# US 5,710,174 A · Factor XIIIA inhibitor

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- Number: US 5,710,174 A
- Document ID: US5710174A
- Status: Granted
- Kind: A
- Application number: 08/483,213
- Filed: 1995-06-07
- Granted: 1998-01-20
- Earliest claimed: 1995-06-07
- Assignees: Zymo Genetics, Inc.; Novo Nordisk A/S
- Inventors: Robert R. West; Teresa Martinez; Hank R. Franklin; Paul D. Bishop; Birgitte R.o slashed.mer Rassing
- Web page: https://patentgrep.com/patent/US5710174A

## CPC

- C12P 17/12: containing a six-membered hetero ring
- A61K 31/365: Lactones
- A61K 38/484: {Plasmin (3.4.21.7)}
- A61K 38/49: Urokinase; Tissue plasminogen activator
- C07D 313/00: Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
- C12P: FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE {(brewing of beer C12C; producing vinegar C12J; producing specific peptides or proteins C07K; producing enzymes C12N9/00; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; measuring or testing processes involving enzymes or microorganisms C12Q; measuring or testing processes involving nucleic acid amplification reactions C12Q1/6844; fermentation processes to form a food composition, A21 or A23; compounds in general, see the relevant compound class, e.g. C01, C07)}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

A compound that is useful for inhibiting FXIIIa catalysis of fibrin cross-linking, and related pharmaceutical compositions and methods, are disclosed. The compound and compositions may be advantageously used to enhance fibrinolysis and resolution of blood clots.

## Claims

### Claim 1

A pharmaceutical composition comprising a compound having the structure: ##STR2## a buffer, and a pharmaceutically acceptable vehicle.

### Claim 2

A pharmaceutical composition comprising a compound having the structure: ##STR3## a pharmaceutically acceptable vehicle, and a fibrinolytic agent.

### Claim 3 (depends on 2)

The pharmaceutical composition of claim 2, wherein the fibrinoloytic agent is selected from the group consisting of plasminogen, one or more plasminogen activators; and a combination of plasminogen and one or more plasminogen activators.

### Claim 4

A method for inhibiting FXIIIa catalysis of fibrin cross-linking in vivo comprising:
administering to a recipient a therapeutic amount of a pharmaceutical composition comprising a compound having the structure: ##STR4## and a pharmaceutically acceptable vehicle, in an amount sufficient to inhibit FXIIIa catalysis of fibrin cross-linking.

### Claim 5 (depends on 4)

The method of claim 4 further comprising the step of administering to the recipient a fibrinolytic agent selected from the group consisting of plasminogen; one or more plasminogen activators; and a combination of plasminogen and one or more plasminogen activators.

### Claim 6 (depends on 5)

The method of claim 5, wherein the fibrinolytic agent is administered before, after or concurrent with administration of the pharmaceutical composition.

### Claim 7 (depends on 5)

The method of claim 5, wherein the recipient is at high risk of thrombosis.

### Claim 8 (depends on 7)

The method of claim 7, wherein the recipient has a medical indication selected from the group consisting of: myocardial infarction; an occluded artery; stroke; phlebitis; deep vein thrombosis; disseminated intravascular coagulation; and pulmonary embolism.

### Claim 9 (depends on 7)

The method of claim 7, wherein the recipient has undergone or will undergo a medical procedure that disposes the recipient to blood clot formation.