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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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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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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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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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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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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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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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7220842 |
Immunoassays for buprenorphine and norbuprenorphine
Methods, compositions and kits are disclosed directed at haptens, immunogens and immunoassays for buprenorphine (BUP) and nor buprenorphine (norBUP). The method comprises providing in combination...
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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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7195882 |
Monoclonal antibodies specific for buprenorphine and metabolites thereof
The present invention relates to monoclonal antibodies that specifically bind buprenorphine and/or at least one metabolic product thereof. The present invention further relates to buprenorphine...
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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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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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6552197 |
Condensed-hexacyclic compounds and a process therefor
Disclosed are a process for the preparation of a compound represented by the formula ( 1 ), which comprises treating a compound represented by the formula ( 2 ) with methanesulfonic acid and then...
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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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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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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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6187782 |
Morphinane derivatives and medicinal use thereof
Novel morphinan derivatives and pharmaceutically acceptable acid addition salts thereof as compounds having abilities to bind to opioid ε-receptor, which have agonist or antagonist activities, are...
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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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6156764 |
Morphine and diamorphine salts of anionic non-narcotic analgesics of the substituted carboxylic acid type
The present invention relates to morphine and diamorphine salts of anionic non-narcotic analgesics belonging to the type of substituted carboxylic acids, preferably the morphine and diamorphine...
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6150524 |
Morphine derivatives with analgesic activity
Morphine derivatives of formula (I), process for perparing them and their use and use as analgesics. ##STR1##
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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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5834478 |
Morphinan hydroxamic acid compounds
This invention provides a compound of the following formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is hydrogen, C 1 -C 5 alkyl or an O-protecting group; B is a...
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5631264 |
Substituted 6,11-ethano-6,11-dihydrobenzo[B]quinolizinium salts and compositions and methods of use thereof
Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or...
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5525727 |
Brain-specific drug delivery
The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are: (a) compounds of the formula [D-DHC] ...
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5232926 |
Morphinane-skeletoned hydrazone derivatives
The present invention relates to novel morphinane-skeletoned compounds of the formula (I) ##STR1## wherein Y in-NH phenyl or --NH dintro phenyl, Z is --CH 2 -- CH 2 , R 2 is hydroxyl and R 3 is...
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4990617 |
N-oxide prodrug derivatives of 3-hydroxy morphinans and partial morphinans and derivatives
N-oxide prodrug derivatives of 3-hydroxy morphinan and partial morphinan analgesics, agonist-antogonists, and narcotic antagonists are useful therapeutic entities which provide enhanced...
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4939264 |
Immunoassay for opiate alkaloids and their metabolites; tracers, immunogens and antibodies
The present invention is directed to a fluorescence polarization assay for opiate alkaloids and their metabolites, to the various components needed for preparing and carrying out such an assay and...
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4912114 |
Morphinan derivatives
Compounds of formula I ##STR1## wherein X and Y each denotes hydrogen or together denote -0-, R 1 denotes allyl optionally substituted by 1 to 3 alkyl groups, the substituent or substituents...
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4806556 |
Gut-selective opiates
Gut-selective agonist or antagonist opiates of the formula: ##STR1## wherein R is (C 1 -C 5 ) alkyl, C 3 -C 6 (cycloalkyl)alkyl, aryl, aralkyl or trans-(C 2 -C 5 )alkenyl; Z is H or OH, R' is...
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4767718 |
Fluorescent opioid reagents and methods of use thereof in the detection of opioid receptors
Fluorescent reagents useful as opioid receptor probes. Opioids labeled at the 3 position with fluorescers are useful in various in vivo and in vitro methods for the detection and quantification of...
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4751307 |
Wittig-reaction processes
Disclosed are improved Wittig reaction processes wherein the Wittig reaction is conducted in an anisole containing solvent.
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4668685 |
Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, which are analgesics or narcotic antagonists
Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans are useful as analgesics or narcotic antagonists and provide enhanced bioavailability of 3-hydroxymorphinans from orally...
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4667037 |
Dealkylation of opioid ethers
An improved process for the dealkylation of alkyl aryl ethers to aryl phenols is provided. In this process, an alkyl aryl ether, such as a methyl ether of an opioid, is contacted with an aqueous...
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