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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/2016/191872A1 |
Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also...
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WO/2016/173397A1 |
The present invention relates to a cholic acid derivative, and a preparation method and a medical use thereof. In particular, the present invention relates to a cholic acid derivative with the structure of formula (I), a stereoisomer, or...
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WO/2016/173524A1 |
Disclosed in the present application are the compounds as shown in formulae I, II, III, IV or V, tautomers thereof, stereoisomers thereof or pharmaceutically acceptable salts thereof, and also disclosed is the use thereof in preparing dr...
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WO/2016/120894A1 |
The present invention relates to crystalline forms of S-[4-(3-fluoro-3-methylbutyryloxy)but-2- ynyl] 6α,9α-difluoro- 17α-(furan-2-yl)carbonyloxy- 11β-hydroxy- 16α-methyl-3-oxoandrosta- 1,4- diene-17β-carbofhioate, an anti-inflammat...
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WO/2016/081029A1 |
What are described are compounds of formulas Π, HI, IV, and V. The compound of formula II consists of a compound in which R1 and R2 are both a linear alkyl consisting of 1 to 12 carbons, an alkenyl or alkynyl consisting of 2 to 12 carbo...
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WO/2016/054280A1 |
A method of preparing a thioic acid intermediate of fluticasone propionate includes: treating a 17β-[(N,N-dimethyl carbamoyl)thio]carbonyl compound in a solution including an alcohol and an alkali metal hydroxide, an alkaline-earth meta...
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WO/2016/037956A1 |
The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or...
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WO/2016/029888A1 |
The present invention provides amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use as medicaments for treating neuropsychiatric disorders associated with an ...
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WO/2016/023082A1 |
H:\dar\Interwoven\NRPortbl\DCC\DAR\8230712_1.doc-12/08/2015 Abstract 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 lymp...
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WO/2016/012982A1 |
The present invention relates to a pharmaceutical combination comprising a PI3K/m TOR inhibitor of Formula (I) (as described herein) or a pharmaceutically acceptable salt or a solvate thereof; and one or more anti-cancer agent selected f...
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WO/2015/188791A1 |
Disclosed is a method for preparing a Zytiga intermediate. The intermediate is trifluoromethanesulfonate of dehydroepiandrosterone acetate and has a chemical structure represented by formula (II). In the method, dehydroepiandrosterone ac...
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WO/2015/181116A1 |
A process for preparing compounds of formula (I), or a salt, solvate or stereoisomer thereof, including Fulvestrant, which process comprises free radical to a compound of formula (III), or a salt, solvate or stereoisomer thereof. The inv...
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WO/2015/181275A1 |
13073PTWO 56 ABSTRACT The present invention relates to compounds having cholane scaffolds of formula (I), said compounds for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases. 5
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WO/2015/177469A1 |
The present invention relates to chemical compounds and the therapeutic use thereof, in particular for improving muscular quality in mammals. More particularly, the invention enables improvement of muscular quality in sarcopenic mammals ...
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WO/2015/170341A1 |
The invention discloses an improved cost-effective process for preparation of 7-Dehydrocholesterol of formula I with good yield and purity, comprising:a) epimerizing 7(alpha+beta) bromo protected cholesterol in presence of tetrabutyl amm...
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WO/2015/118474A1 |
The present disclosure relates to an improved process for the purification of fluticasone propionate by: a) dissolving fluticasone propionate in a ketone solvent to produce a mixture, b) heating the mixture slowly for 1-2 hours to get a ...
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WO/2015/114518A2 |
Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for im...
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WO/2015/074085A1 |
What is described is a compound of formula (I), wherein R1 and R2 are the same or different, each a linear or branched alkyl with 1-9 carbons, or an alkenyl or alkynyl with 2 to 11 carbon atoms; L1 and L2 are the same or different, each ...
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WO/2015/014686A1 |
The present invention relates to a novel process for the synthesis of abiraterone and in particular abiraterone acetate, a compound of formula (I) reported below: having pharmacological activity suitable for slowing down the progression ...
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WO/2015/015246A1 |
The present invention relates to a novel process for the synthesis of abiraterone, and in particular of abiraterone acetate, compound of formula (I) reported below: N O (I) which has pharmacological activity useful tor slowing down the p...
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WO/2014/192027A1 |
The present invention relates to methods of treatment of inflammatory conditions using S -[4-(3-fluoro-3-methylbutyryloxy)-but-2-ynyl]6α,9α-difluor
o-17α-(furan-2-yl)carbonyloxy-11β-hydroxy-16α-methyl-3-ox
oandrosta-1,4-diene-17β-c...
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WO/2014/184271A1 |
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1 is a hydroxy group and R2, R3, R4, R5, and R6 are as described herein. The present inven...
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WO/2014/104400A1 |
Provided is an actinic-ray- or radiation-sensitive resin composition including a resin (A) and any of compounds (B) of general formula (I) below. (In general formula (I), Rf represents a fluorine atom or a monovalent organic group contai...
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WO/2014/079801A1 |
The invention relates to a method for increasing the particle size of crystalline active micro-particles comprising the following steps: (a) a first suspension consisting of crystalline active micro-particles with a first d50value of 0.5...
