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Class 546/46 - A single chalcogen is bonded directly to ring carbon of the pentacyclo ring system (e.g., desoxy morphine, etc.)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein exactly one chalcogen atom (i.e., oxygen,
No. of patents: 70
Last issue date: 04/03/2012


1    
NumberTitleIssue Date
8148528Processes and compounds for the preparation of normorphinans
The invention generally provides processes and intermediate compounds useful for the production of normorphinans and derivatives of normorphinans. ...
04/03/2012
7985858Process for the preparation of 6-alpha-hydroxy-N-alkylated opiates
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. ...
07/26/2011
7671204N-demethylation of N-methyl morphinans
The present invention provides a synthetic process for the N-demethylation of N-methyl morphinans. In particular, the invention provides improved synthetic methods for the preparation of N-demethylated morphinan compounds that may be employed as starting materials, ...
03/02/2010
7435817C-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 (...
10/14/2008
7405301Chemical 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; and (ii) treating said N-oxide morphinane with a reducing agent. This...
07/29/2008
7399858Method 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(PR4R5R6)nXm]p; wherein M is a Grou...
07/15/2008
7399859Method for catalytic preparation of hydromorphone and hydrocodone
The present invention generally relates to catalysts of formula (III) [M(P(Ra)(Rb)N(Rc)(Rd))2Xn]mYp that selectively convert morphin...
07/15/2008
7323565Method 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 as catalyst. ...
01/29/2008
7320984Remedies 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 R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y ...
01/22/2008
7321038Method 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 catalyst of the formula [M(PR3R4R5)nXm]p; ...
01/22/2008
7285665Process 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 anhydrous solvent system, wherein the solvent system comprises an aprotic dip...
10/23/2007
7230005Compounds 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 derivative prior to formulation. Unlike many existing sustained releas...
06/12/2007
7220842Immunoassays 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 in a medium (i) a sample suspected of containing buprenorphine (BUP) o...
05/22/2007
7199129Derivatives 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 thereof. The disclosure also relates to processes for the preparation of ...
04/03/2007
7195882Monoclonal 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 metabolite conjugates for the production of monoclonal antibodies that s...
03/27/2007
7164021Opiate 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 analgesics. Because agonists with selectivity for the δ-opioid recept...
01/16/2007
6825204N-substituted 3-hydroxy-4-pyridinones and pharmaceuticals containing thereof
N-substituted 3-hydroxy-4-pyridinones and metal chelates, methods of preparing N-substituted 3-hydroxy-4-pyridinones and metal chelates, and pharmaceutical compositions containing new N-substituted 3-hydroxy-4-pyridinones and/or their metal chelates. Use of N-substi...
11/30/2004
6784186Therapeutic 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 opioid compounds, particularly morphine and related compounds, in whic...
08/31/2004
6740641Sugar 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 glucuronide derivative of hydromorphone, dihydromorphine, or dihydroi...
05/25/2004
6696457Morphinoid 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 gastritis, diarrhoea, cardiovascular and respiratory disease...
02/24/2004
6559159Kappa 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 as heroin or cocaine addictions....
05/06/2003
6552197Condensed-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 subjecting the thus-treated compound to recrystallization; and ...
04/22/2003
6512117Hydromorphone 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 catalyst wherein the method is carried out in the substantial...
01/28/2003
6440987Antipruritic
This invention provides an antipuritic comprising an opiate .kappa. receptor agonist as an effective component, a new morphian quaternary ammonium salt derivative and a new morphian-N-oxide derivative which are useful in treating puritus complicated with ...
08/27/2002
6365594Heterocycle-condensed morphinoid derivatives (II)
Heterocycle-condensed morphinoid derivatives of formula (I), or solvates or salts thereof, ##STR1## are potent and selective delta opioid agonists and antagonists and are useful as i.a. analgesics. Pharmaceutical compositions containing such compound...
04/02/2002
6359111Opioid 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, fluorochromes, toxins, drugs, polyboron moieties, proteins, biol...
03/19/2002
6323212Morphinan 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 ingredient, and its production process are described. The compound o...
11/27/2001
6316461Antipruritic
This invention provides an antipruritc comprising an opiate .kappa. receptor agonist as an effective component, a new morphinan quaternary ammonium salt derivative and a new morphinan-N-oxide derivative which are useful in treating pruritus complicated wi...
11/13/2001
6225321Long 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 from a saturated or nonsaturated, substituted or u...
05/01/2001
6187782Morphinane derivatives and medicinal use thereof
Novel morphinan derivatives and pharmaceutically acceptable acid addition salts thereof as compounds having abilities to bind to opioid &3xb5;-receptor, which have agonist or antagonist activities, are disclosed. The morphinan derivatives according to the...
02/13/2001
6177438Morphinan 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 derivative or its salt as the active ingredient are described....
01/23/2001
6166211Sequential 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 analog is synthesized by selective phenolic methylation in the ...
12/26/2000
6156764Morphine 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 salts of diclofenac (Formula 1); to processes for their produ...
12/05/2000
6150524Morphine derivatives with analgesic activity
Morphine derivatives of formula (I), process for perparing them and their use and use as analgesics. ##STR1##...
11/21/2000
6013796Preparation 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 nitrogen to form 17-cyclopropylmethylnorcodeine. The latt...
01/11/2000
6008354Preparation 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 including oxycodone, oxymorphone, noroxymorphone and naltrex...
12/28/1999
6008355Preparation 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 two-step-one-pot reaction: first reacting codeinone with hydrogen peroxide ...
12/28/1999
5981751Method 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 that the residual organic solvent molecules are displaced wit...
11/09/1999
5952495Preparation 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 consisting of lower alkyl of 1 to 7 carbon a...
09/14/1999
5948788Normorphine and normorphinone derivatives
Normorphine and normorphinone derivatives are provided as compositions of matter....
09/07/1999
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