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WO/2001/083511A1 |
It is intended to find an efficient method of searching for drugs affecting the cholesteryl ester cycle and establish a system of efficiently searching for defoaming agents or arteriosclerotic lesion shrinkers and a system of searching f...
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WO/2001/079256A1 |
A 19-norbufalin derivative compound of formula (I) and isomers pharmaceutically acceptable salts thereof. Compounds of formula (I) are Na?+¿,K?+¿-ATPase inhibitors and can be used in the treatment of cardiac and/or vascular malfunction...
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WO/2001/079255A1 |
An efficient method for the synthesis of aminosterol compounds such as squalamine and compound 1436 is described. A method of the invention provides for regioselective oxidation and regioselective sulfonation of a fused ring system. The ...
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WO/2001/076531A2 |
Many compounds have poor bioavailability or variable bioavailability because of poor absorption of the compound in the small intestine. Conjugation of the compound with bile acid to form a prodrug will increase the bioavailibility of the...
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WO2000042058A9 |
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 erythromycin and novobiocin.
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WO/2001/074840A2 |
The present invention relates, $i(inter alia), to compounds having the general formula (I) in which: R?1¿ is a member selected from the group consisting of -OCH¿3? -SCH¿3?, -N(CH¿3?)¿2?, -NHCH¿3?, -NC¿4?H¿8?, -NC¿5?H¿10?, -NC¿...
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WO/2001/072707A2 |
This invention provides caspase inhibitors of formula (I): wherein Z is oxygen or sulfur; R?1¿ is hydrogen, -CHN¿2?,R, CH¿2?OR, CH¿2?SR, or -CH¿2?Y; Y is an electronegative leaving group; R?2¿ is CO¿2?H, CH¿2?CO¿2?H, or esters, ...
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WO/2001/070760A1 |
An improved process and composition are dislcosed for isolation of steroids containing a 5,7-diene functionality from a sterol mixture that comprises formation of a Diels-Alder reaction product of the ster-5,7-dienol in the presence of a...
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WO/2001/057064A2 |
A cationic amphiphile for facilitating transport of a biologically active molecule into a cell has the structure A-F-D, in which A is a lipid anchor, D is a head group, and F is a spacer group having the structure described herein. A met...
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WO/2001/055098A1 |
The present invention is directed to a compound having the structure (I): and acceptable salts, polypeptides, and pro-forms thereof, wherein R is selected from the group consisting of: (a) substituted glycerols; wherein n is an integer f...
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WO/2001/051003A2 |
The invention provides novel methods for treating disease based on the medicinal use of lipids and phospholipids covalently bound to physiologically acceptable monomers or polymers. Phosphatidylethanolamine moieties conjugated to physiol...
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WO/2001/051022A1 |
The invention concerns the use of at least a compound selected in the group consisting of dehydroepiandrosterone, its precursors and its metabolic derivatives, for preparing a composition for oral administration and for use in regulating...
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WO/2001/049703A2 |
The invention discloses substituted sapogenins and their use in the treatment of cognitive disfunction and similar conditions. Methods of treatment and pharmaceutical composition are also disclosed.
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WO/2001/049280A2 |
Pregnanes of formula (I) where R¿1?=H, C¿1-4? alkyl, C¿1-4? alkanoyl, SO¿3?H, or a salt thereof, R¿2?=C¿1-4? alkyl, R¿3?=H or methyl, and one or two non-adjacent members of a, b, c, and d are optional double bonds, and pharmaceuti...
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WO/2001/049704A1 |
The present invention relates to the compounds of formula (I), a method for extracting it and a pharmaceutical composition containing it. The said extracting method includes: extracting the corpus radicis and/or radix fibrosa of a ginsen...
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WO/2001/049275A2 |
Methods and therapeutic compounds for treating pain, mitigating inflammation, effecting analgesia and/or effecting sedation in a subject are described. A subject is administered an effective amount of a therapeutic compound which is a ni...
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WO/2001/044198A1 |
The invention relates to amphiphilc amines and the salts thereof, which may complex with biopolymers such as DNA, RNA, anti-sense oligonucleotides, ribozymes, proteins and peptides and transfer them into eucaryotic cells. Polyaminochinol...
