Steroids

Matches 151 - 200 out of 894	< 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 >

Document	Document Title
WO/2003/035668A2	NOVEL ANTI-INFLAMMATORY ANDROSTANE DERIVATIVES -17-CARBOXY-LACTONE SUBSTITUTED STEROIDS WITH AN ARYL-CARBOXYLIC ESTER IN POSITION 17.ALPHA Novel Anti-inflammatory Androstane DerivativesThere are provided compounds of formula (I) wherein R1 represents O, S or NH;R2 represents -C(&equals O)-aryl or -C(&equals O)-heteroaryl;R3 represents hydrogen, methyl (which may be in eithe...
WO/2003/020214A2	BILE-ACID DERIVED COMPOUNDS FOR ENHANCING ORAL ABSORPTION AND SYSTEMIC BIOAVAILABILITY OF DRUGS Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administrat...
WO/2003/015792A1	ANTI-TUMOUR 2-ALKOXYESTRADIOL SULFAMATES The invention relates to the use of 2-alkoxyestrogen sulfamates of general formula (I) for producing a medicament for the treatment of tumorous diseases, which are positively influenced by the inhibition of tubulin polymerisation. In sai...
WO/2003/013427A2	A METHOD FOR PREPARING FLUTICASONE DERIVATIVES A method for preparing 6&agr ,9&agr -difluoro-17&agr -[(2-furanylcarbonyl)oxy]-11ß-hydroxy-16&agr -methyl-3-oxoandrosta-1,4-diene-17ß-carbothioicacid S-fluoromethyl ester from a thiocarboxylic acid by reacting the thiocarboxylic acid w...
WO/2002/100879A1	NOVEL ANTI-INFLAMMATORY 17.ALPHA.-HETEROCYCLIC-ESTERS OF 17.BETA.CARBOTHIOATE ANDROSTANE DERIVATIVES There are provided compounds of formula (I) wherein R¿1? represents C¿1-6? alkyl or C¿1-6? haloalkyl; R¿2? represents a 4-7 membered non-aromatic ring containing 1-3 heteroatoms selected from O, N and S optionally substituted with on...
WO/2002/094849A2	PROCESS FOR THE PRODUCTION OF 6, 7 − DIHYDROXY STEROID COMPOUNDS BY ALLYLIC OXIDATION OF STEROID − 5 − ENE COMPOUNDS TO STEROID − 5 − ENE − 7 − ONE COMPOUNDS FOLLOWED BY HYDROBORATION AND OXIDATION AND INTERMEDIATES OF THIS PROCESS Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding &agr , β−unsaturated ketone using copper iodide and t−butyl hydroperoxide. A steroid compound containing the &agr , β−unsaturated ketone struc...
WO/2002/090375A2	LIVER X RECEPTOR AGONISTS A compound of formula (I), wherein each of R1, R2, R3, R4, R4', R5, R6, R7, R11, R12, R15, R16, and R17, independently, is hydrogen, halo, alkyl, haloalkyl, hydroxy, amino, carboxyl, oxo, sulfonic acid, or alkyl that is optionally insert...
WO/2002/088167A1	ANTI-INFLAMMATORY 17.BETA.-CARBOTHIOATE ESTER DERIVATIVES OF ANDROSTANE WITH A CYCLIC ESTER GROUP IN POSITION 17.ALPHA There are provided compound of formula (I) wherein R¿1? represents C¿1-6? alkyl or C¿1-6? haloalkyl; R¿2? represents C¿3-8? cycloalkyl or C¿3-8? cycloalkenyl either of which may optionally be substituted by one or more groups selec...
WO/2002/072003A2	USE OF STEROID DERIVATIVES FOR THE TREATMENT OF A BENIGHN AND/OR MALIGNANT TUMOUR The present invention relates to steroid derivatives for use as medicaments. More specifically, the invention also relates to the use of a steroid derivative of 5-androstene-, 5-pregnenolone or corresponding saturated derivatives (andros...
WO/2002/070537A2	FUSIDIC ACID DERIVATIVES Novel 17,20-methanofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.
WO/2002/062302A2	STEROIDAL DERIVATIVES A compound of formula (1), wherein each of R¿1?, R¿2?, R¿4?, R¿4'?, R¿7?, R¿11?, R¿12?, R¿15?, R¿16?, R¿17'?, independently, is hydrogen, hydroxy, amino, carboxyl, oxo, halo, sulfonic acid, -O-sulfonic acid, or alkyl that is op...
