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WO/1998/045315A1 |
This invention provides estra-5(10),7-dien-3$g(b)-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3$g(b)-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien...
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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/1998/028266A1 |
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/1998/028322A1 |
Bissteroidal compounds of general formula (I), in which R�1? stands for hydrogen, alkyl, acyl, fluorine, and X�1?R�5?, where X�1? stands for oxygen and sulfur and R�5? can either be hydrogen, alkyl, aryl; R�2? stands for hydr...
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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/1998/024800A2 |
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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WO/1998/017244A1 |
Disclosed is the use of sterolsulfates as active substance for producing means for inhibiting serin proteases, specially elastases. Said means act against skin wrinkling and may be also used against psoriasis.
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WO/1998/017676A1 |
The invention relates to a new polymorphic crystalline form of S-fluoromethyl 6$g(a),9$g(a)-difluoro-11$g(b)-hydroxy-16$g(a)-methyl-3-oxo-
17$g(a)-propionyloxyandrosta-1,4-diene-17$g(b)-carbothiate (fluticasone propionate). The new polym...
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WO/1998/016544A1 |
This invention provides 17$g(a),$g(D)8,9-dehydroestradiol or a pharmaceutically acceptable salt of its 3-sulfate ester, and 17$g(b),$g(D)8,9-dehydroestradiol or a pharmaceutically acceptable salt of its 3-sulfate ester.
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WO/1998/004578A1 |
The invention concerns a method of producing 3-sulfanato-oxy-estra-1,3,5(10)-trien derivates of the general formula (I) where the bonds marked with --- symbolize three single bonds, two single bonds and a double bond or two conjugated do...
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WO/1998/004579A1 |
The invention concerns a method of producing 3-sulfanato-oxy-estra-1,3,5(10)-trien derivates of the general formula (I) where the bonds marked with --- symbolize three single bonds, two single bonds and a double bond or two conjugated do...
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WO/1998/002450A2 |
Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have...
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WO/1997/045441A1 |
The present invention relates to the novel 7'alpha'-(5-methylaminopentyl)-estratrienes of the general formula (I), in which R2 is a hydrogen or fluorine atom, R17 is a hydrogen atom, a methyl or ethynyl group, n is 2, 3 or 4, and x is 0,...
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WO/1997/042215A1 |
A process for preparing 27-hydroxy cholesterol and derivatives thereof. The process includes the conversion of the terminal acid or ester moiety to a reactive halomethyl moiety, which is eventually reduced to a hydroxy moiety after alkyl...
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WO/1997/042214A1 |
The invention provides new androstene derivatives having anti-inflammatory activity, pharmaceutical compositions containing them, and methods of administering them to warm-blooded animals in the treatment of inflammation. The active comp...
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WO/1997/039018A1 |
The invention discloses products with formula (I) in which: either R1 stands for halogen, hydroxyl, (C1-C8) alkyloxy or (C1-C12) acyloxy, and R2 represents halogen or hydrogen; or R1 and R2 together form a double bond, Z is selected from...
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WO/1997/034871A1 |
Disclosed are (i) compounds of a steroid, a 'beta'-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous prod...
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WO/1997/024367A1 |
Compounds of the pregnane series are described having general formula (I) and solvates thereof in which R1 individually represents -OC(=O)C1-6 alkyl; R2 individually represents hydrogen, methyl (which may be in the 'alpha' or 'beta' conf...
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WO/1997/024365A1 |
Compounds of the androstane series are described having general formula (I) and solvates thereof, in which R1 represents O, S or NH; R2 individually represents OC(=O)C1-6 alkyl; R3 individually represents hydrogen, methyl (which may be i...
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WO/1997/021720A2 |
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 -CHR4-CHR5- or -CR4=CR5-; R3, R4 and R5...
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WO/1997/014418A1 |
Compounds of formula (I) are inhibitors of 5'alpha'-reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, prostatic carcinoma, prostatitis and ...
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WO/1997/014712A2 |
The invention relates to novel sulphamate derivatives of 1,3,5(10)-estratriene derivatives of general formula (I) in which the 3-sulphamate group is acylated, sulphonated or amido-sulphonated. Also disclosed are methods of producing thes...
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WO/1997/010256A1 |
Hitherto unknown compounds of formula (II) wherein R1 is hydrogen or methyl; R2 is hydrogen, methyl, CH2OH, CH2OR3, CHO, CH=CH2, COOH or COOR4; R3 is alkyl, aralkyl, aryl, alkanesulfonyl, arene-sulfonyl; alkanoyl or aroyl, optionally sub...
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WO/1997/008187A1 |
The present invention provides (I) wherein X is 'alpha'-CH2OR1 when A is 'alpha'-hydro, A and B together are ethylene, and C and D together are ethylene, 'beta'-CH2OR1, or -CO-; R is -H or n-butylsulfonoyl; R1 is R provided that at least...
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WO/1997/003677A1 |
The present invention relates to a method of inhibiting N-methyl-D-aspartate (NMDA) glutamate receptor-mediated ion channel activity (NMDA receptor activity), comprising contacting a neuronal cell (e.g., hippocampal neuron, spinal cord c...
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WO/1996/040043A2 |
The invention relates to 3'alpha'-hydroxy, 17-(un)substituted derivatives of the androstane series and 3'alpha'-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified ...
