Therapeutic decapeptides

C - Chemistry – Metallurgy – 07 – K

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C07K 7/23 (2006.01) A61K 38/09 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2044137

(57) Abstract A decapeptide of the formula (I), wherein each A1, A2, and A3, independently, is D-.beta.-Nal, D-p-X-Phe(where X is halog- en, H, NH2, NO2, OH, or C1-3 alkyl); A5 is p-X-Phe(where X is halogen, H, NH2, NO2, OH, or C1-3 alkyl); A6 is D-Lys, D-Arg, .beta.-Nal, D-.beta.-Nal, D-Trp, D-p-X-Phe(where X is halogen, H, NH2, NO2, or C1-3 alkyl) or D-Lys-.epsilon.-NH-R(where R is H, a branched or straight chain or cyclo C1-C10 alkyl group, or an aryl group); A7 is p-X-Phe(where X is halogen, H, NH2, NO2, HO, C2F3, or C1-3 alkyl), cyclohexyala, or Trp; A8 is Arg, Lys, or Lys-.epsilon.-NH-R(where R is H, a branched or straight chain or cyclo C1-C10 alkyl group, or an aryl group); A9 is Pro; A10 is D-Ala-NH2, Gly-NH2, D-Ser, or D-Ser-NH2; provided that at least one of A2 or A3 must be D-Phe or D-Trp; and further provoded that at least one fo A6 and A8 must be the following; A6 must be D-Lys-.epsilon.-NH-R (where R is cyclo C1-C10 alkyl group); A8 must be Lys-.epsilon.-NH-R (where R is cyclo C1-C10 alkyl group), or apharmaceutically acceptable salt thereof.

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