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WO/1999/067211A1 |
The invention relates to a multifunctional vitamin D derivative of formula (I) wherein; O represents the oxygen atom of an ether group; X represents a spacer group having a length of 0.8 to 4.2 nm, for example, an amino carboxylic acid r...
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WO/1999/061417A2 |
The present invention provides a method for preparing a novel class of vitamin D compounds in which the C-25 or equivalent position has a double bond. In addition, the side chain is optionally extended by one or two methylene or methyne ...
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WO/1999/061398A2 |
The invention provides 24-hydroxyvitamin D compounds and their use in the treatment and prophylaxis of hyperparathyroidism and hyperproliferative diseases, and in the modulation of the immune and inflammatory responses as well as the tre...
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WO/1999/061418A2 |
The invention provides 1$g(a)-hydroxyvitamin D compounds in which the C-25 or equivalent position of the C-17 side chain has a double bond and their use in the treatment and prophylaxis of hyperparathyroidism and hyperproliferative disea...
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WO/1999/059966A1 |
A method of modifying or altering the structure of a 1$g(a)-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1$g(...
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WO/1999/052863A1 |
Vitamin D derivatives represented by general formula (I), intermediate compounds in the synthesis thereof, and medicinal compositions containing these vitamin D derivatives as the active ingredient wherein A represents linear or branched...
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WO/1999/043646A1 |
Compounds of formula (I) wherein X is C=CH¿2? or CH¿2?; Y and Z are independently of each other hydrogen, fluorine or hydroxy; A is -C$m(Z)C-, -CH=CH- or -CH¿2?-CH¿2?-; R?1¿ and R?2¿ are independently of each other alkyl or perfluo...
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WO/1999/043645A1 |
Vitamin D derivatives having general formula (1) which are hydroxylated at the 24-position and considered as one of metabolites of physiologically active vitamin D derivatives substituted at the 2$g(b)-position wherein R¿1?, R¿2?, R¿3...
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WO/1999/036400A1 |
A method of preparation of cholecalciferol derivatives, particularly 1$g(a),24-dihydroxycholecalciferol of formula (1), wherein substituents R¿1? and R¿2? are hydrogen, hydroxyl, or hydroxyl protecting group, R¿1? and R¿2? being the ...
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WO/1999/031112A1 |
The invention relates to novel vitamin D derivatives of general formula (I), a method for the production thereof, intermediate products of the method as well as the utilization thereof for producing medicaments.
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WO/1999/031055A1 |
The present invention relates to novel vitamin D derivatives of formula (I), wherein X is C=CH¿2? or CH¿2?; Y is hydrogen, fluorine or hydroxy; Z is hydroxy; n is 1 or 2; R?1¿ is lower alkyl; R?2¿ is a branched alkyl having 3 to 8 ca...
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WO/1999/018070A1 |
The present invention relates to compounds of formula (I), in which formula X is hydrogen or hydroxy or protected hydroxy; R?1¿ an R?2¿ stand for hydrogen, methyl or ethyl, or, when taken together with the carbon atom bearing the group...
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WO/1999/016745A1 |
The invention relates to novel vitamin D derivatives of general formula (I), a method for the production thereof, intermediate products of the method and the utilization of vitamin D derivatives for producing medicaments.
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WO/1999/015499A1 |
Novel 22-oxavitamin D derivatives having hydroxyl at each of the 1$g(a)- and 3$g(a)- positions and represented by general formula (I), wherein R¿1? represents linear or branched C¿4-10? alkyl having one to three hydroxyl groups; and RÂ...
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WO/1999/012894A1 |
This invention relates to 1,3-dihydroxy-20,20-dialkyl-vitamin D¿3? analogs of Formula (I), compositions comprising the analogs, methods of preparing the analogs and methods of treatment of osteoporosis, secondary hyperparathyroidism, ca...
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WO/1999/003828A1 |
Polyunsaturated 24a,24b-dihomo-9,10-secocholestane derivatives of formula (I) wherein A is a single or double bond, B?1¿ and B?2¿ are each independently CH=CH or C$m(0)C, T is CH¿2? or CH¿2?CH¿2?, X is -CH2- or > C=CH2, R?1¿ is H, ...
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WO/1999/003829A1 |
This invention provides a novel class of vitamin D compounds, namely, 13-ethyl and 13-vinyl-18,19-dinor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have formula (I): wherein Y¿1? and YÂ...
