18 results about "Pregnane" patented technology

Provided in the present invention are a 3-hydroxyl-5-pregnane-20-one derivative as shown in formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the derivative or the pharmaceutically acceptable salt thereof. The derivative or the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising the above-mentioned derivative or salt of the present invention can be used to prepare a drug for treating a disease caused by abnormalities in the central nervous system.

This invention relates to a cinnabar-2-oxide compound, its preparation method, and its uses. The cinnabar-2-oxide compound is shown in formula (I). By oxidizing a nitrogen atom to an N-oxide and then combining it with a heteroaryl group, the above-mentioned cinnabar-2-oxide compound achieves good α2-GABAA receptor affinity and positive regulatory activity. Simultaneously, it has the potential to significantly reduce PXR (pregnane X receptor) activation, thereby reducing drug-drug interactions and improving drug efficacy or safety.

The present invention provides a crystal of a compound of formula I as a 3-hydroxy-5-pregnane-20-one derivative and a preparation method thereof. Specifically, the invention provides a crystal form G of a compound shown as a formula I and a preparation method thereof. The crystal form G of the present invention has significantly improved solubility, excellent storage stability at various temperatures, and low hygroscopicity, thereby improving druggability, and bringing very excellent effects for production, sales and transportation of drugs.

The invention relates to the technical field of medicine synthesis, in particular to C3 and C20 N-containing pregnane type steroid alkaloid derivatives as well as a preparation method and application thereof. A pregnane type steroid alkaloid skeleton in Miao medicine tri-silver is used as a template, a steroid compound epiandrosterone is used as a raw material, C3-site and C20-site keto compounds are obtained through Wittig alkylenation reaction and oxidation, and the C3-site and C20-site keto compounds are subjected to continuous reductive amination reaction to obtain a series of pregnane type steroid alkaloid derivatives containing N at C3 site and C20 site simultaneously. The C3 and C20 N-containing pregnane type steroid alkaloid derivatives provided by the invention have remarkable anti-inflammatory and anti-gastric ulcer activity, and a scientific basis is provided for searching novel anti-inflammatory and anti-gastric ulcer lead compounds with high selectivity and safety and developing novel anti-inflammatory and anti-gastric ulcer medicines.

The present invention provides a 3-hydroxy-5-pregnan-20-one derivative represented by Formula I or a pharmaceutically acceptable salt thereof, as well as a pharmaceutical composition comprising the derivative or a pharmaceutically acceptable salt thereof. The derivative or a pharmaceutically acceptable salt thereof of the present invention, or a pharmaceutical composition comprising the derivative or salt thereof, can be used to produce a drug for treating diseases caused by central nervous system abnormalities. [Formula 1] JPEG2022545047000052.jpg4199

This application provides a method for preparing pregnanelonone, comprising the following steps: Step 1) under the action of a first catalyst, progesterone reacts with an acid anhydride to obtain the compound shown in formula (I); Step 2) under the action of a dehydrating agent and a second catalyst, a diol reacts with the compound shown in formula (I), and after deprotection, the compound shown in formula (II) is obtained; Step 3) under the action of a ligand and a third catalyst, the compound shown in formula (II) is selectively reduced by hydrogen to obtain the compound shown in formula (III); Step 4) the compound shown in formula (III) reacts with a reducing agent and is then deprotected to obtain pregnanelonone. This application uses progesterone as the starting material, and obtains pregnanelonone through enol esterification, ketal protection, ester hydrolysis, hydrogenation, and reductive hydrolysis. This method is mild, uses conventional reagents, is simple to operate, suitable for industrialization, and yields a high-quality product with a purity of over 99.0% and an overall yield of approximately 90.0%.

A method for preparing and purifying alfasalone (3α-hydroxy-5α-pregnane) from a crude mixture of 3α- and 3β-hydroxy-5α-pregnane, and subsequently purifying the 17α- and 17β-enantiomers to obtain the 17β-enantiomer (alfasalone).

