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8106201 Process for the synthesis of morphinane compounds and intermediates thereof  
This invention relates to intermediates useful in the preparation of opiate alkaloids, particularly morphinane compounds. The invention also relates to processes for preparing such intermediates...
8063059 Use of compositions containing kappa-opioid receptor antagonists for the treatment of dissociative disorders  
The invention relates to the use of a composition comprising kappa opioid receptor antagonists for producing a drug for the treatment of dissociative disorders in humans.
8026252 Large substituent, non-phenolic opioids and methods of use thereof  
8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
8017777 Process for the preparation of buprenorphine and derivatives for buprenorphine  
The invention generally provides processes for the production of buprenophine and derivatives of buprenorphine. In particular, the process may encompass synthetic routes for the production of...
7964610 Buprenorphine derivatives and uses thereof  
Ester derivatives of the phenolic hydroxyl group of buprenorphine can be used in the treatment of opiate dependency and/or moderate to severe pain. The esters have an enhanced bioavailability, an...
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 the...
7534799 Pyridomorphinans, thienomorphinans and use thereof  
Compounds represented by the formulae: wherein each of Y, X and R individually is selected from the group consisting of hydrogen, hydroxy, halo, CF3, NO2, CN, NH2, COR1 and CO2R2 wherein R1 is...
7511054 Transdermally deliverable opioid prodrugs, abuse-resistant compositions and methods of using opioid prodrugs  
Described herein are opioid prodrugs, methods of making opioid prodrugs, formulations comprising opioid prodrugs, and methods of using opioid prodrugs. One embodiment described herein relates to...
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;...
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...
7125884 N-but-3-enyl norbuprenorphine and its use as analgesic  
The present invention provides compound having the structure: and pharmaceutically acceptable salts or derivatives thereof, as well as compositions including such compounds. The invention also...
7119100 Oripavine derivatives and their uses as pharmaceuticals  
The present invention relates to oripavine derivatives of formula (I), wherein R1 is hydrogen or methyl, R2 is methyl, cyclopropyl methyl, cyclobutyl methyl or allyl, R3 is thiophenyl ethyl or...
7084150 Analogs and prodrugs of buprenorphine  
Disclosed are prodrugs and analogs of buprenorphine.
6965029 Method for producing enantiomer-free 6,8 dihydroxy octanoic acid esters by means of asymmetric, catalytic hydrogenation  
The invention relates to a process for the preparation of compounds of the general formula I in which R1 represents a C1-C20-alkyl group, a C3-C12-cycloalkyl group, a C7-C12-aralkyl group or a...
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...
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...
6465479 Pyridomorphinans and use thereof  
Compounds represented by the formula: wherein each of Y, X and R individually is H, OH, alkyl, alkoxy, aryl, halo, CF3 and NO2, provided that at least one of Y, X and R is other than H; and...
6417365 Method for recovering medicaments from preparations, and from the precursors or wastes thereof  
In a process for recovering medicinal substances or active substances from preparations, their initial products or waste, a flat-shaped starting material in the form of a film with adhesive and an...
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....
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,...
6355783 Compounds for mass coloration of high temperature polymers  
The invention relates to novel soluble pigment precursors possessing not only higher thermal stability but also improved solubility characteristics and to a process for mass coloration of high...
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,...
6284769 Nonpeptide kappa opioid receptor antagonists  
The compounds of structural formulae (I) and (II) ##STR1##and use of the compounds and salts and hydrates thereof, as therapeutic agents, is disclosed. A compound of formula (I) or (II) is an...
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 ...
6136976 Process for producing perylene-3, 4-dicarboxylic acid imides  
Perylene-3,4-dicarboximides I ##STR1## (R1 is hydrogen; C1 -C8 -alkyl; C5 -C8 -cycloalkyl; substituted or unsubstituted phenyl or naphthyl; R2 independently at each occurrence is hydrogen; C1 -C18...
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...
5985887 Aza-anthracyclinone derivatives  
Compounds of formula I ##STR1## wherein X1 and X2 are CO, CNH or CH2, X3 is CH2, CO, CHOH, ##STR2## wherein n=2 or, 3 or CN(R9) wherein R9 is hydroxy or amino-aryl, and each of R1, R2, R3, R4, R...
5981540 Heterocycle-condensed morphinoid derivatives  
Compounds of formula (I), are selective delta opioid agonsist and antagonists, and are useful as analgesics and in treating general neurologic disorders. ##STR1##
5948788 Normorphine and normorphinone derivatives  
Normorphine and normorphinone derivatives are provided as compositions of matter.
5861411 4-Acylaminopyridine derivative  
A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for...
5849915 Buprenorphine analgesic analogues  
The object of this invention is to provide novel buprenorphine analgesic analogues represented by following formula(I) and their non-toxic pharmaceutically acceptable salts. ##STR1## wherein R1 is...
