Patent classifications
C07D489/08
DRUG COMBINATIONS FOR INHIBITING INFLAMMATION AND SRC KINASE ACTIVATION FOLLOWING INVASIVE SURGICAL PROCEDURES
Combinations of compounds that inhibit activation of p-Src tyrosine kinase, having particularly utility in the treatment of inflammation resulting from traumatic surgical interventions and the proliferation or metastasis of cancer cells following surgical excision of cancerous tissue.
OPIOID RECEPTOR ANTAGONISTS
The first selective SuFEx antagonists to μ-opioid receptors (MOR) were developed by functionalizing an opioid scaffold with an SO.sub.2—F warhead. Our model, based on a MOR structure with antagonist β-FNA, indicates the naloxone carbonyl as an advantageous point for derivatization as it is chemically accessible and is not involved in interaction with receptors. Of the three accessible Tyr residues in MOR pocket, Tyr77, Tyr130 and Tyr150, Tyr150 in proximity to the carbonyl of the docked naloxone was selected as a target, which resulted in the development of highly potent antagonists.
OPIOID RECEPTOR ANTAGONISTS
The first selective SuFEx antagonists to μ-opioid receptors (MOR) were developed by functionalizing an opioid scaffold with an SO.sub.2—F warhead. Our model, based on a MOR structure with antagonist β-FNA, indicates the naloxone carbonyl as an advantageous point for derivatization as it is chemically accessible and is not involved in interaction with receptors. Of the three accessible Tyr residues in MOR pocket, Tyr77, Tyr130 and Tyr150, Tyr150 in proximity to the carbonyl of the docked naloxone was selected as a target, which resulted in the development of highly potent antagonists.
CONJUGATES FOR ASSAYS FOR OXYCODONE AND OXYMORPHONE
Compositions, methods, and kits are disclosed directed at haptens, immunogens and immunoassays for oxycodone and metabolites thereof. The compounds are exemplified by compounds of the Formula I. The method comprises providing in combination in a medium (i) a sample suspected of containing oxycodone and/or oxycodone metabolites, a compound of the Formula I wherein R.sup.4 or R.sup.5 is a label, and an antibody for oxycodone or a metabolite thereof. The medium is examined for the presence of a complex comprising the labeled compound of Formula I where the presence of such as complex indicates the presence of oxycodone or oxycodone metabolite in the sample.
REDUCTION OF ALPHA, BETA-UNSATURATED KETONE LEVELS IN MORPHINAN DERIVATIVE COMPOSITIONS
The disclosure relates to processes for reducing the amount of a compound of formula (I) or a salt or a solvate thereof present in a composition comprising compounds of formulae (I) and (II) or a salt or a solvate thereof.
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REDUCTION OF ALPHA, BETA-UNSATURATED KETONE LEVELS IN MORPHINAN DERIVATIVE COMPOSITIONS
The disclosure relates to processes for reducing the amount of a compound of formula (I) or a salt or a solvate thereof present in a composition comprising compounds of formulae (I) and (II) or a salt or a solvate thereof.
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SALTS AND COMPOSITIONS USEFUL FOR TREATING DISEASE
The invention provides a combination or salt of lipoic acid and a compound of formula (I): The combinations and salts are useful for treating diabetes.
SALTS AND COMPOSITIONS USEFUL FOR TREATING DISEASE
The invention provides a combination or salt of lipoic acid and a compound of formula (I): The combinations and salts are useful for treating diabetes.
ABUSE-RESISTANT LONG-ACTING RELEASE OPIOID PRODRUGS
There are provided, prodrugs of opioid and other controlled substance, having enhanced physical and chemical stability to resist tampering and to make long-acting release formulations, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds as abuse deterrent products.
ABUSE-RESISTANT LONG-ACTING RELEASE OPIOID PRODRUGS
There are provided, prodrugs of opioid and other controlled substance, having enhanced physical and chemical stability to resist tampering and to make long-acting release formulations, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds as abuse deterrent products.