Description of Invention: The invention relates to novel compounds which are hybrids between two moieties, i.e. non-steroidal anti-inflammatory drugs (NSAID) and Nitroxyl (HNO) releasing agents as well as Nitroxide (an antioxidant and superoxide scavenger). Such modified NSAIDs have shown to be advantageous to conventionally used NSAID, as their toxicity is significantly reduced and they can thus be used in medical treatment for extended periods of time without severe side effects. The adverse side effects (i.e. heart attack, thrombosis and severe gut toxicity) presented by conventional NSAIDs are well documented and some of them (i.e. Vioxx) were therefore withdrawn from the market. The present compounds may alleviate these problems, and may render more anti-inflammatory agents suitable for human use. The HNO releasing moiety of these novel compounds will expand the medical utility of these compounds, as HNO releasing agents possess anticancer activity as well as good antioxidant activities, a property that is beneficial for a variety of human diseases, including acute and chronic inflammation. In summary, the hybrid compounds provided in the invention can be useful in treatment of variety of human diseases (i.e. inflammatory diseases, heart diseases and cancer) with relatively low level of side effects.
Applications: The drugs of this invention will be useful in treatment of anti-inflammatory diseases, and as therapeutic or preventative drugs for cardiovascular diseases, diabetes and cancer.
Advantages: The hybrid structure of the present drugs will render them useful in therapy and prevention of a wide variety of disorders, with reduced toxicity.
For Licensing Information Please Contact: Betty Tong Ph.D. NIH Office of Technology Transfer 6011 Executive Blvd. Suite 325, Rockville, MD 20852 United States Email: tongb@mail.nih.gov Phone: 301-594-6565 Fax: 301-402-0220
Description of Invention:
The invention relates to novel compounds which are hybrids between two moieties, i.e. non-steroidal anti-inflammatory drugs (NSAID) and Nitroxyl (HNO) releasing agents as well as Nitroxide (an antioxidant and superoxide scavenger). Such modified NSAIDs have shown to be advantageous to conventionally used NSAID, as their toxicity is significantly reduced and they can thus be used in medical treatment for extended periods of time without severe side effects. The adverse side effects (i.e. heart attack, thrombosis and severe gut toxicity) presented by conventional NSAIDs are well documented and some of them (i.e. Vioxx) were therefore withdrawn from the market. The present compounds may alleviate these problems, and may render more anti-inflammatory agents suitable for human use. The HNO releasing moiety of these novel compounds will expand the medical utility of these compounds, as HNO releasing agents possess anticancer activity as well as good antioxidant activities, a property that is beneficial for a variety of human diseases, including acute and chronic inflammation. In summary, the hybrid compounds provided in the invention can be useful in treatment of variety of human diseases (i.e. inflammatory diseases, heart diseases and cancer) with relatively low level of side effects.
Applications:
The drugs of this invention will be useful in treatment of anti-inflammatory diseases, and as therapeutic or preventative drugs for cardiovascular diseases, diabetes and cancer.
Advantages:
The hybrid structure of the present drugs will render them useful in therapy and prevention of a wide variety of disorders, with reduced toxicity.
Development Status:
In vitro data available
Inventors:
David A Wink (NCI)
Patent Status:
HHS, Reference No. E-131-2011/0
US, Application No. 61/472,770 filed 07 Apr 2011
Relevant Publication:
For Licensing Information Please Contact:
Betty Tong Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Email: tongb@mail.nih.gov
Phone: 301-594-6565
Fax: 301-402-0220
Ref No: 2340
Updated: 12/2011