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WO/2018/026837A1 |
Compositions comprising oxygenated cholesterol sulfates (OCS) are provided. The OCS is, for example, 5-cholesten-3, 25-diol, 3-sulfate (25HC3S) or 5-cholesten, 3, 25-diol, disulfate (25HCDS). The compositions may be used to prevent and/o...
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WO/2018/013613A1 |
Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a comp...
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WO/2018/010651A1 |
The present invention relates to a method for manufacturing an obeticholic acid and an intermediate thereof. The invention specifically relates to a method for manufacturing a compound represented by formula V. The method comprises: usin...
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WO/2018/009867A1 |
Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, and R6, R11a, and R11b are as defined herein. Compounds of the present invention...
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WO/2018/002897A1 |
The present invention concerns compounds having formula (I) and compositions thereof with a pharmacologically acceptable excipient and uses thereof as a medicament, in particular for the treatment and/or prevention of a disorder selected...
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WO/2017/211820A1 |
The present invention relates to new and improved processes for the preparation of deoxycholic acid (DCA) and pharmaceutically acceptable salts thereof, as well as to novel intermediates useful for the preparation of DCA and pharmaceutic...
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WO/2017/207648A1 |
The invention relates to a process for the preparation of obeticholic acid and derivatives thereof comprising: (a) olefination of a compound of formula (II) or a salt or solvate thereof to obtain a compound of formula (III) or a salt or ...
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WO/2017/208165A1 |
The invention of the present application relates to the process for the preparation of intermediates of obeticholic acid and their conversion to obeticholic acid. The process involves the conversion of compound of formula (VI) to compoun...
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WO/2017/199036A1 |
The invention relates to a process for preparing a compound of general formula (la): wherein R2, Y, R4and R5are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The ...
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WO/2017/199033A1 |
The invention relates to compounds of general formula (I): wherein: R1,R2, R3, R4, R5, R6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditio...
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WO/2017/199039A1 |
The invention relates to a process for preparing a compound of general formula (Ia): wherein R2, Y, R4 and R5 are as defined herein. The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis...
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WO/2017/190420A1 |
A mogrol derivative monomer (4) having broad spectrum antitumor efficacy; the monomer is superior in terms of both activity and efficacy than structurally similar and commercially available antitumor medicament/healthcare product Rg3, al...
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WO/2017/190421A1 |
Provided in the present invention is a novel mogrol derivative monomer (4), which can be prepared into a medicament for use in treating and/or preventing different cancers and/or tumors, can also be prepared into a healthcare product for...
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WO/2017/190422A1 |
A synthesis method for a composition comprising a mogrol derivative monomer (3) and a mogrol derivative monomer (4), compared with an existing method for synthesizing the mogrol derivative monomer (3), the present synthesis method is sim...
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WO/2017/189561A1 |
The present disclosure provides compositions comprising 25-hydroxycholesterol, derivatives and prodrugs thereof, and methods of use thereof. Specifically, disclosed herein are methods of decreasing neuronal cell death.
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WO/2017/187343A2 |
An oxysterol or oxysterol-like compound is provided, which finds use in treating and/or targeting cancer.
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WO/2017/186135A1 |
Disclosed in the present invention are a compound and an application thereof for the treatment of cataracts. The structural formula of the compound is shown in formula I. The compound shown in formula I, a prodrug thereof, or a pharmaceu...
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WO/2017/177326A1 |
The invention provides conjugates that comprise a targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates. The conjugates are useful to ta...
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WO/2017/177945A1 |
Uses of a poria cocos extract, a tumulosic acid and/or a pharmaceutically acceptable salt of the tumulosic acid in the preparation of a drug or food, and the drug or the food is used for protecting muscles. The drug is especially used fo...
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WO/2017/174515A1 |
The invention relates to a process for preparing a compound of formula (I) in particular obeticholic acid and intermediates suitable for its synthesis.
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WO/2017/172615A1 |
Compositions and methods for preparing an OXY133 polymorph are provided. This compositions and methods include subjecting a slurry of OXY133 to conditions sufficient to convert OXY133 to the OXY133 polymorph Form A, polymorph Form B, pol...
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WO/2017/167233A1 |
The present invention relates to a new crystalline form of obeticholic acid and a preparation method therefor. In particular, the present invention relates to an E-type crystal of obeticholic acid and a preparation method therefor. The c...
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WO/2017/156024A1 |
The present application provides Compound 1 : or a pharmaceutically acceptable salt or amino acid conjugate thereof. The present invention relates to an FXR activator and to methods of making and using said compound.
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WO/2017/152677A1 |
The present invention relates to a cholanic acid compound for preventing or treating FXR-mediated diseases. Specifically, disclosed are a cholanic acid compound represented by formula (I) and a pharmaceutical composition containing the c...
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WO/2017/150723A1 |
Algae that generates a sterol and a sterol production method that uses the algae. According to the present invention, a sterol is produced by culturing algae, such as strain AJ7867 (FERM BP-22304) and strains derived therefrom, that has ...
