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WO/1998/033506A1 |
This invention relates to novel inhibitors of androgen synthesis that are useful in the treatment of prostate cancer and benign prostatic hypertrophy. The present invention also provides methods of synthesizing these novel compounds, pha...
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WO/1998/031702A1 |
The present invention relates to 16-hydroxy-11-(substituted phenyl)-estra-4,9-diene derivatives according to formula (I), wherein R�1? is C�1-6?alkyl, C�3-6?cycloalkyl, C�1-6?alkoxy, triflate, pyridyl or phenyl where the phenyl m...
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WO/1998/027106A1 |
An aminosterol compound according to formula (I) wherein R�1? is a member selected from the group of: (a), wherein R�6? is H or (b); (c); and (d); R�2? is H or OH; R�3? is H or OH; R�4? is H or OH; and R�5? is a C�1? to Cï¿...
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WO/1998/013007A2 |
Fatty acid derivatives of disulfide-containing compounds (for example, disulfide-containing peptides or proteins) comprising fatty acid-conjugated products with a disulfide linkage are employed for delivery of the compounds to mammalian ...
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WO/1998/007740A1 |
The present invention describes new substituted 7$g(a)-($g(j)-aminoalkyl)-estratrienes of general formula (I), in which the side chain SK is a radical of partial formula (II), where m equals 4, 5 or 6; n equals 0, 1 or 2; x equals 0, 1 o...
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WO/1998/002161A1 |
Deoxynojirimycin derivatives containing a large hydrophobic moiety, such as cholesterol or adamantame-methanol, linked through a spacer, such as pentamethylene, to the nitrogen atom of deoxynojirimycin, and salts thereof, inhibit glucosy...
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WO/1998/002191A2 |
Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. By this invention, such cationic amphiphile is used in a state in which it is capable of accepting additional pr...
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WO/1998/002190A2 |
Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. The amphiphiles contain lipophilic groups derived from steroids, from mono or dialkylamines, or from alkyl or ac...
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WO/1997/042215A1 |
A process for preparing 27-hydroxy cholesterol and derivatives thereof. The process includes the conversion of the terminal acid or ester moiety to a reactive halomethyl moiety, which is eventually reduced to a hydroxy moiety after alkyl...
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WO/1997/040061A1 |
Estrogen-nucleoside, estrogen-guanine and estrogen-mercapturate adducts are potential biomarkers for determining susceptibility of animals to a number of estrogen related cancers. These adducts may be used as biomarkers for determining r...
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WO/1997/039019A1 |
The present invention discloses compounds which are cationic cholesteryl derivatives having a nitrogen-containing ring structure as their polar head group. These compounds are useful for delivering biologically active substances to cells...
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WO/1997/027211A1 |
Novel potentiating steroid carbamates having the general formula (I) ST-OCONR1R2 wherein ST is a steroid or steroid derivative, R1 and R2 are the same or different, or may together form a ring, and R1, R2 is hydrogen or the group (i) whe...
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WO/1997/011702A1 |
The instant invention involves a method of preventing androgenetic alopecia and promoting hair growth, by administering to a patient in need of such treatment, particularly individuals predisposed to androgenetic alopecia, including men ...
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WO/1997/010217A1 |
Compounds of structural Formula (I), and pharmacologically acceptable salts and esters thereof possess 5'alpha'-reductase inhibitory activity. These compounds inhibit 5'alpha'-reductase type 1 and type 2. The compounds of structural Form...
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WO/1996/041144A2 |
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. Fluorescence immunoassays methods are p...
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WO/1996/040726A1 |
The present invention provides novel carbamate-based cationic lipids of general structure (I) or a salt, or solvate, or enantiomers thereof wherein: (a) R1 is a lipophilic moiety; (b) R2 is a positively charged moiety; (c) n is an intege...
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WO/1996/040725A1 |
The present invention provides novel phosphonic acid-based cationic lipids of general structure (I), or a salt, or solvate, or enantiomers thereof wherein: (a) R1 is a lipophilic moiety; (b) R2 is a positively charged moiety; (c) R3 is a...
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WO/1996/040043A2 |
The invention relates to 3'alpha'-hydroxy, 17-(un)substituted derivatives of the androstane series and 3'alpha'-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified ...
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WO/1996/038464A1 |
The invention discloses steroid conjugates having structures (I) or (II) where Y is NHCH2CH2CH2CH2NH2, NH(CH2)3NH(CH2)4NH(CH2)3NH2, or NHCH2CH2NHCH2CH2NHCH2CH2NH2, and each of R1, R2, R3 and R4 is individually H, OH and OSO3H. These conj...
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WO/1996/038465A1 |
This invention is related to alkyl substituted 2'beta'-morpholino-androstane derivatives, bonded at their 2'beta'-position to the nitrogen of a group of formula (I), wherein Ra represents (3-6C) alkyl; Rb represents H or (3-6C) alkyl; an...
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WO/1996/022100A1 |
Compounds of formula (I) are inhibitors of 5'alpha'-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern...
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WO/1996/018372A2 |
Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. The amphiphiles contain lipophilic groups derived from steroids, from mono or dialkylamines, or from alkyl or ac...
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WO/1996/011206A1 |
The disclosed invention is a process for preparing 17-beta-substituted-androsta-3,5-dien-3-carboxylic acids from 3-halo-17-beta-substituted-androsta-3,5-dienes. The process may be performed in either of two ways: (1) the 3-halo compound ...
