Claims
- 1. A composition comprising:
(a) at least one hormone replacement therapy composition; and (b) at least one sterol or 5α-stanol absorption inhibitor or a pharmaceutically acceptable salt thereof or a solvate thereof.
- 2. The composition according to claim 1, wherein the at least one hormone replacement therapy composition comprises one or more agents selected from the group consisting of androgens, estrogens, phytoestrogens, progestins, their pharmaceutically acceptable salts and derivatives thereof.
- 3. The composition according to claim 2, wherein the androgens are selected from the group consisting of methyltestosterone (17-hydroxy-17-methyl-(17B)- androst-4-en-3-one) and combinations thereof.
- 4. The composition according to claim 2, wherein the estrogens are selected from the group consisting of sodium estrone sulfate, sodium equilin sulfate, sodium 17 α-dihydroequilin sulfate, sodium 17 α-estradiol sulfate, sodium 17 β-dihydroequilin sulfate, sodium 17 α-dihydroequilenin sulfate, sodium 17 β-dihydroequilenin sulfate, sodium equilenin sulfate and sodium 17 β-estradiol sulfate, ethinyl estradiol (19-nor-17 α-pregna-1,3,5(10)-trien-20-yne-3,17-diolestropipate (piperazine estra-1,3,5(10)-trien-17-one, 3-(sulfooxy)- estrone sulfate); and combinations thereof.
- 5. The composition according to claim 2, wherein the phytoestrogens comprises one or more soy isoflavones.
- 6. The composition according to claim 2, wherein the progestins are selected from the group consisting of norethindrone, norgestrel, micronized progesterone (pregn-4-ene-3, 20-dione), medroxyprogesterone and combinations thereof.
- 7. The composition according to claim 2, wherein the hormone replacement therapy composition comprises a combination of progestins and estrogens selected from the group consisting of the combination of estradiol (estra-1, 3, 5 (10)-triene-3, 17 β-diol hemihydrate) and norethindrone (17 β-acetoxy-19-nor-17 α-pregn-4-en-20-yn-3-one), the combination of levonorgestrel (d(−)-13 β-ethyl-17 α-ethinyl-17 β-hydroxygon-4-en-3-one), the combination of ethynodiol diacetate (19-nor-17 α-pregn-4-en-20-yne-3 β, 17-diol diacetate) and ethinyl estradiol, the combination of desogestrel (13-ethyl-11-methylene-18,19-dinor-17 α-pregn-4-en-20-yn-17-ol) and ethinyl estradiol, the combination of norethindrone and ethinyl estradiol, the combination of norgestrel ((±)-13-ethyl-17-hydroxy-18, 19-dinor-17 α-preg-4-en-20-yn-3-one) and ethinyl estradiol, the combination of norethindrone, ethinyl estradiol, mestranol (3-methoxy-19-nor-17 α-pregna-1,3,5(10)-trien-20-yn-17-ol),the combination of 17 β-estradiol (estra-1,3,5(10)-triene-3, 17 β-diol) and micronized norgestimate (17 α-17-(Acetyloxyl)-13-ethyl-18, 19-dinorpregn-4-en-20-yn-3-one3-oxime), the combination of norgestimate (18, 19-dinor-17-pregn-4-en-20-yn-3-one, 17-(acetyloxy)-13-ethyl-,oxime, (17(α)-(+)-) and ethinyl estradiol, and the combination of conjugated estrogens (sodium estrone sulfate and sodium equilin sulfate) and medroxyprogesterone acetate (20-dione, 17-(acetyloxy)-6-methyl-, (6(α))-pregn-4-ene-3).
- 8. The composition according to claim 2, wherein the hormone replacement therapy composition is an androgen and estrogen combination selected from the group consisting of the combination of esterified estrogens (sodium estrone sulfate and sodium equilin sulfate) and methyltestosterone (17-hydroxy-17-methyl-, (17B)- androst-4-en-3-one).
- 9. The composition according to claim 1, wherein the at least one hormone replacement therapy composition is administered to a subject in an amount ranging from about 0.1 to about 3000 milligrams of hormone replacement therapy composition per day.
- 10. The composition of claim 1, wherein the sterol or 5α-stanol absorption inhibitor is represented by Formula (I):
- 11. The composition according to claim 10, wherein the sterol or 5α-stanol absorption inhibitor is represented by Formula (II) below:
- 12. The composition of claim 1, wherein the sterol or 5α-stanol absorption inhibitor is represented by Formula (III):
- 13. The composition of claim 1, wherein the sterol or 5α-stanol absorption inhibitor is represented by Formula (IV):
- 14. The composition of claim 1, wherein the sterol or 5α-stanol absorption inhibitor is represented by Formula (V):
- 15. The composition of claim 1, wherein the sterol or 5α-stanol absorption inhibitor selected is represented by Formula (VI):
- 16. The composition of claim 1, wherein the sterol or 5α-stanol absorption inhibitor is represented by Formula (VIIA) or (VIIB):
- 17. The composition of claim 1, wherein the sterol or 5α-stanol absorption inhibitor is represented by Formula (VII):
- 18. The composition of claim 1, wherein the sterol or 5α-stanol absorption inhibitor is represented by Formula (IX):
- 19. The composition according to claim 1, wherein the at least one sterol or 5α-stanol absorption inhibitor is administered to a subject in an amount ranging from about 0.1 to about 1000 milligrams of sterol absorption inhibitor per day.
