GHRH analogues
AssigneeCentre Hospitalier de L'Universite de Montreal (CHUM)
InventorPierrette Gaudreau
Life of this patent
Estimating the term…
Abstract
The present invention relates to growth hormone-releasing hormone (GHRH) analogues. More particularly, the invention relates to synthetic GHRH analogues of amino acids or more, exhibiting concomitantly an increased resistance to proteolysis and high binding affinity to human GHRH receptor in in vitro studies, in comparison with human native GHRH (1-29)NH2. The present invention also relates to a pharmaceutical composition comprising any one of said GHRH analogues and to the use of these analogues for specific stimulation of in vivo GH release as well as preparation of a drug in the treatment of GH deficiency-related conditions. The present invention also provides for a method for initiating GHRH-induced biological actions in a mammal.
Claims8
1-30. (canceled)
A method for stimulating the secretion or synthesis of growth hormone in a mammal in need thereof, comprising administering an effective amount of a GHRH analogue or pharmaceutically acceptable salt thereof, comprising formula X:
- Tyr-A2-Asp-Ala-Ile-Phe-Thr-A8-Ser-A10-Arg-Lys-Val-Leu-A 15-Gln-Leu-Ser-Ala-Arg-Lys-A22-Leu-Gln-Asp-Ile-Met-Ser-Arg-A30-NH2, wherein
- A2 is Ala or D-Ala;
- A8 is Asn, D-Asn or Ala;
- A10 is Tyr or D-Tyr;
- A15 is Gly, Ala or D-Ala;
- A22 is Leu, D-Leu, Lys or Ala;
- and
- A30 is a bond or any amino acid sequence of 1 up to 15 residues (SEQ ID NO:
- 67) and wherein said analogue comprises at least one of the above amino acid substitutions in comparison with the amino acid sequence of the native form of hGHRH1-29.
36-38. (canceled)
A method for treating a mammal in need of growth hormone synthesis or stimulation comprising administering an effective amount of GHRH analogue or pharmaceutically acceptable salt thereof, comprising formula X:Tyr-A2-Asp-Ala-Ile-Phe-Thr-A8-A9-A10-Arg-Lys-Val-Leu-A 15-Gln-Leu-Ser-Ala-Arg-A21-A22-Leu-Gln-Asp-Ile-Met-Ser-Arg-A30-NH2, wherein
- A2 is Ala or D-Ala;
- A8 is Asn, D-Asn or Ala;
- A9 is Ala or Ser;
- A10 is Tyr or D-Tyr;
- A15 is Gly, Ala or D-Ala;
- A21 is Lys or D-Lys;
- A22 is Leu, D-Leu, Lys or Ala;
- and
- A30 is a bond or any amino acid sequence of 1 up to 15 residues (SEQ ID NO:65) and wherein said analogue comprises at least one of the above amino acid substitutions in comparison with the amino acid sequence of the native form of hGHRH1-29.
Dependencies are inferred from the claim text.