| WARF: P02112US |  |
| (20S)-1Alpha-Hydroxy-2Alpha-Methyl and 2Beta-Methyl-19-Nor-Vitamin D3 and Their Uses |
| INVENTORS | • | Hector DeLuca, Rafal Sicinski, Pawel Grzywacz |
OVERVIEW
Vitamin D is a highly potent regulator of calcium homeostasis and plays an established role in cellular differentiation. A recently discovered class of vitamin D analogs, the 19-nor-vitamin D compounds, shows a selective activity profile with high potency in inducing cellular differentiation and very low calcium mobilizing activity, making it potentially useful for treating various disorders.
This invention provides two new vitamin D analogs, (20S)-1alpha-hydroxy-2alpha-methyl-19-nor-vitamin
D3 and (20S)-1alpha-hydroxy-2beta-methyl-19-nor-vitamin D3. These analogs are characterized by the presence of a methylene substituent at C-2 and the absence of a hydroxyl group at C-25 in the side chain. They bind poorly or not at all to the vitamin D receptor, while having biological activity either higher than or equal to the natural hormone, 1alpha,25-dihydroxyvitamin
D3. The new compounds also show significant calcemic and cell differentiation activities.
KEY BENEFITS
- Slowly activated within the body, providing more controlled and prolonged activity
- Potentially useful as anti-cancer agents, particularly against leukemia, and colon, breast and prostate cancers
- Promising therapeutic agents for treating diseases where bone formation is desired, such as osteoporosis, osteomalacia, and renal osteodystrophy
- Especially useful for treating immune disorders, including multiple sclerosis, lupus, diabetes mellitus, host-versus-graft reaction, and organ transplant rejection
- Prospective treatment for inflammatory diseases, such as rheumatoid arthritis, asthma, and inflammatory bowel diseases
- May be useful for treating skin conditions, such as psoriasis, dermatitis, eczema, keratosis, wrinkles, slack skin, dry skin, and insufficient sebum secretion
- Potential treatment for other disorders including acne, alopecia, hypertension, hypocalcemia, and hypoparathyroidism
- Compounds may be administered orally, topically, parenterally, or transdermally
ADDITIONAL INFORMATION
Intellectual Property Status
Tech Fields
Pharmaceuticals & Vitamin D - Musculoskeletal
Pharmaceuticals & Vitamin D - Skin & connective tissue
Pharmaceuticals & Vitamin D - Vitamin D
CONTACT INFORMATION
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