WO/2002/032922A1	PROCESS AND INTERMEDIATES FOR THE PRODUCTION OF 7-SUBSTITUTED ANTIESTROGENS A process for preparing an intermediate compound of formula (II): where X is as defined in the specification, R1 is haloalkyl, alkyl, alkenyl, cycloalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl or arylalkyl; R?2¿, R?3¿, R?4¿ and R?5�...
WO/2002/016393A1	17-ARYL-LINKER DERIVATISED ESTROGEN 3-SULPHAMATES AS INHIBITORS OF STEROID SULPHATASE There is provided a compound comprising a steroidal ring system and a group R?1¿ selected from any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring o...
WO/2002/016394A1	THIOETHER-SULPHAMATE STEROIDS AS STEROID SULPHATASE INHIBITORS AND ANTI-CANCER COMPOUNDS There is provided a compound of Formula (I) wherein X is a ring having at least 4 atoms in the ring; K is a hydrocarbyl group: R?1¿ is an optional group of the formula -L?1¿-S-R?1'¿, wherein L?1¿ is an optional linker group and R?1'�...
WO/2002/016392A1	OESTROGEN-17-SULPHAMATES AS INHIBITORS OF STEROID SULPHATASE There is provided a compound of Formula (I) wherein X is a ring system ; R?1¿ is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R?2¿ is any one of a sulphamate g...
WO/2002/012266A1	17.BETA.-CARBOTHIOATE 17.ALPHA.-ARYLCARBONYLOXYLOXY ANDROSTANE DERIVATIVE AS ANTI-INFLAMMATORY AGENTS 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...
WO/2002/012265A1	6.ALPHA., 9.ALPHA.-DIFLUORO-17.ALPHA.-`(2-FURANYLCARBOXYL) OXY&excl -11.BETA.-HYDROXY-16.ALPHA.-METHYL-3-OXO-ANDROST-1,4,-DIENE-17-CARBOTHIOIC ACID S-FLUOROMETHYL ESTER AS AN ANTI-INFLAMMATORY AGENT 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.
WO/2002/008243A1	OXIDATION PROCESS FOR PREPARING THE INTERMEDIATE 6.ALPHA.,9.ALPHA.-DIFLUORO-11.BETA.,17.ALPHA.-DIHYDROXY-16.ALPHA.-METHYL-ANDROST -1,4-DIEN-3-ONE 17.BETA.-CARBOXYLIC ACID The present invention relates inter alia to a novel oxidation process for the synthesis of a known intermediate, useful in the preparation of anti-inflammatory steroids, the known intermediate being of formula (I).
WO/2001/085944A2	PRODUCTION OF ADENINE NUCLEOTIDE TRANSLOCATOR (ANT), NOVEL ANT LIGANDS AND SCREENING ASSAYS THEREFOR Compositions and methods are provided for producing adenine nucleotide translocator (ANT) polypeptides and fusion proteins, including the production and use of recombinant expression constructs having a regulated promoter. ANT ligands an...
WO/2001/079255A1	A PROCESS FOR THE PREPARATION OF 7.ALPHA.-HYDROXY 3-AMINOSUBSTITUTED STEROLS USING INTERMEDIATES WITH AN UNPROTECTED 7.ALPHA.-HYDROXY GROUP 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 ...
WO/2001/074840A2	17-ALPHA-SUBSTITUTED-11-BETA-SUBSTITUTED-4-ARYL AND 21-SUBSTITUTED 19-NORPREGNA 21-SUBSTITUTED 19-NORPREGNADIENEDIONE AS ANTIPROGESTATIONAL AGENTS The present invention relates, $i(inter alia), to compounds having the general formula (I) in which: R?1¿ is a member selected from the group consisting of -OCH¿3? -SCH¿3?, -N(CH¿3?)¿2?, -NHCH¿3?, -NC¿4?H¿8?, -NC¿5?H¿10?, -NC¿...
WO/2001/068669A1	6-OXYGENATED STEROIDAL ESTROGENS WITH AROMATIC A AND B RINGS Novel estrogenic compounds of Formula (I) are provided, wherein the bond represented by the wavy line may be a single or double bond such that when the wavy line is a single bond, R¿1? is selected from the group consisting of hydrogen, ...
WO/2001/066562A1	STEROID DERIVATIVES AND PROCESS FOR PRODUCING THE SAME Steroid derivatives from which various estran derivatives (estran-3-O-sulfamate derivatives serving as an inhibitor of estrogen sulfatase producing estrogen which is a causative factor of estrogen-dependent mammary cancer, mammalian ster...
