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WO/1993/010141A2 |
Angiostatic steroids for use in controlling neovascularization and ocular hypertension are disclosed. Pharmaceutical compositions of the angiostatic steroids and methods for their use in treating neovascularization and ocular hypertensio...
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WO/1993/007883A1 |
Linked nucleosides having at least one functionalized nucleoside that bears a substituent such as a steroid molecule, a reporter molecule, a non-aromatic lipophilic molecule, a reporter enzyme, a peptide, a protein, a water soluble vitam...
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WO/1993/005063A1 |
Novel steroid sulphatase inhibitors are disclosed as well as pharmaceutical compositions containing them for use in the treatment of oestrone dependent tumours, especially breast cancer. The novel steroid sulphatase inhibitors are sulpho...
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WO/1993/003732A1 |
Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid recept...
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WO/1992/017185A1 |
The invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein [D] is the residue of a drug having a reactive functional group, said functional group being attached, directly or through a bridg...
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WO/1992/015604A1 |
Compounds are provided which are highly selective inhibitors of the cytochrome P-450C17, commonly known as 17,20-lyase enzyme, responsible for androgen biosynthesis. These compounds can be administered to patients to inhibit the producti...
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WO/1992/014746A1 |
Starting compounds for preparing calcitriol (1$g(a), 25-dihydroxycholecalciferol) and its derivatives showing, as compared with calcitriol, some modifications, particularly in the C-17 lateral chain, a method for preparing these starting...
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WO/1992/014493A1 |
A non-protein intracellular receptor binding molecule conjugated to therapeutic and diagnostic agents via a linker molecule is provided. A method for the intracellular delivery in vivo of therapeutic or diagnostic agents is also provided.
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WO/1992/012983A1 |
The present invention provides a novel compound represented as formula (I). The present novel compound is prepared by reacting fluorine with pyridine-boron trifluoride and is useful as a fluorinating agent in the fluorination of organic ...
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WO/1992/012989A1 |
Described are new sterol esters and sterol phosphorus compounds with an anti-tumour action, methods of preparing them and of preparing spontaneously dispersible agents, as well as methods of developing therapeutic preparations containing...
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WO/1992/009619A1 |
The present invention is directed to 2beta,19-(methyleneamino)androst-4-ene-3,17-dione and the corresponding 17beta-ol which are useful as aromatase inhibitors. The compounds are prepared by the cyclization of an appropriate 19-N-protect...
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WO/1992/005187A1 |
The invention concerns compounds of formula (I), in which SP is a spacer, Z is a valency bond, (a), (b), NH or S, A is hydrogen, a hydroxy group or an amino group which may be substituted by a lower-alkyl group, alk is a straight-chain o...
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WO/1992/001699A1 |
Platinum complexes are disclosed which contain at least one leaving group and at least one detectable group. These complexes can be used for diagnostic purpose and for the labelling of nucleic acids. Specific example is Pt(ethylenediamin...
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WO/1992/000988A1 |
The invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein [D] is the residue of a drug having a reactive functional group, said functional group being attached, directly or through a bridging ...
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WO/1992/000010A1 |
Invented is a method of treating human prostatic adenocarcinoma by employing a steroid 5-alpha-reductase inhibiting compound or a combination of steroid 5-alpha-reductase inhibiting compounds.
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WO/1991/019731A1 |
Novel angiostatic $g(D)?4,9(11)�-steroids (I), C�21?-oxygenated steroids (II) and other known steroidal compounds have been found to be useful in treating angiogenesis in mammals who have a need for the same. These steroids are usefu...
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WO/1991/018918A1 |
Compounds of general formula (III), in which A and B together stand for an additional bond and D stands for a hydrogen atom or B and D together stand for an additional bond and A stands for a hydrogen atom and Y and Y' each stand for a p...
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WO/1991/018007A1 |
Fluorescent dyes which are free of aggregation and serum binding are provided. These dyes are suitable for applications such as fluorescence immunoassays, in vivo imaging and in vivo tumor therapy.
