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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/2001/077139A1 |
The invention relates to novel 8ß-substituted estratrienes of the general formula (I), wherein R?2¿, R?3¿, R?6¿, R?6'¿, R?7¿, R?7'¿, R?9¿, R?11¿, R?11'¿, R?12¿, R?14¿, R?15¿, R?15'¿, R?16¿, R?16'¿, R?17¿ and R?17'¿ are ...
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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/2001/074761A1 |
Substituted tetracycline compounds, methods of synthesis, and methods of use are discussed. Tetracyclines useful for treating tetracycline related disorders are also discussed. Intermediates useful for synthesizing other tetracycline com...
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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/2001/072767A1 |
The invention concerns novel DHEA derivatives of formula (I) and their preparation method. The invention also concerns cosmetic or dermatological compositions containing said compositions and their uses, in particular for preventing or t...
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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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WO2000047603A9 |
The invention relates to novel compounds as pharmaceutical agents which have in vitro a higher affinity to estrogen receptor preparations of the rat prostate than to estrogen receptor preparations of the rat uterus and which preferably h...
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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/2001/053355A1 |
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/2001/049275A2 |
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/2001/047945A1 |
The present invention provides a process for preparing the antiprogestational agent, 17$g(a)-acetoxy-11$g(b)-[4-N,N-(dimethylamino)phenyl]-21-met
hoxy-19-norpregna-4,9-diene-3,20-dione, intermediates useful in the process, and processes ...
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WO/2001/045678A2 |
The invention relates to a composition which comprises as its constituents (a) a local anaesthetic and (b) an anti-inflammatory compound and/or an immunostimulant compound and/or a compound which acts as a supporting material for the loc...
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WO/2001/044268A1 |
A compound is described. The compound has the formula (Ia) as presented in the Figure 1; wherein: X is a ring having at least 4 atoms in the ring; K is a hydrocarbyl group; Rh1 is an optional halo group; Rh2 is an optional halo group; at...
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WO/2001/044267A1 |
The invention relates to novel 11-$g(b)-phenylestradiene derivatives with fluoroalkyl groups in the aromatic side chain, of general formula (I), to a method for producing them and to pharmaceutical preparations containing these compounds...
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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/2001/040253A2 |
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/2001/032680A2 |
The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R?1¿, R?2¿, R?3¿, R?6¿, R?7¿, R?8¿, R?9¿, R?11¿, R?11"¿, R?14¿, R?15¿, R?15"¿, R?16¿, R?17¿ and R?17"¿ have the meaning cited in t...
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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/2001/018028A1 |
The invention relates to novel C¿13?-substituted estra-1,3,5(10)-triene-3-yl-sulfamates of the general formula (I), in which R¿1? represents the acyl radical, oxycarbonyl radical, aminocarbonyl radical, sulfonyl radical or aminosulfony...
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WO/2001/018026A1 |
The present invention relates to steroids of general formula (I), wherein R?1¿ is cyclohexyl, suberyl, R?2¿ is hydrogen or C¿1?-C¿6?-alkyl, R?3¿ is hydrogen, C¿1?-C¿6?-alkyl or hydroxymethyl, R?4¿ is hydrogen or hydroxymethene, o...
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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/2001/017954A1 |
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 $g(b)-OH; and R¿3? is a straight or branched C¿1?-C¿4? alkyl group or a benzyl group, comprising the reduction o...
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WO/2001/014406A1 |
Androstane derivatives having various substituents at the 7- or 11-position, pharmaceutically acceptable salts thereof or prodrugs of the same and substances serving not as an agonist but as an antagonist for androgen receptors, pharmace...
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WO/2001/011068A2 |
The invention concerns the use of a monocationic lipid compound of general formula I(A): R¿1?O-CO-NH-(CH¿2?)¿n?-N?+¿(C¿2?H¿5?)¿3?, I?-¿ wherein: R¿1? represents the cholesteryl radical; n represents an integer equal to 1, 2 or 3...
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WO/2001/005364A1 |
Methods for regulating hair growth comprise administering to a mammal an effective amount of a compound according to formula (I), wherein a is 0 or 1 and each --- represents either a single bond or a double bond, provided that two adjace...
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WO/2001/006261A2 |
The invention relates to a method for screening therapeutic agents, defined as SCAP antagonists, for use in combating diseases associated with elevated lipid levels, said method comprising detecting or assaying the extent or result of tr...
