Back to results
US 5,114,918 AGranted
Endothelin antagonistic cyclic pentapeptides
AssigneeBanyu Pharmaceutical Co., Ltd.
InventorsKiyofumi Ishikawa, Takehiro Fukami, Takashi Hayama, Kenji Niiyama, Toshio Nagase, Toshiaki Mase, Kagari Fujita, Masaru Nishikibe, Masaki Ihara, Mitsuo Yano
Life of this patent
Estimating the term…
Abstract
Cyclic pentapeptides of the formula: cyclo (-X.sup.1 -X.sup.2 -X.sup.3 -X.sup.4 -X.sup.5 -) (I) wherein X.sup.n (n=1-5) represents amino acid residues. These compounds are useful as hypotensive drugs.
Claims2
A cyclic pentapeptide of the formula:
- cyclo (--X.sup.1 --X.sup.2 --X.sup.3 --X.sup.4 --X.sup.5 --) (I)
- wherein X.sup.n (n=1-5) represents amino acid residues, respectively, and X.sup.1 is D-Phe, D-Tyr, D-Tha, D-Tza, D-Nal, D-Bta, D-Trp, D-Trp(O), D-Trp(CHO) or D-Trp((CH.sub.2).sub.m COR.sup.1), wherein m is from 0 to 6, and R.sup.1 is a hydroxyl group, a C.sub.1 -C.sub.6 alkoxy group, an amino group or a C.sub.1 -C.sub.6 monoalkylamino group, provided that when m=0, R.sup.1 is not a hydroxyl group;
- X.sup.2 is D-Asp, D-Glu, or D-Cys(O.sub.3 H);
- X.sup.3 is Pro, Hyp, Pip, Thz, .beta.-Ala, Gly, Ala, .alpha.-Aba, Aib, Val, Nva, Leu, Ile, aIle, Nle, Met, Met(O), Met(O.sub.2), Phe, Tza, Tha, Tyr, Trp, His, Arg, Lys, Lys(CHO), Orn, Orn(CHO), Asn, Gln, Asp, Glu, Cys(O.sub.3 H), Cys, Ser or Thr wherein those .alpha.-amino acids having a hydrogen atom on the .alpha.-amino group are optionally substituted by a C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.7 cycloalkyl group which optionally has a group selected from the group consisting of an imidazolyl group, a carboxyl group, a sulfo group and a hydroxy group;
- X.sup.4 is D-Ala, D-Thr, D-.alpha.-Aba, D-Val, D-Nva, D-Leu, D-Ile, D-aIle, D-Nle, D-tert-Leu, D-Cpg, D-Chg, D-Dpg, D-Pen, Aib, Ac.sub.3 c, Ac.sub.4 c, Ac.sub.5 c, Ac.sub.6 c, Ac.sub.7 c, D-Phg, D-Thg, D-Fug, D-Tzg or D-Itg wherein those .alpha.-amino acids having a hydrogen atom at the .alpha.-position are optionally substituted by a C.sub.1 -C.sub.3 alkyl group;
- X.sup.5 is Pro, Pip, Thz, His, Ala, .alpha.-Aba, Val, Nva, Leu, Ile, aIle, Nle, Met, C.sub.3 al, C.sub.4 al, C.sub.5 al or C.sub.6 al wherein those .alpha.-amino acids having hydrogen atom on the .alpha.-amino group are optionally substituted by a C.sub.1 -C.sub.6 alkyl group;
- or a pharmaceutically acceptable salt thereof.
4 more elements
Dependencies are inferred from the claim text.