WO2000047603A9	16-HYDROXYESTRATRIENES AS SELECTIVE ESTROGENS The invention relates to novel compounds as pharmaceutical agents which have in vitro a higher affinity to estrogen receptor preparations of the rat prostate than to estrogen receptor preparations of the rat uterus and which preferably h...
WO/2001/062722A2	METHOD FOR THE PREPARATION OF FLUTICASONE AND RELATED 17BETA-CARBOTHIOIC ESTERS USING A NOVEL CARBOTHIOIC ACID SYNTHESIS AND NOVEL PURIFICATION METHODS This invention discloses a method of conversion of carboxylic acids to carbothiotic acids by reacting a caarbpxylic acid with a first base, an iodide salt, and a compound of formula (4) wherein the variables are as defined in the claims,...
WO/2001/055171A1	MOMETASONE AND ITS PREPARATION Mometasone (9$g(a),21-dichloro-1 $g(b),17$g(a)-dihydroxy-16$g(a)-methyl-pregna-1,4-dine-3,20- dione) is prepared from icomethasone (9$g(a)-chloro-11$g(b),17$g(a),21-trihydroxy-16$g(a)-methyl- pregna-1,4-diene-3,20-dione) by reaction ther...
WO/2001/052856A2	USE OF DEHYDROEPIANDROSTERONE, ITS PRECURSORS AND DERIVATIVES, BY ORAL ADMINISTRATION, AS HYDRATING AGENTS WITH DIRECT ACTION The invention concerns the use of at least a compound selected in the group consisting of dehydroepiandrosterone, its chemical precursors, its chemical derivatives, its biological precursors and metabolic derivatives, for preparing a com...
WO/2001/051056A1	FULVESTRANT FORMULATION The invention relates to a novel sustained release pharmaceutical formulation adapted for administration by injection containing the compound 7$g(a)-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra -1,3,5(10)-triene-3,17$g(b)-diol, ...
WO/2001/040805A1	STEROID COMPOUNDS FOR STEROID RECEPTOR BINDING ASSAYS The invention provides a compound having binding affinity for a receptor and comprising a steroid skeleton in its molecular structure, which compound is according to formula (1) wherein: Bu is a sterically bulky structure or Bu is a mole...
WO/2001/014406A1	ANTIANDROGEN AGENTS Androstane derivatives having various substituents at the 7- or 11-position, pharmaceutically acceptable salts thereof or prodrugs of the same and substances serving not as an agonist but as an antagonist for androgen receptors, pharmace...
WO/2000/066614A1	3$g(a)-HYDROXY-3$g(b) METHOXYMETHYL-21-HETEROCYCLE SUBSTITUTED STEROIDS WITH ANESTHETIC ACTIVITY This invention relates to compounds having Formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein; R¿1? is H or methyl; R¿2? is 5$g(a)- or 5$g(b)- H; R¿3? is an optionally substituted $i(N)-attached het...
WO/2000/064882A2	ENANTIOMERS OF MERCAPTO LACTONES AND PROCESSES FOR THEIR SYNTHESIS An improved process for the preparation of single enantiomers of formula (I), and novel intermediates and processes thereto.
WO/2000/063228A1	ENT-STEROIDS AS SELECTIVELY ACTIVE ESTROGENS This invention describes the new ent-steroids of general formula (I) in which R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?6¿, R?7¿, R?8¿, R?9¿, R?10¿, R?11¿ and R?19¿ have the meanings that are indicated in the description, as pharmaceut...
WO/2000/056759A1	PROCESSES FOR THE PREPARATION OF STEROID DERIVATIVES, INTERMEDIATES THEREFOR AND PROCESSES FOR THE PREPARATION OF THE INTERMEDIATES Steroid derivatives useful as the intermediate for preparing vitamin D derivatives such as 1$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 ...
WO/2000/053618A1	22R-HYDROXYCHOLESTA-8,14-DIENE DERIVATIVES FOR THE INHIBITION OF MEIOSIS 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 (...
WO/2000/053620A1	NOVEL ESTRADIOL DERIVATIVES Estradiol derivatives represented by general formula (I) (wherein R is optionally substituted phenyl). These derivatives (I) act as steroid sulfatase inhibitors and thus are efficacious against estrone-dependent diseases such as mammary ...
WO/2000/039148A1	NEW 7-ALPHA, 17-ALPHA-BIS-ALKYLATED TESTOSTERONE DERIVATIVES AND THEIR USE IN LONG-TERM THERAPY OF ANDROGEN-DEPENDENT DISEASES The invention relates to new 7$g(a), 17$g(a), 17$g(b)-substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term ant...
