Barry University, Inc.

John Boulos

Novel Gi/o-biased muscarinic agonists selectively activate only one specific signaling pathway and are novel pharmacophores for development of new painkillers (analgesics). Methods of making and using these agonists are also described. The muscarinic agonists are of the formula:  or an analog, derivative or pharmaceutically acceptable salt thereof, wherein: R=H or Me; R=H, Me, Et, OMe, OEt, F, Cl, Br, I, or NO; and R=H, Me, Et, OMe, or COMe (Rmay be bonded to any carbon of the rings).

Muscarinic agonists as non-steroidal and non-opioid analgesics and methods of use thereof

Compositions for treating a condition associated with activity of a muscarinic receptor (e.g., one or more of M, M, M, M, M) and for anesthetizing a subject include a bitopic muscarinic antagonist or agonist. A bitopic muscarinic antagonist named JB-D4 was discovered. Additional bitopic muscarinic antagonists discovered and described herein include BK-23, HD-42, HD153, HD-185, KH-5, JM-31 and JM-32. These bitopic ligands and their structural analogs, as well as bitopic muscarinic agonists, may be used as neuromuscular blocking agents (e.g., for use in compositions for anesthetizing a subject) and for the treatment of central nervous system disorders (e.g., Parkinson's disease, Schizophrenia, etc.), Overactive Bladder Syndrome, Chronic Obstructive Pulmonary Disease, asthma, and many other diseases associated with the activation or inhibition of M-Macetylcholine receptors.

Bitopic muscarinic agonists and antagonists and methods of synthesis and use thereof

The present invention is directed to a composition comprising the following compound:  The compound is associated with activity of a muscarinic receptor (e.g. one or more M, M, M, Mand M.

The present invention is directed to the following compound: 

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Miami Lakes, FL, United States of America

John Boulos