Claims
- 1. A pseudopeptide which has an affinity for a bradykinin receptor having the formula:
- A-B-C-D-E-F-G-Cn
- wherein,
- A is selected from the group consisting of the L-and D-isomers of Arg and Lys;
- B is selected from the group consisting of the L-and D-isomers of Arg and Lys;
- C is selected from the group consisting of: ##STR45## D is a direct bond or selected from the group consisting of Ser, Thr, Gly, Ala and Val;
- E is selected from the group Consisting of a D-Phe, D-Tic and a
- D-trans-Hype wherein aryl is selected from the group consisting of a phenyl, naphthyl, benzyl, and naphthylmethyl group;
- F is selected from the group consisting of Oic, Aoc, Phe, Tic, and a Hype wherein aryl is selected from the group consisting of a phenyl, naphthyl, benzyl, and naphthylmethyl group;
- G is selected from the group consisting of Arg and Lys;
- Cn is selected from the group consisting of a hydroxyl group, an amino group, and an alkoxy group;
- and pharmaceutically accepted salts thereof.
- 2. A pseudopeptide of claim 1 wherein C is selected from the group consisting of: ##STR46##
- 3. A pseudopeptide of claim 1 wherein C is selected from the group consisting of: ##STR47##
- 4. A pseudopeptide of claim 1 wherein:
- A is D-Arg;
- B is Arg;
- C is selected from the group consisting of: ##STR48## D is a direct bond or Ser; E is selected from the group consisting of D-Phe, D-Tic, D-Hype (trans-propyl), D-Hype (trans-thiophenyl), D-Hype (trans-phenyl propyl), D-Hype (trans-2-methylbutyl), D-Hype (trans-ethyl) and D-Hype (trans-methyl);
- F is Oic;
- G is Arg; and
- Cn is OH.
- 5. A pseudopeptide of claim 1 selected from the group consisting of: ##STR49##
- 6. A pseudopeptide of claim 1 selected from the group consisting of: ##STR50##
- 7. A pharmaceutical composition useful as a bradykinin receptor antagonist comprising a pharmaceutical carrier and an effective amount of the peptide of claim 1.
- 8. A pharmaceutical preparation for treating local pain and inflammation from bums, wounds, cuts, rashes or other trauma, and pathological conditions caused by the production of bradykinin or related kinins by an animal, which comprises an effective amount of the peptide of claim 1 to antagonize bradykinin and a suitable pharmaceutical carrier.
- 9. A process for treating local pain and inflammation, which comprises administering an effective amount of the peptide of claim 1 to an animal in need thereof.
Parent Case Info
This application is a continuation-in-part of U.S. application Ser. No. 07/957,879 filed Oct. 8, 1992.
US Referenced Citations (6)
Number |
Name |
Date |
Kind |
4242329 |
Claeson et al. |
Dec 1980 |
|
4483850 |
Patchett et al. |
Nov 1984 |
|
4693993 |
Stewart et al. |
Sep 1987 |
|
4801613 |
Stewart et al. |
Jan 1989 |
|
4822894 |
Geiger et al. |
Apr 1989 |
|
4923963 |
Stewart et al. |
May 1990 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
0334685 |
Sep 1989 |
EPX |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
957879 |
Oct 1992 |
|