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7619088 |
Demethylation of 14-hydroxy substituted alkaloid derivatives
The present invention is directed to a method for demethylating 14-hydroxy substituted alkaloid derivatives, in particular of 14-hydroxy-17-methyl-4,5-epoxymorphinane-6-on-derivatives. This is...
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7619087 |
Method of preparation of oxycodone
A method of preparation of Oxycodone of formula I by reacting thebaine of formula II, or its analogue of formula III, wherein R represents a C 2 to C 5 alkyl, an alkylaryl, preferably benzyl,...
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7563899 |
(S)-N-methylnaltrexone
This invention relates to S-MNTX, methods of producing S-MNTX, pharmaceutical preparations comprising S-MNTX and methods for their use.
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7550592 |
Hydromorphone polymorphs
Hydromorphone hydrochloride forms are disclosed which are useful as analgesic agents either in combination with or as replacements for hydromorphone hydrochloride.
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7534888 |
Oxycodone polymorphs
Oxycodone.HCl polymorph forms are disclosed which are useful as analgesic agents either in combination with or as replacements for oxycodone.
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7501433 |
Opioid and opioid-like compounds and uses thereof
The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations thereof, and use thereof for prevention and treatment of disorders such as septic shock and organ...
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7435817 |
C-14 oxidation of morphine derivatives
The present invention relates to process for the preparation of a 14-hydroxynormorphinone derivative of formula IV
comprising reacting the compound of formula III,
with a cobalt (II)...
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7405301 |
Chemical methods
This invention relates to a method for N-demethylating an N-methyl morphinane comprising the steps of: (i) treating said N-methyl morphinane with an oxidizing agent to form the N-oxide morphinane;...
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7399859 |
Method for catalytic preparation of hydromorphone and hydrocodone
The present invention generally relates to catalysts of formula (III)
[M(P(R a )(R b )N(R c )(R d )) 2 X n ] m Y p
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7399858 |
Method for the catalytic production of hydrocodone, hydromorphone, and derivatives thereof
A method for the catalytic production of hydrocodone derivatives and hydromorphone derivatives, respectively, utilizing a transition metal catalyst of the formula [M(PR 4 R 5 R 6 ) n X m ] p ;...
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7348430 |
Production of opioid analgesics
The present invention includes a process for the manufacture of dihydrothebaine, dihydrocodeinone enol acetate, hydrocodone, and analogs thereof by reacting dihydrocodeine or analogs thereof with...
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7323565 |
Method for the catalytic production of hydrocodone and hydromorphone
A method for the catalytic conversion of codeine, morphine or analogs thereof into hydrocodone, hydromorphone or analogs thereof utilizing a transition metal complex of a tertiary phosphine halide...
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7285665 |
Process for the preparation of quaternary N-alkyl morphinan alkaloid salts
A process for the preparation of a quaternary derivative of the morphinan alkaloid, the process comprising contacting a tertiary N-substituted morphinan alkaloid with an alkyl halide in an...
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7199129 |
Derivatives of morphine-like opioid compounds
The present disclosure concerns compounds of formula (I) and pharmaceutically acceptable salts, hydrates, solvates, pharmaceutically acceptable derivatives, pro-drugs, tautomers and/or isomers...
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7164021 |
Opiate analogs selective for the δ-opioid receptor
Novel compounds which selectively bind to the δ-opioid receptor have been designed. These compounds have greater selectivity, improved water (blood) solubility, and enhanced therapeutic value as...
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7153966 |
Preparation of oxycodone
A process for preparing oxycodone or an oxycodone salt, wherein the oxycodone or oxycodone salt has low levels of impurities (especially 14-hydroxycodeinone) is disclosed. The process comprises the...
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7129248 |
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.
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7071336 |
Process for manufacturing opioid analgesics
Oxycodone is manufactured in high yields and with a high purity using a composition including a thebaine component into 14-hydroxycodeinone and then reduction of 14-hydroxycodeinone to oxycodone.
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7060708 |
Active agent delivery systems and methods for protecting and administering active agents
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active...
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6946556 |
Preparation of opioid analgesics by a one-pot process
A one-pot process for preparing opioid analgesics such as hydrocodone, hydromorphone, and analogues thereof by reacting codeine, morphine, and analogues thereof with hydrogen in a solvent system of...
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6864370 |
Process for manufacturing oxycodone
Oxycodone is manufactured in high yields and with a high purity using codeine or a salt of codeine as the starting material. The manufacturing process involves the following steps:
(a) codeine or...
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6825205 |
N-substituted hydromorphones and the use thereof
This invention relates to N-substituted hydromorphones of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is C 1-6 alkyl. These compounds act as μ opioid receptor agonists....
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6784186 |
Therapeutic compounds
This invention relates to novel structural analogues and derivatives of compounds with general analgesic or related pharmacological activity. In particular the invention relates to derivatives of...
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6740641 |
Sugar derivatives of hydromorphone, dihydromorphine and dihydromorphine, compositions thereof and uses for treating or preventing pain
Glucoside and glucuronide derivatives of hydromorphone, dihydromorphine, and dihydroisomorphine and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising a glucoside or...
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6696457 |
Morphinoid compounds
Heterocycle condensed morphinoid derivatives of formula (I) have therapeutic utility as analgesics, in collagen disease, as anti-allergic and anti-inflammatory agents, brain cell protectants, in...
