Analogs of tyrosine sulfate or tyrosine phosphate containing peptides
AssigneeHoffmann-La Roche Inc.
InventorsWaleed Danho, Jefferson W. Tilley, Joseph Triscari, Rolf Wagner
Life of this patent
Estimating the term…
Abstract
Analogs of Tyrosine Sulfate or Tyrosine Phosphate containing peptides, the novel intermediate compounds used in the preparation of these analogs, as well as a method for suppressing appetite in subjects by administering to the subject an effective amount of CCK analog wherein one or more of any Tyrosine Sulfate present is substituted with a radical of the invention.
Claims30
Ac-(D,L)-Phe( 4-COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D)-Phe(4-COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-Phe(4-COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D,L)-Phe(4-CH.sub.2 COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D)-Phe(4-CH.sub.2 COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-Phe(4-CH.sub.2 COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Desamino-Phe(4-CH.sub.2 COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Desamino-Phe(4-CH.sub.2 COOH)-Nle-Gly-Trp-Nle-Asp-N-methyl-Phe-NH.sub.2.
Desamino-Phe(4-CH.sub.2 COOH)-Nle-D-Ala-Trp-Nle-Asp-N-methyl-Phe-NH.sub.2.
Ac-(D,L)-Phe(4-CF.sub.2 COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D)-Phe(4-CH.sub.2 COOC.sub.2 H.sub.5)-Met-Gly-Trp-Met-Asp-(COOC.sub.2 H.sub.5)-Phe-NH.sub.2.
Ac-Phe(4-CH.sub.2 COOC.sub.2 H.sub.5)-Met-Gly-Trp-Met-Asp-(COOC.sub.2 H.sub.5)-Phe-NH.sub.2.
Ac-Phe(4-CH.sub.2 CH.sub.2 COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D,L)-Phe(3-COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D,L)-Phe(3-CH.sub.2 COOH)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D,L)-Phe(4-tetrazole)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D)-Phe(4-tetrazole)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-Phe(4-tetrazole)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Desamino-Phe(4-tetrazole)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D,L)-Phe(4-CH.sub.2 -tetrazole)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D)-Phe(4-CH.sub.2 -tetrazole)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
Ac-(D,L)-Phe(4-CH.sub.2 -tetrazole)-Nle-Gly-Trp-Nle-Asp-N-methyl-Phe-NH.sub.2.
Ac-(D)-Phe(4-CH.sub.2 -tetrazole)-Nle-Gly-Trp-Nle-Asp-N-methyl-Phe-NH.sub.2.
Ac-Phe(4-CH.sub.2 -tetrazole)-Nle-Gly-Trp-Nle-Asp-N-methyl-Phe-NH.sub.2.
Desamino-Phe(4-CH.sub.2 -tetrazole)-Nle-Gly-Trp-Nle-Asp-N-methyl-Phe-NH.sub.2.
Desamino-Phe(4-CH.sub.2 -tetrazole)-Nle-(D)Ala-Trp-Nle-Asp-N-methyl-Phe-NH.sub.2.
Ac-Phe(4-CH.sub.2 -tetrazole)-Met-Gly-Trp-Met-Asp-Phe-NH.sub.2.
A method for suppressing appetite in subjects by administering an appetite supressing efective amount of a compound selected from the group consisting of:
- ______________________________________ Ac--(D,L)--Phe(3-COOH)--Met--Gly--Trp--Met--Asp-- Phe-- NH.sub. Ac--(D,L).dbd.Phe(4-COOH)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--(D)--Phe(4-COOH)--Met--Gly--Trp--Met--Asp--Phe--NH.sub.2 Ac--Phe(4-COOH)--Met--Gly--Trp--Met--Asp--Phe--NH.sub.2 Ac--(D,L).dbd.Phe(4-CH.sub.2 COOH)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--(D).dbd.Phe(4-CH.sub.2 COOH)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--Phe(4-CH.sub.2 COOH)--Met--Gly--Trp--Met--Asp--Phe--NH.sub.2 Ac--(D)--Phe(4-CH.sub.2 COOC.sub.2 H.sub.5)--Met--Gly--Trp--Met-- Asp--(COOC.sub.2 H.sub.5)--Phe--NH.sub.2 Ac--Phe(4-CH.sub.2 COOC.sub.2 H.sub.5)--Met--Gly--Trp--Met-- Asp--(COOC.sub.2 H.sub.5)--Phe--NH.sub.2 Ac--Phe(4-CH.sub.2 CH.sub.2 COOH)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--(D,L).dbd.Phe(4-CF.sub.2 COOH)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--(D,L).dbd.Phe(4-tetrazole)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--(D).dbd.Phe(4-tetrazole)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--Phe(4-tetrazole)--Met--Gly--Trp--Met--Asp--Phe--NH.sub.2 Desamino.dbd.Phe(4-CH.sub.2 COOH)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--(D,L)--Phe(3-CH.sub.2 COOH)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--(D,L).dbd.Phe(4-CH.sub.2 --tetrazole)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Desamino.dbd.Phe(4-CH.sub.2 COOH)--Nle--Gly--Trp--Nle--Asp-- N--methyl--Phe--NH.sub.2 Desamino.dbd.Phe(4-CH.sub.2 COOH)--Nle--(D)--Ala--Trp--Nle--Asp-- N--methyl--Phe--NH.sub.2 Desamino.dbd.Phe(4-tetrazole)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--(D).dbd.Phe(4-CH.sub.2 --tetrazole)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--Phe(4-CH.sub.2 --tetrazole)--Met--Gly--Trp--Met--Asp-- Phe--NH.sub.2 Ac--(D,L).dbd.Phe(4-CH.sub.2 --tetrazole)--Nle--Gly--Trp--Nle--Asp-- N--methyl--Phe--NH.sub.2 Ac--Phe(4-CH.sub.2 --tetrazole)--Nle--Gly--Trp--Nle--Asp-- N--methyl--Phe--NH.sub.2 and Desamino--Phe(4-CH.sub.2 --tetrazole)--Nle--Gly--Trp--Nle--Asp-- N--methyl--Phe--NH.sub. 2. ______________________________________
Dependencies are inferred from the claim text.