬＫＥＲＳ，Ｋａｕｌ，Ｚ．Ｎａｔｕｒｆｏｒｓｃｈｕｎｇ Ｂ，Ｊａｎ．１９８７，Ｖｏｌ．４２，Ｎｏ．１，ｐ．１０１−１０６
Attorney, Agent or Firm:
Toshio Yano