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Matches 1 - 50 out of 958

Document Document Title
WO/2022/165040A1
The application is directed to an efficient process for crystallizing nalmefene hydrochloride in a hydrated form from an aqueous hydrochloric acid solution (or a mixture) with a high yield.  
WO/2022/144911A1
: Novel Process for the Synthesis of Noroxymorphone from Morphine The present invention relates to a novel, efficient, pot- and atom-economical, and industrially applicable process for converting morphine to noroxymorphone using reagents...  
WO/2022/127320A1
An application of an intermediate or a preparation method therefor in total synthesis of a morphine derivative. On the basis of a possible biogenic pathway of morphine derivatives, efficient production of morphine derivatives, especially...  
WO/2022/127321A1
The invention relates to the field of medicament synthesis and specifically to a novel intermediate, a preparation method for same, and applications thereof. The structural formula of the novel intermediate of the present application is ...  
WO/2022/087422A9
The present disclosure relates to compounds of Formula (I'): and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are use...  
WO/2022/101408A1
Hydromorphone hydrochloride (I·HCl) is converted into hydromorphone base (I) via hydromorphone monohydrate (I·H2O).  
WO/2022/094470A1
The application is directed to a process of purifying noroxymorphone by preparing and isolating noroxymorphone bisulfite adduct and regenerating purified noroxymorphone from noroxymorphone bisulfite adduct. The application is also direct...  
WO/2022/004783A1
This method for producing a morphinan derivative by means of a reduction reaction using formic acid or the like is represented by the following general formula (II).  
WO/2021/178405A1
The first selective SuFEx antagonists to μ-opioid receptors (MOR) were developed by functionalizing an opioid scaffold with an SO2-F warhead. Our model, based on a MOR structure with antagonist β-FNA, indicates the naloxone carbonyl as...  
WO/2021/178541A1
Combinations of compounds that inhibit activation of p-Src tyrosine kinase, having particularly utility in the treatment of inflammation resulting from traumatic surgical interventions and the proliferation or metastasis of cancer cells ...  
WO/2021/144362A1
Disclosed are methods for preparing buprenorphine from, for example, compounds such as nororipavine and northebaine.  
WO/2021/132637A1
The present invention addresses the problem of providing a method for producing a high-purity N-dealkylated cyclic secondary amine via a simple and non-turbulent method. An N-dealkylated cyclic secondary amine can be obtained by reacting...  
WO/2021/067870A1
A compound represented by Formula 1 wherein R1 is selected separately from one of methyl, ethyl, n-propyl, i-propyl, allyl, cyclopropylmethyl, cyclobutylmethyl, N-isopent-2-enyl; R2 is selected separately from hydrogen, methyl, or ethyl;...  
WO/2021/024039A1
Provided herein are (e.g., controlled release) compositions for the treatment of acute or chronic diseases or disorders. Described herein are processable opioid conjugates. Also described herein are compositions and methods for the treat...  
WO/2021/007366A1
In some aspects, the present disclosure provides compounds of the formula: (I) (II) wherein the variables are as defined herein. In some embodiments, these compounds may be used to reduce the pain of a patient. These compounds may be use...  
WO/2020/213911A1
The present invention provides a method for economically preparing high-purity naldemedine with high yield.  
WO/2020/205735A1
The present invention related to novel morphinans, compositions comprising the novel morphinans, and their uses as agonists of the kappa opioid receptor.  
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...  

Matches 1 - 50 out of 958