9 results about "Pharmacodynamic Study" patented technology

This invention relates to the field of medicinal chemistry, specifically disclosing 4-(2-fluoro-4-iodophenoxy)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazoline, its preparation method, and its applications. A novel N-[4-(quinazoline-4-yl)oxyphenyl]biarylsulfonamide compound prepared from this intermediate is a dual inhibitor targeting EGFR and c-Met. The quinazoline core and sulfonamide biaryl side chain in its molecular structure can specifically recognize and bind to mutant EGFR and abnormally activated c-Met, significantly enhancing its selective killing effect on tumor cells. Pharmacodynamic studies show that it exhibits excellent inhibitory activity against the human lung cancer cell line (NCI-H1975) at the cellular level, with an IC50 of [missing information - likely an IC50 value] against p-EGFR. 50 A value of 1.56 nM for p-Met IC 50 The value is 1.8nM.

This invention relates to a CDK12 / PARP dual-target inhibitor, its preparation method, and its application. The inhibitor has the general structural formula (I). Specifically, it relates to a CDK12 / PARP dual-target inhibitor, its preparation method, and its application. Pharmacodynamic studies have demonstrated that the CDK12 / PARP dual-target inhibitor of this invention has significant anti-tumor efficacy. The CDK12 / PARP dual-target inhibitor comprises substituted compounds having the general formula (I), or their stereoisomers, hydrates, or pharmaceutically acceptable salts. Compared with the prior art, the compound structure of this invention is novel, and experiments show that it has good CDK12 and PARP enzyme inhibitory activity, and can be used to prepare drugs with CDK12 / PARP dual-target anti-tumor activity.

The application is a colon-targeting lipid nanoparticle based on ginsenoside Rg3, a calcium alginate microsphere thereof and application thereof in treating ulcerative colitis, and belongs to the technical field of new excipients and new dosage forms of pharmaceutical preparations, and particularly relates to an oral colon-targeting delivery system for treating ulcerative colitis. The system replaces cholesterol in traditional lipid nanoparticles with ginsenoside Rg3, constructs lipid nanoparticles capable of efficiently loading TNF-alpha siRNA, and effectively improves the targeting property and lysosome escape ability of the lipid nanoparticles on inflammatory macrophages. In order to further realize colon-specific delivery, the above-mentioned lipid nanoparticles are loaded in a pH-responsive calcium alginate microsphere, so that the drug is kept stable in the upper gastrointestinal tract and is released in a responsive manner in the colon. Pharmacodynamic studies show that the drug delivery system can significantly relieve the symptoms of colitis, effectively silence the expression of TNF-alpha, repair the intestinal barrier, and regulate the intestinal microbiota. The application provides a safe and efficient new strategy for solving the problems of poor gastrointestinal stability and low targeting efficiency of oral delivery of nucleic acid drugs.

Provided are an interleukin receptor antagonist and an application thereof, and specifically provided is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The provided compound exhibits potent biological activity and good pharmacokinetic properties, or demonstrates good efficacy in animal pharmacodynamic studies. c[X4-X5-X6-X7-X8-X9]-X10-X11-X12-X13-X14-X15-X16 (I)

This invention discloses the pharmaceutical use of schisandrin B in the preparation of analgesic drugs, wherein the analgesia is for the treatment or prevention of chemotherapy-induced neuropathic pain, and the analgesic drug can reduce mechanical and cold hyperalgesia in a chemotherapy-induced neuropathic pain model. Pharmacodynamic studies of this invention demonstrate that oral administration of schisandrin B can reduce chemotherapy-induced neuropathic pain, thereby effectively exerting an analgesic effect, and can be used as a therapeutic or preventative analgesic drug.

This invention belongs to the field of biomedical technology and provides a mussel adhesive protein and azelastine hydrochloride nasal thermosensitive gel, its preparation and application. The mussel adhesive protein and azelastine hydrochloride nasal thermosensitive gel includes an active ingredient and pharmaceutically acceptable excipients. The active ingredient is recombinant mussel adhesive protein mefp-5 subtype and azelastine hydrochloride. The excipients include a thermosensitive polymer, which is mixed with the active ingredient to form a thermosensitive gel system. This invention solves the technical problem that existing single-drug formulations cannot simultaneously provide rapid symptom relief and long-term mucosal barrier repair for allergic rhinitis by combining recombinant mussel adhesive protein mefp-5 subtype with mucosal repair function with azelastine hydrochloride, which has rapid anti-allergic effects. Pharmacodynamic studies have confirmed that the two active ingredients exhibit a significant synergistic effect (CDI < 0.7) in improving allergy symptoms, inhibiting inflammatory responses, and repairing the mucosal barrier.

The application belongs to the field of traditional Chinese medicines, and particularly discloses application of a leech dredging collaterals preparation in preparation of an anti-tumor medicine. The leech dredging collaterals preparation is prepared from four raw medicinal materials of astragalus, ligusticum wallichii, leech and salvia miltiorrhiza, and has the effects of tonifying qi and activating blood and dredging qi and collaterals. Pharmacodynamic studies show that the leech dredging collaterals preparation has the effects of inhibiting growth of liver tumors and lung tumors, is safe and has a good effect, expands the clinical application range of the leech dredging collaterals preparation, and has a good popularization and application prospect.

This application proposes the use of ACSL4 and / or TfR1 genes as targets in the preparation of drugs for the prevention or treatment of non-alcoholic fatty liver disease (NAFLD) under hypoxic conditions. The drugs include resveratrol, which inhibits hypoxia-induced ferroptosis by downregulating the expression of key ferroptosis genes ACSL4 and TfR1. Compared with existing technologies, this application has the following advantages: This application reveals the antioxidant, anti-inflammatory, liver-damage-alleviating, and lipid metabolism-regulating effects of resveratrol using a hypoxic NAFLD model. Pharmacodynamic studies targeting resveratrol demonstrate that ACSL4 and TfR1 have a significant ability to regulate ferroptosis and may affect the progression of NAFLD, which is of great significance for the development of subsequent related drugs and the rational use of medications at high altitudes.

The application discloses a soft capsule of Phellodendri fruit oil, a preparation method thereof and pharmaceutical use, and belongs to the technical field of biological medicines. The application extracts the Phellodendri fruit oil from Phellodendri fruit by using a supercritical CO2 extraction technology, refines the Phellodendri fruit oil by combining with molecular distillation, and obtains high-purity active ingredients with a myrcene content of greater than or equal to 8 mg / g; the soft capsule of the Phellodendri fruit oil is prepared by optimizing the proportion of accessories and a gradient drying process. Each soft capsule contains 100-500 mg of the Phellodendri fruit oil, the content particle size D90 is less than or equal to 30 microns, and the myrcene retention rate is greater than or equal to 90% after an accelerated test for three months. Pharmacodynamic studies show that the soft capsule of the Phellodendri fruit oil prepared by the application has a significant cough-relieving and phlegm-removing effect. The preparation process is advanced, the product quality is stable, and the application provides a cough and asthma treatment medicine with simple components and controllable quality for clinical use.