192 results about "Enzyme inhibitory" patented technology

Compositions comprising one or more practically insoluble proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin, substantially increase the solubility of these proteasome inhibitors and facilitate their administration. Such compositions optionally comprise a buffer. Methods of treatment using such compositions are also disclosed.

The compound represented by the general formula (I):

• • wherein, a fused ring AB represents a 5- to 10-membered fused heterocyclic ring; R¹ represents (1) a hydrogen atom, (2) a halogen atom, (3) a cyano group, (4) an oxo group, (5) an optionally protected hydroxyl group, (6) an optionally protected carboxyl group, (7) an optionally protected amino group, (8) a cyclic group which may have a substituent (s), (9) an aliphatic hydrocarbon group which may have a substituent (s), or (10) an optionally protected thiol group; n represents 0 or an integer of 1 to 8; provided that n represents an integer of not less than 2, plural R¹ are the same or different; a salt thereof, a solvate thereof or a prodrug thereof has a kinase (especially c-Jun N-terminal kinase) inhibitory activity and an inhibitory activity of a function of AP-1 as a transcription factor, it is useful as a preventive and/or therapeutic agent for a for example, a diabetes of metabolic disease, etc., a rheumatoid arthritis of inflammatory, etc.

The invention provides a deuterium-substituted polycyclic pyridone compound, a prodrug thereof, a composition containing the compound and application of the composition. The deuterium-substituted polycyclic pyridone compound is the compound shown in the formula (I) or a tautomer, stereoisomer, prodrug, crystalline form, pharmaceutically acceptable salt, hydrate or solvent compound thereof. The compound and the composition show the cap-dependent endonuclease inhibitory activity and have superior pharmacokinetic properties.

There are disclosed topical compositions for alleviation of skin irritation symptoms or conditions having at least one plant extract effective to inhibit COX-2 enzyme, NGF protein, and/or TNF-alpha protein activity. Preferably, the compositions have a cosmetically, dermatologically, or pharmaceutically acceptable vehicle. In addition to the enzyme inhibitory plant material and acceptable vehicle, compositions may also have at least one active ingredient known to produce skin irritation. There is also a method for treatment of skin irritation symptoms or conditions involving topically applying compositions of the invention. Also disclosed are compositions and methods for topical administration of compositions to the skin that improve the aesthetic appearance of skin and/or provide an anti-aging benefit to the skin.

The invention belongs to the field of medicinal chemistry, and discloses a pyrimidine and triazole containing compound and a preparation method and application thereof in preparation of anti-cancer medicine with lysine specific demethylase 1 (LSD1) being a target. The general formula of the compound is shown in the drawing I. In-vitro LSD1 enzyme inhibition activity experiments prove that by inhibiting LSD1 activity, the compound has obvious inhibiting and killing effects on kinds of cancer cells and can be applied to preparation of the anti-cancer medicine as a further developed lead compound.

Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.

The invention provides a novel herbal composition containing the extracts of the leaves and/or stem of <italic>Argemone mexicana </highlight>plant, optionally containing the extracts of the fruits of <italic>Cuminum cyminum</highlight>, which exhibits useful in vitro, in vivo and interesting immunological and pharmacological activities; a process for preparation thereof; and a method of treatment of psoriasis and related immunological and biological disorders by administration of the said novel herbal composition. The useful in vitro, in vivo and interesting immunological and pharmacological activities exhibited by the extracts and fractions of the leaves and/or stem of <italic>Argemone mexicana </highlight>plant include immunosuppression, lymphoproliferation inhibition, cytokine modulation such as IL-2 inhibition, IFNgamma inhibition, IL-10 induction, keratinocyte proliferation inhibition, keratolytic activity, endothelial cell proliferation inhibition, inhibition of cell adhesion molecule expression such as ICAM-1, MEST inhibition, and enzymes inhibition such as p60src Tyrosine kinase, which are known to be involved in anti-psoriatic activity. The novel herbal composition(s) is useful in the treatment of various disorders, such as psoriasis including plaque psoriasis, gutatte psoriasis, pustular psoriasis and psoriasis of the nails; dermatitis and scleroderma; eczema; inflammatory disorders and other autoimmune diseases like psoriatic arthritis, rheumatoid arthritis, Crohn's disease, multiple sclerosis, irritable bowel disease, ankylosing spondilitis, systemic lupus erythremetosus and Sjogren's syndrome; allergies like asthma and chronic obstructive pulmonary disease and is safe, well-tolerated, non-toxic, with minimal and reversible adverse reactions or side effects, and most importantly, with minimal relapse or recurrence of the disease following completion of a treatment regimen. The invention also describes the presence of phosphodiesterase (III, IV and V) inhibition and 5-Lipoxygenase inhibition in the aqueous, ethanolic or aqueous-ethanolic extracts of fruits of <italic>Cuminum cyminum </highlight>plant.

