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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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7557119 |
Large substituent, non-phenolic opioids
8-Substituted-2,6-methano-3-benzazocines of general structure
are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. One embodiment is...
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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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7538118 |
6-aminomorphinane derivatives, method for production and use thereof
This invention relates to compounds of the formula (I).
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7501434 |
6-carboxy-normorphinan derivatives, synthesis and uses thereof
The present invention relates to compounds of formula I, synthesis thereof, and methods of using the same.
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7495098 |
Extraction of alkaloids from opium
A method for extracting at least one alkaloid from opium that includes dissolving opium in a solvent, heating the dissolved opium solution, cooling the dissolved opium solution, adjusting the pH of...
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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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7320984 |
Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group
The invention provides a morphinan derivative of the Formula (I):
wherein R 1 is methyl, cyclopropylmethyl or the like; R 2 and R 3 are hydroxy, methoxy, acetoxy or the like; both Y and Z...
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7319105 |
Cytotoxic agents
The invention provides compounds of the invention pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for...
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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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7279579 |
Polymorphic forms of naltrexone
This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of...
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7230005 |
Compounds and methods for lowering the abuse potential and extending the duration of action of a drug
The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug...
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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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6972332 |
Process for the production of opiates
A morphine component, e.g., a concentrate of poppy straw, is converted into codeine in high yield and high purity and in a highly controlled manner. The conversion process involves the following...
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6958398 |
Methods for making thebaine or its acid salts
Methods for making thebaine and an acid salt of thebaine are disclosed herein. In one embodiment, an acid salt of thebaine is made from codeinone or an acid salt of one or more of the following:...
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6936709 |
Method for purifying protected 2′-deoxycytidines and hydrated crystals thereof
A protected 2′-deoxycytidine is purified by precipitating the protected 2′-deoxycytidine represented by general formula (3) in the form of a hydrated crystal from a solution containing the...
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6887999 |
Preparation of dihydrocodeine from codeine
A process for the preparation of dihydrocodeine by hydrogenating codeine or a salt thereof in aqueous solution in the presence of a catalytic metal and deactivating agent that decreases impurities...
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6887998 |
Process for 8-carboxamido-2,6-methano-3-benzazocines
8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH 2 —OH, —CH 2 NH 2 , —NHSO 2 CH 3 ,
and Y is O, S or
NOH are useful as analgesics, anti-diarrheal...
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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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6790959 |
Process for manufacturing thebaine
Thebaine 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 a...
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6784187 |
8-carboxamido-2,6-methano-3-benzazocines
8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH 2 —OH, —CH 2 NH 2 , —NHSO 2 CH 3 , and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents,...
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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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6703371 |
Preparations for reducing oxygen consumption during physical efforts
The invention relates to pharmaceutically active substances from the group comprising midazolam and compounds with a methyl-substituted nitrogen atom that is the ring atom of a nitrogenous...
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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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6579985 |
Preparation of codeine from morphine
An improved process for the preparation of codeine from morphine comprises the steps of a) reacting morphine with a methylating agent in the presence of a hydrocarbon solvent at a temperature of...
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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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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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6403602 |
Morphine-6-sulfate analogues and their use for the treatment of pain
3-O-Acetylmorphine-6-sulfate analogues are potent, centrally-acting morphine derivatives. The compounds are useful for the treatment of pain.
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6387917 |
Salts of opioid analgesics, particularly morphine, and methods of using same
The methane sulphonate salt of morphine and compositions thereof have medicinal uses, particularly in the treatment of pain. Compositions comprising a methane sulphonate salt of an opioid analgesic...
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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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6323212 |
Morphinan derivative and its pharmaceutical applications
A morphinan derivative or its pharmacologically allowed acid addition salt represented with compound I, ##STR1## an analgesic and diuretic having its derivative or its salt as the active...
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6310207 |
Process of preparing camptothecin derivatives
A process of preparing camptothecin derivatives of formula 1 is disclosed ##STR1##
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6291675 |
Methods of o-demethylation and n-deprotection
The present invention provides a method for N-deprotecting an opioid compound, a method for N-deprotecting and O-demethylating an opioid compound, a method for O-demethylating an opioid compound,...
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6262265 |
Non-hydrolyzable analogs of heroin metabolites suitable for use in immunoassay
Novel chemical analogs are disclosed for the essential heroin metabolite 6-O-acetyl morphine (6MAM). The analogs optionally can be made to contain protein reactive groups, and can be used to form...
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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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