30 results about "Cyclo-oxygenase" patented technology

ABSTRACTA pharmaceutical composition comprises a combination of a selective or specific COX 2 inhibitor or a pharmaceutically acceptable salt or derivative thereof and an opiate or a pharmaceutically acceptable salt or derivative thereof, for example a combination of meloxicam and codeine, as active ingredients, and a pharmaceutically acceptable carrier. It may include a centrally-acting cyclo-oxygenase inhibitor such as paracetamol or its pharmaceutically acceptable salts or derivatives. The pharmaceutical compositions are used in methods of providing symptomatic relief or treatment of pain, in an algesic and / or hyperalgesic state, with or without fever, in particular that associated with inflammation such as that associated with trauma, osteoarthritis, rheumatoid arthritis, non-inflammatory myalgia or dysmenorrhoea

The invention belongs to the field of pharmaceutical preparations and provides a Celecoxib nanosuspension and a preparation method thereof. Celecoxib is a novel non-steroidal anti-inflammatory drug, inhibits cyclooxygenase -2(COX-2) is through specificity, has anti-inflammatory and pain-easing effects and is clinically used for treating osteoarthritis and rheumatoid arthritis. However, the Celecoxib has very low solubility and in-vivo bioavailability. In order to increase the dissolution and the bioavailability of the drug, a high-speed shearing combined high-pressure homogenizing method is adopted to prepare the Celecoxib nanosuspension, the particle size and the polydispersion index PI are used as indicators for formulation technology optimization, a laser particle analyzer and a transmission electron microscope are adopted to study the particle size and form of the drug, the dissolution of the drug is evaluated through in-vitro dissolution experiments, and rat in-vivo pharmacokinetic study is conducted. Measurement results prove that the drug particle size of the nanosuspension is 50-500 nm, and the dissolution and the in-vivo bioavailability of the drug are increased obviously.

The invention provides a process for simply and efficiently preparing a selective cyclooxygenase-2 (COX-2) inhibitor 4-[3-trifluoromethyl-5-(4-methylphenyl)-1H-pyrazolyl]benzenesulfonamide (celecoxib, I). The process comprises the following steps: reacting an alkyl trifluoroacetate and 4-methylacetophenone which are initial raw materials under the action of an organic alkali solution, directly adding a dilute acid, an organic solvent and 4-aminosulfonylhydrazinobenzene or its acid salt to the resulting system, and heating to prepare the celecoxib. Above reaction adopts one kettle way, so the process has the advantages of mild condition, simple operation, high product yield and high product purity, and is suitable for industrialized production.

The invention provides a new application of Chinese caterpillar fungus. The Chinese caterpillar fungus has a new application in preparation of anti-inflammatory drugs, and further can be used for preparing drugs with neuroprotective effect to ischemic encephalopathy. The new application of Chinese caterpillar fungus is realized through lowering the levels of interleukin, tumour necrosis factor and intercellular adhesion molecules, and reducing the expression of nitric oxide synthase and cyclooxygenase by inhibiting the activity of transcription factor protein family NF-kB. The invention also provides a medicament composition which takes Chinese caterpillar fungus as the main component or one of the main components and is provided with therapeutic effect to ischemic encephalopathy.

The invention discloses an epoxidase-2 selective inhibitor as well as a preparation method and application thereof. According to the epoxidase-2 selective inhibitor, with substituted benzamide and a substituted benzoic acid derivative as raw materials, a 4-[3,5-bis(substituted-phenyl)-1-(1,2,4-triazole)] benzenesulfonic acid derivative is obtained through condensation reaction and ring closing reaction of a p-hydrazino-benzenesulfonic acid derivative. The epoxidase-2 selective inhibitor has the beneficial effects that the epoxidase-2 selective inhibitor has a significant selective inhibiting effect on epoxidase COX-2 activity, and is capable of obviously inhibiting foot swelling in mice caused by carrageenin; and a target compound is expected to become a medicine for treating inflammation, rheumatoid arthritis, and diseases related to epoxidase-2.

The invention discloses a novel styrene mono-cyclooxygenase BrSMO derived from Bradyrhizobium sp. ORS 375, and an application of the novel styrene mono-cyclooxygenase BrSMO in the catalysis of asymmetric oxidation reactions. The enzyme can catalyze styrene or thioether substrates to carry out asymmetric oxidation reactions, and has relatively high activity, wherein the styrene substrates are asymmetrically oxidized to generate S-type epoxy, the enantioselectivity is excellent, and the ee is greater than 99%; and the thioether substrates are asymmetrically oxidized to generate R-type sulfoxide,and the ee value of generated (R)-p-bromophenyl methyl sulfoxide is up to 90%.

The invention relates to a novel selective cyclooxygenase-2 inhibitor compound, a preparation method and use and belongs to the field of chemical drugs. The compound represented by a formula (I) shown in the description can be used for inhibiting cyclooxygenase and interfering with the biotransformation of in-vivo arachidonic acid to prostaglandin, so that the compound and pharmaceutical compositions thereof can be used for treating cyclooxygenase mediated related diseases, i.e., can be used for treating and relieving animal and human inflammations and inflammation caused various diseases such as arthritis, neurodegenerative disease, depression, schizophrenia disease and cancers (including non-small-cell lung cancer, liver cancer, pancreatic cancer, colon cancer, breast cancer, ovarian cancer, prostatic cancer, cervical cancer, skin cancer, head and neck cancer and the like).

