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WO/2002/079220A2 |
The present invention relates to steroid compounds of general formula X, which may advantageously be employed to stimulate meiosis in human oocytes, the steroid being specifically characterized by amino nitrogen bonded to C?17¿ of the s...
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WO/2002/072598A1 |
The invention relates to compounds of formula (I) wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
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WO/2002/066489A2 |
The invention relates to a sterol skeleton based compound wherein one or several amphoteric groups with an isoelectric point of between 4 and 9 are substituted on the 3?rd¿ position of the ring system, in addition to liposomes containin...
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WO/2002/066490A2 |
Disclosed is a sterol derivative having a pKa value of 3.5 - 8 according to the general formula cation - spacer 2 - Y - spacer 1 - X - sterol, wherein Y and X represent bonding groups. The invention also relates to liposomes containing s...
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WO/2002/055531A1 |
The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.
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WO/2002/026759A2 |
The invention relates to 17$g(a) fluoroalkyl steroids of the general formula (I), STEROID (I), wherein R¿3? represents a group of the formula CnFmHo, wherein n = 1, 2, 3, 4, 5 or 6, m > 1 and m+o = 2n+1. The invention further relates to...
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WO/2002/012266A1 |
There are provided according to the invention compounds of formula (I) wherein R¿1? represents C¿1-6? alkyl or C¿1-6? haloalkyl; R¿2? represents -C(=O)-aryl or -C(=O)-heteroaryl; R¿3? represents hydrogen, methyl (which may be in eit...
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WO/2002/012265A1 |
According to one aspect of the invention, there is provided a compound of formula (I) and solvates thereof. There are also provided compositions containing the compound, processes for preparing it, and its use in therapy.
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WO/2002/000680A2 |
Novel lipids for forming liposomes for use as nucleic acid delivery vehicles, e.g. for gene therapy, have structure with a steroid (cholesteryl) domain linked via a carbamoyl linkage to a head group which is positively charged in use (ge...
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WO/2002/000679A2 |
Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals.
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WO/2001/087299A1 |
The present invention describes a method for programming a specific course and rate of metabolism for a parent drug compound that leads to an inactive or very weakly active and nontoxic metabolite when the modified drug compound is admin...
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WO/2001/083512A1 |
A compound of formula (I) and pharmaceutical acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein, independently at each occurrence: R?1¿ and R?2¿ are selected from hydrogen, oxygen so as ...
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WO/2001/081364A1 |
Steroid sulfatase inhibitors containing as the active ingredient estra-1,3,5(10)-triene derivatives represented by the following general formula (I) or pharmacologically acceptable salts thereof: (I) wherein R?1¿ and R?2¿ are the same ...
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WO/2001/078606A1 |
An estrogen/antiestrogen-porphyrin conjugate, their composition and methods for their use are claimed. The active compounds of the invention are conjugates consisting of an estrogen or anti estrogen portion, tether or linker portion and ...
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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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WO/2001/074840A2 |
The present invention relates, $i(inter alia), to compounds having the general formula (I) in which: R?1¿ is a member selected from the group consisting of -OCH¿3? -SCH¿3?, -N(CH¿3?)¿2?, -NHCH¿3?, -NC¿4?H¿8?, -NC¿5?H¿10?, -NC¿...
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WO/2001/064708A1 |
Compounds able to chelate paramagnetic metal ions and the use thereof as contrast agents in the technique known as 'Magnetic Resonance Imaging' (M.R.I.), which consist of at least two chelating agents conjugated via a multivalent linker ...
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WO/2001/053355A1 |
The subject of the invention provides a compound having the formula: H1-X-B-Y-H2, wherein each of H1 and H2 may be the same or different and capable of binding to a receptor which is the same or different; wherein each of X and Y may be ...
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WO/2001/040805A1 |
The invention provides a compound having binding affinity for a receptor and comprising a steroid skeleton in its molecular structure, which compound is according to formula (1) wherein: Bu is a sterically bulky structure or Bu is a mole...
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WO/2001/021642A1 |
The invention relates to substituted 4-benzylaminoquinolines of formula (I), wherein the radicals have the meanings given, and to their heteroanalogues, their pharmaceutically compatible salts and their physiologically functional derivat...
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WO/2001/018025A2 |
The invention is directed to novel class of 17b-acyl-17a-propynyl steroids which exhibit potent antiprogestational activity. The synthetic scheme for the preparation of these compounds are shown in figure 1.
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WO/2001/007462A1 |
The invention is directed to a novel class of 11$g(b)-aryl-17,17-spirothiolane-substituted steroid compounds exhibiting binding to the progestin receptor.
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WO/2001/005364A1 |
Methods for regulating hair growth comprise administering to a mammal an effective amount of a compound according to formula (I), wherein a is 0 or 1 and each --- represents either a single bond or a double bond, provided that two adjace...
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WO/2001/000652A2 |
The invention relates to novel 11$g(b) long-chain substituted estratrienes of general formula (I), wherein R?11¿ is a long-chain residue with one nitrogen and optionally one sulfur atom, that can additionally be terminally functionalize...
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WO/2000/078789A1 |
Novel phytosterol and/or phytostanol derivatives, including salts thereof, are represented by general formulae (I or II) wherein R is a phytosterol or phytostanol moiety; R2 is oxygen or hydrogen (H2) and R3 is an aromatic or heterocycli...
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WO/2000/066614A1 |
This invention relates to compounds having Formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein; R¿1? is H or methyl; R¿2? is 5$g(a)- or 5$g(b)- H; R¿3? is an optionally substituted $i(N)-attached het...
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WO/2000/056759A1 |
Steroid derivatives useful as the intermediate for preparing vitamin D derivatives such as 1$g(a), 25-dihydroxyvitamin D¿3? and 2$g(b)-(3-hydroxypropoxy)-1$g(a), 25-dihydroxyvitamin D¿3?, i.e., halides of general formula (II) (wherein ...
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WO/2000/047604A1 |
The present invention relates to pharmaceutically active unsaturated cholestane derivatives, to pharmaceutical compositions comprising them as active substances and to the use of these novel compounds for the preparation of medicaments. ...
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WO/2000/039148A1 |
The invention relates to new 7$g(a), 17$g(a), 17$g(b)-substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term ant...
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WO/2000/020437A1 |
The invention relates to substituted propanolamine derivatives and their pharmaceutically acceptable salts and physiologically functional derivatives. The invention relates to compounds of formula (I), wherein the radicals have the defin...
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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/2000/006585A1 |
Nitric acid salts with medicines active in bony disorders.
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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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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/1999/044616A1 |
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/1999/045022A1 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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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/1999/033855A1 |
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/1999/025725A1 |
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/1999/016786A1 |
The present invention relates to the use of steroid saponin compounds of formula (I) to prophylactic and therapeutic treatment of senility, for example Alzheimer's disease, and to novel steroid saponin compounds of formula (II), and the ...
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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/1998/051702A1 |
Compounds having an ansamycin antibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic l...
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WO/1998/048848A1 |
The invention relates to a method of preparing a compound of the general formula (I): $i(fac)-[M(CO)�3?(OH�2?)�3?]?+� wherein M is Mn, ?99m�Tc, ?186�Re or ?188�Re, by reacting a metal in the permetallate form with carbon mo...
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WO/1998/045317A1 |
Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are also provided therapeutic compositions prepared typically by contacting a dispersion of one or more ca...
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