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WO/1991/018006A1 |
Marker components are provided which are compatible with aqueous solutions, exhibit favorable fluorescence properties and exhibit decreased non-specific binding to macromolecules in solution. These marker components are useful in applica...
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WO/1991/017175A1 |
The novel intermediate products of general formula (I) in which: R?1� is a hydrogen atom or a straight-chained or branched alkyl group with 1 to 4 carbon atoms; R?2� is a hydrogen atom or a methyl group; R?3� is a hydrogen atom; an...
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WO/1991/013080A1 |
Pseudonucleosides and pseudonucleotides are useful in the synthesis of oligomers which contain these components as a means to derivatize the resulting oligonucleotide. In general, these pseudonucleotide components are of formula (1), whe...
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WO/1991/013083A1 |
3-Monoalkyl thiophosphonate steroid esters are disclosed as inhibitors of steroid sulphatase activity and as potential therapeutic agents in the treatment of oestrogen dependent cancers, in particular oestrone 3-monomethylthiophosphonate...
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WO/1991/012206A2 |
Novel aromatase inhibitors are disclosed for use in therapeutic preparations for treatment of estrogen-dependent diseases. The compounds are specified 7alpha-substituted androstanedione and androstenedione derivatives which show a strong...
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WO/1991/003245A1 |
Pharmaceutical compositions useful in the treatment of ophthalmic inflammation and methods of treating ophthalmic inflammation with those compositions ar disclosed. The compositions contain a combination of a glucocorticoid and an angios...
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WO/1991/000732A1 |
Methods for treating sex steroid-dependent diseases by inhibiting sex steroid activity include administration of novel compounds which include an androgenic nucleus substituted at a ring carbon with at least one substituent specified her...
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WO/1990/015068A1 |
The present invention is a process for conversion of DELTA16-steroids (I), to the corresponding DELTA17(20)-20-silyl ether (III), by reaction with (1) a preformed copper hydride or a metal hydride reducing agent in the presence of a copp...
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WO/1990/014822A1 |
Oligonucleotides modified at their backbones by the attachment of at least one steroid are described. The modified oligonucleotides anchor in the cell membrane to serve as a probe and to provide therapeutic activity.
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WO/1990/013282A2 |
New decorative compositions which contain non-chiral compounds of formula (I), and chiral steroid esters of formula (II), wherein R1, R2, R3, A, X1, X2, Ster, m, and n have the meaning given in Claim 1.
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WO/1990/010448A2 |
A conjugate is provided wherein a lipid is covalently coupled to an oligonucleotide having a nucleotide sequence that is either of interest or substantially complementary to a nucleotide sequence of interest. The conjugate is useful for ...
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WO/1990/010638A1 |
The invention concerns cytostatic conjugates, e.g., antineoplastic alkylants, antibiotics, anthracene diones, metal complexes and substances of vegetable origin or semisynthetic derivatives, which are linked by means of suitable connecti...
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WO/1990/007520A1 |
Oxysteryle phosphates according to formula (I), where R1 is an oxysteryle radical; where R2 is H or a radical derived from: (a) a natural or synthetic nucleotide structure, (b) a non-nucleotide anticancer agent, (c) an immunodepressive o...
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WO/1990/000560A1 |
Steroid compounds represented by general formulae (I), (II) or (III), wherein R1 and R2 each represents a hydrogen atom or a hydroxyprotecting group, R represents -CH2-X, a carboxyl group or a protected carboxyl group, X represents a sub...
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WO/1990/000174A1 |
The invention concerns 13-Alkyl-11beta-phenylgonanes of general formula (I), wherein Z, R1, R2, R3 and R4 have the meaning given, a process for their preparation, pharmaceutical preparations containing these compounds, and their use for ...
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WO/1990/000175A1 |
An ursodeoxycholic acid derivative of formula (I) has therapeutic activity in biliary calculosis, biliary dyscinesia, reflux gastritis and in some hepatopathies.
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WO/1989/001483A1 |
The invention involves a two-step chemical transformation of a steroidal 17-cyanohydrin of formula (II) to a 17alpha-hydroxy-21-halo-20-keto steroid of formula (IV) intermediate which can readily be converted to pharmaceutically useful c...
