38 results about "Mixed Opioid Agonist/Antagonist" patented technology

The present invention is directed to novel opioid receptor modulators of Formula (I).

The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.

The invention is directed to compounds of Formula (I) useful as delta and mu opioid receptor modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.

Opioid receptors form functional heterodimers with each other and with other G-protein coupled receptors, such as dopamine receptors, adrenergic receptors, or chemokine receptors. These receptors can be exploited for high throughput screening of compounds to identify heterodimer opioid receptor modulators (agonists and antagonists). The invention also relates to identification of novel heterodimer receptor ligands and synergistic compositions, which can provide strategies for analgesia, narcotic addiction, hypertension, HIV infection, and immune system function.

The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.

The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.

Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations.

The present invention is directed to Benzomorphan Analog compounds of the Formula (I), Formula (IA), Formula (IB), Formula (IC), or Formula (ID) as shown below, wherein R¹, R^2a, R^2b, R³, R⁴, Z, and G are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

The invention discloses a method for preparing alanine derivatives disclosed as Formula (I). The alanine derivatives can be used as a synthesis intermediate of an opioid receptor regulator, such as a synthesis intermediate of eluxadoline. By using the cheap and accessible chiral tyrosine as the initial raw material, the invention provides a brand-new synthesis route for preparing alanine derivatives. The whole reaction route has the advantages of high total yield, low cost and mild reaction conditions, is simple and safe for operation, and is suitable for large-scale industrial production.

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows:

wherein R₁, R₂, R₃, and L, A, and R_a are defined herein.

The present invention provides a compound having the structure:

or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with pain, a depressive disorder, a mood disorder or an anxiety disorder by administering the compound to the subject.

Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R³, R⁴, R⁵, R⁶, R⁸, m and n are as defined herein. Such compounds modulate the opioid receptor, particulate the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.

Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations.

Provided herein are opioid receptor modulators and pharmaceutical compositions comprising said compounds.