36results about How to "Good inhibitory activity" patented technology

An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I:

wherein wherein A, B, R², R³, L, M¹, M², M³, M⁴, Y¹, Y⁰, Z and Sp are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.

The present invention discloses sialic acid analogues as shown in formula I, or pharmaceutically acceptable salts and application thereof, and belongs to the field of pharmaceutical chemistry. A series of sialic acid analogues are obtained by use of zanamivir as a lead compound for transformation of the side chain of the molecular structure, the sialic acid analogues or the pharmaceutically acceptable salts have good inhibitory activity on influenza virus neuraminidase, so that the sialic acid analogues can be used to prepare anti-influenza virus drugs.

A small molecule inhibitor of MERS-CoV main protease, designed based on the crystal structure of the new coronavirus MERS-CoV main protease, the present invention also provides a synthesis method of the small molecule inhibitor, and its preparation for treatment and prevention Use in medicine for MERS‑CoV infection. The MERS-CoV main protease small molecule inhibitor of the present invention can significantly inhibit the activity of the MERS coronavirus main protease, and at the same time, it also has good inhibitory activity on the coronavirus main proteases such as SARS and MHV, and is used in the preparation for treating or preventing coronavirus infection. It has a good application prospect in medicine.

The invention discloses a 4-hydroxyl pyrroline-2-ketone derivative containing 1,3,4-oxadiazole and a preparation method and application of the 4-hydroxyl pyrroline-2-ketone derivative. The structural general formula (I) is shown in the description, wherein in the formula (I), R1 is substitute arene and substitute benzyl, and R2 is substitute arene and hydrogen. The 4-hydroxyl pyrroline-2-ketone derivative has good bacterium and plant virus resisting activity, and is stable.

The present invention belongs to the field of pharmaceuticals and chemical industry, and discloses preparation of a quinoline-based derivative based on topoisomerase I inhibition, and uses of the quinoline-based derivative as an anti-inflammatory drug, wherein the structural formula of the quinoline-based derivative is represented by a formula (I), R1 is hydrogen, fluorine, chlorine, bromine, iodine, methoxy, methyl, trifluoromethyl, nitro and nitrile, R2 and R3 respectively are hydrogen, chlorine, bromine, iodine, methoxy, methyl, trifluoromethyl, nitro and nitrile, R4 is carboxyl, methyl, phenyl, cyano and hydrogen, n is 0, 1, 2 and 3, and X is CH or N. According to the present invention, the quinoline-based derivative can remarkably inhibit the activity of human DNA topoisomerase I, provides significant inhibition effects in inflammations, and has broad application space in the preparation of anti-inflammatory drugs. The formula (I) is defined in the specification.

The invention belongs to the technical field of medicine, discloses 13 types of novel oleanane-type pentacyclic triterpenoid-type compounds, six types of structures comprising the oleanane-type pentacyclic triterpenoid compounds, and preparation methods, and further provides extraction methods for extractives of shells and carpopodium of shinyleaf yellowhorn, and application of the compounds and the extractives to prevention of human cerebral glioma, human liver cancer, human pancreatic cancer, human stomach cancer and human colorectal cancer. The compounds and the extractives, which have antitumor activity, can be extracted from the shells and the carpopodium of shinyleaf yellowhorn, other plants of Sapindaceae, or other biological resources, and can also be obtained according to chemosynthesis.

The invention provides a thiazole derivative useful as a VAP-1 inhibitor, as well as a pharmaceutical agent for the prophylaxis or treatment of VAP-1 associated diseases and the like, a method of inhibiting VAP-1 in a subject, and a method for the prophylaxis or treatment of VAP-1 associated disease in a subject. The thiazole derivative is a compound represented by the formula (I): R¹—NH—X—Y—Z wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.

