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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/1994/000125A1 |
Invented are 17alpha and 17beta-alkylketone-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-alpha-re...
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WO/1994/000155A1 |
The use of nor- and homo- bile acids derivatives as absorption enhancers for medicaments. Said derivatives show the advantage of improving the absorption of medicaments through mucosae without being metabolized by the intestinal flora, t...
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WO/1993/025568A2 |
Novel antihypercholesterolemic agents are provided. An exemplary group of compounds has structural formula (I), wherein R is a C-17 side chain, R?1¿ is -OH, =O, or the like, R?8¿ and R?9¿ are independently hydrogen or lower alkyl, and...
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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/1993/023376A1 |
Described is a new process for producing 7beta-substituted-4-aza-5alpha-androstan-3-ones and related compounds which are 5alpha-reductase inhibitors, consisting of reducing the corresponding androsteneone with lithium and liquid ammonia,...
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WO/1993/023039A1 |
Described are new 16-substituted and 7,16-disubstituted 4-aza-5alpha-androstan-3-ones and related compounds as 5alpha-reductase inhibitors.
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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/1993/023419A1 |
Described are new 7beta-substituted 4-aza-5alpha-cholestan-3-ones and related compounds as 5alpha-reductase inhibitors.
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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/1993/021204A1 |
A method is provided for synthesizing cholesta-5,7-diene,3beta,25-diol and analogs thereof. A Diels-Alder adduct of a steroid containing a 5,7-diene and a DELTA24 double bond is reacted with an oxidizing agent to provide a 24,25-oxido mo...
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WO/1993/021205A1 |
A method is provided for isolating 5,7-diene-containing steroids, particularly 3 beta-ols and esters of 3 beta-ols, from a sterol mixture. The method involves (1) treating the mixture with a dienophile or with an oxidizable dienophile pr...
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WO/1993/019081A1 |
Polymorph "A" a novel polymorphic form of N-t-butyl-androst-3,5-diene-17beta-carboxamide-3-carboxylic acid. Novel processes for preparing polymorph "A" are also disclosed.
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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/1993/016607A1 |
A method for extraction and removal of cholesterol from egg yolk with simultaneous production of cholesterol as a by-product. The removal of cholesterol from the nontreated egg yolk is achieved by the extraction of cholesterol into the e...
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WO/1993/015104A1 |
Novel 20-substituted-pregnene derivatives, compositions containing such derivatives and methods for their use and manufacture are disclosed. The 20-substituted-pregnene derivatives inhibit the androgen biosynthesis enzymes 17(alpha)-hydr...
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WO/1993/014763A1 |
1alpha-Hydroxy-24-epi-vitamin D4 and novel intermediates formed in a novel method of preparing this compound. The method includes campesterol as a starting material which is converted to 24-epi-vitamin D4 which is in turn hydroxylated to...
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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/1993/012798A1 |
An obesity inhibitor containing 4-cholesten-3-one represented by formula (I) as the active ingredient which is useful for inhibiting an increase of the body weight and accumulation of body fat; a medicinal composition containing 4-choles...
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WO/1993/012082A1 |
To provide a medicine which has a potent vitamin D3-like activity and a reduced toxicity and is useful for treating calcium metabolism disorder and osteoporosis. A 24R,25-dihydroxy-26,27-dimethylvitamin D3 derivative represented by formu...
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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/1993/007878A1 |
Aldosterone biosynthesis inhibitors having substantially no intrinsic antiandrogenic activity are disclosed as well as pharmaceutical compositions containing such compounds and methods of treatment utilizing these compositions.
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WO/1993/005162A1 |
A method for facilitating the transfer of nucleic acids into cells comprising preparing a mixed lipid dispersion of a cationic lipid with a co-lipid in a suitable carrier solvent. The lipid has a structure which includes a lipophilic gro...
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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/1993/001821A1 |
Steroidal and non-steroidal glycosides and a method of producing them are provided, wherein aglycon compounds are glycosylated with tri-O-acyl glucal using molecular or ionized halogen as reaction catalyst. The aglycon, which may be a no...
