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US 5,496,928 AGranted
Endothelin antagonistic substance
AssigneeBanyu Pharmaceutical Co., Ltd.
InventorsKiyofumi Ishikawa, Takehiro Fukami, Takashi Hayama, Kenji Niiyama, Toshio Nagase, Toshiaki Mase, Kagari Fujita, Masaki Ihara, Fumihiko Ikemoto, Mitsuo Yano, Masaru Nishikibe
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Abstract
Peptides having the formula: ##STR1## inhibit the binding of endothelin and are useful in treating diseases associated with excess production or secretion of endothelin.
Claims6
A peptide of the formula:
- ##STR141## wherein A is a group of the formula R.sup.12 R.sup.13 N--C(.dbd.O)--, wherein R.sup.12 and R.sup.13 form, together with the adjacent nitrogen atom, a 5- to 9-membered nitrogen-containing saturated heterocyclic ring having four to eight carbon atoms, and wherein one to four hydrogen atoms on the carbon atoms of the saturated heterocyclic ring may independently be replaced by a lower alkyl group;
- B is a group of the formula --NR.sup.2 --, wherein R.sup.2 is a hydrogen atom or a lower alkyl group;
- R.sup.3 is a lower alkyl group;
- X.sup.1 is a group of the formula --NR.sup.4 --, wherein R.sup.4 is a hydrogen atom or a lower alkyl group;
- R.sup.5 is a 3-indolylmethyl group, wherein the indole ring is substituted at the 2-position by a substituent selected from the group consisting of a lower alkylthio group, a lower alkylsulfinyl group and a lower alkylsulfonyl group;
- X.sup.3 is an oxygen atom;
- R.sup.6 is a hydrogen atom or a lower alkyl group;
- n is 0 or 1;
- Y is a group of the formula CO.sub.2 R.sup.71 wherein R.sup.71 is a hydrogen atom or a lower alkyl group;
- or a pharmaceutically acceptable salt thereof.
7 more elements
Dependencies are inferred from the claim text.