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JP3983796B2 |
This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3 alpha -hydroxy,3 beta -substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereosele...
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JP2007522211A |
The present invention relates to novel compounds which are 7alpha-substituted 17-alkylene-16alpha-hydroxy steroidal estrogens. This invention specifically relates to estrogen derivatives which contain 7alpha-substituents and which exhibi...
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JP2007510723A |
A medicament and a method of producing a medicament are disclosed. The medicament contains a soft steroid and is suitable for administration via a dry powder inhaler.
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JP2007063296A |
To provide a medicinal composition useful for treating human prostatic adenocarcinoma.The medicinal composition for treating human prostatic adenocarcinoma comprises a 5-α-reductase inhibiting compound of 17β-(N-t-butylcarboxamide)-5-Î...
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JP2006528226A |
The present invention relates to methods and uses for preventing or treating hormone-dependent diseases, in particular breast cancer, in a mammal, by a combination of an progesterone-receptor antagonist, in particular the progesterone-re...
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JP2006526025A |
Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering compounds of the general formula: wherein the variables are defined in the specification.
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JP2006524202A |
This invention relates to 8beta-vinyl-11beta-(omega-substituted)alkyl-estra-1,3,5(10)-
trienes of general formula I with ERbeta-antagonistic activity, process for their production, their intermediate products, pharmaceutical preparations...
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JP2006522028A |
A method for the conversion of steroidal 17beta-carboxylic acids to c carbothioic acid and esters thereof such as fluticasone propionate.
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JP3824636B2 |
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JP2006151994A |
To provide a simple method for converting a pregnane-3,20-dione compound into a 3α-hydroxy-3β-substituted-pregnane.An unprotected dione is chemoselectively and stereoselelctively converted into a 3(R)-pregnane-3-spiro-2'-oxiran-20-one ...
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JP2005533851A |
The subject invention provides novel HMG-CoA-reductase inhibitors. In a preferred embodiment, the HMG-CoA reductase inhibitors of the subject invention can be deactivated to a primary inactive metabolite by hydrolytic enzymes. Compounds ...
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JP3715673B2 |
PURPOSE: To stereoselectively provide a synthetic intermediate to give an oxa- vitamin D having a not-natural steric configuration at 20-position corresponding to vitamin D by a novel reductive alkylation of the ketone of the 20-position...
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JP3710470B2 |
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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JP2005530679A |
A method for producing a 6α-fluorinated corticosteroid or derivative thereof by reacting a 17-hydroxy-21-ester epoxide of Formula II with a stereoselective fluorinating agent to stereoselectively form a 21-ester-17-hydroxy 6α-fluorinat...
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JP2005527496A |
According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), or a solvate thereof, together with a long-acting ² 2 -adrenoreceptor agonis...
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JP2005527475A |
Compounds of Formula III are disclosed. Compounds of Formula III are useful in the manufacture of a medicament for the treatment of diabetes, hyperlipidemia, hypercholesterolemia, or atheroschlerosis.
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JP2005524680A |
The process for the preparation of 6alpha-fluoro steroids, comprising the reaction of the corresponding 6beta-fluoro steroids, or of 6alpha/6beta isomeric mixtures with an organic base having a diazo iminic group, in a suitably selected ...
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JP2005519925A |
A pharmaceutical aerosol formulation comprising (i) a compound of formula (I) or a solvate thereof as medicament, (ii) a liquified hydrofluoroalkane (HFA) gas as propellant; and characterised in that the compound of formula (I) or a solv...
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JPWO2003051903A1 |
General formula (I) [In the formula, R1 represents a lower alkyl group, X represents an oxygen atom or a methylene group, m represents an integer of 1 to 10, and n represents an integer of 0 to 5. .. ], A salt thereof or an ester thereof...
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JP2005104862A |
To obtain a therapeutic agent which has an excellent therapeutic effect on aged macular degeneration.This aged macular degeneration therapeutic agent is characterized by containing a progesterone derivative represented by formula (1) (R1...
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JP2004537499A |
Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula (I), wherein the variables are defined in the specification.
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JP3584050B2 |
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JP2004533417A |
The invention relates to the use of corticosteroids and fluitcasone propionate in particular for the treatment of diseases which may be ameliorated by enhancement of epithelium/matrix adhesion.
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JP2004528364A |
17-Methylenandrostan-3alpha-ol analogs are useful as corticotropin releasing hormone (CRH) inhibitors, and especially as anti-depressants, when administered to the vomeronasal organ. An improved synthesis of 17-methylenandrost-4-en-3alph...
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JP2004512359A |
The invention relates to novel medicament compositions based on anticholinergics and corticosteroids, a method for the production thereof and the use thereof for treating respiratory conditions.
