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US 2003/0207435 A1Published application
Protein c derivatives
AssigneeEli Lilly and Company
InventorsBruce Edward Gerlitz, Bryan Edward Jones
Life of this patent
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Abstract
Novel human protein C derivatives are described. These derivatives have increased anti-coagulation activity and resistance to inactivation by serpins compared to wild-type protein C and retain the biological activity of the wild-type human protein C. These derivatives will require either less frequent administration and/or smaller dosage than wild-type human protein C in the treatment of acute coronary syndromes, vascular occlusive disorders, hypercoagulable states, thrombotic disorders and disease states predisposing to thrombosis.
Claims26
A human protein C derivative comprising SEQ ID NO:
- 1 having at least two amino acid substitutions selected from the group consisting of:
- His at position 10 is substituted with Gln;
- Ser at position 11 is substituted with Gly;
- Ser at position 12 is substituted with Lys;
- Gln at position 32 is substituted with Glu;
- Asn at position 33 is substituted with Asp or Phe;
- and, the amino acid at position 194, 195, 228, 249, 254, 302, or 316 is substituted with an amino acid selected from Ser, Ala, Thr, His, Lys, Leu, Arg, Asn, Asp, Glu, Gly, and Gln.
4 more elements
Dependencies are inferred from the claim text.