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WO/2006/039763A1 |
Novel vitamin D analogues are useful for making pharmaceutical compositions for the prevention or treatment of bone disorders such as osteoporosis
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WO/2006/039685A2 |
A method used for synthesizing intermediates for use in the synthesis of carotenoids and carotenoid analogs, and/or carotenoid derivatives. In some embodiments, the invention includes methods for synthesizing optically active intermediat...
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WO/2006/036813A2 |
The invention provides vitamin D3 analogs of cholecalciferol, substituted at carbon-20 with cycloalkyl, e.g., cyclopropyl, wherein carbon-16 is a double bond, and carbon-23 is a single, double, or triple bond. Various alkyl or haloalkyl ...
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WO/2006/024296A1 |
The present invention relates to processes for epimerising alcohols of compounds having a hydroxyl substituent on an asymmetric allylic carbon, such as compounds useful for the synthesis of vitamin D analogues where the epimeric hydroxyl...
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WO/2006/025939A1 |
Provided are novel crystalline forms of 1,24-(S)-dihydroxy vitamin D2, including hydrates and solvates, and methods for making them. Also provided are pharmaceutical and nutraceutical compositions containing the novel crystalline forms.
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WO/2006/019169A1 |
A compound effective in the treatment of secondary hyperparathyroidism. It is a vitamin D3 derivative represented by the following formula: [wherein R1 represents hydrogen or C1-4 alkyl; and R2 represents any of the following groups: (wh...
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WO/2005/110979A2 |
Preparation of sulphonyl derivatives of cholecalciferol of Formula (I), wherein R1 is protective group, preferably t-butyl(dimethyl)silyl, where R2 is heterocyclic group, such as 2-thiazolyl, 2-benzothiazolyl, 1-phenyl-lH-tetrazo-5-yl, 2...
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WO/2005/102995A1 |
2-alkylidene-18,19-dinor-vitamin D compounds are disclosed as well as pharmaceutical uses for these compounds and methods of synthesizing these compounds. These compounds are characterized by low bone calcium mobilization activity and hi...
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WO/2005/095336A2 |
The present invention relates to novel methods for the preparation of intermediates which are useful in the synthesis of cacipotriol. The present invention relates further to the use of intermediates produced with said methods for making...
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WO/2005/087719A1 |
The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.
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WO/2005/082375A2 |
There is provided according to the invention a vitamin D compound for use in the prevention and/or treatment of interstitial cystitis. Also provided is a method for preventing and/or treating interstitial cystitis by administering an eff...
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WO/2005/079464A2 |
Various compounds such as those having the formula (I) and (XIV) where the variables have the values described herein antagonize the vitamin D receptor and are useful in treating conditions such as asthma and in preparing medicaments for...
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WO/2005/074389A2 |
The invention aims at providing a process for synthesizing vitamin D compounds by easy operation at a low cost. The invention provides a process for the production of vitamin D compounds and intermediates for the synthesis thereof, which...
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WO/2005/067673A2 |
Provided herein are enzymatic methods of producing steroid compounds S such as 7-dehydropregnenolone, hydroxy derivatives thereof and vitamin D2- and D3- like compounds and derivatives thereof. Also provided are the derivatives of the ...
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WO/2005/061520A1 |
The invention relates to novel disubstituted phenyl-boronic acid derivatives, methods for the production and use thereof as intermediates in the synthesis of non-steroid derivatives of vitamin D.
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WO/2005/058918A1 |
The invention relates to novel distributed phenyl-boronic acid derivatives of formula (I), to methods for the production and use thereof in the form of synthesis intermediates.
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WO/2005/051903A1 |
The invention relates to novel vitamin D-derived compounds containing a monohalovinyl residue at position C-20. The invention also relates to a method of obtaining said novel compounds, consisting in reacting an aldehyde precursor with a...
