Use of extracts containing phytoestrogen selectively modulating estrogen-receptor-beta

• US 20050220900A1
• Filed: 02/10/2003
• Published: 10/06/2005
• Est. Priority Date: 02/15/2002
• Status: Abandoned Application

• Current Assignee: Bionorica AG
• Original Assignee: Bionorica AG
• Inventors: Popp, Michael, Spengler, Barbara, Wuttke, Wolfgang, Christoffel, Volker, Jarry, Hubertus
• Application Number:
  US10/505,031
• Publication Number:
  US 20050220900A1
• Time in Patent Office: Days
• US Class Current: 424/725
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 36/85 Verbenaceae (Verbena family)
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 5/30 Oestrogens
• CPC Class Codes: A61P 5/34 Gestagens
• 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

The present invention relates to the use of phytoestrogen-containing extracts that selectively modulate estrogen receptor beta (ER-beta) without producing any uterotropic effect, for the treatment of clinical situations and pathophysiological conditions that are selected from the group consisting of: Obesity and thereby to possibly influence the metabolic syndrome, particularly hypertension, asterosclerosis, cardiac infarct, hyperandrogenemia; Menopausal continence disorders; Menopausal heat surges associated with hyperstimulation of the hypothalamic gonadotropin releasing hormone pulse generator; steroid hormonal synthesis disorder, particularly that of progesterone synthesis of the human corpus luteum, resulting in luteal insuffeciency; Alzheimer'"'"'s disease associated with elevated expression of estrogen receptor beta in hippocampal neurons.

Claims

1-3. -3. (canceled)

4. (canceled)

5-7. -7. (canceled)

8. A method for treating clinical situations and pathophysiological conditions comprising the step of administering a phytoestrogen-containing extract, wherein said phyto-estrogen containing extract selectively modulates the estrogen receptor beta without producing a uterotropic effect, and wherein the clinical situations and pathophysiological conditions are selected from the group consisting of obesity;

menopausal continence disorders;

menopausal heat surges associated with hyperstimulation of the hypothalamic gonadotropin releasing hormone pulse generator;

steroid hormonal synthesis disorders; and

Alzheimer'"'"'s disease associated with elevated expression of estrogen receptor beta in hippocampal neurons.

9. The treatment method of claim 8 wherein the clinical situations and pathophysiological conditions is obesity and the treatment influences the metabolic syndrome, thereby influencing the cause of hypertension.

10. The treatment method of claim 8 wherein the clinical situations and pathophysiological conditions is obesity and the treatment influences the metabolic syndrome, thereby influencing the cause of arteriosclerosis.

11. The treatment method of claim 8 wherein the clinical situations and pathophysiological conditions is obesity and the treatment influences the metabolic syndrome, thereby influencing the cause of cardiac infarct.

12. The treatment method of claim 8 wherein the clinical situations and pathophysiological conditions is obesity and the treatment influences the metabolic syndrome, thereby influencing the cause of hyperandrogenemia.

13. The treatment method of claim 8 wherein the steroid hormonal synthesis disorders is that of progesterone synthesis of the human corpus luteum, resulting in luteal insufficiency.

14. The use of claim 8 wherein the phytoestrogen-containing extract is an ethanol or CO₂ extract from the vitex agnus castus.

15. The treatment method of claim 8 wherein the phytoestrogen-containing extract is a standard pharmaceutical formulation.

16. The use of claim 15 wherein the phytoestrogen-containing extract is an ethanol or CO₂ extract from the vitex agnus castus.

17. The treatment method of claim 15 wherein the pharmaceutical formulation of the phytoestrogen-containing extract is selected from the group consisting of drops, tablets, coated tablets, capsules, granulates, dragé

es, suppositories, ointments and creams.

18. The use of claim 17 wherein the pharmaceutical formulation is an ethanol or CO₂ extract from the vitex agnus castus.