Claims
- 1. A method comprising administering an ANGELS compound to a subject by a dosage regimen that is effective to increase or maintain a bone property selected from the group consisting of bone mass, bone density and bone strength.
- 2. The method of claim 1 in which the ANGELS compound is non-phenolic.
- 3. The method of claim 2 in which the ANGELS compound is selected from the group consisting of estrenediol, androstenediol, estranediol, androstanediol, nor-estrenediol, homo-estrenediol, seco-estrenediol, nor-androstenediol, homo-androstenediol, seco-androstenediol, nor-estranediol, homo-estranediol, seco-estranediol, nor-androstanediol, homo-androstanediol, seco-androstanediol, and estratrienol.
- 4. The method of claim 3 in which the ANGELS compound is an estrenediol or an androstenediol.
- 5. The method of claim 4 in which the estrenediol is a 5(10)-estrenediol.
- 6. The method of claim 5 in which the 5(10)-estrenediol is selected from the group consisting of 5(10)-estrene-3α,17α-diol, 5(10)-estrene-3α,17β-diol, 5(10)-estrene-3β,17α-diol, and 5(10)-estrene-3β,17β-diol.
- 7. The method of claim 4 in which the ANGELS compound is a 5(6)-estrenediol or a 5(6)-androstenediol.
- 8. The method of claim 7 in which the ANGELS compound is selected from the group consisting of 5(6)-estrene-3α,17α-diol, 5(6)-estrene-3α,17β-diol, 5(6)-estrene-3β,17α-diol, 5(6)-estrene-3β,17β-diol, 5(6)-androstene-3α,17α-diol, 5(6)-androstene-3α,17β-diol, 5(6)-androstene-3β,17α-diol, and 5(6)-androstene-3α,17β-diol.
- 9. The method of claim 4 in which the ANGELS compound is a 4-estrenediol or a 4-androstenediol.
- 10. The method of claim 9 in which the ANGELS compound is selected from the group consisting of 4-estrene-3α,17α-diol, 4-estrene-3α,17β-diol, 4-estrene-3β,17α-diol, 4-estrene-3β,17α-diol, 4-androstene-3α,17α-diol, 4-androstene-3α,17β-diol, 4-androstene-3β,17α-diol, and 4-androstene-3α,17β-diol.
- 11. The method of claim 3 in which the ANGELS compound is an estranediol or an androstanediol.
- 12. The method of claim 11 in which the ANGELS compound is selected from the group consisting of estrane-3α,17α-diol, estrane-3α,17β-diol, estrane-3β,17α-diol, estrane-3β,17β-diol, androstane-3α,17α-diol, androstane-3α,17β-diol, androstane-3β,17α-diol, and androstane-3β,17β-diol
- 13. The method of claim 11 in which the ANGELS compound is a 5α-estranediol or a 5α-androstanediol.
- 14. The method of claim 12 in which the ANGELS compound is selected from the group consisting of 5α-estrane-3α,17α-diol, 5α-estrane-3α,17β-diol, 5α-estrane-3β,17α-diol, 5α-estrane-3β,17α-diol, 5α-androstane-3α,17α-diol, 5α-androstane-3α,17β-diol, 5α-androstane-3β,17α-diol, and 5α-androstane-3β,17β-diol.
- 15. The method of claim 11 in which the ANGELS compound is a 5β-estranediol or a 5β-androstanediol.
- 16. The method of claim 15 in which the ANGELS compound is selected from the group consisting of 5β-estrane-3α,17α-diol, 5β-estrane-3α,17β-diol, 5β-estrane-3β,17α-diol, 5β-estrane-3β,17β-diol, 5β-androstane-3α,17α-diol, 5β-androstane-3α,17β-diol, 5β-androstane-3β,17α-diol, and 5β-androstane-3β,17β-diol.
- 17. The method of claim 3 in which the ANGELS compound is selected from the group consisting of nor-estrenediol, homo-estrenediol, seco-estrenediol, nor-androstenediol, homo-androstenediol, seco-androstenediol, nor-estranediol, homo-estranediol, seco-estranediol, nor-androstanediol, homo-androstanediol, and seco-androstanediol.
- 18. The method of claim 17 in which the ANGELS compound is selected from the group consisting of nor-estrenediol, homo-estrenediol, and seco-estrenediol.
- 19. The method of claim 17 in which the ANGELS compound is selected from the group consisting of nor-estranediol, homo-estranediol, and seco-estranediol.
- 20. The method of claim 17 in which the ANGELS compound is selected from the group consisting of nor-androstenediol, homo-androstenediol, and seco-androstenediol.
- 21. The method of claim 17 in which the ANGELS compound is selected from the group consisting of nor-androstanediol, homo-androstanediol, and seco-androstanediol.
- 22. The method of claim 3 in which the ANGELS compound is an estratrienol.
- 23. The method of claim 20 in which the estratrienol is selected from the group consisting of estratrien-2-ol, estratrien-3-ol, estratrien-4-ol, and estratrien-5-ol.
