- PEGYLATED OPIOID WITH LOW ADDICTIVE EFFECT
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Provided in the present invention are a conjugate of polyethylene glycol and opioid as shown in general formula (I), and a pharmaceutical composition comprising the conjugate. By means of covalently bonding a plurality of opioids to a polyethylene glycol derivative, the present invention improves water solubility and pharmacokinetic property of the drug with a low addictive effect. ????????PEG-(X-OP)m?????(I)
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Paragraph 0058; 0059
(2018/12/13)
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- COMPOSITIONS, DOSAGE FORMS, AND COADMINISTRATION OF AN OPIOID AGONIST COMPOUND AND AN ANALGESIC COMPOUND
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The present invention relates generally to the co-administration of an opioid agonist compound and an analgesic compound. In addition, the invention relates to, among other things, dosage forms for co-administration of an opioid agonist compound and an analgesic compound, methods for administering an opioid agonist compound and an analgesic compound, compositions comprising an opioid agonist compound and an analgesic compound, dosage forms comprising an opioid agonist compound and an analgesic compound, and so on.
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Paragraph 00248
(2013/05/23)
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- PROCESS FOR REDUCING THE 6-KETO GROUP OF A MORPHINAN ALKALOID TO THE 6-HYDROXY GROUP BY HYDROGENATION
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The present invention relates to a process for the reduction of a 6-keto group in a morphinan alkaloid to the corresponding 6-hydroxy group, comprising hydrogenating the 6-keto group using gaseous hydrogen in the presence of a heterogeneous catalyst and a solvent, to yield the 6-hydroxy morphinan alkaloid, wherein the reduction is carried out at a pH in the range of about 5 to about 7, and the 6-hydroxy morphinan alkaloid has an α:β ratio of > 85: 15.
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Page/Page column 5-6
(2011/04/13)
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- Biotransformations of morphine alkaloids by fungi: N-demethylations, oxidations, and reductions
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Morphine alkaloids and some of its derivatives (morphine, codeine, thebaine, oripavine, hydrocodone, and oxycodone) were subjected to fermentations with six fungal strains. The alkaloids were transformed to a variety of products via biological oxidations, reductions, and oxidative demethylations. The strain Cunninghamella echinulata proved to be the most effective for demethylations of all of the above compounds, except for morphine. The time profile of the conversion of 3-[14CH3]thebaine to 3-[ 14CH3]northebaine by C. echinulata cultures was also determined.
- Chaudhary, Vigi,Leisch, Hannes,Moudra, Alena,Allen, Blake,De Luca, Vincenzo,Cox, D. Phillip,Hudlicky, Tomas
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experimental part
p. 1179 - 1193
(2010/04/26)
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- IMPROVED PROCESS FOR THE PREPARATION OF 6-ALPHA-HYDROXY-N-ALKYLATED OPIATES
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The present invention is directed to the conversion of a 6-keto morphinan to a 6-alpha-hydroxy morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source.
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Page/Page column 25
(2009/01/20)
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- Process for the stereoselective reduction of 6- and 8-keto morphine and morphinan derivatives with formamidinesulfinic acid and compounds obtained thereby
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Process for the stereoselective synthesis of 6β-and 8β- hydroxy epimers by the chemical reduction of 6- and 8-keto derivatives in the morphine and morphinan series utilizing alkaline formamidinesulficic acid. The 6β- and 8β-hydroxy derivatives obtained according to the invention evidence narcotic antagonist and/or agonist activity and are also useful in the chemical and pharmacological standardization of various morphine and codeine derivatives and metabolites.
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