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WO/1996/005216A1 |
The invention concerns novel estra-1,3,5(10)-triene amidosulphamates with an R-SO2-O- group in the 3-position, R being an R1R2N- group in which R1 and R2, independently of each other, are a hydrogen atom, an alkyl group with 1 to 5 C-ato...
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WO/1996/005217A1 |
The invention concerns pharmaceutical compositions containing as the active substance estra-1,3,5(10)-triene derivatives with an R-SO2-O- group on the 3 C-atom, R being an R1R2N- group in which R1 and R2, independently of each other, are...
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WO/1996/003421A1 |
6'alpha'-Hydroxy-21-[4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidiny
l]-1-piperazinyl]-16'alpha'-methylpregna-1,4,9(11)-triene-3,
20-dione, 6'beta'-hydroxy-21-[4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl
]-1-piperazinyl]-16'alpha'-methylpregna-1,4,...
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WO/1996/000235A1 |
Certain sterols which can be extracted from bull testes and from human follicular fluid and chemically related sterols can be used for regulating the meiosis in oocytes and in male germ cells.
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WO/1995/033761A1 |
Invented are 17 'alpha' and 17 'beta'-substituted aromatic A ring steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-'alpha'-reductase.
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WO/1995/029186A1 |
The present invention relates to methods and compositions for the transformation of cells. In particular, compositions and methods are disclosed which include combinations of the nucleic acid of interest and polyhydroxylated or polyglyco...
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WO/1995/028413A1 |
Invented are 17'beta'-substituted 3-carboxy steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-'alpha'-reductase.
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WO/1995/027702A1 |
Novel acridinium esters that are useful, either alone or when incorporated into liposomes, as chemiluminescent agents in binding assays (e.g., immunoassays and gene probe assays) with improved sensitivity are disclosed. In addition, the ...
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WO/1995/024415A1 |
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/1995/021617A1 |
Methods, compositions, and compounds for modulating the GABAA receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.
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WO/1995/021184A1 |
This invention is directed to novel purine-based compounds for inclusion into oligonucleotides. The compounds of the invention, when incorporated into oligonucleotides are especially useful as "antisense" agents -- agents that are capabl...
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WO/1995/020567A1 |
A codrug composition of at least two drug compounds covalently linked to one another via a labile bond to form a single codrug composition, and methods of use of the codrug for the treatment of various medical conditions. The codrug may ...
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WO/1995/018141A1 |
A medicinal composition containing a compound represented by the general formula (I): X-Y-Z (wherein Y represents a group represented by any of general formulae (III) to (V), X represents a monovalent radical derived from a tetracycline ...
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WO/1995/014707A1 |
This invention presents novel purine-based compounds for inclusion into oligonucleotides. The compounds of the invention, when incorporated into oligonucleotides are especially useful as "antisense" agents -- agents that are capable of s...
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WO/1995/011914A1 |
The present invention relates to 'DELTA'16 unsaturated C17 heterocyclic steroids which are useful as steroid C17-20 lyase inhibitors.
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WO/1995/009177A1 |
A glycoside represented by formula (I), wherein dexamethasone or betamethasone is the aglycon and the 21-position is substituted by a simple sugar or an acylated sugar selected from the group consisting of glucose, galactose, mannose, rh...
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WO/1995/009178A1 |
A method of preparing a 3'beta'-hydroxy- or 3'beta'-(lower acyloxy) 16,17-ene-17-(3-pyridyl)-substituted steroid, wherein the 3'beta'-(lower acyloxy) group of the steroid has from 2 to 4 carbon atoms, which comprises subjecting a 3'beta'...
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WO/1995/008559A1 |
Urethane-containing aminosteroid compounds and the pharmaceutically-acceptable acid salts or esters thereof of general formula (I) wherein R1, R2, R3, R4 and R14 are defined in the description, with R3 being a urethane-containing group.
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WO/1995/006474A1 |
Nucleosides and linked nucleosides functionalized to include alkylthiol chemical functionality at ribofuranosyl positions, nucleosidic base positions, or on internucleoside linkages. In certain embodiments, the compounds of the invention...
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WO/1995/000147A1 |
Compounds of formula (I), wherein: R1 is selected from the group consisting of hydrogen and methyl; R2 is selected from the group consisting of methyl and ethyl; R3 is selected from the group consisting of hydrogen and methyl; and the C1...
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WO/1994/027608A1 |
Methods and compositions for interacting with the GABAA receptor complex to induce sleep in humans using certain 5 3alpha-hydroxy-5-reduced steroid derivatives.
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WO/1994/026767A1 |
Androgen nucleus derivatives having specified substituents at the 17alpha position are disclosed for use as antiandrogens for the treatment of androgen-dependent diseases. In some preferred embodiments, the compound EM-250 is formulated ...
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WO/1994/024146A1 |
Androgens and their derivates and analogs, such as anabolic agents, are characterized by at least one substituent or substituent grouping with radical trapping properties. These compounds are used as androgen or anabolic agent substitute...
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WO/1994/022898A1 |
Glucocorticoids have the general formula (I): R-Val-O-GC, in which O-GC stands for the rest of an anti-inflammatory 21-hydroxycorticoid, Val stands for a valine residue located at the 21st position of the corticoid and R stands for a hyd...
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WO/1994/021667A1 |
A compound represented by the following formula: X-Y-Z, wherein Y is represented by any of the formulae (III) to (V), X represents a monovalent group of a tetracycline compound, and Z represents a monovalent group of a stereoid compound ...
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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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