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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/1996/040727A1 |
The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a 19-nor-pregnane steroid, or a pharmaceutical composition containing a vomerophe...
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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/1996/038466A1 |
The invention relates to certains steroidal glycoside derivatives useful as hypocholesterolemic agents and antiatherosclerosis agents. The present invention is also directed to pharmaceutical compositions comprising such derivatives and ...
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WO/1996/032946A1 |
Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising: (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii...
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WO/1996/030390A2 |
Methods for the preparation of the 19-norprogesterone of formula (I) and its intermediates, in crystalline and amorphous forms.
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WO/1996/028414A1 |
This invention relates to triiodo benzoate derivatives useful as X-ray contrast agents for diagnostic imaging the blood pool, liver, spleen, and/or lymph system of a mammal, said derivatives having formula (I), wherein X is H, NR1R2 or C...
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WO/1996/027800A1 |
A method and kit for measurement of a steroid by means of a competitive immunoassay, preferably a competitive enzyme immunoassay. The method and kit involve the use of a steroid analogue conjugated to a label. The steroids that are amena...
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WO/1996/026201A1 |
Certain benzopyran antiestrogens are disclosed for treating estrogen sensitive diseases such as breast cancer. Prodrug forms provide ease of manufacturing, good shelf life, and bioavailibility, and preferred stereoisomers are shown to be...
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WO/1996/022791A1 |
The subject invention provides for novel synergistic compositions useful for inactivating viruses or inducing apoptosis in tumor cells and for treating cancer or retroviral infections. Generally, the compositions comprise one or a plural...
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WO/1996/022303A1 |
The present invention relates to a range of therapeutic compounds conjugated to one to three acyl groups derived from fatty acids. The therapeutic compounds are selected from the following group: 1) the corticosterone family of drugs; 2)...
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WO/1996/020713A1 |
The invention concerns the treatment of hyperandrogenic conditions in humans by the formation of a novel mechanism-based irreversible inhibitor of human 5'alpha'-reductase enzymes from 3-oxo-4-azasteroids having a 1,2-double bond and the...
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WO/1996/020208A2 |
The invention pertains to a new cholesterol derivative for liposomal gene transfer, applicable in the fields of medicine and genetic engineering. The new cholesterol derivative 3'beta' N-(N,N'-dimethylaminoethane)-carbamoyl cholesterol (...
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WO/1996/018609A1 |
The present invention is a method of protecting a sulfonic acid functional group in an organic molecule as a substituted or unsubstituted neopentyl sulfonate ester. The method allows the conversion of R-SO3-H to R'-SO3-H, wherein R and R...
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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/1996/017823A1 |
Cationic lipids of general formula (I), wherein m is an integer from 2 to 6 inclusive; n is an integer from 1 to 9 inclusive, preferably 1-5, where, when n is 2-9, a single R grouping other than hydrogen is present in the general formula...
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WO/1996/016076A1 |
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/1996/015795A1 |
Compositions and method for the minimization or prevention of adhesion formation, whereby an effective amount of at least one lazaroid compound, preferably one of general formula (I), wherein R represents a formula (Ia) or (Ib), or formu...
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WO/1996/011939A1 |
A process for providing novel compounds of formula (I), that are useful as 6-azaadrostenone testosterone 5-alpha-reductase inhibitors, from commercially available compounds of formula (II) wherein, R1 and R2 represent: i) indepedently H ...
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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/1996/010032A1 |
The invention relates to estrene steroid, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. The figure...
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WO/1996/010031A1 |
The invention relates to novel, androstane steroids which are the ligand semiochemicals which bind to neuroepithelial receptors.
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WO/1996/008505A1 |
Described are new steroid esters and amides of formula (I), wherein R1 is an 'alpha' or 'beta'-positioned C1-C3 alkyl group; Sk is -CC-(CH2)r-R2, (E) or (Z) -CH=CH-(CH2)r-R2, -(CH2)2-(CH2)r-R2, with R2 being an esterified or as amide der...