- 24. The method of claim 20 in which the estratrienol is selected from the group consisting of seco-estratrienol, nor-estratrienol, and homo-estratrienol.
- 25. The method of claim 20 in which the estratrienol is selected from the group consisting of
- 26. The method of claim 25 in which R7, R8, R9, R10, R11, and R13 are each individually selected from the group consisting of hydrogen, methyl, ethyl, and trifluoromethyl.
- 27. The method of claim 1 in which the ANGELS compound is selected from the group consisting of
- 28. The method of claim 27 in which R is selected from the group consisting of hydrogen, methyl, and ethyl, and in which R′ and R″ are each individually selected from the group consisting of hydrogen, methyl, ethyl, propyl, trifluoromethyl, phenyl, 2-toluyl, 3-toluyl, and 4-toluyl.
- 29. The method of claim 1 in which the ANGELS compound is selected from the group consisting of
- 30. The method of claim 29 in which R1 is selected from the group consisting of hydrogen, methyl, ethyl, isopropyl, cyclohexyl, and phenyl; R2 is selected from the group consisting of hydrogen, methyl, ethyl, isopropyl, and trifluoromethyl; and R3 is selected from the group consisting of hydrogen, methyl, ethyl, isopropyl, phenyl, cyclohexyl, cyclopentyl, and 4-hydroxycyclohexyl.
- 31. The method of claim 1 in which the subject suffers from a bone disorder.
- 32. The method of claim 31 in which the bone disorder is selected from the group consisting of osteoporosis, Paget's disease, osteogenesis imperfecta, chronic hyperparathyroidism, hyperthyroidism, rheumatoid arthritis, Gorham-Stout disease, McCune-Albright syndrome, osteometastases of cancer, osteometastases of multiple myeloma and alveolar ridge bone loss.
- 33. The method of claim 32 in which the bone disorder is osteoporosis.
- 34. The method of claim 33 in which the osteoporosis is selected from the group consisting of postmenopausal, male, senile, glucocorticoid-induced, alcohol-induced, anorexia/amenorhea-related, immobilization-induced, weightlessness-induced, post-transplantation, migratory, idiopathic, and juvenile.
- 35. The method of claim 1 in which the bone property is bone mass.
- 36. The method of claim 1 in which the bone property is bone density.
- 37. The method of claim 1 in which the bone property is bone strength.
- 38. A method comprising administering an ANGELS compound to a subject by a dosage regimen that is effective to provide a treatment selected from the group consisting of increase libido, control vasomotor disturbance, promote vasodilation, reduce bone loss, reduce mood swings, lower cholesterol, decrease low density lipoproteins (LDL), increase high density lipoproteins (HDL), slow atherosclerosis, slow progression of cancer, slow progression of cardiovascular disease, slow age-related neurodegeneration, slow progression of neurodegenerative disease, reduce risk of cancer, reduce risk of cardiovascular disease, reduce risk of stroke, and reduce risk of neurodegenerative disease.
- 39. The method of claim 38 in which the dosage regimen is effective to control a vasomotor disturbance or promote vasodilation.
- 40. The method of claim 38 in which the dosage regimen is effective to slow progression of cardiovascular disease, slow atherosclerosis, reduce risk of cardiovascular disease, or reduce risk of stroke.
- 41. The method of claim 38 in which the dosage regimen is effective to lower cholesterol, decrease LDL, or increase HDL.
- 42. The method of claim 38 in which the dosage regimen is effective to slow age-related neurodegeneration, slow progression of neurodegenerative disease, or reduce risk of neurodegenerative disease.
- 43. The method of claim 38 in which the dosage regimen is effective to increase libido.
- 44. The method of claim 38 in which the dosage regimen is effective to reduce bone loss.
- 45. The method of claim 38 in which the dosage regimen is effective to reduce mood swings.
- 46. The method of claim 38 in which the dosage regimen is effective to reduce risk of cancer or slow progression of cancer.
- 47. A pharmaceutical composition comprising a compound represented by a formula selected from the group consisting of
- 48. The pharmaceutical composition of claim 47 in which the compound is represented by the formula
- 49. The pharmaceutical composition of claim 48 in which n is 1 or 3.
- 50. The pharmaceutical composition of claim 48 in which m is 1 or 3.
- 51. The pharmaceutical composition of claim 48 in which the compound is represented by the formula
- 52. The pharmaceutical composition of claim 51 in which R2 is selected from the group consisting of hydrogen, C1-C5 alkyl, phenyl, and C1-C5 alkyl substituted phenyl; R4 is selected from the group consisting of hydrogen, C1-C5 alkyl and ethynyl; and R5 is selected from the group consisting of hydrogen and C1-C5 alkyl.
- 53. The pharmaceutical composition of claim 47 in which the compound is represented by the formula
- 54. The pharmaceutical composition of claim 53 in which n is 1 or 3.
- 55. The pharmaceutical composition of claim 53 in which m is 1 or 3.
