USA flag logo/image

An Official Website of the United States Government

SYNTHESIS AND TESTING OF A NEW CLASS OF HEPARINOIDS

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
16732
Program Year/Program:
1991 / SBIR
Agency Tracking Number:
16732
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
RELIABLE BIOPHARMACEUTICAL CORPORATION
RELIABLE BIOPHARMACEUTICAL CORP. BOX 2517, 1945 WALTON RD ST. LOUIS, MO 63114
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 1991
Title: SYNTHESIS AND TESTING OF A NEW CLASS OF HEPARINOIDS
Agency: HHS
Contract: N/A
Award Amount: $50,000.00
 

Abstract:

THE GOAL OF THIS PROJECT IS TO DEVELOP A THERAPEUTIC AGENT WHICH WOULD REPLACE HEPARIN. ALTHOUGH HEPARIN IS THE BEST DRUG FOR TREATMENT OF THROMBOEMBOLIC DISEASE, IT IS UNSTABLE IF ADMINISTERED ORALLY AND MUST THEREFORE BE ADMINISTERED BY THE INTRAVENOUS OR SUBCUTANEOUS ROUTE. IN ADDITION, THE THROMBOCYTOPENIA AND BOTH BLEEDING AND THROMBOSIS, WHICH CAN EMERGE AS COMPLICATIONS OF THIS THERAPY, REMAIN A CLINICAL PROBLEM. RECENTLY, IN A PRELIMINARY REPORT, A GROUP OF SULFONATED BISLACTOBIONIC ACID AMINES HAVE BEEN DEMONSTRATED TO POSSESS ANTICOAGULANT AND ANTIOCCLUSIVE PROPERTIES COMPARABLE TO THOSE CURRENTLY ATTAINABLE WITH COMMERCIAL HEPARIN. STARTING WITH COMPOUNDS SUCH AS MALTOSE AND CELLOBIOSE, THE DISACCHARIDE IS OXIDIZED AND CONDENSED WITH SHORT CHAIN DIAMINES AND THEN SULPHONATED. OUR FIRM PRODUCES LARGE QUANTITIES OF LACTOBIONIC ACID FOR STABILIZATION OF ERYTHROMYCIN AND ORGANS FOR TRANSPLANT. DURING A LITERATURE SEARCH, WE FOUND THAT SULPHONATED BIS-LACTOBIONIC ACID AMINES ARE POTENTIAL ANTICOAGULANTS. IN HEPARIN, THE 3-0'-SULPHATE ON THE MIDDLE SUGAR IS ESSENTIAL FOR ANTICOAGULANT ACTIVITY. WE WILL PRODUCE CARBOHYDRATES OF VARIOUS STRUCTURE WHICH MAY HAVE AN IMPROVED HEPARIN-LIKE ACTIVITY. THE COMPOUNDS WILL BE INITIALLY TESTED FOR ANTICOAGULANT PROPERTIES IN PHASE I AND, LATER IN PHASE II, THEIR ANTITHROMBOTIC ACTIVITY WILL BE EVALUATED. THE ADVANTAGE OF USING MALTOSE AS A BEGINNING DISACCHARIDE IS THAT IT MAY NOT BE DIGESTED TO THE SAME DEGREE AS OTHER SUGARS. CELLOBIOSE IS ANOTHER STARTING DISACCHARIDE WHICH MAY NOT BE CLEAVED BY MAMMALIAN DIGESTIVE ENZYMES. ALSO, THE COMPOUNDS ARE RATHER SMALL, SOLUBLE AND MAY BE READILY ABSORBED. THESE SMALL POLYMERS ARE ALSO NON-TOXIC. ANTICOAGULANT PROPERTIES OF THE FINAL COMPOUNDS GENERATED WILL BE EXAMINED FOR THEIR ABILITY TO PROLONG THE ACTIVATED PARTIAL THROMBOPLASTIN TIME AND THE THROMBIN TIME. THE STANDARD WILL BE HEPARIN, 175 UNITS/MG. DR. TOLLEFSEN, ONE OF THE CONSULTANTS, WILL EXAMINE THE EFFECTS OF ACTIVE COMPOUNDS ON THE RATE OF THROMBIN INHIBITION BY PURIFIED ANTITHROMBIN III AND HEPARIN COFACTOR II AS ESTABLISHED IN HIS LABORATORY.

Principal Investigator:

Toce, Joseph A
Principal Investigator
3149977200

Business Contact:

1 r43 hl47230-01
Small Business Information at Submission:

Reliable Chemical Company
1161 Research Blvd St Louis, MO 63119

EIN/Tax ID:
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No