To provide novel lipid drug conjugates which facilitate stable transport of a pharmaceutical agent to the intestinal lymph and readily revert to a parent drug so as to be active.SOLUTION: Provided is a compound of the following Formula I, wherein A is a therapeutic agent selected from a naturally occurring or non-naturally occurring pregnane neurosteroid, or an analog or prodrug thereof.SELECTED DRAWING: None

The present application relates to the field of medicine, specifically relates to a kind of formula I shown compound, its racemic body, stereoisomer, tautomer, solvate, polymorph or their pharmaceutically acceptable salt:Wherein:R2,R4 respectively independent from H or D;R1,R3 respectively independent from CH3,CH2D,CHD2 Or CD3;Formula I compound contains at least one deuterium atom.The present application is under the premise of retaining allopregnanolone pharmacological activity, by the structure modification of the hydroxyl group of allopregnanolone obtains the allopregnanolone derivative suitable for oral administration, it has good physical / chemical stability.

The aim is to provide plasma biomarkers for bone infections in humans. [Solution] A plasma biomarker for bone infection comprising one or more substances selected from the group consisting of sphingosine-1-phosphate, taurocholic acid, glycololic acid, 11a,b hydroxyprogesterone, 15(S)-HETE-2, 13-dehydrochenodeoxycholic acid, 3,21-didihydroxy-5a-pregnane-20-one-2, aldosterone, bisacron-2, naringenin, tauro-α-mulicolic acid-6, 1-deoxysphingosine, 12(S)-HETE-2, 2-arachidonoylglycerol, 3-hydroxydodecanoic acid, 3-hydroxytetradecanoic acid, 3b-hydroxy-5-cholestic acid, AEA(22:4)-1, AEA(22:4)-2, bilbertin, sphingosine, malic acid, and succinic acid.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to biphenyl monoacyl compounds or pharmaceutically acceptable salts and application thereof. According to the biphenyl monoacyl compound provided by the invention, the expression of PXR downstream key protein is up-regulated by activating a PXR receptor, and the biphenyl monoacyl compound shows a good treatment effect on liver and other metabolic system diseases. The biphenyl monoacyl compound has a good effect in the aspects of promoting liver regeneration, resisting cholestasis and the like, and has a good development prospect.

The present disclosure in one aspect, relates to compounds, compositions, and methods for degrading pregnane X receptor (PXR) protein. The invention further relates to the use of the disclosed compounds in decreasing adverse drug reactions such as, for example, adverse drug reactions associated with administration of an anticancer agent, an antibacterial agent, a non-steroidal anti-inflammatory agent, or an anticonvulsant agent. The invention, in one aspect, further relates to compounds, compositions, and methods for identifying PXR ligands. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Disclosed is a method and an oral composition for treating CNS disorders. An embodiment of the invention comprises orally administering a 3α-OH-5α-pregnan-20-one containing composition to a subject having a CNS disorder. The composition preferably exhibits a high release rate of the 3α-OH-5α-pregnan-20-one, and when mixed with an aqueous solution, a high dispersion value. The composition is also preferably more soluble than a comparable SBE-β-CD containing composition. Further in the embodiment, the solubility of the composition when mixed in a FeSSIF is substantially similar to the solubility of the composition when mixed in a FaSSIF.

The present disclosure relates to 1,4,5-substituted 1,2,3-triazoles useful as modulators of pregnane X receptor (PXR) and in the treatment of disorders associated with PXR dysfunction (e.g., disorders of uncontrolled cellular proliferation, bowel disorders). The invention further relates to uses of the disclosed compounds in decreasing adverse drug reactions such as, for example, adverse reactions associated with administration of an anticancer agent, an antibacterial agent, a non-steroidal anti-inflammatory agent, and an anticonvulsant agent. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Disclosed are methods and oral compositions for treating CNS disorders. An embodiment of the invention comprises orally administering a 3α-OH-5β-pregnan-20-one containing composition to a subject having a CNS disorder. The composition preferably exhibits a fast release rate of the 3α-OH-5β-pregnan-20-one. The current compositions may provide desired serum levels of 3α-OH-5β-pregnan-20-one to effectively treat CNS disorders. The oral compositions and methods disclosed herein may be administered to a subject in need of CNS disorder therapy, to deliver therapeutically effective amounts of 3α-OH-5β-pregnan-20-one for treating CNS disorders.