- 20. The composition according to claim 1, wherein the subject is a post menopausal woman.
- 21. The composition according to claim 1, further comprising at least one cholesterol biosynthesis inhibitor.
- 22. The composition according to claim 21, wherein the at least one cholesterol biosynthesis inhibitor comprises at least one HMG CoA reductase inhibitor.
- 23. The composition according to claim 22, wherein the at least one HMG CoA reductase inhibitor is selected from the group consisting of lovastatin, pravastatin, fluvastatin, simvastatin, atorvastatin, cerivastatin and mixtures thereof.
- 24. The composition according to claim 23, wherein the at least one HMG CoA reductase inhibitor is simvastatin.
- 25. The composition according to claim 1, further comprising at least one PPAR activator.
- 26. The composition according to claim 1, further comprising at least one bile acid sequestrant.
- 27. The composition according to claim 1, further comprising nicotinic acid or a derivative thereof.
- 28. The composition according to claim 1, further comprising at least one AcylCoA:Cholesterol O-acyltransferase Inhibitor.
- 29. The composition according to claim 1, further comprising probucol or a derivative thereof.
- 30. The composition according to claim 1, further comprising at least one low-density lipoprotein receptor activator.
- 31. The composition according to claim 1, further comprising at least one Omega 3 fatty acid.
- 32. The composition according to claim 1, further comprising at least one natural water soluble fiber.
- 33. The composition according to claim 1, further comprising at least one of plant sterols, plant stanols or fatty acid esters of plant stanols.
- 34. The composition according to claim 1, further comprising at least one antioxidant or vitamin.
- 35. A pharmaceutical composition for the treatment or prevention of a vascular condition, hypertension, diabetes, obesity, lowering a concentration of a sterol or 5α-stanol in plasma of a subject, or as a hormone replacement therapy/vascular condition treatment for a subject, comprising a therapeutically effective amount of the composition of claim 1 and a pharmaceutically acceptable carrier.
- 36. A method of treating or preventing a vascular condition, hypertension, diabetes, obesity, lowering a concentration of a sterol or 5α-stanol in plasma of a subject, or as a hormone replacement therapy/vascular condition treatment for a subject, comprising the step of administering to a mammal in need of such treatment an effective amount of the composition of claim 1.
- 37. The method according to claim 36, wherein the vascular condition is hyperlipidemia.
- 38. A therapeutic combination comprising:
(a) a first amount of at least one hormone replacement therapy composition; and (b) a second amount of at least one sterol or 5α-stanol absorption inhibitor or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein the first amount and the second amount together comprise a therapeutically effective amount for the treatment or prevention of a vascular condition, hypertension, diabetes, obesity, lowering a concentration of a sterol or 5α-stanol in plasma of a subject or as a hormone replacement therapy/vascular condition treatment for a subject.
- 39. A therapeutic combination according to claim 38, wherein the at least one hormone replacement therapy composition is administered concomitantly with the at least one sterol or 5α-stanol absorption inhibitor.
- 40. A therapeutic combination according to claim 38, wherein the at least one hormone replacement therapy composition and the at least one or 5α-stanol sterol absorption inhibitor are present in separate treatment compositions.
- 41. A method of treating or preventing a vascular condition, hypertension, obesity, lowering a concentration of a sterol or 5α-stanol in plasma of a subject or as a hormone replacement therapy/vascular condition treatment for a mammal, comprising the step of administering to a subject in need of such treatment an effective amount of the therapeutic combination of claim 31.
- 42. A hormone replacement therapy/vascular condition treatment composition comprising: (a) at least one hormone replacement therapy composition; and (b) at least one sterol or 5α-stanol absorption inhibitor or a pharmaceutically acceptable salt thereof or a solvate thereof.
- 43. A method of treating a vascular condition, hypertension, obesity, or lowering a concentration of a sterol or 5α-stanol in plasma of a post menopausal woman, comprising administering to a post menopausal woman at least one sterol or 5α-stanol absorption inhibitor or a pharmaceutically acceptable salt thereof or a solvate thereof.
- 44. The method according to claim 43, wherein the at least one sterol or 50α-stanol absorption inhibitor is represented by Formula (II):
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of priority from U.S. Provisional Patent Application Serial No. 60/324,118, filed Sep. 21, 2001, and is a continuation-in-part of U.S. patent application Ser. No.10/166,942, filed Jun. 11, 2002, each incorporated herein by reference.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60324118 |
Sep 2001 |
US |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
10166942 |
Jun 2002 |
US |
Child |
10247085 |
Sep 2002 |
US |