33 results about "Hydroxysteroids" patented technology

The present invention relates to the use of inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment or prophylactically treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions mediated by excessive glucocorticoid action.

The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydro-genase type 1 (11βHSD1) and the use of these compounds as pharmaceutical composi-tions, are described. Also a novel class of substituted amides, their use in therapy, phar-maceutical compositions comprising the compounds, as well as their use in the manufac-ture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active gluco-corticoid is desirable.

The invention provides a stable detection kit of total bile acid. The kit comprises a reagent R1 and a reagent R2, wherein the reagent R1 comprises the following components: a buffering solution, beta-thionicotinamide adenine dinucleotide, a surface active agent, a stabilizing agent and a preservative; the reagent R2 comprises the following components: a buffering solution, reduction type coenzyme I (NADH), 3alpha-hydroxysteroid, a surface active agent, antioxidant enzyme, a stabilizing agent and a preservative. The stable detection kit provided by the invention has the advantages that since the antioxidant enzyme is added into the reagents, NADH can be stored for a long time, the influence caused by more interference components in the reaction process is eliminated, so that the NADH can be utilized efficiently, the speed of circulating reaction is increased, the detection accuracy is improved, the sensitivity is high, the linear range is wide, simultaneously, the used amount of main reaction materials can be reduced and the cost of the reagents is reduced.

The present invention relates to a hydroxysteroid dehydrogenase and an application thereof in synthesis of an ursodeoxycholic acid precursor, and specifically discloses a 12-alpha-hydroxysteroid dehydrogenase derived from rhodococcus ruber and a mutant thereof, encoding gene and amino acid sequences, a recombinant expression vector containing the gene, a recombinant expression transformant, and anapplication of the hydroxysteroid dehydrogenase catalyzing oxidation of 12-alpha-hydroxysteroids to form 12-carbonyl steroids. Compared with the prior art, a used recombinant steroid dehydrogenase-catalyzed oxidation reaction is NAD+coenzyme-dependent type. The hydroxysteroid dehydrogenase has advantages of low application cost, simple operation, mild reaction conditions, environmental friendliness, high yield, etc., and thus has a very good prospect in an application of cholic acid as a raw material for production and preparation of the ursodeoxycholic acid precursor.

The invention relates to 12 α-hydroxysteroid dehydrogenases, nucleic acid sequences coding for the same, expression cassettes and vectors, recombinant microorganisms containing the corresponding coding nucleic acid sequences, a method for producing said 12 α-hydroxysteroid dehydrogenases, a method for enzymatic oxidation of 12 α-hydroxysteroids using said enzyme, a method for enzymatic reduction of 12-ketosteroids using said enzyme, a method for qualitative or quantitative determination of 12-ketosteroids and/or 12α-hydroxysteroids using said 12α-hydroxysteroid dehydrogenases and a method for production of ursodesoxycholic acid, comprising the enzyme-catalysed cholic acid oxidation using said 12 α-hydroxysteroid dehydrogenases.

Synthetic methods for preparing deoxycholic acid and intermediates thereof, high purity synthetic deoxycholic acid, compositions and methods of use are provided. Also, provided are processes for the synthesis of 12-keto or 12-a-hydroxysteroids from Delta-9,11-ene, 11-keto or 11-hydroxy-ss-steroids. This invention is also directed to novel compounds prepared during the synthesis. This invention is also directed to the synthesis of deoxycholic acid starting from hydrocortisone.

Antisense compounds, compositions and methods are provided for modulating the expression of hydroxysteroid 11-beta dehydrogenase 1. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding hydroxysteroid 11-beta dehydrogenase 1. Methods of using these compounds for modulation of hydroxysteroid 11-beta dehydrogenase 1 expression and for treatment of diseases associated with expression of hydroxysteroid 11-beta dehydrogenase 1 are provided.

The present invention relates to NIP thiazole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-β-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.

Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R¹ to R⁴ are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors.

The invention relates to a preparation method for a pregna-16-ene-3, 20-dione steroid derivative (II). The method is characterized by: reacting 17alpha-ethynyl-17beta-hydroxysteroid derivative I with a reagent A or an organic solvent containing the reagent A to obtaining the derivative (II). The reaction temperature ranges from 25DEG C to a solvent reflux temperature, and the reagent A is a solution formed by dissolving 5%-15% of phosphorus pentoxide in methanesulfonic acid.

Disclosed is a new synthetic pathway for the production of precursors for the production of compounds having general formula (8,10,12). During said synthesis, compounds of general formal (4,B) are produced in a microbiological reaction. The meanings of radicals R<7>, R<10>, R<11>, R<13>, R<17> and R<17'> and group U-V-W-X-Y-Z are defined in the patent claims.