1. A compound having the formula:
where X1 and X2, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
2. The compound of claim 1 wherein X2 is hydrogen.
3. The compound of claim 1 wherein X1 is hydrogen.
4. The compound of claim 1 wherein X1 and X2 are all t-butyldimethylsilyl.
5. A pharmaceutical composition containing an effective amount of at least one compound as claimed in claim 1 together with a pharmaceutically acceptable excipient.
6. The pharmaceutical composition of claim 5 wherein said effective amount comprises from about 0.01 \u03bcg to about 1000 \u03bcg per gram of composition.
7. The pharmaceutical composition of claim 5 wherein said effective amount comprises from about 0.1 \u03bcg to about 500 \u03bcg per gram of composition.
8. (20R)-23,23-difluoro-1\u03b1-hydroxy-2-methylene-19-nor-bishomopregnacalciferol having the formula:
9. A pharmaceutical composition containing an effective amount of (20R)-23,23-difluoro-1\u03b1-hydroxy-2-methylene-19-nor-bishomopregnacalciferol together with a pharmaceutically acceptable excipient.
10. The pharmaceutical composition of claim 9 wherein said effective amount comprises from about 0.01 \u03bcg to about 1000 \u03bcg per gram of composition.
11. The pharmaceutical composition of claim 9 wherein said effective amount comprises from about 0.1 \u03bcg to about 500 \u03bcg per gram of composition.
12. A method of treating psoriasis comprising administering to a subject with psoriasis an effective amount of a compound having the formula:
where X1 and X2 which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
13. The method of claim 12 wherein the compound is administered orally.
14. The method of claim 12 wherein the compound is administered parenterally.
15. The method of claim 12 wherein the compound is administered transdermally.
16. The method of claim 12 wherein the compound is administered topically.
17. The method of claim 12 wherein the compound is administered rectally.
18. The method of claim 12 wherein the compound is administered nasally.
19. The method of claim 12 wherein the compound is administered sublingually.
20. The method of claim 12 wherein the compound is administered in a dosage of from about 0.01 \u03bcgday to about 1000 \u03bcgday.
21. The method of claim 12 wherein the compound is (20R)-23,23-difluoro-1\u03b1-hydroxy-2-methylene-19-nor-bishomopregnacalciferol having the formula:
22. A method of treating a disease selected from the group consisting of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer comprising administering to a subject with said disease an effective amount of a compound having the formula:
where X1 and X2 which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
23. The method of claim 22 wherein the compound is administered orally.
24. The method of claim 22 wherein the compound is administered parenterally.
25. The method of claim 22 wherein the compound is administered transdermally.
26. The method of claim 22 wherein the compound is administered rectally.
27. The method of claim 22 wherein the compound is administered nasally.
28. The method of claim 22 wherein the compound is administered sublingually.
29. The method of claim 22 wherein the compound is administered in a dosage of from about 0.01 \u03bcgday to about 1000 \u03bcgday.
30. The method of claim 22 wherein the compound is (20R)-23,23-difluoro-1\u03b1-hydroxy-2-methylene-19-nor-bishomopregnacalciferol having the formula:
31. A method of treating an autoimmune disease selected from the group consisting of multiple sclerosis, lupus, diabetes mellitus, host versus graft rejection, and rejection of organ transplants, comprising administering to a subject with said disease an effective amount of a compound having the formula:
where X1 and X2 which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
32. The method of claim 31 wherein the compound is administered orally.
33. The method of claim 31 wherein the compound is administered parenterally.
34. The method of claim 31 wherein the compound is administered transdermally.
35. The method of claim 31 wherein the compound is administered rectally.
36. The method of claim 31 wherein the compound is administered nasally.
37. The method of claim 31 wherein the compound is administered sublingually.
38. The method of claim 31 wherein the compound is administered in a dosage of from about 0.01 \u03bcgday to about 1000 \u03bcgday.
39. The method of claim 31 wherein the compound is (20R)-23,23-difluoro-1\u03b1-hydroxy-2-methylene-19-nor-bishomopregnacalciferol having the formula:
40. A method of treating an inflammatory disease selected from the group consisting of rheumatoid arthritis, asthma, and inflammatory bowel diseases, comprising administering to a subject with said disease an effective amount of a compound having the formula:
where X1 and X2, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
41. The method of claim 40 wherein the compound is administered orally.
42. The method of claim 40 wherein the compound is administered parenterally.
43. The method of claim 40 wherein the compound is administered transdermally.
44. The method of claim 40 wherein the compound is administered rectally.
45. The method of claim 40 wherein the compound is administered nasally.
46. The method of claim 40 wherein the compound is administered sublingually.
47. The method of claim 40 wherein the compound is administered in a dosage of from about 0.01 \u03bcgday to about 1000 \u03bcgday.
