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Claims for Patent: 5,861,379

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Claims for Patent: 5,861,379

Title: Chimeric fatty body-pro-GRF analogs with increased biological potency
Abstract:The present invention relates to chimeric fatty body-pro-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-pro-GRF analogs include an hydrophobic moiety (tail), and can be prepared, either by anchoring one or several hydrophobic tails to the GRF, or by substituting one or several amino-acids by a pseudomicellar residue 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): Ibea; Michel (Montreal, CA), Abribat; Thierry (Montreal, CA), Brazeau; Paul (Montreal, CA)
Assignee: Theratechnologies Inc. (Montreal, CA)
Application Number:08/702,114
Patent Claims: 1. A chimeric fatty bodyGRF analog with increased biological potency, of the following general formula:

wherein,

A1 is Tyr or His;

A2 is Val or Ala;

A8 is Asn or Ser;

A18 is Ser or Thr

A15 is Ala or Gly;

A24 is Gln or His;

A27 is Met, Ile or Nle;

A28 is Ser or Asp;

A30 is any amino acid sequence of 1 to 15 residues;

R.sub.0 is NH2;

wherein A1 is N-anchored by a hydrophobic tail of the following general formula I: ##STR6## wherein, G is a carbonyl group;

X is a oxygen atom, sulfur atom or an amino group (NH);

(W.dbd.Y) represents cis or trans (CH.dbd.CR5);

(W'.dbd.Y') represents cis or trans (CH.dbd.CR6);

Z is an oxygen or a sulfur atom;

R.sub.1, R.sub.2 and R.sub.3, independently, are selected from a hydrogen atom, and a linear or branched C.sub.1 -C.sub.6 alkyl group;

R.sub.4 is a hydrogen atom;

R.sub.5 and R.sup.6, independently, are a hydrogen atom or a linear or branched C.sub.1 -C.sub.4 alkyl group;

a is 1;

b is 0;

c is 0 to 3;

d is 0 or 1;

e is 0 to 3;

f is 0 or 1;

g is 0 to 4;

h is 0 to 1;

wherein the sum of d+f=1 or 2 and the sum of a, b, c, d, e, f, g and h is such that the hydrophobic tail of formula I has a linear main chain of between 5 and 7 carbon atoms.

2. The chimeric fatty bodyGRF analog of claim 1, wherein c is 0.

3. The chimeric fatty bodyGRF analog of claim 2, wherein A30 is Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu.

4. The chimeric fatty bodyGRF analog of claim 3, wherein R.sub.0 is NH.sub.2.

5. The chimeric fatty bodyGRF analog of claim 4, of the formula cisCH.sub.3 --CH.sub.2 --CH.dbd.CH--CH.sub.2 --CO-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Rsn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-S er-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln- Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH.sub.2 or transCH.sub.3 --CH.sub.2 --CH.dbd.CH--CH.sub.2 --CO-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-S er-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-AsH-Gln- Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH.sub.2.

6. The chimeric fatty bodyGRF analog of claim 1, wherein the sum d+f=2; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 =hydrogen atom and the sum c+e+g=2, 3 or 4.

7. The chimeric fatty bodyGRF analog of claim 1, wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 =hydrogen atom; and the sum c+e+g=3, 4 or 5.

8. The chimeric fatty body GRF analog of claim 4, of the formula transCH.sub.3 --CH.sub.2 --CH.dbd.CH--CH.sub.2 --CO-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-S er-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln- Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH.sub.2.

9. A pharmaceutical formulation for inducing growth hormone release which comprises as an active ingredient a GRF analog as claimed in claims 1 or 8, in association with a pharmaceutically acceptable carrier, excipient or diluent.

10. 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 claims 1 or 8.

11. A method for the diagnosis of growth hormone deficiencies in patients, which comprises administering to said patient a GRF analog as claimed in claims 1 or 8 and measuring the growth hormone response.

12. 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 claims 1 or 8.

13. 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 claims 1 or 8.

14. 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 claims 1 or 8.

15. 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 claims 1 or 8.

16. 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 claims 1 or 8.

17. 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 claims 1 or 8.
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