Polypeptides and process for the production thereof

Details Polypeptides and process for the production thereof Polypeptides and process for the production thereof

C - Chemistry, Metallurgy

07

K

530/7.06, 167/10

C07K 7/06 (2006.01) C07K 14/665 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1267997

ABSTRACT OF THE DISCLOSURE Novel peptides are disclosed which are useful as analgesics and which have the formula: Image (I) wherein R1 and R2 may be the same or different and each represents a hydrogen atom or a lower alkyl or lower alkenyl group, A represents a D-amino acid, Gly or Sar provided that when the D-Amino acid is D-Cys, it is bonded with L-Cys or D-Cys in position 5 through a S-S bond to effect intramolecular ring closure, B represents optionally substituted L-Phe or D-Phe or an .alpha.-N-alkyl derivative thereof, C represents an L-amino acid, D-Cys or an .alpha.-N-alkyl derivative thereof, D and E each represent an L- or D-basic amino acid or an .alpha.-N-alkyl derivative thereof, F represents a group of the formula -OR3, Image -G-OR6 (in which G is an .alpha.-amino acid, .beta.-alanine, .gamma.-aminobutyne acid or an .alpha.-N-alkyl derivative thereof), Image (in which G is as defined above), -G-L-Arg-OR9 or -G-D-Arg-OR9 (in which G is as defined above, Image (in which G as defined above), -G-J-OR12 in which G is defined as above, and J is a neutral amino acid group or an acidic amino acid group) or -G-Arg-M-OR13 (in which M is a D- amino acid group), in which R3 to R13 are the same or different and each reprsents hydrogen or lower alkyl provided that, at least one of A to F comprises a D-amino acid or N-alkyl derivative thereof or an L-amino acid, and pharmacologically acceptable salts thereof.

494974

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