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|Title:||GRF analogs with increased biological potency|
|Abstract:||The present invention relates to chimeric fatty body-GRF analogs with increased biological potency, their application as anabolic agents and in the diagnosis and treatment of growth hormone deficiencies. The chimeric fatty body-GRF analogs include an hydrophobic moiety (tail), and can be prepared, either by anchoring at least one hydrophobic tail to the GRF, in the chemical synthesis of GRF. The GRF analogs of the present invention are biodegradable, non-immunogenic and exhibit an improved anabolic potency with a reduced dosage and prolonged activity.|
|Inventor(s):||Brazeau; Paul (Montreal, CA), Gravel; Denis (St-Lambert, CA)|
|Assignee:||Theratechnologies, Inc. (Montreal, CA)|
1. A hydrophobic GRF analog of formula A:
the GRF peptide is a peptide of formula B:
A1 is Tyr or His;
A2 is Val or Ala;
A8 is Asn or Ser;
A13 is Val or Ile;
A15 is Ala or Gly;
A18 is Ser or Tyr;
A24 is Gln or His;
A25 is Asp or Glu;
A27 is Met, Ile or Nle;
A28 is Ser or Asn;
A30 is a bond or any amino acid sequence of 1 up to 15 residues;
R.sub.0 is NH.sub.2 or NH--(CH.sub.2)n--CONH.sub.2, with n=1 to 12 and;
X is hydrophobic tail anchored via an amide bond at the N-terminus of said peptide, and said hydrophobic tail defining a backbone of 5 to 7 atoms;
wherein said backbone can be substituted by C.sub.1-6 alkyl, C.sub.1-6 cycloalkyl, or C.sub.6-12 aryl;
and comprises at least one rigidifying moiety connected to at least two atoms of the backbone;
said rigidifying moiety selected from the group consisting of double bond, triple bond, saturated or unsaturated C.sub.3-9 cycloalkyl, and C.sub.6-12 aryl.
2. A pharmaceutical formulation for inducing growth hormone release which comprises as an active ingredient a GRF analog as claimed in claim 1, in association with a pharmaceutically acceptable carrier, excipient or diluent.
3. A method of increasing the level of growth hormone in a patient which comprises administering to said patient an effective amount of a GRF analog as claimed in claim 1.
4. A method for the diagnosis of growth hormone deficiencies in patients, which comprises administering to said patient a GRF analog as claimed in claim 1 and measuring the growth hormone response.
5. A method for the treatment of pituitary dwarfism or growth retardation in a patient, which comprises administering to said patient an effective amount of a GRF analog as claimed in claim 1.
6. A method for the treatment of wound or bone healing in a patient, which comprises administering to said patient an effective amount of a GRF analog as claimed in claim 1.
7. A method for the treatment of osteoporosis in a patient, which comprises administering to said patient an effective amount of a GRF analog as claimed in claim 1.
8. A method for improving protein anabolism in human or animal, which comprises administering to said human or animal an effective amount of a GRF analog as claimed in claim 1.
9. A method for inducing a lipolytic effect in human or animal inflicted with clinical obesity, which comprises administering to said human or animal an effective amount of a GRF analog as claimed in claim 1.
10. A method for the overall upgrading of somatroph function in human or animal, which comprises administering to said human or animal an effective amount of a GRF analog as claimed in claim 1.
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