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WO/1996/007652A1 |
Synthetic calicheamicin mimics employ alternative activation triggers and trigger sites and include tethers for conjugation to DNA targeting systems.
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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/1996/004296A1 |
The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a pregnane or cholane steroid, or a pharmaceutical composition containing a vomer...
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WO/1996/003875A1 |
A water-soluble delivery system for nucleic acids to cells having androgen receptors, preferably prostate cells, is provided comprising a steroid moiety capable of binding to said receptors, said steroid moiety being covalently linked to...
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WO/1996/003420A1 |
The present invention provides a compound of formula (I), wherein A is a bond or a straight or branched C1-C6 alkylene chain; W is a group -R1, -OR2, -NR3R4 or (a) wherein: Y is oxygen or sulphur; R1, R2 and R4 are: a C1-C10 alkyl group,...
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WO/1996/002500A1 |
The invention relates to novel chelate formers containing sulphonamide groups and their metallic chelates of general formula (I) in which n, m, p, V1, V2, V3, V4, X1, X2, X3, R1, R2, R3 and R4 have different meanings, pharmaceutical agen...
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WO/1996/001840A1 |
The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two arginine, lysin...
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WO/1996/001841A1 |
The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two substituted arg...
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WO/1996/000230A1 |
The present invention relates to a process for the preparation and manufacture of 3-amino-substituted glycosylated bile acid derivatives. Novel intermediates and related compounds are also disclosed. In particular, the present invention ...
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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/1995/030684A1 |
17'beta'-Cyano-3,17'alpha'-dihydroxy-6-methylandrosta-3,5,9(
11)-triene 3-ethyl ether (II) is prepared by reacting 3-hydroxy-6-methylandrosta-3,5,9(11)-trien-17-one 3- ethyl ether (I) with hydrogen cyanide at a pH of about 7 to about 11....
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WO/1995/029931A1 |
Described is a method for stereoselective insertion of an alkynyl side chain --R2, where R2 is a hydrogen atom, a methyl group or a hydroxymethyl group in which the hydroxy group is protected, in the 17'beta'-position of a 13'alpha'-alky...
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WO/1995/029932A1 |
The present invention provides 4-nitro-'DELTA'4-3-ketosteroids, their use as steroid C17-20 lyase and 5'alpha'-reductase inhibitors and to a novel process for preparing a compound of formula (I), comprising sequentially: a) reacting a st...
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WO/1995/029155A1 |
Novel N-acyl-aminoalkyl phenyl ether compounds having general formula (I), wherein A is an aromatic ring such as phenyl, thienyl, furyl, pyridyl; R1, R2 and R3 are selected from H, alkyl, halogen, electron acceptors and electron donors; ...
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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/1995/024415A1 |
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/1995/021185A1 |
Invented are 17'alpha' and 17'beta'-substituted acyl 3-carboxy aromatic A ring steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-'alpha'-redu...
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WO/1995/019567A1 |
The invention is directed to synthetic receptor(s) which comprises a polyfunctional organic template covalently linked to two or more oligomers which may independently be the same or different and may independently be straight chain, cyc...
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WO/1995/019186A2 |
Metabolically labile esters, and contrast media for X-ray and magnetic resonance imaging comprising these esters, wherein the esters have formula (I) in which R3 is a steroid residue, the esters containing at least one iodine atom and/or...
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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/1995/014709A1 |
The present invention provides compounds of formula (I) wherein A, R1, R2, R3 and Z are defined in the description. The compounds of formula (I) are testosterone 5'alpha'-reductase inhibitors and are therapeutically useful in the treatme...
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WO/1995/013287A1 |
Steroids are disclosed with radical-attracting aromatic substituents of general formulae (I) and (II). The new steroids with radical-attracting aromatic substituents are suitable active ingredients in pharmaceuticals for use in the preve...
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WO/1995/012398A1 |
Compounds of formula (I) are inhibitors of 5'alpha'-reductase and are useful alone or in combination with 5'alpha'-reductase 1 and/or 2 inhibitors for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hi...
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