| WARF: P97011US |
 |
| 2-Alkylidene-19-Nor-Vitamin D Compounds |
| INVENTORS |
• |
Hector DeLuca, Rafal Sicinski |
OVERVIEW
The inventors have developed a novel class of vitamin D-related compounds, the 2-alkylidene-19-nor-vitamin D derivatives.
Early in vivo data indicate these analogs may be up to 1,000 times more effective for building bone density than leading pharmaceutical treatments, while producing little hypercalcemia.
The 19-nor- class of vitamin D compounds is characterized by the replacement of the A-ring exocyclic methylene group (carbon 19), typical of the vitamin D system, by two hydrogen atoms. The 2-alkylidene class of 19-nor- compounds is further characterized by the substitution of an alkylidene group at carbon 2; see the issued patent (link below) for a figure of the chemical structure. These 2-substituted compounds exhibit low intestinal calcium transport and high bone calcium mobilization activities, thus showing promise as treatments for disorders where bone formation is desired. Because they arrest the proliferation of undifferentiated cells, these compounds may also be used as anti-cancer agents or in the treatment of psoriasis.
KEY BENEFITS
- In vivo studies of a selected analog demonstrated a 1,000-fold increase in bone density over leading osteoporosis treatments
- Compound development is in TOX/PK stage, moving rapidly toward Phase I trials
- Useful for treating several diseases, including osteoporosis, psoriasis, cancer, lupus and rheumatoid arthritis, and for preventing organ transplant rejection
- Proven synthesis in commercial quantities
- Use of analogs may be enhanced when combined with method patents for treating psoriasis (P92176US, P94140US, P95052US, P95146US), rheumatoid arthritis (P96141US), and lupus erythematosis (P00062US), and for preventing organ transplant rejection (P98272US)
ADDITIONAL INFORMATION
Intellectual Property Status
Tech Fields
Pharmaceuticals & Vitamin D - Oncology & hematology
Pharmaceuticals & Vitamin D - Musculoskeletal
Pharmaceuticals & Vitamin D - Skin & connective tissue
Pharmaceuticals & Vitamin D - Vitamin D
CONTACT INFORMATION
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