Use of calpain inhibitors in the inhibition and treatment of...

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/37 (2006.01) A61K 31/35 (2006.01) A61K 31/365 (2006.01) A61K 38/04 (2006.01) A61K 38/55 (2006.01) C12N 5/00 (2006.01)

Patent

CA 2138124

The present invention provides a method of treating a medical condition associated with increased proteolytic activity of Calpain in a mammal. The method includes administering a pharmaceutical composition containing a Calpain inhibitor com- pound to the mammal in an amount that is pharmacologically effective to treat the condition. The inhibitor is a compound in one of the following groups of compounds: Peptide Keto-Compounds, Substituted Heterocyclic Compounds or Halo-Ketone Pep- tides. Examples of conditions that can be treated using the methods of the present invention include cardiac muscle tissue da- mage, cataracts, smooth muscle damage and vasospasm. The present invention also provides a method of inhibiting smooth mus- cle cell proliferation and thereby preventing the restenosis of a blood vessel which has been undergone therapeutic angioplasty. This method includes the administration of a calpain inhibitor to the blood vessel during or after the angioplasty procedure. Fur- ther, methods of blocking the establishment of the tonically contracted state in smooth muscle and relaxing tonically contracted smooth muscle are disclosed. These methods involve the administration of a calpain inhibitor, thereby reducing or preventing smooth muscle contraction associated with vasospasm and bronchospasm.

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