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WO/2000/014104A1 |
The present invention relates to crystalline 11$g(b)-fluoro- 7$g(a)-(14, 14,15,15,15- pentafluoro-6- methyl-10-thia- 6-azapentadecyl) estra-1,3,5(10)- triene-3, 17$g(b)-diol (compound (1)) in the form of a solvate. The crystalline solvat...
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WO/2000/011019A1 |
The present invention relates to novel compounds comprising a steroid hormone linked to a DNA-interacting molecule that target nucleic acids to the cell nucleus. Further, the invention relates to a method for introducing nucleic acids in...
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WO/2000/011018A1 |
The present invention relates to novel compounds comprising a steroid hormone linked to a DNA-interacting molecule that target nucleic acids to the cell nucleus. Further, the invention relates to a method for introducing nucleic acids in...
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WO/2000/009137A2 |
Newly isolated aminosterol compounds and pharmaceutical compositions based on the aminosterol compounds are described. Methods for the treatment of various disorders, for example, a microbial infection, are also described.
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WO/1999/067274A1 |
The invention concerns compounds of formula (I) wherein, in particular: X = halogen; Y = single bond, O, NH, S, SO or SO¿2?; Z = hydrogen or halogen; n, R¿1?, R¿2?, R¿3? and R¿4? are as defined in the description. The invention also...
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WO/1999/062929A1 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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WO/1999/062928A1 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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WO/1999/058549A1 |
Certain novel sterol derivatives can be used for regulating the meiosis in oocytes and in male germ cells.
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WO1999033858A9 |
Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have structural formula (I) wherein r1 is an optional double bond, R<1> and R<2> are selected from the group consisting of hydrogen and lower alkyl, or...
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WO/1999/052932A1 |
The present invention relates to bile acid or bile salt fatty acid conjugates (hereinafter called 'BAFAC'), to their use in dissolving cholesterol gallstones in bile, preventing their occurrence or recurrence, to their use in reducing or...
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WO1999033859A9 |
Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependant disorders. Preferred compounds have 1,3,5-estratiene nucleus, and are substituted at the C-17 or C-11 position...
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WO/1999/046279A2 |
Novel methods of medical treatment and/or inhibition of development of diseases are disclosed for diseases that are sensitive to androgenic or estrogenic activity. The treatments utilize inhibitors of type 5 and/or type 3 17$g(b)-hydroxy...
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WO/1999/046280A1 |
The invention concerns compounds of formula (I) wherein: R1 represents a C1-C31 hydrocarbon radical, in particular an alkyl radical, linear or branched, saturated or unsaturated; OR2 represents a cholesteryl radical; said compounds being...
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WO/1999/044616A1 |
A series of novel steroid derivatives are described. The steroid derivatives are antibacterial agents. The steroid derivatives also act to sensitize bacteria to other antibiotics including erythromicin and novobiocin.
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WO/1999/045023A1 |
The invention relates to S-substituted 11$g(b)-benzaldoxime-estra-4,9-diene-carbonic acid thiolesters of general formula (I) and the pharmaceutically acceptable salts thereof. The invention additionally relates to a method for the produc...
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WO/1999/045024A1 |
Novel sterol derivatives of formula (I), in which: R?1¿ represents a hydroxyl group or protected hydroxyl group, R?2¿ represents a hydrogen atom and a double bond is present at c, or R?1¿ and R?2¿ together represent an oxo group and ...
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WO/1999/035161A1 |
A process for producing a compound of formula (I) wherein the dotted lines --- independently represent a single or double bond and R, R¿1?, R¿2? and R¿3? are each hydrogen or an organic radical, comprises treating the corresponding 17...
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WO/1999/033855A1 |
The invention relates to novel 11$g(b)-halogen-7$g(a)-substituted estratrienes of formula (I), wherein R?11¿ is a fluorine or chlorine atom and the other substituents have the meanings given in the description. The inventive compounds h...
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WO/1999/032127A1 |
Compositions of angiostatic agents for treating GLC1A glaucoma and methods for their use are disclosed.
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WO/1999/027935A1 |
A sulphamate compound suitable for use as an inhibitor of oestrone sulphatase (E.C.3.1.6.2) is described. The compound is a polycyclic compound comprising at least two ring components, wherein the polycyclic compound comprises at least o...
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WO/1999/027936A1 |
A sulphamate compound suitable for use as an inhibitor of oestrone sulphatase (E.C.3.1.6.2) is described. The compound is a polycyclic compound comprising at least two ring components, wherein the polycyclic compound comprises at least o...
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WO/1999/025725A1 |
The invention concerns compounds of formula (I) in which: X is a halogen atom; D represents the radical of a pentagonal or hexagonal cycle optionally substituted and optionally unsaturated; R¿1?, R¿2?, R¿3?, R¿4?, X and n are as defi...
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WO/1999/020646A1 |
The invention provides estrogens and antiestrogens of formula (I) having structure (I) wherein R is (II), (III), (IV), or (V); R?1¿ and R?2¿ are each, independently, alkyl of 1-6 carbon atoms, or are alkyl groups which are taken togeth...
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WO/1999/018798A1 |
The invention relates to the use of arsenic compounds to treat a variety of neoplastic diseases (see the dose response curves in the Figure). Further, the arsenic compounds may be used to treat metastatic neoplastic diseases.
