Claims
- 1. A peptide of the formula ##STR8## R is Asn or Ala; R.sub.2 is Thr or Ser; R.sub.3 is Arg, Lys or Orn; R.sub.4 is Leu or Phe; R.sub.5 is Arg or Lys; R.sub.6 is Nle, Ile or Leu; R.sub.7 is Asn or Thr; R.sub.8 is Ser or Thr; R.sub.9 is Ile or Val; R.sub.10 is Asn or Thr; X is hydrogen, ##STR9## R.sub.11 is C.sub.1-3 alkyl; Y is --OR.sub.12 or NHR.sub.12 ; R.sub.12 is hydrogen or C.sub.1-3 alkyl; or with the proviso that (Nle).sup.17 -VIP is excluded from the scope of Formula I; and the pharmaceutically acceptable acid or base addition salts thereof.
- 2. A compound according to claim 1 wherein X is ##STR10##
- 3. A compound according to claim 2 wherein R.sub.6 is Nle and Y is --OH or --NH.sub.2.
- 4. A compound according to claim 3 wherein R.sub.3 is Lys, R.sub.8 is Thr and R.sub.9 is Val.
- 5. A compound according to claim 3 wherein R.sub.3 is Orn, R.sub.8 is Ser and R.sub.9 is Val.
- 6. A compound according to claim 3 wherein R.sub.3 is Lys, R.sub.4 is Leu, R.sub.8 is Ser and R.sub.9 is Val.
- 7. A compound according to claim 3 wherein R.sub.3 is Lys, R.sub.7 is Thr, R.sub.8 is Ser and R.sub.9 is Val.
- 8. A peptide which is
- Ac-(Lys.sup.12, Nle.sup.17, Val.sup.26, Thr.sup.28)-VIP.
- 9. A peptide which is
- Ac-(Orn.sup.12, Nle.sup.17, Val.sup.26, Thr.sup.28)-VIP.
- 10. A peptide which is
- Ac-(Lys.sup.12, Lys.sup.14, Nle.sup.17, Val.sup.26, Thr.sup.28)-VIP.
- 11. A peptide which is
- Ac-(Lys.sup.12, Nle.sup.17, Thr.sup.25, Val.sup.26, Thr.sup.28)-VIP.
- 12. A pharmaceutical composition comprising an active agent which is a peptide having bronchotracheal smooth muscle relaxant activity and a pharmaceutically acceptable carrier, wherein said peptide has the formula: ##STR11## R is Asn or Ala; R.sub.2 is Thr or Ser; R.sub.3 is Arg, Lys or Orn; R.sub.4 is Leu or Phe; R.sub.5 is Arg or Lys; R.sub.6 is, Ile or Leu; R.sub.7 is Asn or Thr; R.sub.8 is Ser or Thr; R.sub.9 is Ile or Val; R.sub.10 is Asn or Thr; X is hydrogen, ##STR12## R.sub.11 is C.sub.1-3 alkyl; Y is --OR.sub.12 or NHR.sub.12 ; R.sub.12 is hydrogen or C.sub.1-3 alkyl; with the proviso that (Nle).sup.17 -VIP is excluded from the scope of Formula I; and the pharmaceutically acceptable acid or base addition salts thereof.
- 13. A composition according to claim 12 wherein said peptide is selected from the group consisting of:
- Ac-(Lys.sup.12, Nle.sup.17, Thr.sup.25, Val.sup.26, Thr.sup.28)-VIP
- Ac-(Orn.sup.12, Nle.sup.17, Val.sup.26, Thr.sup.28)-VIP
- Ac-(Lys.sup.12, Lys.sup.14, Nle.sup.17, Val.sup.26, Thr.sup.28)-VIP and
- Ac-(Lys.sup.12, Nle.sup.17, Val.sup.26, Thr.sup.28)-VIP.
- 14. A pharmaceutical composition according to claim 13 wherein said pharmaceutically acceptable carrier is suitable for aerosol administration.
- 15. A method of treating bronchotraceal constriction disorders which comprises administering a bronchotracheal smooth muscle relaxing effective amount of a peptide having the formula: ##STR13## R is Asn or Ala; R.sub.2 is Thr or Ser; R.sub.3 is Arg, Lys or Orn; R.sub.4 is Leu or Phe; R.sub.5 is Arg or Lys; R.sub.6 is Nle, Ile or Leu; R.sub.7 is Asn or Thr; R.sub.8 is Ser or Thr; R.sub.9 is Ile or Val; R.sub.10 is Asn or Thr; X is hydrogen, ##STR14## R.sub.11 is C.sub.1-3 alkyl; Y is --OR.sub.12 or NHR.sub.12 ; R.sub.12 is hydrogen or C.sub.1-3 alkyl; with the proviso that (Nle).sup.17 -VIP is excluded from the scope of Formula I; and the pharmaceutically acceptable acid or base addition salts thereof.
- 16. A method according to claim 15 wherein said peptide is selected from the group consisting of:
- Ac-(Lys.sup.12, Nle.sup.17, Thr.sup.25, Val.sup.26, Thr.sup.28)-VIP
- Ac-(Orn.sup.12, Nle.sup.17, Val.sup.26, Thr.sup.28)-VIP
- Ac-(Lys.sup.12, Lys.sup.14, Nle.sup.17, Val.sup.26, Thr.sup.28)-VIP and
- Ac-(Lys.sup.12, Nle.sup.17, Val.sup.26, Thr.sup.28)-VIP.
- 17. A method according to claim 16 wherein the administration of said compound is by aerosol application.
Parent Case Info
This application is a continuation-in-part application of U.S. Ser. No. 658,736, filed Oct. 9, 1984, now U.S. Pat. No. 4,605,641.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4605641 |
Bolin et al. |
Aug 1986 |
|
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
658736 |
Oct 1984 |
|