The present invention includes multifunctional compositions, methods and binding systems to provide disinfecting and deodorizing coatings for hard and soft surfaces, inorganic and organic solid surfaces and particulate media and other related substrates, including human and animal skin and skin lesions; to provide neutralizing functions for malodors generated by both human, animal and industrial fluids and solid wastes; and to provide neutralizing and degrading functions for nuisance and noxious chemicals. The present invention provides compositions and methods for producing disinfecting, oxidizing and enzyme-inhibiting fluids enabling preparation of durable, stable biocidal and deodorizing coatings and media which can be widely used for biological agent control, prevention and elimination of odors, and degradation of noxious agents susceptible to chemical oxidation, and which take forms that are inoffensive to users and offer high convenience.

The invention discloses an angiotensin-converting enzyme inhibitory peptide, and a preparation method and an application thereof, wherein the amino acid sequence of the inhibitory peptide is Leu-Ala-Ser-Pro-Thr-Met. The angiotensin-converting enzyme inhibitory peptide is prepared by tracking, screening and estimating an active ingredient for inhibiting the angiotensin-converting enzyme in mactra veneriformis by virtue of modern biochemical technical means, and purifying the active ingredient by methods of enzymolysis, ultrafiltration, reversed-phase high-performance liquid chromatography and the like; and experiment results indicate that the inhibitory peptide has an excellent effect of inhibiting the angiotensin-converting enzyme and a good anti-hypertension effect, and is good in safety performance, and thus has a bright application prospect.

The invention belongs to the field of medicinal chemistry, and discloses a class of pyrimidotriazole compounds, a preparation method thereof and the use of lysine-specific demethylase (hereinafter referred to as LSD1) as a target in the preparation of antitumor drugs Applications. The general formula of the compound of the present invention is shown in I. The LSD1 enzyme inhibitory activity experiment in vitro proves that this type of compound has obvious inhibitory and killing effects on a variety of tumor cells by inhibiting the activity of LSD1, and can be used as a lead compound for further development and applied to the preparation of anti-tumor drugs.

According to this invention, there is provided an indole derivative having the general formula (I) wherein A is an oxygen atom or a nitrogen atom which nitrogen atom is optionally substituted with an alkyl group, and (i) R<1 >and R<2 >each stand for a hydrogen atom or an alkyl group, independently, or (ii) R<1 >and R<2 >as taken together form a cycloalkyl group or an aromatic ring, or (iii) R<1 >and R<2 >as taken together form a heterocyclic ring, and R<3 >is a hydrogen atom, a (C1-C10)alkyl group or others, R<4 >is a substituted alkyl group and R<5 >is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group and so on, as novel compounds by a novel chemical synthetic process. The indole derivative of formula (I) exhibits a useful chymase inhibitory activity.

The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R¹, G, T, Y¹, Y², Y³, and Y⁴ are as defined herein.

The invention relates to an acetamides compound and application thereof, and discloses an N-(4-substituted phenyl ethyl) amides compound with a novel structure. An in vitro activity test experiment proves that the compound has the enzyme inhibitory activity on cysteine proteinase (FP-2) and dihydrofolate reductase (DHFR); a malaria-killing experiment result proves that the compound has an inhibition effect on wild and drug-resistant malaria protozoon.