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WO/1999/019342A1 |
The present invention relates to bile acid metal salts of therapeutical interest, as well as to pharmaceutical and veterinary compositions containing said salts.
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WO/1999/015656A2 |
A new gene in the G-coupled protein receptor family is discribed that is induced by IL-9, thereby providing a therapeutic target in IL-9 mediated development of atopic allergy, asthma-related disorders and certain lymphomas or leukemias....
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WO/1999/015547A1 |
The invention concerns beverage compositions and acetic acid compositions that contain hydroxy acid, keto acid, dicarboxylic acid or amino acid esters of a phytosterol and/or a phytostanol, or their salts, the amine salts of amino acid e...
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WO/1999/015546A1 |
The invention concerns dietary fat compositions that contain the hydroxy acid or dicarboxylic acid or amino acid esters of a phytosterol and/or phytostanol, or the mixed esters formed with the alcohols, polyols or polyol (C¿2?...C¿22?)...
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WO/1999/005094A1 |
This invention features permeability enhancer molecules, and methods, to increase membrane permeability of negatively charged polymers thereby facilitating cellular uptake of such polymers.
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WO/1999/003503A1 |
Methods for treating ocular neovascularization using photodynamic therapy in combination with an angiostatic steroid are disclosed.
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WO/1999/003876A1 |
Sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.
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WO/1998/056812A2 |
Crystal comprising at least part of the ER$g(a) ligand binding domain, optionally bound to a ligand, ligands that bind to ER receptors, and methods of designing them, and a homology model of the ER$g(b) receptor.
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WO/1998/055499A1 |
The invention relates to 11$g(b)-aryl-substituted 14,17-ethano-oestratriens of general formula (I), in which R?1� is a hydrogen atom, a C�1?-C�12?-alkanoyl-, a benzoyl-, a straight-chain or branched C�1?-C�12?-alkyl-, a C�3?-...
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WO/1998/055496A1 |
New non-estrogenic estradiol derivatives with an antioxidant effect are disclosed. These estradiol derivatives, which have no estrogenic effect but a high antioxidant effect, are potentially useful as non-estrogenic antioxidants, in part...
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WO/1998/052965A1 |
The invention relates to 20-aralkyl-5$g(a)-pregnane derivative having general formula (I), or a pharmaceutically acceptable salt thereof, wherein R�1? is (H,OR), (H,OSO�3?H) or NOR; R is H, (C�1-6?)alkyl or (C�1-6?)acyl; each of ...
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WO/1998/050418A1 |
Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more ca...
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WO/1998/050417A1 |
Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more ca...
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WO/1998/050416A1 |
Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more ca...
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WO/1998/045316A1 |
The invention concerns compounds of formula (I) in which X is a halogen atom; D represents the residue of a pentagonal or hexagonal cycle, optionally substituted and optionally unsaturated; R�1?, R�2?, R�3?, R�4?, Y and n are suc...
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WO/1998/043994A1 |
Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more ca...
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WO/1998/042729A2 |
The invention relates to novel estratrienes of general formula (I) containing several sulfamoyoxy groups per molecule (m = 1-5). They are produced by reacting the appropriate steroid alcohols with sulfamoy or n-alkyl or alkanoylsulfamoyl...
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WO/1998/034947A1 |
New 17$g(a)-fluoralkyl steroids have general formula (I), in which R?1� stands for a methyl or ethyl group; R?2� for a radical of formula C�n?F�m?H�o?, in which n equals 2, 3, 4, 5 or 6, m$m(g)1 and m+o = 2n+1; R?3� stands fo...
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WO/1998/031702A1 |
The present invention relates to 16-hydroxy-11-(substituted phenyl)-estra-4,9-diene derivatives according to formula (I), wherein R�1? is C�1-6?alkyl, C�3-6?cycloalkyl, C�1-6?alkoxy, triflate, pyridyl or phenyl where the phenyl m...
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WO/1998/028324A1 |
The invention concerns steroid compounds of general formula (I) in which n = 2, 3, either R�1? and R�2? = H, (C�1?-C�4?) alkyl, or R�1? and R�2? form with nitrogen a heterocyclic compound, X = OH optionally esterified, Y = (C...
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WO/1998/027106A1 |
An aminosterol compound according to formula (I) wherein R�1? is a member selected from the group of: (a), wherein R�6? is H or (b); (c); and (d); R�2? is H or OH; R�3? is H or OH; R�4? is H or OH; and R�5? is a C�1? to Cï¿...
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WO/1998/025948A2 |
Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of formula (I) wherein: -A-A- represents the group -CHR?4�-CHR?5�- or -CR?4�=CR?5�-...
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WO/1998/024801A1 |
Disclosed are 3-oxyiminopregnan-21-carbolactone, $i((E,Z)) mixtures and isomerically pure $i((E)) and $i((Z)) compounds, the production and use thereof as medicaments.
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WO/1998/024760A1 |
The present invention provides a library of compounds, each comprised of a common animobenzenedicarboxylic acid core structure (scaffold) that serves as a template for synthesizing approximately 10?1�-10?6� compounds which are analog...
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WO/1998/024802A2 |
A compound is described. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound has formula (I); wherein A is a first group; B is an aryl ring structure having at least 4 carbon atoms in the ring and wherei...
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WO/1998/024800A2 |
A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereose...
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