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Patent
Abide Therapeutics | Date: 2016-09-21

This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.


News Article | November 17, 2016
Site: news.yahoo.com

Heavy Marijuana Use May Be Bad for Your Bones As abuse of prescription opioids in the United States has reached epidemic proportions, researchers around the nation have been searching for other ways to offer people pain relief, ways that don't bring such a risk of addiction. Now, two independent teams of researchers have developed drugs similar to marijuana that show evidence of providing pain relief in laboratory animals, but have no apparent addictive properties and do not cause a "high" that impairs motor function. The researchers presented their work today (Nov. 14) at a news conference at the annual meeting of the Society for Neuroscience in San Diego. [11 Odd Facts About Marijuana] Nearly 50 million American adults have significant chronic pain, according to a government-funded study published last year in the Journal of Pain. And opioids — a class of drugs that includes OxyContin, Vicodin and morphine — are commonly prescribed for pain. An estimated 20 percent of patients with pain receive an opioid prescription, a rate that has quadrupled since 1999, according to the Centers for Disease Control and Prevention (CDC). However, opioids are highly addictive. The CDC estimates that 2 million Americans abused or were dependent on prescription opioids in 2014, contributing to about 14,000 deaths that year (CDC data shows that an equal number of yearly deaths are due to heroin, which is an illegal opioid.) Researchers in recent years have attempted to create drug compounds that can target pain receptors in the brain but not affect opioid receptors, the source for opioid addiction. Marijuana can provide some pain relief, but the drug has unwanted side effects, such as motor impairment and memory loss, and can be potentially addictive, although it is not an opioid drug. [‪America's Opioid-Use Epidemic: 5 Startling Facts] One research group, led by Andrea Hohmann, a professor of neuroscience at Indiana University, has developed a class of compounds that partially mimics the action of the main psychoactive ingredient in marijuana, THC, short for tetrahydrocannabinol. THC stimulates cannabinoid receptors in the brain to release endocannabinoids, natural pain-relieving molecules. Hohmann's compounds, called positive allosteric modulators, or PAMs, bind to a recently discovered site on a cannabinoid brain receptor called CB1, but they do not bind to the typical THC receptor or the opioid receptor. As a result, the compound produces pain relief without the high associated with marijuana and without the risk of addiction. In experiments, the compound provided pain relief to laboratory mice that were given paclitaxel, a common cancer chemotherapy drug known to damage nerves and cause pain. The PAMs acted in "a very targeted way [and] amplified the therapeutic effect of endocannabinoids," Hohmann told Live Science. "You can view it as 'turning up the gain.'" [5 Surprising Facts About Pain] Unlike marijuana or prescription opioids, the PAM compounds "do not hit every receptor everywhere," she added. Another group of researchers, led by Jason Clapper, a scientist at Abide Therapeutics in San Diego, took a different approach and developed a compound that indirectly increased the amount of natural cannabinoids in the brains of rats, which relieved the animals' chronic pain symptoms. Clapper's compound blocked the body's production of a protein called MGLL, which through a series of events, triggered a release of the brain's natural endocannabinoids, and brought subsequent pain relief. "Today's findings reveal a better understanding of the body's cannabinoid system and how to modulate it," said Margaret Haney, a drug-abuse expert at Columbia University in New York who was not associated with either research project. "There are now a number of ways to target this system and possibly alleviate pain and other disease without relying on marijuana." Hohmann noted the path to humans studies "can be a long, slow road" but she's very excited about the potential for this line of therapy. Follow Christopher Wanjek @wanjek for daily tweets on health and science with a humorous edge. Wanjek is the author of "Food at Work" and "Bad Medicine." His column, Bad Medicine, appears regularly on Live Science.