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WO/1998/058909A1 |
Vitamin D¿3? derivatives represented by general formula [1] and a process for producing the same: wherein R¿1? and R¿2? represent each hydrogen, trialkylsilyl, etc.; R¿3? and R¿4? represent each hydrogen, hydroxy, etc.; R¿5? to R¿...
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WO/1998/051664A1 |
Novel 3-epi vitamin D2 compounds having the orientation of the substituent attached to the carbon at position 3 of the A-ring of vitamin D2 inverted from a beta ($g(b)) to an alpha ($g(a)) configuration are described. These compounds wer...
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WO/1998/051678A1 |
Novel cyclic ether vitamin D3 compounds having a cyclic ether side chain are disclosed. These compounds were first identified as metabolites of 3-epi vitamin D3 produced via a tissue-specific metabolic pathway which catalyzes the formati...
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WO/1998/051663A2 |
Novel 3-epi vitamin D�3? compounds having the orientation of the substituent attached to the carbon at position 3 of the A-ring of vitamin D�3? inverted from a beta ($g(b)) to an alpha ($g(a)) configuration are described. These 3-epi...
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WO/1998/050353A1 |
1,25-Dihydroxy-2-methyl vitamin D�3? derivatives represented by general formula (I) wherein R�1? and R�2? each independently represents hydrogen or tri(C�1-7?alkyl)silyl; and the asymmetric carbon atoms at the 1-, 2- and 3-positi...
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WO/1998/049138A2 |
This invention provides Vitamin D�3? analogs of the Formula (I) wherein: X is H�2? or CH�2?; Y is hydrogen, hydroxy or fluorine; Z is hydroxy; R�1? and R�2? are a (C�1?-C�4?) alkyl or fluoroalkyl, or R�1? and R�2? toget...
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WO/1998/047866A2 |
24-Nor-secochola-5,7-diene derivatives of formula (I) wherein A is a single or double bond, B is a group CH�2?CH�2?, CH=CH or C$m(Z)C, T is a group CH�2? or CH�2?CH�2?, R?1� and R?3� are H or OH, C(R,R) is CH�2? or C=CHï¿...
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WO/1998/041500A1 |
This invention provides a novel class of vitamin D related compounds, namely, the 2-alkyl-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have formula (I), where Y�1? and Y�2?, wh...
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WO/1998/041501A1 |
The invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula (I) where Y�1? and Yï¿...
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WO/1998/039292A1 |
20-Epi-22(R)-lower alkyl-substituted vitamin D derivatives represented by general formula (I), wherein R?1�, R?2� and R?3� represent each hydrogen or a hydroxy-protective group; and R?4� represents lower (C�2-6?) alkyl.
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WO/1998/029123A1 |
The invention provides therapeutic methods for inhibiting, ameliorating or alleviating the hyperproliferative cellular activity of diseases of the prostate, e.g., prostatic cancer and prostatic hyperplasia, which includes administering t...
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WO/1998/028266A1 |
Vitamin D derivatives of general formula (1) wherein X represents oxygen or sulfur; R�11? represents saturated or unsaturated aliphatic hydrocarbyl which may be substituted by hydroxyl or protected hydroxyl, or -COR�12? (wherein R�...
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WO/1998/024762A1 |
A compound of formula (I) in which formula Q is a C�1?-C�6? hydrocarbylene diradical; Y is either a single bond, a carbonyl group or a methylene, ethylene, -CH(OH)-, -O-(C�6?H�4?)- (ortho, meta, para) or -S-(C�6?H�4?)- (ortho...
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WO/1998/021580A2 |
Compound comprising an analogue of 1,25-dihydroxy vitamin D, modified at the C?20� position, which is adapted to bind to at least an existing or readily produced antibody, wherein the analogue comprises a substituent adapted for quanti...
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WO/1998/018759A1 |
The present invention relates to compounds of formula (I) in which formula X is hydrogen or hydroxy; R?1� and R?2� which may be the same or different, stand for hydrogen or C�1?-C�5? hydrocarbyl; or R?1� and R?2�, taken toget...
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WO/1998/009935A1 |
A process for preparing a compound having structure (I) wherein n is an integer from 1-5; each of R�1? and R�2? independently is optionally substituted C�1?-C�6? alkyl; each of W and X is independently hydrogen or C�1?-C�6? a...
