US 6,136,781 AGranted

LH-RH receptor antagonists

AssigneeTakeda Chemical Industries, Ltd.

InventorsChieko Kitada, Shuichi Furuya, Koichi Kato

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Abstract

The LH-RH receptor antagonists containing cyclic pentapeptides or salts thereof and novel cyclic pentapeptide or salts thereof are provided. The LH-RH receptor antagonists of the present invention are effective as medicines for preventing and curing sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, mammary cancer, pituitary tumor, etc.), prostatomegaly, endometriosis, hysteromyoma, puberty precox, amenorrheal syndromes, multilocular ovarian syndromes, comedo, etc. and are also effective as pregnancy controlling agents (e.g., contraceptives, etc.) and menstrual cycle controlling agents. Moreover, these are also useful in the livestock industry for the control of the estrus of animals and also for the improvement in the quality of meat and for the control of the growth of animals, as well as in the marine products industry as spawning promoters for fishes.

Claims19

Dependent claims

A cyclic pentapeptide of the formula:

cyclo(-A.sub.1 '-A.sub.2 '-A.sub.3 '-A.sub.4 '-A.sub.5 '-)
wherein A.sub.1 ' is Arg, Arg(Tos) or Arg(Mtr);
and A.sub.2 ', A.sub.3 ', A.sub.4 ', and A.sub.5 ' are defined as follows:
when A.sub.2 ' is Lys, Lys(Isopropyl), Lys(SO.sub.2 Nap(1)), Lys(SO.sub.2 Nap(2)), Lys(COPh), Lys(COCH.sub.2 Ph), Lys(CO--(CH.sub.2).sub.3 -Ph), Lys(CO--(CH.sub.2).sub.5 -Ph), Lys(Ac), Lys(CO-Nap(1)), Lys(Nic), or Trp then A.sub.3 ' is Tyr or Trp, A.sub.4 ' is Tyr or Trp, and A.sub.5 ' is Leu;
when A.sub.2 ' is Glu, Glu(NH--CH.sub.2 --CH.sub.2 -Ph), Glu(NH--CH.sub.2 -Ph), Glu(NH--CH-Ph.sub.2), Glu(NH--CH.sub.2 -Nap(1)), Glu(Php), Glu(Bzlp), Glu((2)-Pyp), Glu(2-MeOPhp), or Glu(4-MeOPhp), then A.sub.3 ', is Lys, Lys(Isopropyl), Lys(SO.sub.2 Nap(1)), Lys(SO.sub.2 Nap(2)), Lys(COPh), Lys(COCH.sub.2 Ph), Lys(CO--(CH.sub.2).sub.3 -Ph), Lys(CO--(CH.sub.2).sub.5 -Ph), Lys(Ac), Lys(CO-Nap(1)), Lys(Nic), or Tyr, A.sub.4 ' is Trp, and A.sub.5 ' is Leu;
or
when A.sub.2 ' is Phe, (p-Cl)Phe or (p-F)Phe, then A.sub.3 ' is Ala, A.sub.4 ' is Trp and A.sub.5 ' is Phe, (p-Cl)Phe, (p-F)Phe, or Phg;
wherein A.sub.1 ', A.sub.3 ' and A.sub.5 ' have an L-configuration, and A.sub.2 ' and A.sub.4 ' have a D-configuration;
or A.sub.2 ', A.sub.4 ' and A.sub.5 ' have an L-configuration, and A.sub.1 ' and A.sub.3 ' has a D-configuration;
or a salt thereof.

7 more elements

Dependencies are inferred from the claim text.

Facts

Application: 08/656,244Filed 6 Jun 1996
Priority: JP 7-10677528 Apr 1995
Granted: 24 Oct 2000
Term ends: Not estimatedThe source records don’t support an estimate.

Classification8 codes

C07K 7/64
Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof: cyclic peptides containing only normal peptide links
C07K 7/23
Linear peptides containing only normal peptide links: luteinising hormone-releasing hormone [LHRH]; Related peptides
A61K 38/00
Medicinal preparations containing peptides
Y10S 424/813
Drug, bio-affecting and body treating compositions: viral vaccine for bovine species, e.g. cattle