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WO/2001/040253A2 |
The invention concerns a 3-methylene steroid derivative having general formula (1) wherein R?1¿ is H or together with R?3¿ forms a $g(b)-epoxide or R?1¿ is absent if there is a 5-10 or 4-5 double bond; R?2¿ is (C¿1?-C¿5?)alkyl or C...
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WO/2001/040254A1 |
Compounds of general formula (I) or salts thereof, being useful as reagents for gene transfer: R?4¿-X?2¿-(CH¿2?)¿q?-N(R?3¿)-[(CH¿2?)¿p?-N(R?2¿)]¿s
?-[(CH¿2?)¿n?-N(R?1¿)]¿r?-CO-(CH¿2?)¿m?-X?1¿-A wherein R?1¿, R?2¿, R?3¿...
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WO/2001/037841A1 |
The invention concerns a pharmaceutical composition comprising trimegestone optionally associated with an oestrogen, characterised in that it comprises a buffer solution whereof the pH, when it is introduced in the composition, ranging e...
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WO/2001/032681A1 |
The present invention provides a method of obtaining highly pure phytosterols practically and efficiently from crude phytosterol compositions derived from vegetable fats and oils. That is, the present invention provides a method of sapon...
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WO/2001/032682A1 |
The present invention provides a process for producing a highly pure phytosterol, at high yield in particular, by an easy treatment from a crude fatty acid ester derived from a vegetable fat and/or oil. That is, the present invention pro...
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WO/2001/029060A2 |
Novel sterol/stanol esters of a conjugated fatty acid are provided through the esterification or transesterification of a sterol such as beta-sitosterol or a hydrogenated form thereof (stanol). Such novel esters exhibit the combined prop...
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WO/2001/029061A1 |
Novel 17,20-dihydrofusidic acid derivatives (Ia) are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.
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WO/2001/028562A1 |
The present invention provides a pharmaceutical composition for application to the mucosa to be used in drug therapy comprising a water-insoluble and/or water-low soluble substance, ciclesonide, and an aqueous medium, and having an osmot...
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WO/2001/027133A1 |
The process of the present invention transforms a steroidal ketone of formula (III) to androst-4-en-17$g(b)-carboxylic acid (IV) by reaction with K¿2?SO¿5?•KHSO¿4?•K¿2?SO¿4?.
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WO/2001/027134A1 |
The present invention relates to a process for extracting estrogens from pregnant mare urine (PMU) comprising the following steps: (a) adding a salt to the pregnant mare urine, (b) conducting a liquid-liquid extraction of the pregnant ma...
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WO/2001/026618A2 |
The invention relates to composition containing at least one steroid selected from: dihydroepiandrosterone and/or a biological precursor and/or a metabolic derivative thereof, in a physiologically suitable medium and characterised in tha...
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WO/2001/023407A1 |
The invention discloses the use of sapogenin derivatives in the treatment of cognitive disfunction and similar conditions. Methods of treatment and pharmaceutical composition are also disclosed.
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WO/2001/021642A1 |
The invention relates to substituted 4-benzylaminoquinolines of formula (I), wherein the radicals have the meanings given, and to their heteroanalogues, their pharmaceutically compatible salts and their physiologically functional derivat...
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WO/2001/017954A1 |
The invention relates to substituted acylguanidines and their pharmaceutically compatible salts and physiologically functional derivatives. The invention also relates to compounds of formula (I), wherein the radicals have the meanings gi...
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WO/2001/016157A2 |
A process for the preparation of the compounds of general formula (I) in which R¿1? is H or OH; R¿2? is H, $g(a)-OH, or $g(b)-OH; and R¿3? is a straight or branched C¿1?-C¿4? alkyl group or a benzyl group, comprising the reduction o...
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WO/2001/015552A1 |
Triglycerides and cholesterol in the bloodstream are important factors in the development of cardiovascular disease. The present invention discloses a nutritional supplement comprising a sterol and an omega-3 fatty acid, or an ester ther...