The invention discloses alisma orientale squalene cyclooxygenase and an application thereof. The alisma orientale squalene cyclooxygenase has an amino acid sequence shown in SEQ ID NO.2 or SEQ ID NO.4. The invention clones the full length of alisma orientale squalene cyclooxygenase gene for the first time, provides alisma orientale squalene cyclooxygenase, a prokaryotic expression method of the enzyme gene, prepares a polyclonal antibody of the enzyme protein, provides an ELISA detection method and a Western Blot detection method of the protein, and can be used for improving the biosynthesis efficiency of alisma orientale prototerpane triterpene and monitoring the dynamic accumulation process of pharmacodynamic components.

A transparent stable injection preparation of a new selective epoxide hydrolase II(cyclooxygenase II) inhibitor, is used for the treatment of pain and the inflammation that causes by cyclooxygenase II, especially the preparation is prepared by dissolving the selective active cyclooxygenase II inhibitor such as cyclooxygenase II inhibitor selected from example choose from celebrex, vioxx and their homologous compounds, into solvent such as isobide ester isosorbide as shown by the chemical formula I, wherein, R[1] and R[2] are hydrogen atom or the alkyl or acetic acid ester of 1 - 3 carbons; also disclosed is a simple and cost-rational preparation method of tha said new medicine preparation.

In the compound of the present invention and in an anti-inflammatory agent, a cyclooxygenase-2 inhibitor, a therapeutic agent for brain diseases, and an MRI contrast medium, which each comprise the same compound, the compound of the present invention has the structure represented by chemical formula 1 according to the present invention.

The invention relates to the field of medicine application, in particular to a marker for viral pneumonia and application of the marker. The marker for viral pneumonia is prostaglandin E2 and / or prostaglandin M. According to the invention, prostaglandin E2 and / or prostaglandin M are / is taken as the marker of viral pneumonia, and an epoxidase II inhibitor is used, so that prostaglandin can be effectively and rapidly reduced, the development of ordinary and severe diseases can be reversed, the occurrence of critical diseases can be blocked, and the conversion of viruses into negative, pneumonia absorption and health recovery can be promoted. Under the condition that the curative effect is further confirmed, the clinical application range of the medicine is expanded, the treatment method is incorporated into a clinical diagnosis and treatment scheme, and a new strategy and a diagnosis and treatment method are provided for comprehensive treatment of novel coronavirus pneumonia.

The invention discloses a method for determining seven kinds of non-selective cyclooxygenase inhibitory drug residues in poultry and livestock meat. Extraction and purification of non-selective COX inhibitory drug residues, using ultra-high performance liquid chromatography-triple quadrupole mass spectrometry with the advantages of high sensitivity and strong anti-interference to detect seven non-selective COX inhibitors in poultry and livestock meat Qualitative and quantitative analysis of drug residues. Seven non-selective cyclooxygenase inhibitors: salicylic acid, ibuprofen, diclofenac sodium, indomethacin, piroxicam, naproxen, phenylbutazone. The invention well solves the problem in the process of detecting seven kinds of non-selective COX inhibitory drug residues in poultry meat.

The present invention discloses a Chinese medicine composition having anti-allergic reaction and selective cyclooxygenase 2 inhibition functions and a preparing method and a quality control method thereof. The composition is mainly composed of bright leaf Tung, hooked uncaria, cicada slough, viola yedoensis, and glossy ganoderma spore powder. When preparing the Chinese medicine composition, the bright leaf Tung, the hooked uncaria, the cicada slough and the viola yedoensis are crushed and mixed, and then the mixture is dipped by 80-95% ethanol for 22-28 hours for one to three times, the extracted liquid is collected and the ethanol is reclaimed, the mixture is then dried under 70-85 DEG C, the reclaim rate is 20-28%, and the mixture is mixed with glossy ganoderma spore powder and is made to acceptable preparation in clinic directly by conventional procedure or by adding acceptable excipient in pharmacy. The invention also provides a quality control method for discriminating the components and measuring the content for the composition. The composition has excellent anti-allergic reaction and selective cyclooxygenase 2 inhibition functions.

The invention discloses aromatic thiazole micro-molecular organic compounds with the structural formula represented by formula (I), or hydrates thereof or pharmaceutically acceptable salts thereof. The compounds of the invention or compositions containing the compounds can be used for sun protection, anti-ultraviolet and skin damage protection as a cosmetic additive and for inhibition of the cell apoptosis caused by excess ultraviolet irradiation and the expression of cyclooxygenase COX2. The invention also discloses preparation methods of the aromatic thiazole micro-molecular organic compounds and derivatives thereof.

The invention provides a pyridine-containing compound, relating to the field of medicines. The chemical structure of the compound is shown as in a formula I: The formula I is shown in the description.The compound can be taken as an inhibitor of cyclooxygenase 2 for treating inflammation. The invention further provides an extration method of the compound for preparing the pyridine-containing compound which has the effect of inhibiting cyclooxygenase 2 and has application value in the aspect of inflammation-related diseases.

