Method of using deuterated calcium channel blockers

• US 6,334,997 B1
• Filed: 04/26/2000
• Issued: 01/01/2002
• Est. Priority Date: 03/25/1994
• Status: Expired due to Fees

• Current Assignee: Isotechnika Inc. (Endo International PLC)
• Original Assignee: Isotechnika Inc. (Endo International PLC)
• Inventors: Foster, Robert T., Caille, Gilles, Lewanczuk, Richard
• Primary Examiner(s): Hartley, Michael G.
• Application Number:
  US09/558,325
• Time in Patent Office: 615 Days
• Field of Search: 424/1.81, 424/1.65, 424/1.11, 514/649, 514/717, 514/741, 514/821, 514/929, 514/721
• US Class Current: 424/1.81
• CPC Class Codes: C07B 59/002 Heterocyclic compounds

Abstract

A method of enhancing the efficiency and increasing the duration of action of drugs (e.g. dihydropyridines and anti-bacterials) and particularly of nifedipine and penicillins wherein one or more hydrogen atoms are deuterated and wherein the deuterated drug has unexpectedly improved properties when used in much lower concentrations than unmodified drug. A method for determining the identity and bioequivalency of a new drug is also disclosed wherein the molecular and isotope structure of a new drug is determined by isotope ratio mass spectrometry and compared with the molecular and isotope structure of a known human drug.

Claims

1. A method of blocking calcium channels with enhanced efficacy in an animal comprising administering to an animal in need thereof, an effective amount of a deuterated verapamil wherein an aromatic position of the verapamil is deuterated.

2. The method of claim 1 wherein the deuterated verapamil is represented by the formula:

3. The method of claim 1 wherein the enhanced efficacy is in the form of increased duration of action.

4. The method of claim 1 wherein the enhanced efficacy is in the form of increased use dependence.

5. A method of treating hypertension with enhanced efficacy in an animal comprising administering to an animal in need thereof, an effective amount of a deuterated verapamil wherein an aromatic position of the verapamil is deuterated.

6. The method of claim 5 wherein the deuterated verapamil is represented by the formula:

7. The method of claim 5 wherein the enhanced efficacy is in the form of increased duration of action.

8. The method of claim 5 wherein the enhanced efficacy is in the form of increased use dependence.