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WO/1993/021198A1 |
Sialic acid derivatives of cortison, dexamethasone and vitamin D3 represented by general formula (I), wherein R1 represents a steroid residue selectd from among cortisone, dexamethasone and vitamin D3; R2 represents hydrogen or acetyl; a...
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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/1993/019080A1 |
Polymorph "B" is a novel polymorphic form of N-t-butyl-androst-3,5-diene-17beta-carboxamide-3-carboxylic acid. Novel processes for preparing polymorph "B" are also disclosed.
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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/1993/018773A1 |
An aminosterol antibiotic, (3beta(N-[3-aminopropyl]-1,4-butanediamine)-7alpha,24 zeta-dihydroxy-5alpha-cholestane 24-sulfate), which can be isolated from the stomach of the common dogfish shark, Squalus acanthias, is 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/1993/016098A1 |
Invented is an improved process for the preparation of substituted steroidal dienes.
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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/1993/015104A1 |
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/1993/015103A2 |
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/1993/014107A1 |
Invented is an improved process for the preparation of benzo esters and benzo acids. Also invented are novel intermediates used in said process.
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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/1993/013122A1 |
Described are 3-methylsulphonylhydrazono and 3-oxyimino steroids of the general formula (I), in which X is an oxygen atom or an NH group; the C¿4?-C¿5? bond is a single or double C-C bond and the C¿15?-C¿16? bond is a single or doubl...
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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/1993/013124A1 |
The present invention relates to certain substituted 17$g(b)-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) wherein R?1¿ and R?1¿ are: i) independently hydrogen or lower alkyl and the bon...
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WO/1993/012137A1 |
Compounds of formula (I) in which the dotted line indicates the optional presence of a double bond joining the 6 and 7 positions, A is a divalent group having a chain of at least four atoms joining the oxy group and the group BX, which g...
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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/1993/010741A2 |
Inhibitors of sex steroid activity, for example those having general structure (A) may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositi...
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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/1993/005064A1 |
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/1993/005162A1 |
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/1993/002096A1 |
The preparation of a compound of formula (I) wherein X is oxygen or sulphur; R1 is hydrogen or C1-C6 alkyl; each of R2 and R3 is, independently, hydrogen, C1-C6 alkyl, C5 or C6 cycloalkyl or C6-C9 cycloalkylalkyl; R4 is hydrogen, C1-C6 a...
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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/1992/020646A1 |
The invention relates to organic chemistry and more especially to therapeutic chemistry. It concerns, in particular, novel quaternary ammonium salts of general formula (I), in which Hal is a halogen atom other than fluorine, R and R1, th...
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WO/1992/018524A1 |
The N-alkyl-tauroursodeoxycholic acids and their pharmaceutically acceptable derivatives are useful in the therapy of hepatic diseases and troubles. For the preparation of these acids a conjugation reaction is effected between a mixed an...
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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/1992/011277A1 |
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 $g(b) position, whereas R?12¿...
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WO/1992/011279A1 |
A new type of D-homo-(16-en)-11$g(b)-aryl-4-estrenes having general formula (I), as well as their pharmacologically acceptable addition salts with acids are disclosed. In formula (I), X stands for an oxygen atom, the hydroxyimino groupin...
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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/1992/004309A1 |
15,16-Seco-19-nor progestins are provided which display elevated progestational activity with a minimum of ancillary hormonal activity. Processes for the preparation of the novel progestins are provided as are methods of use. A preferred...
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WO/1992/001706A1 |
The invention relates to the field of organic chemistry and more particularly to therapeutical chemistry. It relates in particular to 6-methyl 19-nor pregna 4,6-diene 20-one having general formula (I) wherein R1 is hydrogen and R2 is a r...
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WO/1992/000991A1 |
The invention relates to a process for producing unsaturated 17-alpha-cyanomethyl-17-beta-hydroxysteroids of general formula (I) in which R¿1?=Me, Eth; R¿2?=H, Me; R¿3?=H, OH, O-acyl or O-alkyl group; R¿4?=H; R¿5?=OH, O-acyl, O-alky...
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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/1991/019482A1 |
Methods and compositions for preventing or treating ophthalmic diseases or disorders wherein an ophthalmically effective amount of the C20 through C26 aminosteroids of formula (XI) and their pharmaceutical, acceptable salts, hydrates or ...
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WO/1991/019732A1 |
Invented are 3-acetic acid-steroidal compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5alpha-reductase including using these compounds to reduce prostate size and to...
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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/1991/016897A1 |
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/1991/008218A1 |
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/1991/004265A1 |
A process is described for producing progesterone derivatives of general formula (I), in which .... is a single or double bond, X is a hydrogen or fluorine atom or a methyl group and V is a methylene, ethylene, ethylidene or vinylidene g...
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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/1991/001958A2 |
New 11$g(b)-aryl-gona-4,9-dienes of general formula (I), in which R?1�, R?2�, R?3�, R?4� and R?5� have the meaning given in the derscription, possess a marked antigestagenic activity and are suitable for the manufacture of drugs.
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WO/1991/000733A1 |
A method of treatment of androgen-related diseases such as prostate cancer in susceptible male animals, including humans, comprises administering novel antiandrogens and/or novel sex steroid biosynthesis inhibitors as part of a combinati...
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WO/1991/000731A1 |
A combination therapy for the prophylaxis and/or treatment of benign prostatic hyperplasia in susceptible warm-blooded animals which comprises administering a combination of two or more compounds selected from the group consisting of an ...
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