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JP2004504403A |
The present invention relates to a process for the preparation of a compound of formula (I) which comprises the following step: wherein step (a) comprises oxidation of a solution containing the compound of formula (II) wherein the soluti...
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JP2003531200A |
The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazo...
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JP3445271B2 |
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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JP2003517472A |
The invention concerns a 3-methylene steroid derivative having general formula (1) wherein R1 is H or together with R3 forms a beta-epoxide or R1 is absent if there is a 5-10 or 4-5 double bond; R2 is (C1-C5) alkyl or CF3; R3 is betaH, b...
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JP2003513102A |
The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R<1>, R<2>, R<3>, R<6>, R<7>, R<8>, R<9>, R<11>, R<11'>, R<14>, R<15>, R<15'>, R<16>, R<17> and R<17'> have the meaning cited in the description,...
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JP2003511462A |
The process of the present invention transforms a steroidal ketone of formula (III)to androst-4-en-17beta-carboxylic acid (IV)by reaction with K2SO5.KHSO4.K2SO4.
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JP3378245B2 |
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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JP2002543216A |
Steroid derivatives of this invention interact with nuclear liver X receptor (LXR) and ubiquitous receptor (UR) and can be used to treat a variety of LXR- or UR-mediated disorders.
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JP2002540119A |
The invention provides compositions comprising formula 1 steroids, e.g., 16alpha-bromo-3beta-hydroxy-5alpha-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. Th...
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JP3346873B2 |
The invention relates to a process for preparing the compounds (I): where R is hydrogen or an ester residue, starting with the compound (II): by oxidative degradation, then fluorination in 6 and hydrofluorination of the epoxide. The comp...
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JP2002322168A |
To provide pharmaceutical compounds which reduce undesirable effects occurred at the region where is apart from the target site.Pharmaceutical compounds represented by general formula (I) or their salts or solvates, which are effective i...
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JP3340514B2 |
The subject of the invention is a process for the preparation of the compound of formula (I): characterised in that the corresponding 9 alpha -OH compound is treated with chlorosulphonic acid in an organic solvent.
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JP2002302476A |
To provide a method for simply producing an α-arylalkyl nitrile deriva tive useful as a biologically active compound, e.g. a phosphodiesterase(PDE)-IV inhibitor or a Ca antagonist or their synthetic intermediates from a styrene derivati...
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JP3328938B2 |
The invention provides new androstene derivatives having anti-inflammatory activity, pharmaceutical compositions containing them, and methods of administering them to warm-blooded animals in the treatment of inflammation. The active comp...
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JP2002531397A |
The invention provides the use of 17-ketosteroid compounds, as well as derivatives, metabolites and precursors of such compounds, and pharmaceutically acceptable salts of any of these compounds, collectively defined herein as the "compou...
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JP2002531407A |
The invention provides the use of 17-ketosteroid compounds, as well as derivatives, metabolites and precursors of such compounds, and pharmaceutically acceptable salts of any of these compounds, collectively defined herein as the "compou...
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JP3310301B2 |
A compound having the structure: wherein n is an integer from 1-5; each of R1 and R2 independently is optionally substituted C1-C6 alkyl; each of W and X is independently hydrogen or C1-C6 alkyl; Y is O, S or NR3 where R3 is hydrogen, C1...
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JP3295426B2 |
Novel antihypercholesterolemic agents are provided. An exemplary group of compounds has the structural formula (I) (I) wherein R is a C-17 side chain, R1 is -OH, =O, or the like, and X and Y are CH, C-OH, C-OCH3 or C-Z. Methods of using ...
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JP2002502404A |
The invention relates to 17beta-allyloxy(thio)alkyl-androstane derivatives having general formula (I) wherein R1 is (H, OR), (H, OSO3H) or NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1...
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JP2001526233A |
Compositions of angiostatic agents for treating GLC1A glaucoma and methods for their use are disclosed.
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JP2001523638A5 |
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JP3227263B2 |
PURPOSE: To obtain the subject compound useful as an intermediate for steroids having physiological activities in high selectivity and in high yield by reacting a specific compound of raw material with formic acid in the presence of a ca...
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JP3202240B2 |
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.
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JP2001510170A |
Methods for treating ocular neovascularization using photodynamic therapy in combination with an angiostatic steriod are disclosed.
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JP3181589B2 |
PCT No. PCT/EP91/02493 Sec. 371 Date Oct. 27, 1993 Sec. 102(e) Date Oct. 27, 1993 PCT Filed Dec. 21, 1991 PCT Pub. No. WO92/11277 PCT Pub. Date Jul. 9, 1992Compounds of the general formula I (I) are described, in which x represents an ox...
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