| 摘要 |
The aspects of the disclosed embodiments are directed to novel compounds, specifically, quaternary ammonium derivatives of tertiary amine containing opioid drug compounds such as hydrocodone, hydromorphone and oxycodone, formulations containing said. compounds or pharmaceutically acceptable salts thereof, which are capable of providing controlled release of the opioid drug upon administration to a patient in order to treat pain. |
| 主权项 |
1. A compound of the formula wherein R1 is CHR4O(C═O)OR5, CHR4O(C═O)R6, CHR4O(C═O)NR6R7, CHR4O(C═O)CHR8NR6R7, CHR4O(C═O)CHR8NH(COCHR8NH)nH, CHR4R9, CHR4O(C═O)CR5R6OR7, CHR4O(C═O)O(CH2)nNR5R6, CHR4O(C═O)O(CH2)nCO2R5, CHR4O(C═O)(CH2)nNR5R6, CHR4O(C═O)(CH2)nCO2R5, R2 is H, OH, or O(C═O)CH3;R3 is H, CH3, or (C═O)CH3;R4 is H or optionally substituted alkyl; wherein said substituents are independently selected from the group OR3 and (C═O)OR5;R5 is optionally substituted alkyl, cycloalkyl, phenylalkyl, heteroalkyl, heterocycloalkyl, aryl, or heteroaryl; wherein said substituents are independently (CH2)nCO2alkyl;R6 is H or R5;R7 is H or R5;R8 is H or R5;R9 is 4-isoxazoyl;wherein each n is independently an integer from 1-12; andA is an anion selected from the group consisting of: Br−, Cl−, I−, R7CO2−, H2PO4−, NO3−, Etodolate, Mefenamate, Urosodeoxycholate and R6SO3. |
