Anf derivatives with novel bridging

C - Chemistry – Metallurgy – 07 – K

Patent

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530/7.1, 167/103

C07K 14/58 (2006.01) A61K 38/22 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1337891

Disclosed herein are derivatives of atrial natriuretic peptides wherein the exocyclic N- terminal peptide segment is deleted and the two cysteinyl residues (at positions 105 and 121) of the natural sequence are replaced with a trivalent unit, -NHCH(CO-)-Q-X-Y-CH2CH2CO- wherein Q is methyl- ene, ethylene or CR'R" wherein R' and R" each in- dependently is lower alkyl, X is oxy or thio, and Y is methylene or des-Y. The derivatives may be optionally substituted at various positions includ- ing positions 106, 107 and 124. The derivatives possess protracted ANF-like activity and are indi- cated for treating hypertension and for treating pathological conditions resulting from an imbalance of body fluids and electrolytes.

554516

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