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WO/1992/022300A1 |
The invention relates to chemotherapy and concerns particularly the preparation of pharmaceutical compositions for ocular application, said compositions being characterized in that they contain at least one selected compound of steroidal...
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WO/1992/019640A1 |
The invention relates to a substance which lowers cholesterol levels in serum and which is a beta-sitostanol fatty acid ester or fatty acid ester mixture, and to a method for preparing the same. The substance can be used as such or added...
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WO/1992/016300A1 |
The method separates a first class of lipoprotein from a second class of lipoprotein in a sample and analyzes the first class of lipoprotein. The second class of lipoprotein is first precipitated. The sample is then contacted with magnet...
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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/1992/012960A2 |
Linear chain dicarboxylic acids having 6 to 12 carbon atoms and novel derivatives thereof, such as amides with natural amino acids and esters with biliary acids, are useful in the formulation of pharmaceutical compositions suitable for e...
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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/1992/012165A1 |
1alpha,24-dihydroxy vitamin D2 which is useful as an active compound of pharmaceutical compositions for the treatment of disorders of calcium metabolism and for various skin disorders. The invention also includes preparation of synthetic...
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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 $g(b) position, whereas R?12¿...
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WO/1992/004431A1 |
A method for extracting minor fatty compounds, particularly steroids, from biological matter by means of cyclodextrin. According to the method, the cyclodextrin is stirred into said biological matter in a water-containing reaction medium...
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WO/1992/004430A1 |
A method for extracting minor fatty compounds, particularly steroids, from biological matter by means of cyclodextrin. According to the method, the cyclodextrin is stirred into said biological matter in a water-containing reaction medium...
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WO/1992/003465A1 |
Disclosed are 20-methyl-5,7-pregnadiene-3$g(b),21-diol derivatives of general formula (I), in which R¿1? is a hydrogen atom or a lower-alkyl group and R¿2? is a lower-alkyl group, or R¿1? and R¿2? together represent a tetramethylene ...
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WO/1992/001803A1 |
The present invention relates to a method for hydroxylation of an acyclic or cyclic methylene radical in the allylic position, characterized in that a peroxydase, iodide ions and hydrogen peroxyde (H2O2) are reacted on said methylene rad...
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WO/1992/000316A1 |
A novel bile alcohol of general formula (I), having an efficacious physiological activity and being specified in the configurations of particularly the 20-, 24- and 25-positions; formula (I) wherein one of the groups R1 and R2 represents...
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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/1991/016898A1 |
Compounds of general formula (7), wherein X is a hydrogen atom or a hydroxyl group, Y is a hydrogen atom or a hydroxyl group and at least one of X and Y is a hydroxyl group and Z is a hydroxyl group or a methylol (-CH2OH) group, have ant...
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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/1991/014500A1 |
The present invention relates to ceramic materials containing a homogeneous dispersion of one or more metals, particularly sol-gel ceramic materials, a method of preparing the same, and processes for hydrogenating or oxidizing organic co...
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WO/1991/014700A2 |
A process for preparing novel corticosteroid intermediates of formula (XXX) are disclosed. The process entails contacting a 9alpha-hydroxysteroid of formula (XX) with (A) in step (a) an anhydride, an organic acid and an acid reagent havi...
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WO/1991/014689A1 |
A process for synthesizing polyoxa heterocycle compounds and in particular the antimalarial agent known as quinghaosu or artemisinin and its analogs is disclosed. A family of new antimalerial analogs of quinghaosu is also disclosed.
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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/1991/005557A1 |
Antigestagens (competitive progesterone antagonists) are suitable for the manufacture of medicaments to treat breast cancers with an increased content of tumour cells in the S phase of the cell cycle, regarded as of high risk.
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WO/1991/005754A2 |
Derivatives of long-chain fatty alcohols, and methods of obtaining them, are provided, as well as pharmaceutical compositions containing derivatives and their uses, in particular in treating or preventing neuro-degenerative illnesses, co...
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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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