2-propylidene-19-nor-vitamin D compounds
1 Assignment
0 Petitions
Accused Products
Abstract
2-propylidene-19-nor-vitamin D compounds are disclosed as well as pharmaceutical uses for these compounds and methods of synthesizing these compounds. These compounds are characterized by high bone calcium mobilization activity and high intestinal calcium transport activity. This results in novel therapeutic agents for the treatment and prophylaxis of diseases where bone formation is desired, particularly osteoporosis, as well as autoimmune diseases such as multiple sclerosis, diabetes mellitus and lupus. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis. These compounds also increase both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements.
-
Citations
103 Claims
- 1. A compound having the formula:
-
12. 2-[(3′
- -methoxymethoxy)propylidene]-19-nor-1α
,25-(OH)2D3 having the formula;
- -methoxymethoxy)propylidene]-19-nor-1α
-
13. 2-(3′
- -hydroxypropylidene)-19-nor-1α
,25-(OH)2D3 (E-isomer) having the formula;
- -hydroxypropylidene)-19-nor-1α
-
14. 2-(3′
- -hydroxypropylidene)-19-nor-1α
,25-(OH)2D3 (Z-isomer) having the formula;
- -hydroxypropylidene)-19-nor-1α
-
15. 2-(3′
- -hydroxypropylidene)-19-nor-(20S)-1α
,25-(OH)2D3 (E-isomer) having the formula;
- -hydroxypropylidene)-19-nor-(20S)-1α
-
16. 2-(3′
- -hydroxypropylidene)-19-nor-(20S)-1α
,25-(OH)2D3 (Z-isomer) having the formula;
- -hydroxypropylidene)-19-nor-(20S)-1α
-
20. The pharmaceutical composition containing 2-[(3′
- -methoxymethoxy)propylidene]-19-nor-1α
,25-(OH)2D3 in an amount from about 0.01 μ
g to about 100 μ
g per gram of composition. - View Dependent Claims (21)
- -methoxymethoxy)propylidene]-19-nor-1α
- 30. A method of treating metabolic bone disease where it is desired to maintain or increase bone mass comprising administering to a patient with said disease an effective amount of a compound having the formula:
- 46. A method of treating psoriasis comprising administering to a patient with psoriasis an effective amount of a compound having the formula:
- 57. A method of treating leukemia, colon cancer, breast cancer, skin cancer or prostate cancer comprising administering to a patient an effective amount of a compound having the formula:
- 67. A method of increasing the strength of a bone comprising administering to a patient in need of such treatment an effective amount of a compound having the formula:
- 79. A method of treating an autoimmune disease comprising administering to a patient with said disease an effective amount of a compound having the formula
- 92. A method of treating an inflammatory bowel disease comprising administering to a patient with said disease an effective amount of a compound having the formula
Specification