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WO/1989/000578A1 |
New 11beta-phenyl-4,9,15-estratrienes have general formula (I) where X is an oxygen atom or an N-OH hydroxyimino grouping, R1 is a hydrogen atom or a methyl group, R2 is a hydrogen atom, or an alkyl or acyl residue with 1 to 10 carbon at...
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WO/1988/008002A1 |
This invention provides novel cyclic hydrocarbons of formula (I), wherein R is selected from the group consisting of CH2=CH-CH2-, HO-CH2CH2CH2-, and CH3; wherein R1 is selected from the group consisting of m-trifluoromethylphenylmethyl, ...
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WO/1988/007545A1 |
Pregnane derivatives represented by general formula (I) (wherein A1 represents a hydrogen atom or a hydroxy group, A2 represents a substituent such as a hydroxy group when A1 represents a hydrogen atom, or A2 represents a hydrogen atom w...
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WO/1988/005439A1 |
Complex comprised of a bioreagent alkilated-complexed by an organo-metallic compound. Said organo-metallic compound comprises a cluster of alcyne-carbonyle metal. Application of complexes of bioreagents as tracers for dosings of biologic...
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WO/1988/003534A1 |
17beta-Cyano-17alpha-hydroxy steroids (I) are transformed to 17alpha-halo silyl ethers (II) which are intermediates useful in the production of progesterones (V), 17-hydroxyprogesterones (VI), corticoids (VII) and 21-halo corticoids (III...
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WO/1988/002753A2 |
New 9-alpha-hydroxy steroids are prepared by the introduction of substituents on the D-ring of 9-alpha-hydroxy-androst-4-ene-3,17-dione. The resulting compounds are useful intermediates in the synthesis of corticosteroids.
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WO/1988/001868A1 |
Steroids of formula (I) which are characterized by a 17alpha-cyanomethyl, azidomethyl, methoxymethyl, phenylmethyl, or ethynylmethyl substituent and a 17beta-hydroxy/esterified hydroxy substituent. The steroids of this invention have glu...
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WO/1988/001274A1 |
A compound of general formula (I), in substantially pure form, wherein A is a cation. A method for preparation is also disclosed, together with compositions and methods of use thereof.
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WO/1987/007612A1 |
Process for the production of a DELTA17(20)-steroid of formula (II) which comprises starting with a 16-unsaturated corticoid of formula (I) and contacting the 16-unsaturated corticoid (I) with a methylating agent in the presence of a cop...
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WO/1987/006936A1 |
Sodium salt of sialosylcholesterol which has an excellent solubility in water and is useful as a drug for treating various diseases induced by disturbances of a peripheral or central nervous system.
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WO/1987/006237A1 |
A process is used for producing 7alpha-propylsteroids having general formula (I), wherein R1 is a beta-hydroxy group and R2 is hydrogen or a alpha linked -CH2-CH2COOR5 residue, R1 and R2 form together the residue (A), R3 and R4 are hydro...
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WO/1987/002672A1 |
Novel tetrahydro steroids which are useful in inhibiting angiogenesis and have the following structure: A compound of formula (I), wherein R15 is = O or -OH; wherein R23 with R10 forms a cyclic phosphate of formula (II) or wherein R23 is...
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WO/1987/002367A2 |
Provided are cyclic hydrocarbons of Formula (I) with an aminoalkyl sidechain that are useful for treating phospholipase A2-mediated conditions, diabetes and obesity.
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WO/1986/001208A1 |
Stereoisometrically pure DELTA2 compound of formula (I) wherein R1 is hydrogen or -(C=O)-R2, wherein R2 is an organic substituent selected from the group consisting of alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkylalkylenes, haloalk...
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WO/1986/000312A1 |
Cycloartenyl ferulate-cyclodextrin complex can be prepared by including cycloartenyl ferulate, a difficultly water-soluble component of gamma-oryzanol, with cyclodextrin. The complex has an increased water solubility and an improved abso...
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