- 56. The pharmaceutical composition of claim 53 in which the compound is represented by the formula
- 57. The pharmaceutical composition of claim 56 in which R2 is selected from the group consisting of hydrogen, C1-C5 alkyl, phenyl, and C1-C5 alkyl substituted phenyl; R4 is selected from the group consisting of hydrogen, C1-C5 alkyl and ethynyl; and R5 is selected from the group consisting of hydrogen and C1-C5 alkyl.
- 58. The pharmaceutical composition of claim 47 in which the compound is represented by the formula
- 59. The pharmaceutical composition of claim 58 in which n is 1 or 3.
- 60. The pharmaceutical composition of claim 58 in which m is 1 or 3.
- 61. The pharmaceutical composition of claim 58 in which the compound is represented by the formula
- 62. The pharmaceutical composition of claim 61 in which in which R2 is selected from the group consisting of hydrogen, C1-C5 alkyl, phenyl, and C1-C5 alkyl substituted phenyl; R4 is selected from the group consisting of hydrogen, C1-C5 alkyl and ethynyl; and R5 is selected from the group consisting of hydrogen and C1-C5 alkyl.
- 63. The pharmaceutical composition of claim 47 in which the compound is represented by the formula
- 64. The pharmaceutical composition of claim 63 in which n is 1 or 3.
- 65. The pharmaceutical composition of claim 63 in which m is 1 or 3.
- 66. The pharmaceutical composition of claim 63 in which the compound is represented by the formula
- 67. The pharmaceutical composition of claim 66 in which in which R2 is selected from the group consisting of hydrogen, C1-C5 alkyl, phenyl, and C1-C5 alkyl substituted phenyl; R4 is selected from the group consisting of hydrogen, C1-C5 alkyl and ethynyl; and R5 is selected from the group consisting of hydrogen and C1-C5 alkyl.
- 68. A pharmaceutical composition comprising a compound represented by a formula selected from the group consisting of
- 69. The pharmaceutical composition of claim 68 in which the compound is represented by a formula selected from the group consisting of
- 70. The pharmaceutical composition of claim 69 in which R2 is selected from the group consisting of hydrogen, C1-C5 alkyl, phenyl, and C1-C5 alkyl substituted phenyl; R4 is selected from the group consisting of hydrogen, C1-C5 alkyl and ethynyl; and R5 is selected from the group consisting of hydrogen and C1-C5 alkyl.
- 71. The pharmaceutical composition of claim 68 in which the compound is represented by a formula selected from the group consisting of
- 72. The pharmaceutical composition of claim 71 in which R2 is selected from the group consisting of hydrogen, C1-C5 alkyl, phenyl, and C1-C5 alkyl substituted phenyl; R4 is selected from the group consisting of hydrogen, C1-C5 alkyl and ethynyl; and R5 is selected from the group consisting of hydrogen and C1-C5 alkyl.
- 73. The pharmaceutical composition of claim 68 in which the compound is represented by a formula selected from the group consisting of
- 74. The pharmaceutical composition of claim 73 in which R2 is selected from the group consisting of hydrogen, C1-C5 alkyl, phenyl, and C1-C5 alkyl-substituted phenyl; R4 is selected from the group consisting of hydrogen, C1-C5 alkyl and ethynyl; and R5 is selected from the group consisting of hydrogen and C1-C5 alkyl.
- 75. A pharmaceutical composition comprising a compound represented by a formula selected from the group consisting of
- 76. The pharmaceutical composition of claim 75 in which the compound is represented by a formula selected from the group consisting of
- 77. The pharmaceutical composition of claim 76 in which R13 and R14 are each individually selected from the group consisting of hydrogen, C1-C5 alkyl, cycloalkyl and phenyl; and in which R16 is hydroxyl.
- 78. The pharmaceutical composition of claim 75 in which the compound is represented by a formula selected from the group consisting of
- 79. The pharmaceutical composition of claim 78 in which R13, R14 and R15 are each individually selected from the group consisting of hydrogen, C1-C5 alkyl, cycloalkyl and phenyl.
- 80. The pharmaceutical composition of claim 75 in which the compound is represented by a formula selected from the group consisting of
- 81. The pharmaceutical composition of claim 80 in which R13, R14 and R15 are each individually selected from the group consisting of hydrogen, C1-C5 alkyl, cycloalkyl and phenyl.
- 82. A pharmaceutical composition comprising a compound represented by a formula selected from the group consisting of
- 83. The pharmaceutical composition of claim 82 in which the compound is represented by a formula selected from the group consisting of
- 84. The pharmaceutical composition of claim 83 in which R3 is selected from the group consisting of hydrogen, methyl and ethyl; and in which R5 and R6 are each individually selected from the group consisting of hydrogen and C1-C5 alkyl.
RELATED APPLICATION INFORMATION
[0001] This application claims priority to U.S. Provisional Application No. 60/299,009, filed Jun. 18, 2001, which is hereby incorporated by reference in its entirety.
FEDERAL FUNDING
[0002] This invention was funded in part through a grant from the National Institutes of Health. Therefore, the federal government has certain rights in this invention.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60299009 |
Jun 2001 |
US |