The invention discloses an epoxidase-2 and an application of an inhibitor thereof for bladder cancer. According to the invention, the selective inhibitor nimesulide of epoxidase-2 can restrain the multiplication of bladder cancer cells T24 by reducing the expression of the epoxidase-2. A model is adopted for screening and acquiring four epoxidase-2 inhibitors. The four inhibitor compounds are all 2-amido benzoxazole derivative, all can reduce the expression of the epoxidase-2 and can restrain the multiplication of T24. The invention proves that epoxidase-2 can be used as a drug target for screening the drug for restraining the bladder cancer.

Selected sulfonic acids, their derivatives and pharmaceutical compositions containing such compounds are useful in inhibiting the chernotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCRI and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, the selected sulfonic acids and their derivativas are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrofil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

The invention provides a cyclooxygenase targeted near infrared dye metal complex photosensitizer and preparation and application thereof. The photosensitizer has a structure shown in the following formula (I): M(L1)m(L2)n(X1)o(I), wherein M is a non-radioactive metal with an atomic number greater than 40; L1 is a neutral or anionic ligand; L2 has a structure of: R1-L3-R2, wherein R1 is a cyclooxygenase targeted compound group, L3 is a linking group, R2 is a near-infrared dye group; X1 is a counterion; m and n are each an integer greater than or equal to 1; o is an integer from 0 to 4; the cyclooxygenase targeted compound includes: indomethacin and indomethacin derivatives; and the near-infrared dye includes rhodamine and rhodamine derivatives. The photosensitizer integrates functions of tumor targeting, tumor imaging, drug tumor treatment and prognosis monitoring, and is a multifunctional organic small molecule photosensitizer.

(R) and (S) 2-Aryl-propionic acids, and pharmaceutical compositions that contain them, are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The acids are used for the prevention and treatment of pathologies deriving from said activation. In particular, the (R) enantiomers of said acids are lacking cyclo-oxygenase inhibition activity and are particularly useful in the tratment of neutrofil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bollous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

The invention discloses a new bacterial strain-spectacular byssochlamys ZRV2011F2-P3 and application to serving as an active inhibitor of soluble epoxidase (sEH). The spectacular byssochlamys ZRV2011F2-P3 is preserved in China General Microbiological Culture Collection Center, the preserving serial number is CGMCC NO.10637, the preserving date is March 19, 2015, the preserving address is Institute of Microbiology of Chinese Academy of Sciences, number 3 of the first courtyard of west beichen road of the chaoyang district of Beijing, and the postcode is 100101; and the bacterial strain comes from traditional rice vinegar fermented vinegar mash, the inhibitor of cardiovascular disease target sEH enzyme can be produced, the activity of the N end phosphatase of the sEH is powerfully restrained, the effect of preventing and treating hypercholesteremia is achieved, and the new physiological function of the cardiovascular disease target sEH is easily disclosed.

The invention belongs to the technical field of medicine, and specifically relates to the application of a 2(ammonia alkyloxy) phenyl pentadiene ketone compound in the preparation of drugs for treating chemical ache and / or immunologic injury. The 2(ammonia alkyloxy) phenyl pentadiene ketone compound can inhibit cells induced by lipopolysaccharide from generating IL-12, IL-1beta and / or cyclooxygenase-2 in vitro.

The invention provides a method for regulating and controlling adenovirus protein with double promoter, which comprises the following steps: inserting the human end granule enzyme catalysis subunit promoter and cyclooxygenase 2 promoter to E1A and E1B front promoter domain of adenovirus vector Pxc1 by cutting with Agel single enzyme and Eagl single enzyme and the vector of an adenovirus Pxc1; regulating and controlling the early gene E1A and E1B of adenovirus. The method is fit for the application of tumor gene medicine for regulating and controlling the early gene E1A and E1B of adenovirus. The method has the rational design, and the experiment indicates that the restructuring adenovirus can express the breeding and the killing of the adenovirus in the adenovirus of the end granule enzyme and the cyclooxygenase 2, but the adenovirus doesn't breed in the normal cell.

The invention belongs to the technical field of biological medicine, and relates to application of bacillus marinus sp. BS11 exopolysaccharide in preparation of anti-inflammatory drugs or pharmaceutical compositions. According to the invention, the anti-inflammatory activity of the bacillus marinus sp. BS11 exopolysaccharide (EPS11) disclosed in the invention with a publication number of CN107988105A is determined. Results show that EPS11 has significant anti-inflammatory activity, significantly reduces the expression quantity of epoxidase 2 (COX2) in a bacterial lipopolysaccharide (LPS) induced mouse peritoneal macrophage (RAW264.7) model, inhibits the generation of inflammatory factors such as NO, IL-6, IL-1beta and TNF alpha, and has no significant cytotoxicity. Therefore, the bacillusmarinus sp. BS11 exopolysaccharide provided by the invention can be used for preparing anti-inflammatory related immunosuppressive drugs or health products, and has good development and utilization values.