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Class 546/44 - One of the five cyclos is five-membered and includes ring chalcogen (e.g., codeine, morphine, etc.)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein one of the cyclos of the pentacyclo ring
No. of patents: 164
Last issue date: 05/01/2012


1          
NumberTitleIssue Date
8168790Process for the preparation of 6-beta hydroxy morphinan compounds
The invention provides processes for the conversion of a 6-keto morphinan to a 6-hydroxy morphinan. In particular, the invention provides a stereoselective process for the conversion of a 6-keto morphinan to a 6-beta-hydroxy morphinan. ...
05/01/2012
7803942Crystals of morphinan derivative and process for producing the same
The present invention is directed to provide 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride consistent in quality after production and having high purity. A crystal of 17-cyclopropylmethyl-3,14β-d...
09/28/2010
7671203Method and system for separation and purification of at least one narcotic alkaloid using reverse phase preparative chromatography
An apparatus and method for separating at least one narcotic alkaloid that includes loading a stationary phase media into a high performance preparative liquid chromatography column, feeding a crude narcotic alkaloid solution into the chromatographic column, applyin...
03/02/2010
7495098Extraction 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 the dissolved opium solution with at least one first weak acid, filt...
02/24/2009
74657976-monoacetylmorphine derivatives useful in immunoassay
Analogs of 6-monoacetyl morphine (6-MAM) are described. These include analogs derivatized at either the C-3 position, the C-6 position, or the nor position of the molecule. These analogs allow for elaboration with linkers terminated by a functional group such as an ...
12/16/2008
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
7348430Production 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 benzophenone in the presence of potassium tert-alkylate in a hydrocarb...
03/25/2008
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
7319105Cytotoxic 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 preparing compounds of the invention, and therapeutic methods for treat...
01/15/2008
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
7279579Polymorphic 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 naltrexone impart advantages in pharmaceutical formulations incorpora...
10/09/2007
7232829Therapeutic compounds and methods
The invention provides kappa receptor agonists of formula (I) and delta receptor antagonists of formula (II), wherein R1–R6 X and n have any of the meanings given in the specification, as well as compositions comprising them, methods for thei...
06/19/2007
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
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
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
7153966Preparation 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 steps of: a) preparing a mixture ...
12/26/2006
7129248Process 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. ...
10/31/2006
6972332Process 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 steps: (a) providing a solution or suspension of a morphine component i...
12/06/2005
6958398Methods 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: 8-methoxy-Δ6-dihydrothebaine, codeinone dimethyl ketal, and...
10/25/2005
6949645Process 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 steps: (a) providing a solution or suspension of a morphine component i...
09/27/2005
6946556Preparation 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 benzophenone and neutral solvent in the presence of a metal catalyst...
09/20/2005
6936709Method 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 protected 2′-deoxycytidine and water, and by recovering the protected 2...
08/30/2005
6887998Process for 8-carboxamido-2,6-methano-3-benzazocines
8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as ana...
05/03/2005
6887999Preparation 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 formation. ...
05/03/2005
6864370Process 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 a codeine salt (e.g., codeine phosphate) is converted int...
03/08/2005
6825205N-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 C1-6 alkyl. These compounds act as μ opioid receptor...
11/30/2004
6790959Process 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 codeine salt (e.g., codeine phosphate) is converted into the i...
09/14/2004
67841878-carboxamido-2,6-methano-3-benzazocines
8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesi...
08/31/2004
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
6703371Preparations 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 heterocycle. These substances are used to reduce the oxygen consum...
03/09/2004
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
6579985Preparation 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 100 to 215° C. under reflux conditions such that approximat...
06/17/2003
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
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
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