5808073 Preparation and purification of perylene-3,4-dicarbimides  
Preparation of perylene-3,4-dicarbimides by reaction of a perylene-3,4,9,10-tetracarboxylic acid or of the corresponding anhydrides with a primary amine by performing the reaction in the presence...
5770604 Aconitine compound and an antipyretic/analgesic/anti-inflammatory agent  
This invention provides novel aconitine compounds of the formula (I) or salt thereof ##STR1## wherein, R1 is a hydrogen atom or hydroxyl group; R2 is an acetyloxy group; R3 is an alkyl having 1-4...
5648359 Tumor necrosis factor production inhibitors  
There is provided a composition for inhibiting the production or secretion of tumor necrosis factor effective for the treatment of cachexia, septic shock, multiple organ failure, rheumatoid...
5631263 Use of delta opioid receptor antagonists to treat immunoregulatory disorders  
A therapeutic method is provided to elevate a depressed mammalian autologous mixed lymphocyte response and to alleviate the diseases associated therewith by the administration of an effective...
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...
5552406 Method for treating pain and brain perfusion abnormalities using mixed opioid agonist-antagonists  
A method for treating pain and brain perfusion abnormalities using mixed opiate agonist/antagonists is provided.
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] (I)wherein [D] is a...
5514684 Aconitine compounds and analgesic/anti-inflammatory agent containing the same  
Novel aconitine compounds of the formula ##STR1## wherein the symbols are as defined in the description, as well as analgesic/anti-inflammatory agent containing them or salts thereof as active...
5281710 Dynemicin analogs: synthesis, methods of preparation and use  
A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have...
4912114 Morphinan derivatives  
Compounds of formula I ##STR1## wherein X and Y each denotes hydrogen or together denote -0-, R1 denotes allyl optionally substituted by 1 to 3 alkyl groups, the substituent or substituents having...
4673679 Use of prodrugs of 3-hydroxymorphinans to prevent bitter taste upon buccal, nasal or sublingual administration  
Aliphatic, aromatic, carbonate, carbamate, or sulfonate ester prodrugs of 3-hydroxymorphinans lack the bitter taste of the parent compounds and provide enhanced bioavailability of...
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...
4599341 Substituted and bridged pyridines useful as calcium channel blockers  
Novel substituted and bridged pyridine compounds useful as calcium channel blockers, pharmaceutical compositions thereof, and methods of treatment are disclosed.
4587253 Bridged pyridine compounds useful as calcium channel blockers and analgesics  
Novel substituted and bridged pyridine compounds useful as calcium channel blockers and analgesics, pharmaceutical compositions thereof, and methods of treatment are disclosed.
4476007 Hemispherands and sodium-selective compositions and electrodes containing same  
Ion-selective compositions which comprise an ion carrier, a compound capable of solvating the ion carrier, and a supporting matrix are disclosed.The ion carriers of this invention are hemispherand...
4443605 7β-Arylalkyl-6α, 7 α-oxymethylene-3-methoxy or 3-hydroxy-4, 5α-epoxy-17 methyl or 17-cycloalkyl-methyl morphinans  
Disclosed are 7β-arylalkyl substituted morphinan compounds characterized by the formula: ##STR1## In the above formula, R is H or methyl, R1 is methyl, cyclopropylmethyl or cyclobutylmethyl and n ...
4440931 7β-Arylalkyl-3-methoxy or 3-hydroxy-4,5α-epoxy-6β-hydroxy-7α-hydroxymethyl-17-met hyl or 17-cycloalkylmethylmorphinans  
Disclosed are 7β-alkyl or arylalkyl-3-methoxy or hydroxy-4,5α-epoxy-6β-hydroxy-7α-hydroxymethyl-17-methyl or cycloalkylmethylmorphinans of the formula: ##STR1## In the above formula, R is H or met...
4440932 7β-Arylalkyl-7α-methyl-6-oxo or 6α-hydroxy-3-methoxy or 3-hydroxy-4,5α-epoxy-17-methyl or 17-cycloalkyl-methylmorphinans  
Disclosed are 7β-arylalkyl-7α-methyl-6-oxo or 6α-hydroxy-3-methoxy or 3-hydroxy-4,5α-epoxy-17-methyl or 17-cycloalkylmethyl-morphinans of the formula: ##STR1## wherein R is H or methyl, X is oxo...
4148794 Lower-alkyl 3-R5 CO-octahydro-2,5-methanobenzo[g]quinoline-3-carboxylates  
Lower-alkyl 1-R1 -3-R5 CO-4aα-R3 -5α-R4 -6-R2 "-7-R2 -8-R2 '-9-R2 '"-1,2,3,4,4a,5,10,10a-octahydro-2,5-methanobenzo[g]quinolin e-3-carboxylat es, useful as intermediates for the preparation of 3...
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