1227471-76-2Relevant academic research and scientific papers
Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: Identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4. 5]decane as lead scaffolds
Meyers, Marvin J.,Long, Scott A.,Pelc, Matthew J.,Wang, Jane L.,Bowen, Scott J.,Walker, Mark C.,Schweitzer, Barbara A.,Madsen, Heather M.,Tenbrink, Ruth E.,McDonald, Joseph,Smith, Sarah E.,Foltin, Susan,Beidler, David,Thorarensen, Atli
, p. 6538 - 6544 (2011/12/04)
Herein we report the identification of two new fatty acid amide hydrolase (FAAH) inhibitor lead series with FAAH kinact/Ki potency values greater than 1500 M-1s-1. The two novel spirocyclic cores, 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane, clearly distinguished themselves from the other spirocyclic cores on the basis of their superior potency for FAAH. Lead compounds from these two series have suitable FAAH potency and selectivity for additional medicinal chemistry optimization.
1-OXA-8-AZASPIRO [4, 5 ] DECANE- 8 -CARBOXAMIDE COMPOUNDS AS FAAH INHIBITORS
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Page/Page column 28, (2010/07/10)
Provided herein are 1-oxa-8-azaspiro[4.5]decane-8-carboxamide compounds of formula I wherein Ar1, Ar2, R1, R2, R3 and R4 are as defined herein and the pharmaceutically acceptable salts of such compounds useful in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, conditions including acute pain, chronic pain, neuropathic pain, nociceptive pain, inflammatory pain, fibromyalgia, rheumatoid arthritis, inflammatory bowel disease, lupus, diabetes, allergic asthma, vascular inflammation, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.