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6559159 |
Kappa opioid receptor ligands
Structurally novel kappa opioid receptor antagonists are provided and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such...
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6512117 |
Hydromorphone and hydrocodone compositions and methods for their synthesis
A method for the preparation of a ketone from a narcotic alkaloid having an allyl alcohol moiety is disclosed. The method includes mixing the narcotic alkaloid with an acid in the presence of a...
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6469170 |
Method for preparing oxycodone
A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine...
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6440987 |
Antipruritic
This invention provides an antipuritic comprising an opiate κ receptor agonist as an effective component, a new morphian quaternary ammonium salt derivative and a new morphian-N-oxide derivative...
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6365742 |
Preparation of opiates, intermediates and uses of salts
A process for the preparation of thebaine, its salts such as the bitartrate, and analogues thereof, together with a novel intermediate useful in said process are disclosed. Thebaine bitartrate is...
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6365594 |
Heterocycle-condensed morphinoid derivatives (II)
Heterocycle-condensed morphinoid derivatives of formula (I), or solvates or salts thereof, are potent and selective delta opioid agonists and antagonists and are useful as i.a. analgesics....
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6359111 |
Opioid receptor targeting
A compound comprising a ligand portion which has binding affinity for an opioid receptor, and a therapeutically or diagnostically effective group selected from radionuclide chelating agents,...
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6235906 |
Preparation of opiates
A novel process for the preparation of codeinone and analogues thereof comprising the oxidation of a compound of formula, ##STR1## or a salt thereof, wherein R 1 is lower alkyl or a group...
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6225321 |
Long analgesic acting nalbuphine polyester derivative and method of use
The nalbuphine polyester derivative is related to a novel long acting agent. The nalbuphine polyester derivative is R--[CO-NAL] n wherein n is an integer from 2-4 and, in which the R is selected...
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6194422 |
Anthracycline derivatives
The present invention provides imino aza-anthracyclinones and a method of treating amyloidoses using the same.
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6187783 |
Phenanthridinium derivatives
A novel phenanthridinium derivative represented by general formula (A): ##STR1## wherein R 1 is a substituted or unsubstituted lower aliphatic hydrocarbon group; R is an aliphatic hydrocarbon...
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6177438 |
Morphinan derivatives and pharmaceutical use thereof
A morphinan derivative or its pharmaceutically acceptable acid addition salt represented with, for example, ##STR1## and an analgesic, diuretic, antitussive and brain cell protector having its...
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6166211 |
Sequential benzylic oxidations of the naloxone ring system
The present invention pertains to a process for the preparation of the 10-keto analogs of morphinan compounds. In the case of compounds having a 3-hydroxyl group, the 3-methyl ether protected...
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6136817 |
Opioid receptor antagonist compounds
New morphinane derivatives of the formula ##STR1## their pharmaceutically acceptable salts, a process for their preparation and their use in the manufacture of pharmaceutical preparations.
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6124310 |
Enediyne compounds
The present invention provides compounds of formulae (I) and (II), where X in formula (I) represents a group cleavable by a nitroreductase or carboxypeptidase enzyme. Enzymatic activation of the...
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6013796 |
Preparation of naltrexone from codeine and 3-benzylmorphine
For the synthesis of 3-methylnaltrexone from codeine in this invention, codeine is converted to 6-acetylcodeine, which is N-demethylated to 6-acetylcodeine hydrochloride, followed by alkylating the...
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6008355 |
Preparation of oxycodone from codeine
A process is provided for preparing oxycodone from codeine comprising either: (A) the steps of (1) oxidizing codeine so as to form codeinone; (2) converting codeinone to oxycodone in a...
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6008354 |
Preparation of noroxymorphone from morphine
The invention provides processes for the conversion of normorphinone and its derivatives, which can be synthesized from morphine, to the corresponding 14-hydroxynormorphinone and its derivatives...
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5981751 |
Method for removal of residual organic solvents and use thereof in manufacturing pharmaceuticals
A method for removing residual organic solvents from a bulk substance, for example from a pharmaceutical drug substance, comprises drying the bulk substance in the presence of water vapor, such...
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5952495 |
Preparation of 14-hydroxynormorphinones from normorphinones
A process is provided for preparing 14-hydroxynormorphinones having the formula: ##STR1## which comprises reacting normorphinones having the formula: ##STR2## wherein R is selected from the group...
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5948788 |
Normorphine and normorphinone derivatives
Normorphine and normorphinone derivatives are provided as compositions of matter.
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5922876 |
Preparation of oxymorphone from morphine
A process is provided for preparing oxymorphone from morphine by: (a) reacting morphine with an acyl halide or anhydride to form 3-acylmorphine, or (b) reacting morphine with benzyl-halide to form...
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5886001 |
Agonist compounds
New morphinane derivatives of the formula (I) ##STR1## their pharmaceutically acceptable salts, a process for their preparation and their use in therapy. The variables in the above structure are as...
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5869669 |
Preparation of 14-hydroxynormorphinones from normorphinone dienol acylates
The invention provides processes for the conversion of normorphinone and its derivatives, which can be synthesized from morphine, to the corresponding 14-hydroxynormorphinone and its derivatives...
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5847142 |
Preparation of narcotic analgesics
A novel process for preparing narcotic analgesics such as hydrocodone and hydromorphone using catalytic amounts of homogeneous organometallic complexes is disclosed.
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