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WOBURN, MA, United States

Grant
Agency: Department of Health and Human Services | Branch: | Program: SBIR | Phase: Phase II | Award Amount: 436.88K | Year: 2007

DESCRIPTION (provided by applicant): Obesity affects millions of people in the U.S. and worldwide, and this disease has enormous health and economic consequences for our society. Existing treatments show limited efficacy, can possess troubling side effects, and often require long-term therapy. Discovery of a new treatment for obesity would have a very considerable scientific and commercial value. One approach to pharmacotherapy for appetite suppression is the development of 5-HT2C receptor agonists, which was the focus of our Phase One work. In Phase Two, we propose to optimize and further develop these leads through a Structure-Activity Relationship (SAR) program of synthesis and biological evaluation. From this project we specifically aim to discover one or more indole analogs showing efficacy in our animal model for appetite suppression that is equal to or better than approved medications. Such leads will also display favorable drug-like properties. The long-term goal of this project is to discover a new, improved pharmaceutical agent for treatment of obesity that can be licensed and developed for ultimate market approval. 7. Project Narrative Obesity is a serious health problem in the Unites States, and the existing drugs to help people lose weight are often not effective and have side effects. We are carrying out research to discover and develop a new drug for obesity. If we are successful, doctors will have another option to help obese people with their weight problem.


Grant
Agency: Department of Health and Human Services | Branch: | Program: SBIR | Phase: Phase II | Award Amount: 1.46M | Year: 2006

DESCRIPTION (provided by applicant): Obsessive Compulsive Disorder (OCD) is a serious mental illness that affects millions of people throughout the world. Existing therapies for OCD show limited efficacy, can possess troubling side effects, and often require long-term treatment. Discovery of a new treatment for OCD would have considerable scientific and commercial value. One approach to pharmacotherapy for OCD is the development of selective 5-HT2C receptor agonists, which was the focus of our Phase One work. In Phase Two, we propose to optimize and further develop these leads through a Structure-Activity Relationship (SAR) program of synthesis and biological evaluation. From this project we specifically aim to discover one or more indole analogs showing efficacy in our animal model for OCD that is comparable to approved medications. Such leads will also display favorable drug-like properties. The long term goal of this project is to discover a new, improved pharmaceutical agent for treatment of OCD that can be licensed and developed for ultimate market approval.


Grant
Agency: Department of Health and Human Services | Branch: | Program: SBIR | Phase: Phase I | Award Amount: 130.50K | Year: 2008

DESCRIPTION (provided by applicant): Neuropathic pain is a type of chronic pain state caused by injury or disease to the nervous system. Annual medical spending due to pain has been estimated to be over 100 billion. Currently there are no medications ava ilable to prevent or cure this devastating disease condition. Hence, there is an urgent need to discover effective drugs to treat this chronic pain condition. A promising drug target for neuropathic pain is the cannabinoid CB2 receptor. In phase I of this proposal our focus will be on the optimization of our lead compound to discover one or more CB2 receptor agonists with high receptor affinity and selectivity. In order to distinguish between agonist and antagonist activity, analogs that bind effectively to the CB2 receptor, will be evaluated for their ability to stimulate [35S]GTP?S binding. Our specific goal is to develop one or more lead CB2 agonists that show good activity and efficacy in an animal model for neuropathic pain. If this goal is accomplished in Phase I, we will have a drug candidate for further development in Phase II. The long-term goal of this proposal is to develop a medication for neuropathic pain that is effective and without undesirable side effects.


Grant
Agency: Department of Health and Human Services | Branch: | Program: SBIR | Phase: Phase I | Award Amount: 279.26K | Year: 2013

DESCRIPTION (provided by applicant): Chronic pain can result from various disease conditions and about 45% of the U. S. population seeks medical help for treatment of pain. Neuropathic pain is a type of chronic pain which is very difficult to treat, and most patients do not get adequate relief. A promising therapeutic drug target for the treatment of inflammation and pain is the cannabinoid CB2 receptor. In Phase I of this proposal our focus will be on the structural optimization of our lead template to develop a high efficacy CB2 selective agonist with pain suppression potential and with no CNS side effects. Established in vivo and in vitro pharmacological assays will be used to identify compounds that: 1) are highly selective for CB2 over CB1 receptors; 2)possess high efficacy and high potency in binding and activating the CB2 receptor; 3) possess high efficacy in reversing allodynia (i.e., nociceptive behavior in response to normally non-noxious stimuli); and 4) lack cannabimimetic side effects in whole animals that are typically indicative of CB1 receptor activation. The long-term objective of this proposal is to develop a novel drug for treatment of chronic pain which is both safe and effective. PUBLIC HEALTH RELEVANCE PUBLIC HEALTH RELEVANCE:8. Project Narrative Neuropathic pain is a type of chronic pain which is very difficult to treat since most patients do not get adequate relief with existing medications. The goal of this proposal is to develop CB2 receptor agonists with limited or no CNS side effects for the treatment of chronic pain.


Grant
Agency: Department of Health and Human Services | Branch: | Program: SBIR | Phase: Phase I | Award Amount: 504.21K | Year: 2005

Obesity has reached epidemic proportions and in a year about 300,000 people die of obesity-related diseases. Annual medical spending due to obesity and overweight is about $117 billion. There is an urgent need to discover effective drugs to treat this disease since existing drugs have modest efficacy and significant side effects. A potentially promising target for anti-obesity drugs is the cannabinoid (CB1) receptor. In Phase I of this proposal our focus will be on the structural optimization of our novel THC/anandamide template to discover one or more CB1 receptor antagonists. In order to distinguish between agonist and antagonist activity, analogs that bind effectively to the CB1 receptor, will be evaluated for their ability to stimulate [35S]GTPgS binding. Our specific objective is to discover and select the best analogs in this series that manifest in vivo activity in a mouse model for appetite suppression. If the above objective is accomplished in Phase I, we will have a drug candidate for further development in Phase II. The long-term objective of this proposal is to develop a novel anti-obesity drug that is both safe and effective.

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