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Last Updated: March 28, 2024

Claims for Patent: 6,107,277


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Summary for Patent: 6,107,277
Title: Calcitonin salmon analogues
Abstract:Salcatonin (i.e. salmon calcitonin) analogues of formula R1-Ser-Asn-Leu-Ser-Thr-Cys(SR2)-Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Ly s-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn-Thr-Gly-Ser-Gly-Thr-Pro-NH2 (I) are disclosed, in which R1=-Cys-S--H, -Cys--OH, -Cys-S-ether or -Cys-S-ester (where the ether or ester residue has 2-5C) or a corresponding salt or isomer; R2=H, OH, ester or ether residue of 2-5C or acetamidomethyl, or a corresponding salt or isomer.
Inventor(s): Veronesi; Paolo Alberto (Milan, IT), Peschechera; Emanuela (Milan, IT), Veronesi; Anna Maria (Umbra, IT)
Assignee: Therapicon S.R.L. (Milan, IT)
Application Number:08/907,602
Patent Claims:1. A salcatonin analogue of the formula: ##STR2## wherein R.sub.1 is -Cys-S-H or -Cys-S-OH or -Cys-S-ester or Cys-S-ether wherein the ester or ether has from 2 to 5 carbon atoms or pharmaceutically acceptable salts or isomers thereof and

R.sub.2 is hydrogen or hydroxy or an ester or an ether having from 2 to 5 carbons atoms or a pharmaceutically acceptable salt of isomer thereof,

provided that when R.sub.1 is -Cys-S--H, then R.sub.2 is not hydrogen.

2. A salcatonin analogue of the formula: ##STR3## Where R.sub.1 and R.sub.2 are selected from the following:

3. The salcatonin analogue of claim 1, wherein R.sub.1 is -Cys-S--OH or -Cys-S-ester, wherein the ester has from 2 to 5 carbon atoms or pharmaceutically acceptable salts or isomers thereof, and

R.sub.2 is hydrogen.

4. The salcatonin analogue of claim 1, wherein

R.sub.1 is -Cys-S--H, and

R.sub.2 is hydroxy or an ester having from 2 to 5 carbons atoms or a pharmaceutically acceptable salt of isomer thereof.

5. A pharmaceutical formula comprising an analogue as claimed in claim 1.

6. A pharmaceutical formula as claimed in claim 5 wherein the analogue is in solution or suspension in a suitable pharmaceutical carrier.

7. A pharmaceutical formula as claimed in claim 6 further comprising sterile water, other sterile liquid, pharmaceutically acceptable excipients or adjuvants or a combination of two or more thereof.

8. A process for the preparation of an analogue as claimed in claim 1 comprising oxidation of salcatonin in the presence of a suitable agent and anhydrous methanol at a temperature in the range of from -10.degree. C. to 20.degree. C. for up to approximately 21/2 hours followed by purification.

9. A process as claimed in claim 8 wherein the suitable agent is H.sub.2 O.sub.2, performic acid, percloric acid, O.sub.3, chloranil or a combination of two or more thereof.

10. An analogue as claimed in claim 1 for use in the inhibition of physiological or pathological bone re-absorption.

11. An analogue as claimed in claim 1 for use as a hypocalcemic agent.

12. An analogue as claimed in claim 1 for administration in a daily dose of 10 I.U. to 400 I.U.

13. An analogue as claimed in claim 1 for administration in a daily dose of 100 I.U. to 200 I.U.

14. A process for determining the content of hydroxysalcatonins in a salcatonin preparation comprising comparing the amount of hydroxysalcatonin in the salcatonin preparation to a standard containing a known amount of a hydroxysalcatonin analogue as claimed in claim 1.

15. A process as claimed in claim 14 which is a chromatographic analytical test.

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