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WO/2001/001135A1 |
The present invention provides a method for the measurement of an analyte in biological samples whereby an uncompetitive inhibitor is coupled to a ligand and utilized in a homogeneous assay. The analyte can be a drug or drug derivative, ...
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WO/2001/000652A2 |
The invention relates to novel 11$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/2000/073471A1 |
Disclosed are cationic lipids for gene transfer, which are capable of transferring nucleic acid materials into cells at very high efficiency with low cell toxicity. They are synthesized by forming a carbamate ester linkage between lysine...
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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 $g(b)-configuration; R?4¿ represents a hyd...
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WO/2000/066613A1 |
The present invention relates to compounds of formula (I) or formula (II) or pharmaceutically acceptable salts thereof useful for the prophylaxis and treatment of degenerative bone disorders, wherein A is (a), B is (b) and X, Y, E, V, Q,...
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WO/2000/066611A1 |
Steroid derivatives of this invention interact with nuclear liver X receptor (LXR) and ubiquitous receptor (UR) and can be used to treat a variety of LXR- or UR-mediated disorders.
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WO/2000/061604A2 |
Steroidal compounds or their salts having general formulas (I) and (II) wherein: s is an integer equal to 1 or 2, preferably s = 2; b0 = 0 or 1; A = R-, wherein R is the steroidal drug radical, C and C¿1? are two bivalent radicals. The ...
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WO/2000/058337A1 |
Novel glucocorticoid receptor ligands as provided which have general formula (I) in which: R is a hydrogen atom, an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereo...
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WO/2000/054756A2 |
Compounds and methods for mitigating neurodegeneration, effecting neuroprotection and/or effecting cognition enhancement in a subject are described. Neurological or cognitive conditions are treated by administering to a subject an effect...
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WO/2000/053618A1 |
The invention relates to 22R-hydroxycholesta-8,14-diene derivatives having general formula (I) wherein R¿1? is OR, OSO¿3?H or =NOR; with R being H, (C¿1-6?)alkyl or (C¿1-6?)acyl; each of R¿2? and R¿3? is independently hydrogen or (...
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WO/2000/051618A1 |
The invention relates to (androst-5-en-17$g(b)-yl)alkyl sulfoxides and sulfones having general formula (I), wherein R¿1? is (H, OR), (H, OSO¿3?H) or NOR; with R being H, (C¿1-6?)alkyl or (C¿1-6?)acyl; each of R¿2? and R¿3? is indep...
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WO/2000/050441A1 |
The invention concerns compounds of formula (I) wherein: X, Y, R¿1?, R¿2?, Z, G are as defined in the description, the methods for preparing them and the intermediates in said method, their use as medicine and the pharmaceutical compos...
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WO/2000/047649A1 |
The invention relates to novel double metal cyanide (DMC) catalyts for producing polyether polyols by polyaddition of alkylene oxides to starter compounds with active hydrogen atoms. The catalyst contains a) double metal cyanide compound...
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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/2000/046234A1 |
The invention concerns steroid derivatives of general formula (I) wherein: OR is selected in the group consisting of the hydroxyl radical (OH), the ether functions wherein R, containing 1 to 8 carbon atoms, is selected among the linear o...
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WO/2000/043408A2 |
Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and...
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WO/2000/039148A1 |
The invention relates to new 7$g(a), 17$g(a), 17$g(b)-substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term ant...
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WO/2000/034232A1 |
Serine carbonates of formula I are precursors for organoleptic compounds, masking agents and antimicrobial agents. Further they are alternative substrates for malodor producing enzymes. The symbols in formula I are defined in claim 1.
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WO/2000/034306A1 |
The invention is directed to a novel class of 17$g(b)-acyl-17$g(a)-propynyl steroids which exhibit potent antiprogestational activity.
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WO/2000/030688A2 |
Substituted polycarboxylic ligand molecules and corresponding metal complexes of said ligands, preferably paramagnetic metals complexes for generating responses in the field of magnetic resonance imaging (MRI). The paramagnetic complexes...
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WO/2000/024761A1 |
The invention relates to substituted phenyl alkenoyl guanidines, the pharmaceutically acceptable salts thereof, and physiolgically functional derivatives. Compounds of formula (I) are disclosed, wherein the radicals have the meanings thu...
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