Disclosed relates to a novel chalcone derivative, pharmaceutically acceptable salt thereof, a method for preparing the same and uses thereof, the chalcone derivative being readily obtained through the steps of: reacting aminoacetophenone with sulfonylchloride under the presence of an appropriate salt; and reacting the compound prepared in the above step with hydroxybenzaldehide under the presence of an appropriate catalyst. The chalcone derivative of formula 1 in accordance with the present invention having strong enzyme inhibitory activities for glycosidase can be effectively used in preventing and treating various diseases induced by glycosidase, and the chalcone derivative of the invention having tyrosinase and melanin synthesis inhibitory activities can be effectively used as a skin-whitening compound.

The invention particularly relates to a xanthine oxidase inhibitory peptide. The amino acid sequence of the xanthine oxidase inhibitory peptide is Glu-Glu-Ala-Lys (EEAK). The IC50 value of the tetrapeptide EEAK on xanthine oxidase inhibitory activity is 173.00+/-0.06 [mu]M, the tetrapeptide EEAK has a continuous and stable inhibitory effect on xanthine oxidase, and the tetrapeptide EEAK has the outstanding advantages of safety, no toxic or side effect, easiness in absorption, industrialization and the like. The active tetrapeptide EEAK or the derivative thereof can be used for preparing gout treatment/prevention medicines or used as a functional food additive for long-term treatment and health care of gout patients, and has a wide application prospect and very important significance.

The invention discloses a method for screening a triglyceride enzyme inhibitor from a plant extract. The method comprises the following steps of: performing enzyme immobilization by utilizing an adsorption carrier; performing affinity selective separation by utilizing the adsorption carrier loaded with an enzyme to obtain an active compound from the plant extract. According to the method disclosed by the invention, a hollow fiber is used as the adsorption carrier, and a traditional active screening mode of screening after separating is improved into a novel active screening mode of separating after screening and identifying, and thereby, the blindness of compound preparation and separation is greatly reduced. The method can be popularized to be applied to rapidly screen compounds with triglyceride enzyme inhibitory activity in natural products or traditional Chinese medicine mixtures.

The invention relates to a tyrosine kinase inhibitor and a preparation method and use thereof, and belongs to the technical field of pharmaceutical chemistry. The tyrosine kinase inhibitor having the structural features shown in the general formula I, or its pharmaceutically acceptable salts or stereoisomers can effectively inhibit tyrosine kinase activity, and can inhibit kinases such as DDR1, DDR2, Abl, Src, Btk and Kit. Compared with a positive contrast dasatinib, the tyrosine kinase inhibitor has higher half inhibitory concentration or the same half inhibitory concentration, and especially, aiming at DDR1, DDR2, Src, Btk and Kit, the compound 8j has lower K562 cell half inhibitory concentration. The tyrosine kinase inhibitor has good enzyme inhibitory activity and cell activity and has a large application prospect.

Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain.

The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.

A method for determination of acid phosphatase with carbon quantum dots as a photo active mimetic enzyme is disclosed. A carbon-quantum-dot-based photo active mimetic enzyme is provided, and the activity of the mimetic enzyme is found to be inhibited / recovered in the presence of Ce<3 + >/ PO4<3->, so that a new method for determination of the acid phosphatase (ACP) is established. A simple hydrothermal method is used to synthesize the carbon quantum dots, and the carbon quantum dots show high mimetic enzyme activity under visible light (lambda >= 400nm), and can catalyze chromogenic reactionof 3, 3 ', 5, 5'-tetramethyl benzidine. The catalytic activity is weakened by aggregation of the carbon quantum dots due to complex reaction of the Ce <3+> with carboxyl groups on the surface of theCDs (carbon quantum dots); in the presence of the PO4<3-> which is a hydrolysate of the ACP, a precipitate is formed by the Ce <3+>, so that the mimetic enzyme inhibitory effect on the CDs is eliminated, and the enzyme like catalytic activity of the system is restored. The detection limit of the activity of the ACP detected by the method can reach 0.02U / L, and the method has the advantages of convenient operation, high sensitivity and good selectivity and the like.

The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]:

wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as a prolyl hydroxylase inhibitor or erythropoietin production-inducing agent containing the compound. The compound of the present invention shows a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability and is useful as a prophylactic or therapeutic agent for various diseases and pathologies (disorders) caused by decreased production of erythropoietin.