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WO/1994/020520A1 |
Compounds having a broad range of antimicrobial activity generally have a structure including a steroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compou...
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WO/1994/016709A2 |
Sex steroid precursors such as dehydroepiandrosterone and dehydroepiandrosterone sulphate, and compounds converted in vivo to either of the foregoing, are utilized for the treatment and/or prevention of vaginal atrophy, hypogonadism, dim...
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WO/1994/011386A1 |
Invented are 17alpha and 17beta-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-alpha-red...
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WO/1994/011004A1 |
Invented are 17alpha and 17beta-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-alpha-red...
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WO/1994/001449A1 |
This invention relates to a method for the preparation of (25R)-26-aminocholesterol, a potent inhibitor of cholesterol biosynthesis, from (25R)-16-oxo-26-phthalimidocholesterol.
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WO/1993/025539A1 |
The invention relates to novel piperazinyl-bis(alkylamino)pyrimidine derivatives of formula (I), wherein two of X, Y and Z mean a nitrogen atom each and the third one is a methine group; R?1¿ and R?2¿ represent, independently from each...
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WO/1993/025570A1 |
The invention relates to novel, therapeutically active 21-aminosteroids of formula (I) with pregnane skeleton, wherein two of X, Y and Z mean a nitrogen atom each and the third one is a methine group; R?1¿ and R?2¿ represent, independe...
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WO/1993/023038A1 |
Novel amino substituted 4-azasteroid 5alpha-reductase inhibitors of formula (I), wherein A is (a), (b) or (c), are claimed as well as pharmaceutically acceptable salts and formulations thereof. These compounds are effective in inhibiting...
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WO/1993/023053A1 |
Inhibitors of testosterone 5alpha-reductase activity, for example those of formula (I) wherein novel substituents are provided at the R4, R6, R7, R17alpha and/or R17beta positions are useful for the treatment of diseases whose progress i...
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WO/1993/023020A1 |
Competitive progesterone antagonists, including two novel steroids, viz., 11$g(b),19-[4-(cyanophenyl)-o-phenylene]-17$g(b)-hydroxy-17$
g(a)-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one and 11$g(b),19-[4-(3-pyridinyl)-o-phenylene]-17$g(b)-...
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WO/1993/022333A1 |
Invented are 17$g(a) and 17$g(b)-substituted acyl-3-carboxy aromatic A ring analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-$g...
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WO/1993/020097A1 |
Compounds of general formula (1) wherein X represents the residue of the A, B and C rings of a steroid, R represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, R?14¿ represents a hydrogen atom and R?15¿ represents a hydr...
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WO/1993/018053A1 |
This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3alpha-hydroxy,3beta-substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereoselectiv...
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WO/1993/017717A1 |
Compositions and methods for modulating the activity of RNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. The reactive portions preferably compris...
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WO/1993/018010A1 |
Benzimidazole anthelmintic agents of formula (I) and their non-toxic salts in which R is H, CO2(C1-C10 alkyl), -CO2(cholester-3-yl) or -CO2(CH2)COOH or -CO2(CH2)nCO2(C1-C6 alkyl), n = 1 to 10, R1 is optionally substituted benzoyl, phenyl...
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WO/1993/017692A1 |
Viral infection is inhibited in mammals by administration of metabolically stable, non-toxic 2',5'-oligoadenylate (2-5A) derivatives that have a dual therapeutic effect. The compounds activate the intracellular latent 2-5A dependent endo...
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WO/1993/016097A1 |
Invented is an improved process for the preparation of substituted steroidal dienes. Also invented are novel intermediates used in said process.
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WO/1993/015103A2 |
Novel steroids having a 9alpha-hydroxy or a 9alpha-carbonate substituent can be prepared from 9alpha-hydroxyandrostenedione and can be utilized in the synthesis of commercially valuable corticosteroids such as betamethasone. The 9alpha-c...
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WO/1993/014106A1 |
The invention provides an improved process for the preparation of a halogenated steroidal diene. The process involves the simultaneous transformation of the steroidal 3-one to 3-halo and 17-carboxylic acid to 17-carboxamide in a single r...
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WO/1993/013123A1 |
Compounds of formula (I), wherein R17 and R'17 are such that: either R17 and R'17 together form ketone, hydrazono, oxime or methylene, or R17 is hydroxyl, hydroxymethyl or acyloxy and R'17 is hydrogen, alkyl or optionally substitued alke...