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WO/2017/147174A1 |
The present invention provides compounds of Formula (I), pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
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WO/2017/142028A1 |
A metal-supported macromolecule and a use thereof as a catalyst, said metal-supported macromolecule being obtained by causing a ligand to react with a zinc compound or a cobalt compound, said ligand having an imidazole group that is bond...
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WO/2017/137931A1 |
The present application relates to amine salt of obeticholic acid. Specifically, the present application relates to (S)-α-methylbenzylamine and diethylamine salt of obeticholic acid. The present application also relates to a process for...
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WO/2017/137958A1 |
The present disclosure relates generally to Cellular Signalling inhibitors of compound of Formula (I), compositions and formulations comprising the same, methods, processes, and uses thereof. In particular, the present disclosure provide...
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WO/2017/136549A1 |
Described herein are compounds that inhibit or prevent protein aggregation, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of ...
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WO/2017/134087A1 |
Steroidic calixarene compounds according to formula (I): (I) wherein: ∙ R represents -(CH2)x-L-(CH2)y-Ster, wherein : ○ x and y are integers comprised between 0 and 2; ○ n is an integer comprised between 1 and 5; ○ L represents a...
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WO/2017/129125A1 |
The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases.
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WO/2017/131144A1 |
The objective of the present invention is to provide: a novel lithocholic acid derivative having vitamin D activity; and a pharmaceutical product, a vitamin D receptor activator and a prophylactic and/or therapeutic agent for vitamin D r...
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WO/2017/130127A1 |
The present invention relates to extraction of phytosterolsfrom alkaline tall oil soap which is obtained from the Kraft process black liquor by skimming.In the method according to the present invention, phytosterols are extracted using d...
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WO/2017/117903A1 |
A method for preparing 20(S)-protopanaxadiol, comprising: adding an extract containing panaxadiol saponins to an alkaline solution under the protection of an inert gas; and performing hydrolysis at high temperature to obtain 20(S)-protop...
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WO/2017/115324A1 |
The invention relates to solid forms of Obeticholic Acid and hydrates or solvates thereof and processes for preparation of the same.
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WO/2017/111979A1 |
The present application relates to crystalline forms A, D, F, G and I of obeticholic acid. These crystalline forms are useful in the production of Obeticholic acid (in particular its purification), which is a drug useful for the treatmen...
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WO/2017/100153A1 |
The invention provides compounds of formula (I): and salts thereof, wherein R1, R2, R3, B, X, Y, and Z have any of the values defined herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I) or...
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WO/2017/093192A1 |
The present invention relates to a method of purification of compound of formula (I) which comprises the step of crystallization of compound of formula (I) from a composition comprising the compound of formula (I) and the compound of for...
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WO/2017/092702A1 |
Provided are a crystal form II of obeticholic acid, preparation method and usage thereof. In an X-ray powder diffraction pattern, the crystal form II of obeticholic acid has characteristic peaks at 2θ values of 4.9° ± 0.2°, 5.3 ± 0....
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WO/2017/092703A1 |
Provided is a method for preparing amorphous obeticholic acid. The method comprises: (1) contacting an obeticholic acid raw material with an alkaline solution in order to obtain a first mixture containing obeticholic acid; (2) formulatin...
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WO/2017/079062A1 |
The present application relates to a method of preparing a bile acid derivative, or a pharmaceutical acceptable salt, solvate, or amino acid conjugate thereof, comprising direct alkylation at the C-6 position of KLCA.
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WO/2017/075257A2 |
Disclosed herein are compounds having structural Formula (I), or salts thereof. These compounds are useful as sweet tasting agents and/or sweetness enhancers. Also disclosed are compositions comprising the present compounds and methods o...
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WO/2017/062763A1 |
The present application provides a compound of formula I: or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, as described herein. The present invention relates generally to FXR modulators and to methods of m...
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WO/2017/053826A1 |
The present invention relates to methods and novel intermediates useful in the preparation of a compound or a pharmaceutically acceptable salt thereof. An objective of the present invention is to provide methods of preparing bile acid de...
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WO/2017/049307A1 |
Disclosed herein are compounds comprising dicarba-closo-dodecaborane. The compounds can be, for example, estrogen receptor beta (ERβ) agonists. In some examples, the compounds can be selective ERβ agonists. Also provided herein are met...
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WO/2017/035501A1 |
Disclosed herein are novel sialyltransferase inhibitors, and compositions and methods for treating diseases and/or conditions associated with the activation of sialyltransferase, such as a cancer, an immune disease or an inflammatory dis...
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WO/2017/027396A1 |
The present application relates to a method of preparing compounds of Formula (A) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof.
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WO/2017/019524A1 |
The present application relates to a method of preparing compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, R1 is H, α-OH, β-ΟΗ, or an oxo group.
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WO/2017/008773A1 |
Obeticholic acid is a semi-synthetic bile acid analogue with an agonist effect upon the farnesoid X receptor (FXR). It is designed for the treatment of liver diseases, e.g. primary biliary cirrhosis (PBC), non-alcoholic steatohepatitis (...
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