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Matches 1 - 50 out of 1,289

Document Document Title
WO/2020/188583A1
The present invention discloses an improved process for O-demethylation of methoxy-substituted morphinan-6-one derivatives using boron-based complex as a demethylating boron complex in an inert reaction solvent.  
WO/2020/172248A1
The present invention relates to a solution for preservation, perfusion, and/or reperfusion of an organ, preferably the heart for transplantation or after coronary angioplasty/cornary arterial bypass. The solution contains a compound of ...  
WO/2020/167566A1
Compounds of formulas II and III (including nalfurafine and naltrexone) or their pharmaceutically acceptable salts administered in combination at low dosages may be used to reduce alcohol consumption in a person in need thereof. Addition...  
WO/2020/103945A1
Disclosed are an oxycodone compound, and an intermediate and a preparation method therefor. Specifically disclosed is a preparation method for a compound represented by formula A9, comprising the following steps: under a protective gas, ...  
WO/2020/107015A1
The present invention provides the application of binary naltrexone derivatives in the preparation of Toll-like receptor 4 signaling pathway inhibitors, the application of binary naltrexone derivatives in the preparation of inflammatory ...  
WO/2020/094634A1
The present invention provides compounds useful for the treatment of opioid dependence, alcohol dependence, alcohol use disorder, or the prevention of relapse to opioid dependence in a subject in need thereof. Related pharmaceutical comp...  
WO/2020/085234A1
The present invention relates to a morphinan derivative that has an opioid κ receptor agonist effect and that is represented by general formula (I). (In the formula, R1 indicates a hydrogen atom, a C1-6 alkyl group that may have a subst...  
WO/2020/077235A1
The disclosure provides methods for treating, preventing, and reducing the incidence of opioid- induced respiratory depression, opioid-induced apnea, and opioid overdose in patients by administering buprenorphine or a pharmaceutically ac...  
WO/2020/041159A1
Non-peptide MOR opioid receptor modulators are provided. The compounds exhibit predominantly central activity and are used to treat e.g. opioid addiction. The compounds described herein are generally delivered (administered) in a pharmac...  
WO/2020/012248A1
The present invention provides compounds useful for the treatment of opioid dependence, alcohol dependence, alcohol use disorder, or the prevention of relapse to opioid dependence in a subject in need thereof. Related pharmaceutucal comp...  
WO/2020/014342A1
The present disclosure relates to methods for treating patients with pruritus associated with liver disease with anti-pruritic compositions; methods for treating patients with pruritus associated with obstructive cholestasis secondary to...  
WO/2019/246353A1
A novel structure of an opioid antagonist is provided. One of the exemplary compounds of the present disclosure has the structure of Formula (II). The present disclosure overcomes the discomfort of conventional opioid antagonist due to r...  
WO/2019/214726A1
This disclosure relates to crystalline forms of 3-acyl-buprenorphine derivatives and sustained release injectable pharmaceutical compositions for treatment of opioid dependence, pain or depression, including an aqueous suspension of crys...  
WO/2019/189749A1
A method for producing compounds represented by the following general formula through a dealkylation reaction in which a boron trifluoride complex is used (in the formula, R1 is a C1-10 alkyl group, etc., R2 is a C1-10 alkyl group, etc.,...  
WO/2019/168025A1
Provided is a method for producing morphinan derivatives having the buprenorphine skeleton. In the method, compounds represented by formula (III) are obtained using a Diels-Alder condensation reaction between (I) and (II). By introducing...  
WO/2019/165298A1
This invention relates to novel opioid derivatives of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R3, R4 and Z are as defined herein in the disclosure. The invention also relates to the use of such co...  
WO/2019/118205A1
The present invention relates to pharmaceutical combinations comprising a cannabinoid in particular dronabinol and an opioid, wherein the pharmaceutical combination is synergistically effective. Methods of treating or preventing pain com...  
WO/2019/109170A1
Disclosed are methods for converting a first morphinan alkaloid compound into a second morphinan alkaloid compound in the presence of a neopinone isomerase enzyme under reaction conditions permitting the conversion of the first alkaloid ...  
WO/2019/102175A1
The present invention provides a process for the preparation of a compound of formula (2) : the process comprising reacting a compound of formula (1), a base and an alkylating agent R4-X in a nitrile-containing polar aprotic solvent to f...  
WO/2019/094528A1
An improved heroin conjugate vaccine is detailed; to accomplish this task the systematic exploration of twenty vaccine formulations with varying combinations of carrier proteins and adjuvants were undertaken. In regard to adjuvants, a To...  
WO/2019/079327A1
Disclosed herein are methods of methods of treating pain in a subject, reducing opioid dose without increasing pain to a subject, and decreasing pain in a subject without decreasing an opioid dose.  
WO/2019/073247A1
There is provided a novel process for the preparation of a compound of formula I, wherein R1, R2,W, Z and II are as described in the description, by demethylation of a corresponding O-methyl derivative with a borohydride-based reagent. T...  
WO/2019/058387A1
The present invention relates to an improved process for the preparation of (5α, 6α)-17-allyl-6-(2, 5, 8, 11, 14, 17, 20- heptaoxadocosan-22-yloxy)-4, 5-epoxymorphinan-3, 14-diol which is represented by the following structural formula...  
WO/2019/045006A1
A morphinan derivative represented by general formula (I) (in the formula, R1 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R2 and R3 are the same or different and represent a hydrogen atom, a hydro...  
WO/2019/018638A1
There are provided, prodrugs of opioid and other controlled substance, having enhanced physical and chemical stability to resist tampering and to make long-acting release formulations, and pharmaceutically accepted salts and solvates the...  
