123 results about "Steroid dehydrogenase" patented technology

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor MR, and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1.

The invention provides a method for catalyzing chenodeoxycholic acids to compound ursodesoxycholic acids through efficient whole-cells. A 7a-hydroxysteroid dehydrogenase (7a-HSDH) and a lactic dehydrogenase (LDH) for regeneration of coenzyme nicotinamide adenine dinucleotide (NAD) are efficiently co-expressed in escherichia coli, escherichia coli whole cells are used to catalyze chenodeoxycholic acids (CDCA) to generate 3 alpha (Alpha)-hydroxyl-7-oxo-5bata (Beta)- cholanic acids (7-KLCA), and a reaction liquid which is obtained by catalyzing the chenodeoxycholic acids through whole cells is adjusted to be 7-KLCA crude products. Reconstitution cells can be easily obtained in low cost through a fermentation process, are better than a chemical synthesis method in production cost and product quality, and are suitable for commercial process.

The present invention relates to tetra-substituted urea compounds which are modulators of 11-β hydroxyl steroid dehydrogenase type 1 (11βHSD1), their pharmaceutical compositions, and methods of using the same.

The invention discloses artificial bear gall powder and a preparation method thereof. The preparation method comprises the following steps: step (a) dissolving livestock gall powder by using a buffer solution of which the pH value is equal to 7-9 and then filtering to obtain filter residues and a filtrate; step (b) adding the filtrate into a reactor filled with 7alpha-hydroxyl steroid dehydrogenase, 7beta-hydroxyl steroid dehydrogenase and coenzyme I or coenzyme II and reacting; step (c) after the reaction ends, freeze-drying a reaction liquid and then mixing the freeze-dried reaction liquid with the filter residues to obtain the artificial bear gall powder. According to the preparation method disclosed by the invention, completely natural livestock gall is taken as a raw material for preparing the artificial bear gall, no other chemical substances are added, common animal gall is adopted and a gall source is easy to pick, obtain and process; through an in-vitro enterohepatic circulation simulation process, the livestock gall is biologically transformed into the artificial bear gall powder which is equivalent to natural bear gall powder in chemistry, and the artificial bear gall powder is used as a natural bear gall replacement to protect the endangered animal Asian black bear and promote healthy development of the bear gall industry.

The invention relates to tanshinone derivatives represented by a general formula (I), wherein the tanshinone derivatives are substituted by different groups on A ring, B ring, C ring, and D ring. The invention also relates to medicine compositions with the derivatives as active components, preparation methods of the medicines, and applications thereof in preparing a 1-type 11beta-hydroxysteroid dehydrogenase (11beta-HSD1) inhibiting agent. The invention also provides applications of the compounds represented by the general formula (I) in preparations of medicines used for treating diabetes and related metabolic diseases (such as hypertension, obesity, senile dementia, and the like).

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The invention provides a mutant of 7 beta-hydroxyl steroid dehydrogenase, application of the mutant and a synthesis method. The mutant of the 7 beta-hydroxyl steroid dehydrogenase is characterized in that amino acid sequences of the mutant are Seq ID NO:4, and coded nucleotide sequences are Seq ID NO:3; or amino acid sequences of the mutant are Seq ID NO:6, and coded nucleotide sequences are Seq ID NO:5. The mutant, the application and the synthesis method have the advantages that cholic acid compounds, particularly ursodeoxycholic acid, can be catalytically synthesized by the efficient 7 beta-hydroxyl steroid dehydrogenase, mutant enzymes of the 7 beta-hydroxyl steroid dehydrogenase and coenzyme regeneration systems, accordingly, the substrate concentration can reach 100 g / L, the conversion rate is 99.2-99.5%, and the weight yield can reach 94-96%; and the enzymes can be inexpensively and easily obtained by the aid of a fermentation process, accordingly, the production cost and the product quality are superior to the production cost and the product quality of chemical synthesis methods, and the mutant and the synthesis method are applicable to industrial production.

The present invention relates to compounds with the formula (I)and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11 β-hydroxy-Steroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

The present invention relates to certain spirocyclic compounds that are inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 (11βHSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases.

The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

The present invention relates to compounds with the formula (I), (II), (III) or (IV):wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

The invention discloses a codon-optimized 7 beta-hydroxy steroid dehydrogenase gene, a recombination expression vector Pgex-6P-1-7 beta-HSDH containing an optimized gene and escherichia coli containing the recombination expression vector. Glutathione S-transferase (GST) fusion expression of the codon-optimized 7 beta-hydroxy steroid dehydrogenase gene and a prokaryotic expression vector Pgex-6P-1 in the escherichia coli is adopted, so that a large quantity of active target proteins with an integral structure can be generated in a short time; and a method for purifying the GST fusion expression protein is simple and quick, so that the active target proteins can be quickly obtained.

The invention discloses 7alpha-hydroxyl steroid dehydrogenase gene optimized by a codon, a recombinant expression vector pGEX-6p-1-7alpha-HSDH containing the optimized gene, and escherichia coli containing the recombinant expression vector. The 7alpha-hydroxyl steroid dehydrogenase gene optimized by the codon is used to carry out GST (glutathione S-transferase) fusion expression with a prokaryotic expression vector pGEX-6p-1 in the escherichia coli. A lot of target proteins with activity and intact structure can be generated within a short time, and the purification method of GST fused protein is simple and fast, thereby rapidly obtaining the target protein with activity.

The invention relates to a method for preparing an ursodesoxycholic acid by using a biological enzyme catalysis technology and 7beta-hydroxysteroid dehydrogenase for preparation of the ursodesoxycholic acid. The method comprises the following steps: adopting a 3alpha-hydroxyl -7-oxo-5beta-cholanic acid as a substrate and catalyzing the 3alpha-hydroxyl -7-oxo-5beta-cholanic acid by using the 7beta-hydroxysteroid dehydrogenase to prepare the ursodesoxycholic acid in the presence of an NADP, glucose, glucose dehydrogenase and a buffer solution, wherein the 7beta-hydroxysteroid dehydrogenase is from Turneriella parva. The method is simple in operation, short in reaction time, the reaction conditions are mild and easy to control, the conversion rate of the substrate can reach 99.8% and the content of the obtained product is greater than 98.5%.