1268881-20-4Relevant articles and documents
Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain
Han, Sangdon,Thoresen, Lars,Jung, Jae-Kyu,Zhu, Xiuwen,Thatte, Jayant,Solomon, Michelle,Gaidarov, Ibragim,Unett, David J.,Yoon, Woo Hyun,Barden, Jeremy,Sadeque, Abu,Usmani, Amin,Chen, Chuan,Semple, Graeme,Grottick, Andrew J.,Al-Shamma, Hussein,Christopher, Ronald,Jones, Robert M.
, p. 1309 - 1313 (2017/12/26)
The discovery of a novel, selective and fully efficacious CB2 agonist with satisfactory pharmacokinetic and pharmaceutical properties is described. Compound 6 was efficacious in a rat model of osteoarthritis pain following oral administration and, in contrast to morphine, maintained its analgesic effect throughout a 5-day subchronic treatment paradigm. These data were consistent with our hypothesis that full agonist efficacy is required for efficient internalization and recycling of the CB2 receptor to avoid tachyphylaxis. Based on its overall favorable preclinical profile, 6 (APD371) was selected for further development for the treatment of pain.
CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF CONDENSED AZACYCLES ( CANNABINOID RECEPTOR MODULATORS)
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, (2012/09/11)
The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)- 1a,2,5.5a-tetrahydro- 1 H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)- 1 - hydroxymcthyl-2.2-dimcthyl-propyl)-amidc (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor and are therefore useful in t treatment of CB2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS rumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.