WO/2019/009820A1
The invention describes the process of catalytic O-demethylation of 3-methoxy-morphinane compounds using boron tribromide. Addition of catalysts reduces the reaction time, improves reacting the substrate to give the product in very good ...  
WO/2018/234748A1
A process for preparing oxycodone hydrochloride, said process comprising hydrogenating 14- hydroxycodeinone in an alcoholic solvent and hydrochloric acid to form oxycodone hydrochloride, wherein (a) the hydrogenation is carried out in th...  
WO/2018/211331A1
Disclosed are methods for preparing buprenorphine from, for example, compounds such as nororipavine and northebaine.  
WO/2018/200607A1
Disclosed and described is a novel dose titration procedure for administering the opioid antagonist, nalmefene, to a patient diagnosed with post-traumatic stress disorder (PTSD).  
WO/2018/183264A1
The invention describes pharmaceutical compounds and compositions comprised of a ligand attached to opioids in a manner that substantially decreases or deters the potential for opioid abuse, addiction, illicit and illegal use, and overdo...  
WO/2018/178879A1
A method of recovering a highly pure hydrocodone base from an impure hydrocodone preparation includes contacting the impure hydrocodone preparation with a weak acid in water to form a solution and adding a strong base to the solution in ...  
WO/2018/165183A1
An abuse deterrent opioid formulation for rectal use. The formulation contains a therapeutically effective amount of the opioid buprenorphine or salts and homologs thereof; and either a gel with a diminishing agent or a suppository base ...  
WO/2018/141192A1
The present invention relates to a compound as represented by structural formula (I) and a non-toxic, pharmaceutically acceptable salt thereof. In formula (I), R1 is H, CH3 or deuterated methyl(CD3); R2 is CH3 or CH2CH3; each of R3, R4 a...  
WO/2018/128798A1
Novel antagonists of toll-like receptor 4 (TLR-4) are provided. More specifically, the novel antagonists of TLR-4 are derived from morphinan. Further, use of said morphinan derivatives in the treatment of diseases and/or disorders mediat...  
WO/2018/125716A1
The application is directed to compounds of formula (I): and pharmaceutically acceptable salts, radiolabeled isomers, solvates, or hydrates thereof, wherein R1, R2, R3, X, and n are defined as set forth in the specification. The applicat...  
WO/2018/080838A1
The invention provides haptens and methods of preparation thereof, for producing immunoconjugates of oxycodone and hydrocodone suitable for raising antibodies in animals specific for the opioid drugs. Adminislration of the opioid-speeifi...  
WO/2018/070943A1
The invention describes a method for purification of naltrexone base from reaction mixtures concentrated by evaporation and/ or from mixtures containing naltrexone in the presence of other organic or inorganic substances by trituration a...  
WO/2018/009856A1
Methods are provided for efficient preparation of hydromorphone or hydrocodone by redox isomenzation of morphine or codeine allylic alcohols, respectively, using transition metal aminophosphine catalysts formed in situ.  
WO/2017/218518A1
Compositions and methods for treatment of acute and chronic pain are disclosed herein. These compositions include fixed dose oral formulations containing an atypical antipsychotic drug and an opioid. Also provided here are methods of tre...  
WO/2017/211879A1
The present invention relates to the process for the manufacture of hydrocodone or hydromorphone from their enol derivatives codeine and morphine respectively. Particularly, the invention discloses a metal catalyst that is used in low am...  
WO/2017/210105A1
Peripherally selective compounds that modulate both the mu opioid receptor (MOR) and the kappa opioid receptor (KOR) are provided. The compounds are substituted derivatives of 6p-N-heterocyclic naltrexamine (NAP) and are used in the trea...  
WO/2017/207519A1
The present invention relates to a new process for obtaining 3,14-diacetyloxymorphone from oripavine, a process to transform the obtained 3,14-diacetyloxymorphone into a noroxymorphone and a process to transform said noroxymorphone into ...  
WO/2017/200970A1
Analogues of 6 α/β-naltrexamine (NAQ) are provided. The analogues are selective, reversible antagonists of the mu opioid receptor (MOR) that exhibit good blood brain barrier penetration. The compounds are used in the treatment of opioi...  
WO/2017/184979A1
The present disclosure relates to N-demethylation of a compound containing a tertiary N-methylamine, including for example a morphinan alkaloid, in a continuous flow system. In particular, the present disclosure relates to N-demethylatio...  
WO/2017/185004A1
The present invention relates to processes useful in the preparation of morphine analogs and derivatives, such as naltrexone, naloxone and nalbuphine and intermediates in the synthesis of said morphine analogs and derivatives. In a parti...  
WO/2017/165558A1
The invention provides compounds, compositions, and methods for treating pain.  
WO/2017/133634A1
The present invention relates to an opioid receptor antagonist conjugate and a use thereof. In particular, the present invention relates to a covalent coupling conjugate of a hydrophilic polymer and an opioid receptor antagonist and the ...  
WO/2017/120468A1
The present invention relates to methods for treating pruritus with anti-pruritic compositions, wherein the method provides a therapeutic effect without producing a substantial aquaretic effect.  
WO/2017/095734A1
The invention describes pharmaceutical compounds and compositions comprised of a ligand attached to the opioid oxymorphone, in a manner that substantially decreases or deters the potential for opioid abuse, addiction, illicit and illegal...  
WO/2017/092638A1
The present invention relates to an opioid receptor antagonist derivative, a preparation method thereof and a use thereof in medicine. In particular, the present invention relates to a naloxone derivative as shown by general formula (I) ...  

Matches 1 - 50 out of 1,289