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WO/2014/075978A1 |
The present invention relates to a process for making abiraterone-3-acetate of formula (1) starting from dehydroepiandrosterone-3-acetate of formula (2) by converting it into the triflate of formula (5) in an inert solvent in the presenc...
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WO/2014/071984A1 |
The present invention relates to an improved process for making abiraterone-3-acetate of formula (1) starting from dehydroepiandrosterone-3-acetate (DHEA) of formula (2). In particular, it relates to an improved process of converting the...
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WO/2013/169647A1 |
The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods f...
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WO/2013/154752A1 |
5-cholesten, 3β, 25-diol, disulfate (25HCDS) has been found to be an authentic PPARϒ agonist and LXR antagonist, and is used for the therapy of lipid disorders and inflammatory diseases, including without limitation fatty liver, inflam...
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WO/2013/056181A1 |
Provided herein are 3,3-disubstituted 19-nor- steroidal compounds according to Formula (I) and (III): where R1,R2, R3, R3', R4, R6a, R6a, R11a, and R11b are as defined herein. Compounds of the present invention are contemplated useful fo...
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WO/2013/036835A1 |
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L1, L2, L3, X1, X2, Y, Rz4, Rz5, Rz6, n, R1, R2, R3a, R3b, R4a...
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WO/2012/160338A1 |
The present invention relates to a method of preparing an organic biologically active compound of formula (I), wherein R1, R2, R3, R4,. X1, X2 and X3 are as defined in the specification, to certain novel intermediates obtainable from suc...
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WO/2012/079275A1 |
Provided is a method for preparing fluticasone furoate (fluoromethyl 6α,9α-difluoro-11β-hydroxy-16a-methyl-17α-[(2-furoyl)oxy
]-3-one androsta-1,4-diene-17β-thiocarboxylate) represented by Formula I. The method comprises: 1) forming...
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WO/2012/056201A2 |
The invention provides a compound of formula A, B, C or D, methods for making them, intermediates therefor, and their use in making organic biologically active compounds: (Formula (A)). Wherein: • X = F, CI, Br, I, sulfonate esters, ph...
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WO/2011/151625A1 |
The present invention describes processes for the preparation of, monofluoromethylated organic biologically active compounds, such as Fluticasone Propionate and Fluticasone Furoate, in the presence of fluorodecarboxylating reagents such ...
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WO/2011/151624A1 |
The present invention describes a process for the preparation of monofluoromethylated organic biologically active compounds using monofluoromethylated reagents. Fluticasone Propionate and Fluticasone Furoate can be prepared using, for ex...
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WO/2011/009531A2 |
The invention relates to 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl derivatives of formula (I) exhibiting progesterone-antagonistic effects and to methods for the production thereof, to the use thereof for the treatment and...
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WO/2010/136940A1 |
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to th...
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WO/2010/108107A1 |
The present invention provides crystalline forms of Fluticasone furoate, characterized by the data disclosed in the specification; pharmaceutical compositions comprising any one or combination of the crystalline forms of Fluticasone furo...
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WO/2010/059853A1 |
The invention relates to compounds of Formula A: (A) or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory ...
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WO/2010/052896A1 |
Fluticasone propionate microparticles useful as active ingredients for a preparation for local administration which enables the long-term retention of microparticles of an active ingredient in a mucosa for a long period to achieve a high...
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WO/2010/043404A1 |
The invention relates to a compound of formula (1) wherein R1 represents hydrogen or an acetyl group and R2 represents a methyl, acetyl, or benzyl group, to its preparation, and to its use in the preparation of fulvestrant.
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WO/2010/016931A2 |
Provided are polymorphs of fluticasone furoate and processes for preparation thereof.
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WO/2010/014836A2 |
The invention relates to compounds of Formula A: (A) or a salt, solvate, or hydrate thereof. The compounds of formula A are TGR5 modulators useful for the treatment of disease.
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WO/2009/085880A2 |
The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the gener...
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WO/2009/059765A2 |
The present invention describes a process for the preparation of drospirenone (I) using androstendione as a starting material. In particular, androstendione protected on carbonyl group in position 3 as an enol-ether is functionalized in ...
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WO/2009/043577A2 |
The invention relates to compounds of general formula (I), methods for the production thereof, pharmaceutical or cosmetic compositions or forms of administration containing said compounds, and contraceptive methods by administering said ...
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WO/2009/039700A1 |
The present invention provides a novel multi-step process for the manufacturing Fulvestrant, which is economical and convenient to operate at commercial scale, and requires only simple chromatographic separations after the coupling step ...
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WO/2009/013310A2 |
A process is described for the industrial scale preparation of 7α-[9-(4,4,5,5,5- 5 pentafluorothiopentyI)nonyl]estra-1,3,5(10)-triene-3,17β-di
ol, a precursor of steroids with hormonal activity which include Fulvestrant.
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WO/2008/115069A2 |
The present invention relates to certain unsaturated fatty acid derivatives of therapeutically active glucocorticoidesfatty acid esters of glucocorticoids as anti-inflammatory and anti-cancer agents and pharmaceutical formulations contai...
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