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WO/2005/030222A1 |
The invention provides (1,3)di-acylated vitamin D3 analogs of cholecalciferol, substituted at carbon (20) with methyl or cyclopropyl wherein carbon (16) is a single or double bond, and carbon (23) is a single, double, or triple bond. Var...
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WO/2005/030223A1 |
There is provided according to the invention the use of Vitamin D compounds such as 1-alpha-fluoro-25-hydroxy-16,23e-diene-26,27-bishomo-20-epi-
cholecalciferol in the prevention or treatment of bladder dysfunction.
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WO/2005/018658A1 |
2-Methylene-19-nor-24(S) and 24(R) derivatives of 1a,25-dihydroxyvitamin D2 are disclosed. These compounds are characterized by minimal bone calcium mobilization activity and relatively high intestinal calcium transport activity. This re...
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WO/2005/018648A1 |
The compound (20S)-1 &agr -hydroxy-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor are described herein. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing thei...
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WO/2005/011706A1 |
This invention provided a novel vitamin D analog, namely, 2-methylene-19-nor-20(S)-25-methyl-1&agr -hydroxycalciferol. The compound has the formula (I). This 2-substituted compound is characterized by relatively high intestinal calcium t...
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WO/2004/110380A2 |
The present invention relates to a method for treating, ameliorating, or preventing immune-mediated disorders in an animal by administering to the animal active vitamin D compounds. The invention further relates to a method for treating,...
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WO/2004/098507A2 |
The invention provides 1,3 acylated, 24-keto vitamin D3 compounds of formula I: wherein: X1and X1 are each independently H2 or =CH2, provided X1 and X1 are not both =CH2; R1 and R2 are each independently, hydroxyl, OC(O)C1-C4 alkyl, OC(O...
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WO/2004/082631A2 |
A method of inhibiting the hyperproliferation of malignant or neoplastic cells, comprising treating the cells with an antiproliferative amount of l&agr ,24(S)-dihydroxyvitamin D2. The method also includes the co-administration of cyotoxi...
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WO/2004/080467A2 |
This invention relates to a method for treating or preventing hyperthyroidism associated with chronic kidney disease by administering a sufficient amount of a vitamin D2 or vitamin D4 compound, the chronic kidney disease being stages 1-4.
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WO/2004/080922A2 |
The present invention relates to analogues of vitamin D namely 14-epi-2-alkyl-19-nor vitamin D derivatives. Also a general method for the synthesis and the biological activities are described. The general formula is: (I) where R (&agr or...
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WO/2004/067504A1 |
A novel vitamin D derivative. It is a compound represented by the general formula (1); wherein R1 represents optionally hydroxylated, linear or branched C3-8 alkyl or optionally hydroxylated, linear or branched C3-8 alkenyl; and R2 repre...
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WO/2004/054968A2 |
The present invention provides novel D-ring and side-chain analogs of l&agr ,25-dihydroxyvitamin D3, compositions comprising these compounds and methods of using these compounds as selective inhibitors of CYP24. In particular, the compou...
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WO/2004/046097A1 |
Provided is a crystallization method for reducing the level of impurities in calcipotriene in which a solution of a starting calcipotriene in a first process solvent, for example THF, is combined with second process solvent, for example ...
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WO/2004/037781A1 |
Compounds according to formula I: in which formula R1 and R2, which may be the same or different, represent halogen, (C1-C6) hydrocarbyl, optionally substituted with one or two hydroxyl group on one or more fluorine atoms, or, together w...
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WO/2004/033420A1 |
A novel 2,2-di-substituted 19-norvitamin D derivative. It is a compound represented by the general formula (I): (I) wherein R1 and R2 are the same or different and each represents hydroxy, etc. and A represents hydrogen, unsubstituted li...
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WO/2004/002996A1 |
A novel ferrocene compound; a reagent containing the compound; and a high-sensitivity method of determining a vitamine D compound with the reagent. Specifically, a ferrocene compound represented by the following formula (1): (1) is react...