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WO/1993/011772A1 |
Novel glycosylated steroid derivatives for facilitating the transport of compounds across biological membranes, either in admixture or as conjugates, are disclosed. A novel process for efficient synthesis of these glycosylated steroid de...
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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/1993/005064A1 |
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: sulph...
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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/1992/020700A1 |
The present invention concerns steroidic 5alpha-reductase inhibitors having formula (I), wherein Y is oxygen or sulphur; R is a group: a) -OR4, wherein R4 is hydrogen or a C1-C6 alkyl group; b) (1), wherein each of R5 and R6, independent...
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WO/1992/018089A2 |
The sensitizing amines of the present invention, illustrated by the steroidal amines (I), the alkyl amines (II), bicyclic amines (III), bicyclic ethers (IV), tricyclic compounds (V), indoles (VI) and various species are useful in treatin...
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WO/1992/014474A1 |
Methods of treatment for osteoporosis in a human or other animal subject, comprising: administering a bone-active phosphonate to said subject, at a level of at least about 0.1 LED per day of said treatment; and administering an estrogen ...
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WO/1992/011277A1 |
Compounds have general formula (I), in which X stands for an oxygen atom or for the hydroxyimino grouping >N$m(k)OH; R?1¿ stands for a hydrogen atom or for a methyl group; G stands for a hydrogen, halogen atom, a C¿1?-C¿4? alkyl resid...
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WO/1992/011278A1 |
New compounds having the general formula (I), as well as their pharmacologically acceptable addition salts with acids, are disclosed. In the formula (I), either (Ia) R?11¿ stands for a hydrogen atom in the $g(b) position, whereas R?12¿...
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WO/1992/003568A1 |
Compositions and methods are provided for the treatment and diagnosis of diseases amenable to modulation of the production of selected proteins. In accordance with preferred embodiments, oligonucleotides and oligonucleotide analogs are p...
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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/1991/018917A1 |
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' stand for protecte...
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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/1991/016897A1 |
Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine r...
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WO/1991/011453A2 |
The present invention discloses 5-oxygenated amino substituted pyrimidines (X), where R1 is (1) steroid substituent of formula (Steroid), (2) trolox substituent of formula (trolox), (3) an alkyl substituent selected from the group consis...
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WO/1991/010743A1 |
The invention is directed to the control of cellular autophagy, cellular agglutination and the immobilization of motile cells. Such control is useful in, for example, the treatment of cancer, contraception, termination of pregnancy, remo...
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WO/1991/010671A1 |
Compositions and methods for modulating the activity of RNA and DNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. Reactive portions which act, alt...
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WO/1991/008218A1 |
A process for preparing oxazoline corticosteroid intermediates of formula (V) wherein R1 represents hydrogene (H), loweralkyl, phenyl or phenylalkyl; R4 represents H or loweralkyl, preferably methyl having either the alpha or beta stereo...
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WO/1991/006527A1 |
A substituted aminoalkylbenzene derivative of general formula (I) or its salt, and anti-inflammatory and antirheumatic drugs containing the same as the active ingredient. These compounds have excellent anti-inflammatory and antirheumatic...
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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/1990/015798A1 |
The invention relates to novel aminoalkyl maleimides of general formula (I) in which R¿1? and R¿2? are the same or different and represent hydrogen or a C¿1?-C¿4? alkyl group and A is a straight or branched-chain, saturated or unsatu...
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WO/1990/015816A1 |
The invention is a method of treating angiogenesis in a warm blooded mammal who is in need of such treatment which comprises administration of an angiogenic inhibiting amount of a combination of a suramin-type compound and an angiostatic...
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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/1990/013558A1 |
Method for preparing 21-brom-4-pregnen-3,20-dione derivatives of general formula (I), in which R¿1? is a hydrogen atom, a hydroxy group or an alkanoyl group with 1 to 6 carbon atoms, R¿2? is a hydrogen atom or a methyl group, or in whi...
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WO/1990/012577A2 |
A method of inhibiting hair growth in mammals which comprises the topical administration of a composition comprising an anti-angiogenic effective amount of an angiostatic compound of formula (I). The formula (I) compound is present in an...
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WO/1990/008128A1 |
Compounds of formula (I), wherein D represents the dehydrogenated residue of a hydroxyl group-containing drug or the dehydrogenated residue of an NH-acidic group-containing drug; the substituents in the phenyl ring alpha and beta are in ...
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WO/1990/003385A1 |
New 11beta-phenyl-14betaH-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N ~ OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an alpha-permanent hydroxy group ...
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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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