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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.,...
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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...
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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...
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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...
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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 ...
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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...
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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...
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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.
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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...
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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...
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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...
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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...
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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 ...
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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...
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WO/2018/211331A1 |
Disclosed are methods for preparing buprenorphine from, for example, compounds such as nororipavine and northebaine.
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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).
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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...
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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 ...
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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 ...
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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...
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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...
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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...
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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...
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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...
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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.
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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...
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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...
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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...
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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 ...
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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...
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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...
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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...
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WO/2017/165558A1 |
The invention provides compounds, compositions, and methods for treating pain.
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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 ...
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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.
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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...
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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) ...
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WO/2017/091827A1 |
The invention describes pharmaceutical compounds and compositions comprised of a ligand attached to the opioid oxycodone, in a manner that substantially decreases or deters the potential for opioid abuse, addiction, illicit and illegal u...
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WO/2017/073710A1 |
The purpose of the present invention is to provide a compound that is effective as a prophylactic agent or a therapeutic agent for various diseases and symptoms associated with the orexin receptor, as well as to provide a medical usage t...
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WO/2017/066249A1 |
An invention includes a process for the preparation of (S)-2((4R,4aS,6R,7R,7aR,12bS)-7,9-dimethoxy-1,2,3,4,5,6,7,7a
-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinol
in-6-yl)-3,3-dimethylbutan-2-ol.
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WO/2017/046814A1 |
The present invention discloses a short, simplified and eco-friendly process for producing Nalbuphine or its pharmaceutically acceptable salts thereof. In particular, the process of the present invention avoids use of any hazardous, corr...
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WO/2017/041139A1 |
The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.
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WO/2017/040607A1 |
An abuse deterrent pharmaceutical composition including an acid soluble salt of a pharmaceutically active ingredient and a buffering ingredient; wherein the acid soluble salt of the pharmaceutically active ingredient and the buffering in...
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WO/2017/017436A1 |
There is provided a novel process for the preparation of a compound of formula (I), wherein R1 is as described in the description, by demethylation of a corresponding O-methyl derivative.
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WO/2016/187522A1 |
The present invention is directed to a process for the preparation oxymorphone freebase, comprising hydrogenation of 14-hydroxymorphinone in DMF, to yield oxymorphone freebase, preferably oxymorphone freebase of improved appearance, puri...
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WO/2016/181218A1 |
The present invention provides an abuse deterrent oral fixed-dose composition, comprising a stimulant or opioid and an abuse deterrent active, wherein the abuse deterrent active is configured to be bioavailable only when the composition ...
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WO/2016/169662A1 |
Crystalline salts of 4,5 α-epoxy-3-methoxy-17-methylmorphinan-6- one tartrate (1:1) (hydrocodone bitartrate) are disclosed and three polymorphic forms of these salts are reported. The invention further relates to a pharmaceutical compos...
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WO/2016/169663A1 |
Crystalline salts of 7,8-Didehydro-4,5 alpha-epoxy-17-methylmorphinan-3,6 alpha-diol sulfate(2:1), i.e. of morphine sulphate, are disclosed and four polymorphic forms of these salts are reported. The invention further relates to a pharma...
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WO/2016/167318A1 |
Provided are: a memory-improving agent and memory-improving composition containing as an active ingredient a compound that is an inverse agonist of opioid δ receptors, a pharmacologically acceptable salt thereof, or a solvate of these; ...
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WO/2016/152953A1 |
The objective of the present invention is to provide an analgesic drug that is a peripherally selective opioid κ-receptor agonist and reduces side effects based on opioid μ-receptor agonists such as drug dependency and respiratory depr...
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