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Details for Patent: 6,238,878

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Details for Patent: 6,238,878

Title: FVlla/TF activity inhibiting compounds
Abstract:The invention relates to compounds inhibiting the activation of FX to FXa by TF/FVIIa. The compounds are anticoagulants. The invention also relates to a method of identifying a drug candidate.
Inventor(s): Jakobsen; Palle (V.ae butted.rl.o slashed.se, DK), Persson; Egon (.ANG.karp, SE)
Assignee: Novo Norkisk AIS (Bagsvaerd, DK)
Filing Date:Jul 13, 2000
Application Number:09/616,010
Claims:1. A method for identifying a compound having an inhibitory action on FVII-TF activity, said method comprising:

a) testing the effect of the compound in a FX activation assay,

b) testing the effect of the compound in a FXa amidolytic assay,

c) testing the effect of the compound in a TF/FVIIa amidolytic assay, and

d) selecting the compound as a compound having an inhibitory action on TF-FVII activity if the compound exhibits:

(i) half-maximal inhibition at a concentration of 20 .mu.M or less in a FX activation assay,

(ii) half-maximal inhibition at a concentration of 100 .mu.M or more in a FXa amidolytic assay, and

(iii) half-maximal inhibition at a concentration of 20 .mu.M or more in a TF/FVIIa amidolytic assay.

2. The method according to claim 1, wherein the method further comprises subjecting the selected compound to a FVIIa/TF-initiated clotting assay and selecting compounds showing clotting activity in said assay.

3. A method according to claim 2, wherein compounds showing an activity corresponding to a clot ratio of more than 1 in a FVIIa/TF-initiated clotting assay are selected.

4. The method for inhibiting the formation of FVIIa/TF/FX complex in a subject, comprising administering a drug candidate selected as described in claim 1 to a subject in need of such treatment.

5. The method according to claim 4, wherein the drug candidate substantially acts as an inhibitor of the activation of FX to FXa by TF/FVIIa.

6. Compounds identifiable by a method comprising the following steps:

a) testing the compound in a FX activation assay,

b) testing the compound in a FXa amidolytic assay,

c) testing the compound in a TF/FVIIa amidolytic assay, and

d) selecting the compound as a compound having an inhibitory action on TF-FVII activity if the compound exhibits:

(i) half-maximal inhibition at a concentration of 20 .mu.M or less in a FX activation assay,

(ii) half-maximal inhibition at a concentration of 100 .mu.M or more in a FXa amidolytic assay, and

(iii) half-maximal inhibition at a concentration of 20 .mu.M or more in a TF/FVIIa amidolytic assay.

7. Compounds according to claim 6, wherein the method further comprises subjecting the selected compound to a FVIIa/TF-initiated clotting assay and selecting compounds showing clotting activity in said assay.

8. Compounds according to claim 7, wherein compounds showing an activity corresponding to a clot ratio of more than 1 in a FVIIa/TF-initiated clotting assay of Example 4, are selected.

9. A pharmaceutical composition comprising a compound according to claim 6 and a pharmaceutical acceptable carrier or excipient.

10. A method for treatment of a FVIIa/TF-related disease or disorder in a subject, which method comprises administering an effective amount of at least one compound according to claim 6 to a subject in need of such treatment.

11. A method for treatment of a FVIIa/TF-related disease or disorder in a subject, which method comprises administering an effective amount of at least one drug candidate selected according to the method of claim 1 to a subject in need of such treatment.

12. A method according to claim 10, wherein the FVIIa/TF-related disease or disorder is deep venous thrombosis, arterial thrombosis, post surgical thrombosis, coronary artery bypass graft (CABG), percutaneous transdermal coronary angioplastry (PTCA), stroke, tumour metastasis, angiogenesis, thrombolysis, arteriosclerosis and restenosis following angioplastry, acute and chronic indications such as inflammation, septic chock, septicemia, hypotension, adult respiratory distress syndrome (ARDS), disseminated intravascular coagulopathy (DIC), pulmonary embolism, platelet deposition, myocardial infarction, or the prophylactic treatment of mammals with atherosclerotic vessels at risk for thrombosis, ex vivo FVIIa/TF related processes such as coagulation that may result from the extracorporeal circulation of blood, e.g. dialysis procedures, blood filtration, or blood bypass during surgery.
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