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WO/2003/106411A1 |
The present invention provides novel sulfoximine compounds, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseas...
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WO/2003/106412A1 |
Provided is a method of general applicability of epimerizing a vitamin-D analog having an asymmetric allylic carbon atom at the C-24 position, which comprises the steps of: a) esterifying the hydroxyl group on the asymmetric allylic carb...
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WO/2003/106629A2 |
The present invention relates to therapeutics for the prevention and treatment of vitamin D responsive diseases in humans, as well as other animals, through the use of biologically active vitamin D compounds in combination with at least ...
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WO/2003/088976A1 |
This invention relates to a method for treating or preventing hyperthyroidism associated with aging and/or with Aging-Related Vitamin D Deficiency (ARVDD) syndrome by administering a sufficient amount of an active vitamin D compound util...
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WO/2003/087048A2 |
Disclosed is a process for the preparation of 24-alkyl analogs of cholecalcyferol of Formula (1) having a (5E) or (5Z) configuration, wherein X represents a hydrogen atom, a hydroxy group or an OR1 group, wherein R1, R2 and R3 may be the...
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WO/2003/084925A1 |
A method of making 1&agr -hydroxy-2-methylene-19-norhomopregnacalciferol. The method includes the steps of condensing a bicyclic ketone with an allylic phosphine oxide to produce a protected 19-norpregnacalciferol analog, thereafter clea...
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WO/2003/075932A1 |
This invention discloses 1&agr -a-hydroxy-2-methylene-19-nor-pregnacalciferol and pharamaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their diffe...
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WO/2003/074480A1 |
A halovinylidenemethylenecyclohexane compound represented by the following formula (1); a borovinylidenemethylenecyclohexane compound represented by the formula (2); and a process for producing a vitamine D derivative from these compound...
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WO/2003/070697A1 |
A binding activity can be detected by measuring a change in the degree of fluorescence polarization of a fluorescent-labeled low-molecular weight compound showing a difference between the degree of fluorescence polarization at binding to...
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WO2003018545B1 |
The present invention provides novel C24-aryl sulfone analogs of 1 alpha ,25-dihydroxy vitamin D3 of formula (I) : wherein R<1>-R<7> have the meanings given in the description, x is 0-2; and represents a single or a double bond, composit...
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WO/2003/055854A1 |
The invention aims at synthesizing novel vitamin D derivatives and provides vitamin D derivatives represented by the general formula (1): (1) wherein R1 and R2 may be the same or different and are each linear or branched alkyl which may ...
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WO/2003/051828A2 |
This invention discloses (20S)-1$g(a)-hydroxy-2-methylene-19-nor-bishomopregnacalcife
rol, pharmaceutical uses therefor, and a method of purifying this compound to obtain it in crystalline form. This compound exhibits pronounced activity...
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WO/2003/042171A1 |
The invention relates to novel vitamin D derivatives of general formula (I), to a method for the production thereof and to the use thereof in the production of medicaments.
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WO/2003/035612A1 |
The present invention relates to stable cholecalciferol derivatives represented by the following formula (1) and a preparing method thereof, which has a moisturizing effect. The compounds of the formula (1) are novel cholecalciferol deri...
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WO/2003/031455A1 |
Optically active dihydroxycyclohexane compounds represented by the following general formulae (1) and (2) or the enantiomers of these. (In the formulae, R represents halogeno, substituted silyl, or a substituted boron or substituted tin ...
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WO/2003/031402A1 |
A process for preparation of 19−norvitamin D derivatives represented by the general formula (3): (3) [wherein W is hydrogen, halogeno, or the like&semi Z is C1−26 alkyl or the like&semi and X1 and X2 are each independently hydrogen, ...
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WO/2003/031400A1 |
The present invention provides novel 16-ene-C25-oxime and 16-ene-C-25-oxime ether analogs of 1$g(a),25-dihydroxy vitamin D¿3?, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In parti...
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