48. The method of claim 40 wherein the compound is (20R)-23,23-difluoro-1\u03b1-hydroxy-2-methylene-19-nor-bishomopregnacalciferol having the formula:
49. A method of treating a skin condition selected from the group consisting of wrinkles, lack of adequate skin firmness, lack of adequate dermal hydration and insufficient sebum secretion which comprises administering to a subject with said skin condition an effective amount of a compound having the formula:
where X1 and X2 which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
50. The method of claim 49 wherein the compound is administered orally.
51. The method of claim 49 wherein the compound is administered parenterally.
52. The method of claim 49 wherein the compound is administered transdermally.
53. The method of claim 49 wherein the compound is administered topically.
54. The method of claim 49 wherein the compound is administered rectally.
55. The method of claim 49 wherein the compound is administered nasally.
56. The method of claim 49 wherein the compound is administered sublingually.
57. The method of claim 49 wherein the compound is administered in a dosage of from about 0.01 \u03bcgday to about 1000 \u03bcgday.
58. The method of claim 49 wherein the compound is (20R)-23,23-difluoro-1\u03b1-hydroxy-2-methylene-19-nor-bishomopregnacalciferol having the formula:
59. A method of treating renal osteodystrophy comprising administering to a subject with renal osteodystrophy an effective amount of a compound having the formula:
where X1 and X2, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
60. The method of claim 59 wherein the compound is administered orally.
61. The method of claim 59 wherein the compound is administered parenterally.
62. The method of claim 59 wherein the compound is administered transdermally.
63. The method of claim 59 wherein the compound is administered rectally.
64. The method of claim 59 wherein the compound is administered nasally.
65. The method of claim 59 wherein the compound is administered sublingually.
66. The method of claim 59 wherein the compound is administered in a dosage of from about 0.01 \u03bcgday to about 1000 \u03bcgday.
67. The method of claim 59 wherein the compound is (20R)-23,23-difluoro-1\u03b1-hydroxy-2-methylene-19-nor-bishomopregnacalciferol having the formula:
68. A method of treating or preventing obesity of an animal, inhibiting adipocyte differentiation, inhibiting SCD-1 gene transcription, andor reducing body fat in an animal comprising administering to an animal in need thereof an effective amount of a compound having the formula
where X1 and X2, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
69. The method of claim 68 wherein the compound is administered orally.
70. The method of claim 68 wherein the compound is administered parenterally.
71. The method of claim 68 wherein the compound is administered transdermally.
72. The method of claim 68 wherein the compound is administered rectally.
73. The method of claim 68 wherein the compound is administered nasally.
74. The method of claim 68 wherein the compound is administered sublingually.
75. The method of claim 68 wherein the compound is administered in a dosage of from about 0.01 \u03bcgday to about 1000 \u03bcgday.
76. The method of claim 68 wherein the compound is (20R)-23,23-difluoro-1\u03b1-hydroxy-2-methylene-19-nor-bishomopregnacalciferol having the formula:
77. The method of claim 68 wherein the animal is a human.
78. The method of claim 68 wherein the animal is a domestic animal.
79. The method of claim 68 wherein the animal is an agricultural animal
80. A method of treating secondary hyperparathyroidism comprising administering to a subject with secondary hyperparathyroidism an effective amount of a compound having the formula:
where X1 and X2, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
81. The method of claim 80 wherein the compound is administered orally.
82. The method of claim 80 wherein the compound is administered parenterally.
83. The method of claim 80 wherein the compound is administered transdermally.
84. The method of claim 80 wherein the compound is administered rectally.
85. The method of claim 80 wherein the compound is administered nasally.
86. The method of claim 80 wherein the compound is administered sublingually.
87. The method of claim 80 wherein the compound is administered in a dosage of from about 0.01 \u03bcgday to about 1000 \u03bcgday.
88. The method of claim 80 wherein the compound is (20R)-23,23-difluoro-1\u03b1-hydroxy-2-methylene-19-nor-bishomopregnacalciferol having the formula:
89. The method of claim 90 wherein the subject has chronic kidney disease.
90. The method of claim 80 wherein the subject is on dialysis.
91. A compound having the formula:
where R is selected from hydrogen or a hydroxy-protecting group.
92. A compound having the formula:
The claims below are in addition to those above.
All refrences to claims which appear below refer to the numbering after this setence.