News Article | November 22, 2016
Site: www.scientificamerican.com

Debate over whether pot is a gateway drug that leads to more serious abuse problems—think heroin or cocaine dependence—has raged on seemingly forever. But what if the gate swings the other way? What if the marijuana plant contains chemicals that might help a user avoid or get off the hard stuff? The Society for Neuroscience’s gargantuan annual fall gathering last week in San Diego, which draws an attendance each year in the tens of thousands, witnessed presentations that suggest the cannabis plant could become a source of drugs for combating addiction. At the meeting, a group from the Scripps Research Institute in La Jolla, Calif., reported on preliminary research showing that a non-psychoactive marijuana constituent, cannabidiol, can quell urges for cocaine in rats trained over three months to compulsively crave a drug. Researchers allowed rats to dose themselves at will with cocaine until they became addicted. At the end of the period, they gave some of the animals transdermal patches that provided an infusion of cannabidiol. Rats that received the patches reduced cocaine intake, whereas the ones that didn’t continued to consume as much cocaine as before. Other researchers—from Miguel Hernandez University in Spain—reported on an initial study showing that cannabidiol reduced alcohol consumption, as well as the desire to drink and any impulse toward relapse. Another possible measure discussed at the meeting would steer pain sufferers away from opioids by recruiting the signaling system in the brain that is triggered by marijuana, and by the pot-like chemicals (endocannabinoids) that the body produces on its own. A chemical in pot, tetrahydrocannabinol (THC), can alleviate pain but it also makes the user high by interacting with a particular docking site, the CB1receptor, on brain cells. Scientists from Indiana University found a possible way to treat intransigent neuropathic pain—the kind produced by nerve damage—by using a molecule that enhances the effects of endocannabinoids. The result was long-lasting pain relief without intoxication. Another presentation came from Abide Therapeutics, a San Diego-based biotech company, which showed that a drug that raises levels of an endocannabinoid, 2-AG, might help treat chronic pain. Marijuana is chemically complex, and the plant’s therapeutic potential comes freighted with its own paradoxical entanglements. Pot ingredients may reduce cravings for some drugs, for example, but they may also produce dependence among teenagers. At the conference, scientists from the University of California, Los Angeles discussed early research, which found that behavioral therapy techniques that tamp down negative emotions might be effective in reducing cravings for marijuana. In attempts to find out what helps and what doesn’t, scientists who research the benefits and perils of cannabis still face enormous challenges in working with the plant, despite the growing trend toward legalization. Margaret Haney, a professor of neurobiology at Columbia University Medical Center (as well as director of Columbia’s marijuana research laboratory and co-director of its substance use research center), told an SFN press conference that “our scientific understanding of the therapeutic potential of the marijuana plant is really in its infancy.” Haney described continuing difficulties in conducting research on the plant.  “Even cannabidiol, which has absolutely no psychoactive or abuse-related effects, [must be treated] like it’s heroin and it’s locked up in a triple drug-safe room. The regulations make studying the plant and its components extremely tricky.” “The FDA (Food and Drug Administration) and the DEA (Drug Enforcement Administration) are pretty fierce,” Haney said. I think everybody—no matter where you stand in this medical marijuana discussion—everybody agrees we need research because society has moved ahead. [Users are] taking any combination of marijuana and believing that it’s curing 96 ailments. We need research on this, and it’s extremely difficult. Nothing has loosened up, and I’ve been studying it for 20 years.” “It’s been very difficult to be a cannabis researcher and see society move ahead with no input from the scientific community. There’s been very little consideration of science on this topic,” Haney added. “I’m very concerned that the whole country has decided to believe the medical properties of marijuana, [and] I believe there are some, but we have to decide and test for which indication and under what conditions. It’s just an open-door policy and [people] are being swayed by marketers. Marketers are telling patients what kind of cannabis is good for PTSD vs. migraines, and that’s not based on anything.”


Blankman J.L.,Scripps Research Institute | Blankman J.L.,Abide Therapeutics | Cravatt B.F.,Scripps Research Institute
Pharmacological Reviews | Year: 2013

The endocannabinoid signaling system regulates diverse physiologic processes and has attracted considerable attention as a potential pharmaceutical target for treating diseases, such as pain, anxiety/ depression, and metabolic disorders. The principal ligands of the endocannabinoid system are the lipid transmitters N-arachidonoylethanolamine (anandamide) and 2-arachidonoylglycerol (2-AG), which activate the two major cannabinoid receptors, CB1 and CB2. Anandamide and 2-AG signaling pathways in the nervous system are terminated by enzymatic hydrolysis mediated primarily by the serine hydrolases fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), respectively. In this review, we will discuss the development of FAAH and MAGL inhibitors and their pharmacological application to investigate the function of anandamide and 2-AG signaling pathways in preclinicalmodels of neurobehavioral processes, such as pain, anxiety, and addiction. We will place emphasis on how these studies are beginning to discern the different roles played by anandamide and 2-AG in the nervous system and the resulting implications for advancing endocannabinoid hydrolase inhibitors as next-generation therapeutics. © 2013 by The American Society for Pharmacology and Experimental Therapeutics.


Patent
Abide Therapeutics and Scripps Research Institute | Date: 2013-01-07

This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.


Patent
Abide Therapeutics and Scripps Research Institute | Date: 2013-03-15

Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.


Patent
Abide Therapeutics | Date: 2016-03-16

Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.


The invention provides pyrrolo-pyrrole carbamate and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., solid tumor cancer, obesity, Downs syndrome, Alzheimers disease, or pain, in a patient. The octahydropyrrolo pyrrole carbamates could be derived from hexafluoroisopropanol, N,N-disuccinimide and such. The activity of carbamates in MAGL, FAAH, and ABHD6 assays are also described.


Patent
Abide Therapeutics and Scripps Research Institute | Date: 2015-01-16

This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.


SAN DIEGO, Dec. 14, 2016 /PRNewswire/ -- Abide Therapeutics, a developer of innovative pharmaceuticals, announced today initiation of dosing in a Phase 1b study to evaluate the effects of ABX-1431, a first-in-class investigational monoacylglycerol lipase (MGLL) inhibitor, on gastric...

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