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WO/2024/074963A1 |
Methods and compositions of using transdermal delivery to facilitate delivery of a therapeutically effective amount of Naltrexone Hydrochloride, Naltrexol Hydrochloride, and/or Naltrexone Diol Ester for, for example, treatment of, for ex...
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WO/2024/054953A1 |
The invention provides heterobifunctional compounds, pharmaceutical compositions, and their use in treating disease, such as cancer.
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WO/2024/036337A2 |
Disclosed herein is deuterated buprenorphine as a protective agent for fetal subjects against full-agonist opioid exposure. Use of deuterated buprenorphine prevents or reduces exposure of the fetus to opioids used by the mother. Use of d...
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WO/2024/006977A1 |
This invention reports rational design, synthesis, and characterization of a series of a delta opioid receptor (DOR)-selective bitopic ligands targeting a conserved sodium site in DOR. The design is based on modifications in a selective ...
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WO/2023/248161A1 |
Solid state forms of Dibuprenorphine-ethyl-ether and Dibuprenorphine-ethyl-ether 2HCl are provided, as well as processes for the preparation thereof, and pharmaceutical compositions thereof.
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WO/2023/197934A1 |
The present invention relates to the technical field of pharmaceutical crystals, and relates to a solid salt form of an opioid receptor antagonist conjugate, a crystal form, a preparation method therefor, a composition, and a use. Specif...
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WO/2023/190665A1 |
The present invention provides a therapeutic agent, an ameliorative agent, or a preventative agent that have kappa opioid receptor agonist activity and reduced side-effects and are for treating for various diseases relating to kappa opio...
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WO/2023/183795A1 |
The present disclosure provides opioid antagonist compounds and prodrugs. Also provided herein are compositions and formulations comprising opioid antagonist compounds and prodrugs, as well as methods of using said compounds, composition...
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WO/2023/168502A1 |
The present invention relates to a novel anhydrous crystalline form, called the anhydrous crystalline T form, of the Active Pharmaceutical Ingredient (API) naloxone hydrochloride and to a process for producing same.
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WO/2023/164889A1 |
Disclosed are a method for preparing codeine and a derivative and intermediate thereof. Simple, cheap and easily-available commercially available compounds are used as starting materials in the present invention, various intermediates th...
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WO/2023/156493A1 |
This disclosure provides crystalline forms of naltrexone, and methods of making and using these forms.
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WO/2023/136785A1 |
The invention relates to a standardized extraction method for obtaining noscapine from opium capsules.
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WO/2023/130158A1 |
The present invention provides a liquid-liquid extraction process for the extraction of alkaloids from a source, using an alkyl phosphine oxide of Formula A (as described herein) as an extractant in combination with a diluent selected fr...
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WO/2023/129114A1 |
The invention relates to obtaining thebaine from thebaine-rich poppy capsule by using the method of alcohol extraction.
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WO/2023/079362A1 |
Provided herein are compounds having the formula D1-L-D2, wherein D1 is a processable group, L is a linker, and D2 is a drug. Also described herein are pharmaceutical compositions comprising said compounds and methods for the treatment o...
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WO/2023/023038A1 |
The present application provides pharmaceutical compositions and methods for treating diseases or disorders. The pharmaceutical composition comprises N-methyl-Daspartate receptor modulator and μ-opioid receptor modulator. The present ap...
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WO/2022/212471A1 |
Bivalent ligands which bind to MOR-CCR5 heterodimers are provided. The bivalent ligands comprise two discrete pharmacophores, naltrexone and maraviroc, linked by a spacer and bind to MOR-CCR5 heterodimers, e.g. at the surface of a cell. ...
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WO/2022/212868A1 |
Naloxone variants that are both long lasting and responsive are disclosed. One version of the compound has a boron ester functional group and the antagonist compound is capable of a sustained release of antagonist based on reaction with ...
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WO/2022/194022A1 |
A method for preparing nalbuphine sebacate and an intermediate thereof. By means of using the method, nalbuphine sebacate can be prepared efficiently, conveniently and safely, and the purity and yield of a nalbuphine sebacate final produ...
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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.
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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...
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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...
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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 ...
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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...
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WO/2022/101408A1 |
Hydromorphone hydrochloride (I·HCl) is converted into hydromorphone base (I) via hydromorphone monohydrate (I·H2O).
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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...
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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).
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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...
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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 ...
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WO/2021/144362A1 |
Disclosed are methods for preparing buprenorphine from, for example, compounds such as nororipavine and northebaine.
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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...
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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;...
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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...
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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...
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WO/2020/213911A1 |
The present invention provides a method for economically preparing high-purity naldemedine with high yield.
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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.
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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.
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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 ...
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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...
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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, ...
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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 ...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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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