Method of using motility increasing peptides

C - Chemistry – Metallurgy – 07 – K

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167/103.8

C07K 7/06 (2006.01)

Patent

CA 1177401

Abstract of the Disclosure Peptides of the formula A - Tyr - B - C - D - E wherein A denotes hydrogen, alkyl, alkenyl, or alkenyleycloalkyl, each having up to 7 carbon atoms, an .alpha.-amino acid or a peptide with 2 or 3 amino acids, B denotes an .alpha.-amino acid or .alpha.-amino-isobutyric acid, C denotes glycine or azaglycine, D denotes phenylalanine which can be substituted in the benzene nucleus by methyl, methoxy, halogen, nitro or trifluoromethyl; dehydro- or hexahydrophenylalanine; aza- or N-methylphenylalanine, and E denotes (a) -O-R1 or Image wherein, R1, R2 and R3 are identical or different and are hydrogen, alkyl with 1 to 6 carbon atoms; cycloalkyl with 3 to 6 carbon atoms; alkenylcycloalkyl with 4 to 8 carbon atoms; hydroxyalkyl or dihydroxy- alkyl, thio alkyl or mercaptoalkyl with 1 to 6 carbon atoms; aryl with 6 to 10 carbon atoms; aralkyl with 7 to 11 carbon atoms, or R2 and R3 together denote poly- methylene with 2 to 6 carbon atoms, or Rl denotes methyl-polyethylene glycol having a degree of poly- merization of up to about 50, (b) an amino alcohol or an amino acid, which on its part may carry one of the groups defined sub (a); or (c) homoserine or homocysteine thiolactone in association with a pharmaceutically acceptable carrier: with the proviso that peptides of the formula H-Tyr X-Gly-Phe-Met-Y, wherein X denotes D-Ala, D-Leu, D-He, D-Val, D-Phe, D-Tyr, D-Trp, D-Ser, D-Thr, D-Met, D-Glu, D-Gln, D-Asp, D-Asn, D-Lys, or D-Arg and Y denotes NH2 or OH are excluded. These compounds stimulate the motility of the muscles of the gastro-intestinal tract and, therefore, they can be used for treating paralytic symptoms of these organs. - 2 -

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