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US 6,958,322 B1Granted
Factor X analog with an improved ability to be activated
AssigneeBaxter Aktiengesellschaft
InventorsMichele Himmelspach, Uwe Schlokat
Life of this patent
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Abstract
This invention describes a factor Xa analog which has a substitution of a minimum of one of the amino acid between Glu226 and Arg234 and possibly Ile235, relative to the amino acid numbering according to FIG. 1, a preparation containing the activated form of the factor X analog, and a method for the production of these molecules.
Claims29
A Factor X analog which contains one or more modifications in SEQ ID NO:2 selected from the group consisting of:
- a) Ile235 is Val or Ala;
- b) Thr233 is Ser or Asn;
- c) Leu232 is Phe, Arg or Ile;
- d) Asn231 is Asp, Lys, Thr, or Glu;
- e) Asn230 is Ser, Lys, Met, Thr, or Asp;
- f) Asp229 is Phe, Thr, Ser, Pro, Leu, or Ile;
- g) Gly228 is Ser, Gln, Ile, Thr, Asn, or Pro;
- and
- h) Arg227 is Gln, Ser, His, Tyr, or Glu.
6 more elements
A Factor X analog which
- (i) contains one or more modifications in SEQ ID NO:2 selected from the group consisting of:
- a) Ile235 is Val or Ala;
- b) Thr233 is Ser or Asn;
- c) Leu232 is Phe, Arg or Ile;
- d) Asn231 is Asp, Lys, Thr, or Glu;
- e) Asn230 is Ser, Lys, Met, Thr, or Asp;
- f) Asp229 is Phe, Thr, Ser, Pro, Leu, or Ile;
- g) Gly228 is Ser, Gln, Ile, Thr, Asn, or Pro;
- and
- h) Arg227 is Gln, Ser, His, Tyr, or Glu;
- and
- (ii) has a further modification occurring at Lys370 and/or within a segment extending from Arg 469 to Ser476 of SEQ ID NO:2.
9 more elements
A Factor X analog which
- (i) contains one or more modifications in SEQ ID NO:2 selected from the group consisting of:
- a) Ile235 is Val or Ala;
- b) Thr233 is Ser or Asn;
- c) Leu232 is Phe, Arg or Ile;
- d) Asn231 is Asp, Lys, Thr, or Glu;
- e) Asn230 is Ser, Lys, Met, Thr, or Asp;
- f) Asp229 is Phe, Thr, Ser, Pro, Leu, or Ile;
- g) Gly228 is Ser, Gln, Ile, Thr, Asn, or Pro;
- and
- h) Arg227 is Gln, Ser, His, Tyr, Glu;
- and
- (ii) has a further modification which is a deletion of Factor X β-peptide (Gly470 to Lys488 of SEQ ID NO:2).
9 more elements
Dependencies are inferred from the claim text.