Estrogen beta receptor agonists to prevent or reduce the severity of cardiovascular disease

• US 20100152144A1
• Filed: 02/19/2010
• Published: 06/17/2010
• Est. Priority Date: 11/22/2002
• Status: Abandoned Application

• Current Assignee: Hermsmeyer R. Kent
• Original Assignee: Hermsmeyer R. Kent
• Inventors: Hermsmeyer, R. Kent
• Application Number:
  US12/660,088
• Publication Number:
  US 20100152144A1
• Time in Patent Office: Days
• US Class Current: 514/170
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/26 Androgens
• CPC Class Codes: A61P 5/30 Oestrogens
• CPC Class Codes: A61P 5/34 Gestagens
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 Antihypertensives

Abstract

A method for preventing or treating vascular hyperreactivity in which a chemical compound that is an estrogen beta receptor agonist is administered to a subject suffering from or at risk of vascular hyperreactivity. Preferably, the administration is topically to the skin.

Claims

1. A method for reducing the incidence or severity of vascular hyperreactivity in a patient in need thereof comprising administering to the patient an effective amount of a selective estrogen beta receptor agonist that has a higher relative potency for estrogen receptor beta compared to estrogen receptor alpha than that of genistein.

2. The method of claim 1 wherein the vascular hyperreactivity of the patient is manifested by coronary arterial vasospasm.

3. The method of claim 1 wherein the vascular hyperreactivity of the patient is manifested by hyperreactivity of peripheral arteries.

4. The method of claim 1 wherein the estrogen beta receptor agonist is co-administered with a hormone replacement therapy.

5. The method of claim 4 wherein the hormone replacement therapy is selected from the group consisting of estrogen, androgen, and progestin therapy.

6. The method of claim 1 wherein the estrogen beta receptor agonist is administered to the patient by topical application to skin.

7. The method of claim 6 wherein the estrogen beta receptor agonist is in a topical preparation selected from the group consisting of a liquid, cream, gel, lotion, ointment, and transdermal patch.

8. The method of claim 1 wherein the estrogen beta receptor agonist is administered to the patient by other than topical administration to skin.

9. The method of claim 8 wherein administration is by oral, rectal, vaginal, topical, sublingual, nasal, intradermal, inhalation, or sustained implant administration routes.

10. A kit for administering an estrogen beta receptor agonist compound to a patient suffering from or at risk of vascular hyperreactivity comprising a container, a topical preparation containing an estrogen beta receptor agonist in the container, and instructions for dispensing an amount of the preparation which provides an amount of the estrogen beta receptor agonist that is effective to prevent or reduce the severity of vascular hyperreactivity.

11. The kit of claim 10 wherein the estrogen beta receptor agonist is 5α

-androstane-3β

,17β

-diol.

12. The kit of claim 10 wherein the estrogen beta receptor agonist is a derivative of 5α

-androstane-3β

,17β

-diol that has estrogen beta receptor agonist activity.

13. The kit of claim 12 wherein the derivative of 5α

-androstane-3β

,17β

-diol is selected from the group consisting of 5α

-androstan-3β

,17β

-diol-3 hemisuccinate, 5α

-androstan-3β

,17β

-diol-17-sulphate sodium salt, 5α

-androstan-3β

,17β

-diol-3-acetate, 5α

-androstan-3β

,17β

-diol-17-acetate, 5α

-androstan-3β

,17β

-diol-diacetate, 5α

-androstan-3β

,17β

-diol-dibenzoate, 5α

-androstan-3β

,17β

-diol-dihemisuccinate, 5α

-androstan-3β

,17β

-diol-diproprionate, and 5α

-androstan-3β

,17β

-diol-17-hexahydrobenzoate.

14. The kit of claim 10 wherein the estrogen beta receptor agonist is epiestriol.

15. The kit of claim 10 wherein the estrogen beta receptor agonist is genistein or diarylpropionitrile.

16. The kit of claim 10 wherein the topical preparation is selected from the group consisting of a liquid, cream, gel, lotion, ointment, and transdermal patch.