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WO/2001/015717A1 |
Medicinal compositions and preparations for administration comprising ginseng, which is useful as a cell protecting agent and a remedy for nerve trauma, its extract, ginseng components, metabolites thereof or salts thereof (for example, ...
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WO/2001/012186A1 |
A cell adhesion inhibitor of the general formula: R?3¿-L-L'-R?1¿ is disclosed. An inhibitor of the present invention interacts with VLA-4 molecules and inhibits VLA-4 dependent cell adhesion. Also disclosed are methods for preparing an...
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WO/2001/005807A1 |
A process of subjecting a steroid compound represented by the general formula (I) (wherein R is hydrogen or lower alkyl) to chromic acid oxidation in the presence of anhydrous calcium carbonate to thereby form the corresponding 5-ene-3-o...
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WO/2001/000653A1 |
Novel phystosterol and/or phytostanol derivatives, including salts thereof, are represented by general formulae: (I), (II), (III), wherein R is a phytosterol or phytostanol moiety, R2 is derived from ascorbic acid and R3 is hydrogen or a...
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WO/2000/075165A1 |
Processes for preparing high purity sulfated sterol derivatives in high yield, which processes include: (a) providing a sterol; (b) reacting the sterol with a source of SO¿3?, whereby a sulfated sterol derivative is formed; (c) neutrali...
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WO/2000/068245A1 |
The present invention relates to pharmaceutically active 14$g(b)-H-sterols, to pharmaceutical compositions comprising them and to the use of these novel compounds for the preparation of medicaments. More particularly it has been found th...
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WO/2000/068246A1 |
Compounds of Formula (I) in which: R?1¿ and R?2¿, which may be the same or different, each represents a lower alkyl, alkenyl or alkynyl group; R?3¿ represents a methyl group having $g(a)- or $g(b)-configuration; R?4¿ represents a hyd...
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WO/2000/068170A1 |
A method of fluorinating a substance comprises providing a reaction mixture comprising a liquid or supercritical carbon dioxide reaction medium, a first reactant, and a second reactant, wherein the first reactant is a fluorinating reagen...
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WO/2000/066068A2 |
The present invention provides a method of inducing growth or enhancing survival of nervous tissue comprising contacting the nervous tissue with an amount of ebaf effective to induce the growth or enhance the survival of the nervous tiss...
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WO/2000/066611A1 |
Steroid derivatives of this invention interact with nuclear liver X receptor (LXR) and ubiquitous receptor (UR) and can be used to treat a variety of LXR- or UR-mediated disorders.
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WO/2000/064923A1 |
A method for separating sterols from neutral substances containing the sterols, the method comprising: a) providing a hydrocarbon fraction containing the neutral substances; b) subjecting the hydrocarbon fraction to a first purification ...
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WO/2000/064924A1 |
A method for separating sterols from neutral substances comprising the sterols, the method comprising: (a) providing a hydrocarbon fraction containing in the neutral substances; (b) optionally washing the hydrocarbon fraction with water;...
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WO/2000/064921A2 |
A universal process for purifying phytosterols from a wood or plant derived source comprises extracting from the source a concentrated extract comprising phytosterols and a hydrocarbon; complexing the extract so formed with a metal salt;...
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WO/2000/064922A1 |
A method for purifying 4-desmethylsterols from neutral substances containing the 4-desmethylsterols and undesired neutral components, the method comprising the step of treating the neutral substances with a solvent mixture comprising met...
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WO/2000/061694A1 |
The present invention provides a method for manufacturing fat-soluble phytosterol or phytostanol ester of unsaturated fatty acid for inhibiting the absorption of cholesterol and foodstuffs containing the same. The method for manufacturin...
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WO/2000/061603A1 |
The invention relates to a method for producing phytosterols from mixtures containing fatty acid esters and methanol by using known crystallization, filtration, washing and drying techniques. The inventive method is characterized in that...
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WO/2000/059513A1 |
Novel sulfur-containing analogs of 1$g(a),25- dihydroxyvitamin D¿3? are provided. These analogs are synthesized in a convergent manner by joining A-ring and C,D ring fragments. Each analog with 1$g(a),3$g(b)-substituent stereochemistry ...
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