33 results about "Hydroxysteroids" patented technology

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-catalyzed cholic acid oxidation using said 12 α-hydroxysteroid dehydrogenases.

The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds.

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.

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 are a process and catalysts useful for carrying out asymmetric methlyallylations. The catalysts used in the invention have the formula (IV): wherein X1, X2, R3 and R4 are as defined herein. Compounds made by the process of the invention can be used to prepare pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors including 1,3-disubstituted oxazinan-2-ones.

Disclosed is a compound of formula (I)and salts thereof. Also disclosed are methods of making the compound of formula (I) and the use of the compound as an intermediate for making pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors.

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.

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 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 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.

The present invention relates to a process for the preparation of 17a-(3-hydroxypropyl)- 17ss-hydroxysteroids of the formula (I) starting from 17-ketosteroids of the formula (III) via the intermediates of the formula (V) wherein the radicals R3, R5, R6, R7, R10, R13, R15, R16, R40, R41 and R42 have the meaning indicated in the description.

The invention provides a carbonyl reductase mutant and its application in catalytically synthesizing 17β-hydroxy steroid compounds. The mutant has a mutation in a core amino acid of the wild-type carbonyl reductase. The mutants provided by the invention can significantly improve the ability of carbonyl reductase to convert a series of 17-carbonyl steroid compounds, and have high stereoselectivity. The recombinant cell provided by the invention is used as a biocatalyst, which can obtain a high yield target product with a high substrate feeding concentration, has few by-products, and the yield is not lower than 95%, and the conversion time is short, and the amount of the biocatalyst used is small, The space-time yield is much higher than the current reported level, the preparation method is simple and convenient, the conditions are mild, and the environment is friendly.

The invention relates to a composition and purposes of deoxycholic acid, and methods for the purification of deoxycholic acid. 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-[alpha]-hydroxysteroids from [delta]-9,11-ene, 11-keto or 11-hydroxy-[beta]-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.

Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L and Z are defined herein.

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

The invention discloses a derivative of 17-hydroxysteroid, a detection reagent and a preparation method thereof, and relates to the technical field of biological detection. A 17-hydroxysteroid immunogen prepared by using the 17-hydroxysteroid derivative has high immunogenicity, and antibody specificity is strong and titer is high. A 17-hydroxyl steroid conjugate in a homogeneous enzyme immunoassayreagent prepared by using the derivative is linked to genetically engineered recombinant glucose-6-phosphate dehydrogenase. Thereby, detection sensitivity is significantly enhanced, and a sample withthe concentration being as low as 80 nmol / L can be detected effectively; and the detection reagent has strong specificity and has no cross reaction with common 92 interferents. High-throughput and rapid detection of the 17-hydroxysteroid content can be realized by a fully automatic biochemical analyser. The detection result is stable, accuracy is high, and the detection method is simple and is easy for implementation and promotion and application.

The present invention provides novel compounds that are inhibitors of type I 11-beta-hydroxysteroid dehydrogenase. Type I 11-beta-hydroxysteroid dehydrogenase inhibitors may be used to treat, prevent or delay the progression of diseases requiring treatment with a type I 11-beta-hydroxysteroid dehydrogenase inhibitor. These novel compounds or stereoisomers or pharmaceutically acceptable salts thereof have the structure of formula (I), wherein W, L, R3, R3a, R3b and R4 are as defined in this application.

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.

Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L, R3, R3a, R3b and R4 are defined herein.