WO/1999/033855A1	11$g(b)-HALOGEN-7$g(a)-SUBSTITUTED ESTRATRIENES, METHOD FOR PRODUCING PHARMACEUTICAL PREPARATIONS CONTAINING SAID 11$g(b)-HALOGEN-7$g(a)-SUBSTITUTED ESTRATRIENES AND USE OF THE SAME FOR PRODUCING MEDICAMENTS The invention relates to novel 11$g(b)-halogen-7$g(a)-substituted estratrienes of formula (I), wherein R?11¿ is a fluorine or chlorine atom and the other substituents have the meanings given in the description. The inventive compounds h...
WO/1999/032127A1	ANGIOSTATIC AGENTS AND COMPOSITIONS FOR CONTROLLING OCULAR HYPERTENSION Compositions of angiostatic agents for treating GLC1A glaucoma and methods for their use are disclosed.
WO/1999/025725A1	NOVEL 19-NOR STEROIDS SUBSTITUTED IN POSITION 11$g(b), PREPARATION METHOD AND INTERMEDIATES, APPLICATION AS MEDICINES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 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...
WO/1999/020646A1	ESTRA-1,3,5(10)-TRIENE-7ALPHA-THIOETHERS 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...
WO/1999/001467A2	THERAPEUTICALLY ACTIVE COMPOUNDS WITH LOW SYSTEMIC ACTIVITY DUE TO REDUCE HALF LIFE There are described therapeutically active compounds or salts or solvates thereof, hydrolysable in human or animal blood to compounds with reduced therapeutic activity. There is also described a method of identifying a compound capable o...
WO/1998/055496A1	NON-ESTROGENIC ESTRADIOL DERIVATIVES WITH AN ANTIOXIDANT EFFECT 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...
WO/1998/052965A1	20-ARALKYL-5$g(a)-PREGNANE DERIVATIVES The invention relates to 20-aralkyl-5$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 ...
WO/1998/050413A1	PHARMACEUTICALLY ACCEPTABLE SALTS OF 3-HYDROXY-ESTR-5(10)-EN-17-ONE 3-SULPHATE ACTIVE AS ESTROGENS This invention provides a pharmaceutically acceptable salt of 3$g(b)-hydroxy-5(10)-estrene-17-one 3-sulfate ester and a pharmaceutically acceptable salt of 3$g(a)-hydroxy-5(10)-estrene-17-one 3-sulfate ester, which are useful as estrogens.
WO/1998/050414A1	B-RING ESTRATRIENE DIOL SULPHATES This invention provides estrogenic agents having formula (I) wherein A and B are each, independently, (a), (b), (c), or (d), R is SO�3??-�X?+�; X?+� is alkali metal, alkaline earth metal, ammonium, alkylammonium containing 1-6 ca...
WO/1998/050412A1	ESTROGENIC 19-NORADNROST-17-ONE DERIVATIVES WITH AN AROMATIC B-RING This invention provides 3$g(b)-hydroxy-5,7,9-estratriene-17-one and a pharmaceutically acceptable salt of its 3-sulfate ester, which is useful as an estrogen.
WO/1998/050415A1	PREGNANE 3,2O DIOL MONO- AND DI-SULPHATES This invention provides a compound having formula (I) wherein R and R?1� are each, independently, hydrogen or SO�3??-�X?+�; X?+� is alkali metal, alkaline earth metal, ammonium, alkylammonium containing 1-6 carbon atoms, or dia...
WO/1998/050411A1	PHARMACEUTICALLY ACCEPTABLE SALTS OF 5ALPHA-PREGNAN-3BETA, 16ALP HA-DIOL-20-ONE 3-SULFATE USEFUL AS PROGESTINS AND CNS DISORDERS The invention provides a pharmaceutically acceptable salt of 5$g(a)-pregnan-3$g(b), 16$g(a)-diol-20-one 3-sulfate ester, which is useful as a progestational agent.
WO/1998/050410A1	SALTS OF 5.ALPHA.-PREGN-16-EN-3.BETA.-OL-20-ONE 3-SULPHATE ESTER WITH PROGESTIN ACTIVITY This invention provides a pharmaceutically acceptable salt of 5$g(a)-pregn-16-en-3$g(b)-ol-20-one 3-sulfate ester, which is useful as a progestational agent.

Matches 151 - 200 out of 894	< 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 >