C07D489/02

Opioid ketal compounds and uses thereof

This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): ##STR00001##
or a pharmaceutically acceptable salts thereof, wherein R.sub.1 is H or CH.sub.3, R.sub.2 is H or OH, n is 0, 1, 2 or 3, R.sub.3 and R.sub.4 are independently H or optionally substituted C.sub.1-C.sub.4 alkyl, or when n is 0, then R.sub.3 and R.sub.4 and the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C.sub.1-C.sub.4 alkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): ##STR00002##
or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain.

Opioid ketal compounds and uses thereof

This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): ##STR00001##
or a pharmaceutically acceptable salts thereof, wherein R.sub.1 is H or CH.sub.3, R.sub.2 is H or OH, n is 0, 1, 2 or 3, R.sub.3 and R.sub.4 are independently H or optionally substituted C.sub.1-C.sub.4 alkyl, or when n is 0, then R.sub.3 and R.sub.4 and the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C.sub.1-C.sub.4 alkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): ##STR00002##
or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain.

PROCESS FOR PREPARING OXYCODONE HYDROCHLORIDE HAVING LESS THAN 25 PPM 14-HYDROXYCODEINONE

In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.

PROCESS FOR PREPARING OXYCODONE HYDROCHLORIDE HAVING LESS THAN 25 PPM 14-HYDROXYCODEINONE

In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.

NEOPINONE ISOMERASE AND METHODS OF USING
20230357810 · 2023-11-09 ·

Disclosed are methods for converting a first morphinan alkaloid compound into a second morphinan alkaloid compound in the presence of a neopinone isomerase enzyme under reaction conditions permitting the conversion of the first alkaloid compound into the second alkaloid compound. The first alkaloid compound can be neopinone or neomorphinone. The second alkaloid compound can be codeinone or morphinone. Related compositions are also disclosed.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF PAIN AND DEPENDANCE DISORDERS

Provided herein are (e.g., controlled release) compositions for the treatment of acute or chronic diseases or disorders. Described herein are processable opioid conjugates. Also described herein are compositions and methods for the treatment of central nervous system (CNS) diseases or disorders including chronic pain (e.g., cancer pain), acute pain, opioid addiction, alcohol addiction, alcohol dependence, opioid-induced constipation, and narcotic depression. Said compositions and methods comprise opioid agonists and/or opioid antagonists, which demonstrate CNS activity and/or other desirable activities. Injection of said compositions subcutaneously or intraspinally provides therapeutic benefit to individuals suffering from CNS diseases or disorders

COMPOSITIONS AND METHODS FOR THE TREATMENT OF PAIN AND DEPENDANCE DISORDERS

Provided herein are (e.g., controlled release) compositions for the treatment of acute or chronic diseases or disorders. Described herein are processable opioid conjugates. Also described herein are compositions and methods for the treatment of central nervous system (CNS) diseases or disorders including chronic pain (e.g., cancer pain), acute pain, opioid addiction, alcohol addiction, alcohol dependence, opioid-induced constipation, and narcotic depression. Said compositions and methods comprise opioid agonists and/or opioid antagonists, which demonstrate CNS activity and/or other desirable activities. Injection of said compositions subcutaneously or intraspinally provides therapeutic benefit to individuals suffering from CNS diseases or disorders

Process for preparing oxycodone hydrochloride having less than 25 ppm 14-hydroxycodeinone

In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.

Process for preparing oxycodone hydrochloride having less than 25 ppm 14-hydroxycodeinone

In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.

6-ACETYLMORPHINE ANALOGS, AND METHODS FOR THEIR SYNTHESIS AND USE
20220080042 · 2022-03-17 ·

The present invention relates to novel 6-acetylmorphine analogs, and methods for their synthesis and use. Such analogs are designed to provide a convenient linkage chemistry for coupling under mild conditions to a suitable group on a target protein, polypeptide, solid phase or detectable label.