1. A rubbing apparatus, comprising: a platform; a conveyor arranged on the platform; a based plate disposed on the conveyor; a rubbing roller arranged above the base plate and connected to the platform; a rubbing cloth disposed on a surface of the rubbing roller, wherein a surface of the rubbing cloth has a plurality of first pile fibers; a conditioning roller arranged aside to the rubbing roller, above the base plate and connected to the platform; and a conditioning cloth disposed on a surface of the conditioning roller, wherein a surface of the conditioning cloth has a plurality of second pile fibers, wherein the rubbing roller rotates in a first rotating direction opposite to a second rotating direction in which the conditioning roller rotates, and wherein a predetermined distance is arranged between the rubbing roller and the conditioning roller, so that the second pile fibers of the conditioning cloth on the conditioning roller are in contact with the first pile fibers of the rubbing cloth on the rubbing roller, thereby rejuvenating the rubbing cloth on the rubbing roller.
2. The apparatus of claim 1, wherein if the conditioning roller rotates clockwise, the rubbing roller rotates counter-clockwise.
3. The apparatus of claim 1, wherein if the conditioning roller rotates counter-clockwise, the rubbing roller rotates clockwise.
4. The apparatus of claim 1, wherein the second rotating speed of the conditioning roller is faster than the first rotating speed of the rubbing roller.
5. The apparatus of claim 1, wherein the conveyor is constructed to move the substrate on the base plate to a predetermined location.
6. The apparatus of claim 1, further comprising a cover plate under the conditioning roller to prevent the conditioning roller in contact with the substrate.
7. A liquid crystal display device comprising: a pair of substrate members, at least either one of the pair of substrate members being capable of transmitting light, and a liquid crystal disposed between the pair of substrate members, wherein at least either one of the substrate members includes an alignment layer which is rubbed using a rubbing apparatus comprising: a rubbing roller having a rubbing cloth on a surface of the rubbing roller, wherein a surface of the rubbing cloth has a plurality of first pile fibers, wherein the rubbing roller to be moved together with the substrate member in relation to each other to thereby perform rubbing to the alignment layer; and a conditioning roller arranged aside to the rubbing roller, having a conditioning cloth on a surface of the conditioning roller, wherein a surface of the conditioning cloth has a plurality of second pile fibers, wherein the rubbing roller rotates in a first rotating direction opposite to a second rotating direction in which the conditioning roller rotates, and wherein a predetermined distance is arranged between the rubbing roller and the conditioning roller, so that the second pile fibers of the conditioning cloth on the conditioning roller are in contact with the first pile fibers of the rubbing cloth on the rubbing roller.
8. The apparatus of claim 7, wherein if the conditioning roller rotates clockwise, the rubbing roller rotates counter-clockwise.
9. The apparatus of claim 7, wherein if the conditioning roller rotates counter-clockwise, the rubbing roller rotates clockwise.
10. The apparatus of claim 7, wherein the second rotating speed of the conditioning roller is faster than the first rotating speed of the rubbing roller.
11. The apparatus of claim 7, further comprising a cover plate under the conditioning roller and above the substrate member to prevent the conditioning roller in contact with the substrate member.
12. A method for manufacturing a liquid crystal display device, said method comprising: a first step of transporting a liquid crystal display substrate under a rubbing apparatus comprising a rotated rubbing roller and a rotating conditioning roller arranged aside to the rubbing roller, the liquid crystal display substrate having an alignment layer thereon, the rubbing roller having a rubbing cloth on a surface of the rubbing roller, wherein a surface of the rubbing cloth has a plurality of first pile fibers, so that the alignment layer is rubbed by the first pile fibers during rotation of the rubbing roller, the conditioning roller having a conditioning cloth on a surface of the conditioning roller, wherein a surface of the conditioning cloth has a plurality of second pile fibers, so that the second pile fibers of the conditioning cloth on the conditioning roller are in contact with the second pile fibers of the rubbing cloth on the rubbing roller, and wherein the rubbing roller rotates in a first rotating direction opposite to a second rotating direction in which the conditioning roller rotates; a second step of binding a pair of substrates to each other, at least one of the pair of substrates having gone through rubbing in the first step; and a third step of injecting liquid crystal between the substrates.
13. The method of claim 12, wherein if the conditioning roller rotates clockwise, the rubbing roller rotates counter-clockwise.
14. The method of claim 12, wherein if the conditioning roller rotates counter-clockwise, the rubbing roller rotates clockwise.
15. The method of claim 12, wherein the second rotating speed of the conditioning roller is faster than the first rotating speed of the rubbing roller.
16. The method of claim 12, wherein the rubbing apparatus further comprises a cover plate under the conditioning roller and above the liquid crystal display substrate to prevent the conditioning roller in contact with the substrate.