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WO/1996/025935A1 |
A method of treating adenosine depletion in a subject in need of such treatment is disclosed. The method comprises administering to the subject folinic acid or a pharmaceutically acceptable salt thereof in an amount effective to treat ad...
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WO/1996/018609A1 |
The present invention is a method of protecting a sulfonic acid functional group in an organic molecule as a substituted or unsubstituted neopentyl sulfonate ester. The method allows the conversion of R-SO3-H to R'-SO3-H, wherein R and R...
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WO/1996/011206A1 |
The disclosed invention is a process for preparing 17-beta-substituted-androsta-3,5-dien-3-carboxylic acids from 3-halo-17-beta-substituted-androsta-3,5-dienes. The process may be performed in either of two ways: (1) the 3-halo compound ...
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WO/1996/010032A1 |
The invention relates to estrene steroid, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. The figure...
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WO/1996/010031A1 |
The invention relates to novel, androstane steroids which are the ligand semiochemicals which bind to neuroepithelial receptors.
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WO/1996/005216A1 |
The invention concerns novel estra-1,3,5(10)-triene amidosulphamates with an R-SO2-O- group in the 3-position, R being an R1R2N- group in which R1 and R2, independently of each other, are a hydrogen atom, an alkyl group with 1 to 5 C-ato...
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WO/1996/003420A1 |
The present invention provides a compound of formula (I), wherein A is a bond or a straight or branched C1-C6 alkylene chain; W is a group -R1, -OR2, -NR3R4 or (a) wherein: Y is oxygen or sulphur; R1, R2 and R4 are: a C1-C10 alkyl group,...
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WO/1996/002500A1 |
The invention relates to novel chelate formers containing sulphonamide groups and their metallic chelates of general formula (I) in which n, m, p, V1, V2, V3, V4, X1, X2, X3, R1, R2, R3 and R4 have different meanings, pharmaceutical agen...
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WO/1996/000230A1 |
The present invention relates to a process for the preparation and manufacture of 3-amino-substituted glycosylated bile acid derivatives. Novel intermediates and related compounds are also disclosed. In particular, the present invention ...
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WO/1995/029186A1 |
The present invention relates to methods and compositions for the transformation of cells. In particular, compositions and methods are disclosed which include combinations of the nucleic acid of interest and polyhydroxylated or polyglyco...
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WO/1995/028413A1 |
Invented are 17'beta'-substituted 3-carboxy steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-'alpha'-reductase.
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WO/1995/027697A1 |
A compound represented by general formula (I) and an intermediate therefor, and a process for synthesizing the both, wherein R1 represents optionally hydroxylated C1-C10 alkyl; R2 represents hydrogen or hydroxy; and R3 represents hydroge...
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WO/1995/024415A1 |
Compounds having a broad range of antimicrobial activity generally have a structure including a steroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compou...
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WO/1995/021617A1 |
Methods, compositions, and compounds for modulating the GABAA receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.
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WO/1995/015943A1 |
21-norvitamin D3 analogs in which the methyl group normally attached to the side chain at carbon 20 has been replaced by a hydrogen atom. The compounds are characterized by a marked intestinal calcium transport activity while exhibiting ...
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WO/1995/013287A1 |
Steroids are disclosed with radical-attracting aromatic substituents of general formulae (I) and (II). The new steroids with radical-attracting aromatic substituents are suitable active ingredients in pharmaceuticals for use in the preve...
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WO/1995/010528A1 |
The invention relates to a process for producing sulfuric acid semi-esters of general formula (I): RO-SO2-OH, in which R is an organic radical, from hydroxy compounds of general formula (II): R-OH, in which R is the same as in formula (I...
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WO/1995/009178A1 |
A method of preparing a 3'beta'-hydroxy- or 3'beta'-(lower acyloxy) 16,17-ene-17-(3-pyridyl)-substituted steroid, wherein the 3'beta'-(lower acyloxy) group of the steroid has from 2 to 4 carbon atoms, which comprises subjecting a 3'beta'...
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WO/1995/006474A1 |
Nucleosides and linked nucleosides functionalized to include alkylthiol chemical functionality at ribofuranosyl positions, nucleosidic base positions, or on internucleoside linkages. In certain embodiments, the compounds of the invention...
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WO/1995/004535A1 |
The application discloses methods of making medicaments for treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural ...
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WO/1995/000478A1 |
Described are aryltriflates and related derivatives of raclopride, riluzole, cisapride, omeprazole, lanzoprazole, pantoprazole, paroxetine, fenfluramine, sotalol, estradiol, RU 486, tacrine, moclobemide, ifenprodil, brofaromine, melatoni...
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WO/1994/027608A1 |
Methods and compositions for interacting with the GABAA receptor complex to induce sleep in humans using certain 5 3alpha-hydroxy-5-reduced steroid derivatives.
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WO/1994/026769A1 |
Novel anti-inflammatory compounds, compositions of these compounds and use of such compounds to treat inflammed ocular tissue are described. The compounds are derivatives and analogues of known steroid compounds (e.g., dexamethasone) and...
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WO/1994/025053A1 |
An antigen comprising 5,7 cholestadien-3beta-ol (7-dehydrocholesterol) or a compound having a structure similar to 5,7 cholestadien-3beta-ol and a quaternary ammonium salt is provided. Also provided is a method of generating an antibody ...
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