Inventions, Patents and Portfolios - WARF

Pharmaceuticals & Vitamin D : Immunity & auto-immune

Pharmaceuticals & Vitamin D Portfolios


Use of Salate Derivatives to Treat Multiple Sclerosis

UW–Madison researchers led by Prof. Hector DeLuca have discovered that two specific salate esters commonly found in sunscreen almost completely prevented experimental autoimmune encephalomyelitis (EAE) development in mice without affecting body weight. Salicylates are well-known nonsteroidal anti-inflammatory drugs (NSAIDs); the complete suppression of EAE by topical administration of homosalate and octyl salicylate is a novel finding.

Efficient In Vitro Assay for Antigen-Specific Tolerance

Building on their work, UW–Madison researchers have now developed a T cell-bound cytokine (T-CBC) assay for detecting and quantifying regulatory T cells specific to self-antigens or donor alloantigens. The new method comprises (a) culturing the subject’s T cells for 24 hours in the presence of one or more target antigens and (b) analyzing the cultured T cells for expression of a marker (EBi3; TGFβ/LAP) indicative of antigen-specific immune suppression.

Vitamin D Analog “DA2HE” to Treat and Prevent Polyps, Hyperplastic Intestinal Disorders

UW–Madison researchers have developed a vitamin D analog, seco-A-2,19-dinor-1,25-dihydroxyvitamin D3. Known as DA2HE, the compound exhibits high activity in vivo, especially in intestinal tissues. Relatively low receptor binding, differentiation and transcription activities suggest strong cell selectivity for use against polyps, some cancers and intestinal disorders. The compound’s high intestinal calcium transport activity may be useful against bone diseases.

Vitamin D Analogs “2EG” and “T-2EG-S” for Treating Cancer and Bone Disease

UW–Madison researchers have developed vitamin D analogs (20S) and (20R)- 1a,25-dihydroxy-2-methylene-vitamin D3 and (5E)-(20S)-1a,25-dihysroxy-2-methylene-vitamin D3.These compounds exhibit high binding affinity and cell differentiation activity, suggesting anticancer properties. Also, high calcemic activity may be harnessed for the treatment of bone diseases where less frequent doses are desired.

Vitamin D Analogs “1D-QM” and “1D-QMS” for Cancer, Bone Disease Therapy

UW–Madison researchers have developed vitamin D analogs (20S) and (20R)-25-hydroxy-2-methylene-vitamin D3. In vivo, these compounds could act as prodrugs since 1-hydroxylation can occur in a regulated manner and extended vitamin release activity is predicted. The compounds exhibit high binding affinity and cell differentiation activity, suggesting anticancer properties. Also, high calcemic activity may be harnessed for bone disease treatments in which less frequent doses are preferred, like senile osteoporosis.

Vitamin D Analogs “3D-QM” and “3D-QMS” for Treating Cancer and Bone Diseases

UW–Madison researchers have developed vitamin D analogs (20S) and (20R)-3-desoxy-1a,25-dihydroxy-2-methylene vitamin D3.These compounds are known also as 3D-QMS and 3D-QM, respectively. They exhibit anticancer properties of high binding affinity and cell differentiation activity. High calcemic activity suggests treatment for bone ailments and diseases.

Vitamin D Analog “UW-05” for Skin Therapy, Parathyroid and Autoimmune Disease Treatment

UW–Madison researchers have developed a vitamin D analog, 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-1α-hydroxyvitamin D3. Known as UW-05, the compound shows high transcription activity, pronounced activity in arresting proliferating cells and inducing their differentiation. Bone calcium mobilization activity is lower compared to the native hormone. UW-05 may be useful against autoimmune diseases, some cancers, skin wrinkles and disorders, inflammatory problems and obesity.

Vitamin D Analogs for Treating Bone Cancers and Diseases

UW–Madison researchers have developed vitamin D analogs,(20S)-3-desoxy-2-methylene-1a,25-diydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1a,25-diydroxy-19-nor-vitamin D3.These compounds exhibit promising anti-cancer activities: high receptor binding, and the arrest and induced-differentiation of proliferating cells. High calcemic mobilization suggests particular effectiveness in the treatment of bone diseases.

Novel Tautomycetin Analogs Provide Potential Natural Products for the Treatment of Cancer or Autoimmune Disease

A UW–Madison researcher has developed novel TTN analogs, which may be potentially useful for the treatment of cancer or autoimmune disorders. The researcher previously cloned and sequenced the biosynthetic gene cluster for TTN.  He discovered that inactivating two genes, ttnD and ttnF, abolishes production of TTN and leads to the production of five new TTN analogs. 

WARF reference number P100290US03 describes the use of the analogs to inhibit the oncogene SHP-2. In addition to autoimmune disorders, the analogs can be used to treat diseases related to SHP-2, including Noonan syndrome, Leopard syndrome, leukemia and solid tumors.

Calcitonin and Calcitonin-Like Compounds for Multiple Sclerosis

UW-Madison researchers have developed methods of preventing and treating MS by administering synthetic calcitonin, calcitonin-like peptides or calcitonin mimetics to a patient to diminish MS symptoms.  Vitamin D analogs can be administered in combination with the calcitonin to further reduce symptoms. 

Vitamin D Receptor Antagonists for the Treatment of Asthma

UW-Madison researchers have identified several antagonists of the vitamin D receptor that are useful for treating asthma and eczema. The antagonists include various 19-nor 2 alkylidene and 2alpha-alkyl analogs of vitamin D. These compounds interfere with binding between vitamin D and its receptor both in vivo and in vitro.

Method of Increasing Longevity and Preventing Body Weight Wasting in Autoimmune Disease by Using CLA

UW-Madison researchers have developed a method of treating an autoimmune complex disease by administering an amount of conjugated linoleic acid (CLA). Administering CLA is believed to be effective because CLA can affect the production of prostaglandins and leukotrienes in humans and animals. This in turn reduces the formation of damaging immune complexes and cellular infiltrates.