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WO/1998/008522A1 |
Multivitamin products targeted to specific groups.
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WO/1998/000397A1 |
A crystal of the compound of the structural formula (I); crystals of vitamin D derivatives prepared by purifying unpurified or roughly purified vitamin D derivatives by reversed phase chromatography and crystallizing the purified derivat...
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WO/1997/046522A1 |
The present invention relates to compounds of formula (I), in which formula X is hydrogen or hydroxy; R1 and R2, which may be the same or different, stand for hydrogen or a C1-C3 alkyl radical; or R1 and R2, taken together with the carbo...
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WO/1997/041096A1 |
The invention concerns new vitamin D derivatives of general formula (I) a process for their production, their use for production of medicaments, and intermediate products used in the process.
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WO/1997/037972A1 |
The present invention relates to compounds of formula (I) in which Q stands for a C1-C8 hydrocarbylene diradical, R stands for hydrogen or C1-C6 hydrocarbyl, or two R groups, taken together with the carbon atom bearing the hydroxy group ...
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WO/1997/024127A1 |
Biotin, fluorescent and chemiluminescent labeled vitamin D compounds are disclosed as well as their use in assays for the presence of vitamin D, its metabolites and vitamin D analogs in biological fluids.
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WO/1997/023453A1 |
1-Hydroxy pregnacalciferol derivatives of formula (I) and their corresponding 5,6-trans isomers wherein R1 is hydroxyl or lower alkoxy and R2 is optionally hydroxylated or lower alkoxylated lower alkynyl or R1 is C(RA) (RB)CH3 where RA i...
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WO/1997/020811A1 |
The present invention relates to compounds of formula (I) in which formula X is hydrogen or hydroxy; R1 and R2 stand for methyl or ethyl, or, when taken together with the carbon atom bearing the group X, can form a C3-C5 carbocyclic ring...
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WO/1997/019058A1 |
The invention relates to a compound of formula (I) wherein A is a carbon-carbon double bond having the E or Z stereochemical configuration, or A is a carbon-carbon triple bond, Et is ethyl, and R is hydroxy and R1 is hydrogen or =CH2, or...
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WO/1997/016423A1 |
The invention relates to a compound of formula (I) wherein A is a carbon double bond having the stereochemical configuration E or Z, i.e. of formula (a) or (b), respectively, R is hydroxy and R1 is hydrogen or =CH2 or R is hydrogen or fl...
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WO/1997/011053A1 |
A method of treating metabolic bone diseases such as osteoporosis, as well as other disease states treatable with vitamin D compounds, comprises administering an effective amount of one or more modified vitamin D compounds. The modified ...
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WO/1997/000242A1 |
The invention concerns novel vitamin D derivatives with C-25 substituents of general formula (I). The invention also concerns a process for their preparation and their use in preparing medicaments.
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WO/1996/040154A1 |
Novel 1'alpha'-hydroxy vitamin D4 and novel analogues, 1,25 dihydroxy vitamin D4 and 1,24 dihydroxy vitamin D4 which are useful as active compounds of pharmaceutical compositions for the treatment of disorders of calcium metabolism and v...
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WO/1996/040153A1 |
Novel 1'alpha'-hydroxy vitamin D4 and novel analogues, and preferably 1,24 dihydroxy vitamin D4, which are useful as active compounds of pharmaceutical compositions for the treatment of disorders of calcium metabolism and breast and colo...
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WO/1996/030338A1 |
Vitamine D3 analogues which include a hydroxyalkyl substituent in the 1-position and a modified D-ring side chain are described. These novel compounds are potent anti-proliferative substances with activity comparable to that of calcitrio...
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WO/1996/022776A1 |
Vitamin D derivatives of formula (I), wherein: X is =CH2 or H,H; Y is a moiety (a) -CH(CH3)-(A)n-C(O)-OR1, (b) -CH(CH3)-CH2-O-C(O)-R2 or (c) -C(O)-OR1; A is -CH=CH- or CH2-CH2-; R1 is lower alkyl, cycloalkyl, cycloalkylmethyl, -CH2R3 or ...
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WO/1996/022973A1 |
A compound represented by general formula (I), wherein R1 and R2 are the same or different and each represents C1-4 alkyl; and R3 represents C1-7 alkoxy optionally substituted by hydroxy, halogeno, cyano, C1-4 alkoxy, amino or acylamino;...
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