The invention discloses a 6-chloro-2-aminobenzothiazole derivative as well as a preparation method and application thereof. The structure of the 6-chloro-2-aminobenzothiazole derivative is shown in a formula (I), wherein R is selected from substituted or unsubstituted benzyl, C2-C5 alkyl, substituted or unsubstituted benzolyl or C1-C6 alkyl acyl; and the benzyl or a substituent group on the benzyl is independently selected from C1-C4 alkyl, C1-C4 alkoxy, nitryl or halogen. The 6-chloro-2-aminobenzothiazole derivative has better inhibitory activity on tumor cells highly expressed by EGFRWT, provides a new strategy and a new thought for tumor treatment and provides a new direction and a new thought for research and development of anti-tumor drugs. (The formula (I) is described in the specification).

The invention discloses an anti-inflammatory tetrapeptide, an extraction and separation method therefor and application of the anti-inflammatory tetrapeptide in preparation of drugs for improving memory. The anti-inflammatory tetrapeptide has an amino acid sequence of Gly-Val-Tyr-Tyr. The extraction and separation method for the anti-inflammatory tetrapeptide comprises the following steps: extracting walnut proteins from walnut meal through alkali-solution and acid-isolation, weighing the walnut proteins, adding deionized water into the weighed walnut proteins for mixing, carrying out enzymolysis, and taking supernatant, so as to obtain a walnut protein enzymolysis solution; collecting permeate with an ultrafiltration membrane with the molecular weight of 3kDa; and introducing a lower-molecular-weight component sample of the walnut protein enzymolysis solution to a gel filtration chromatographic column, carrying out eluting with deionized water, employing a detection wavelength of 220nm, collecting and merging a plurality of elution peak components, carrying out mass spectrometric detection on the component with relatively high anti-inflammatory activity, and confirming that the component contains the anti-inflammatory tetrapeptide disclosed by the invention. The anti-inflammatory tetrapeptide disclosed by the invention has relatively good inhibiting activity to LPS stimulatedBV-2 cell inflammation reactions and can be used for preparing memory improving drugs or healthy products.

The invention discloses a Yacon antidiabetic extraction, which is characterized in that the weight percentage of smallanthus sonchifolius diterpenoid acid with the general formula (I) is 0.1 to 100 percent. The preparation method of the Yacon antidiabetic extraction comprises the following steps: first, using water or low-concentration ethanol to extract Yacon leaf and get Yacon leaf concentrated extractant via concentration; next, using water or/and low-concentration ethanol first and then high-concentration ethanol to elute the macroporous resin column on Yacon leaf concentrated extractant to collect high-concentration ethanol eluate; then, concentrating the high-concentration ethanol eluate via reduced pressure; finally, drying and refining. The extract has the advantages of good antidiabetic function proven in vitro test so as to be used for preparing the antidiabetic medicine and easy preparation method, thus being suitable for industrial production.

The invention provides a 6H-indolo[2,3-b]quinoxaline derivative, and a preparation method and application thereof. The general formula is as shown in the specification. The preparation method comprises a step of preparing the 6H-indolo[2,3-b]quinoxaline derivative by taking o-phenylenediamine, indoldione, dihaloalkane and amine compounds as raw materials. The compounds provided by the invention show good antitumor activity.

The invention provides the application of myricetin and a pharmaceutically acceptable salt thereof to the preparation of a medicine for inhibiting the interaction of an integrase and an integrated cofactor for a human immunodeficiency virus infection-related disease. The pharmaceutically acceptable salt is an acid addition salt formed by a compound of formula I and an inorganic acid or an organicacid. The inorganic acid is one or more of hydrochloric acid, phosphoric acid or sulfuric acid, and the organic acid is one or more of acetic acid, maleic acid, citric acid, benzenesulfonic acid, methyl benzenesulfonic acid, fumaric acid or tartaric acid.

(The formula I is as shown in the description.) The invention provides a preparation process and application of an aryl bisphosphonate derivative with the structure as shown in the formula (I) or physiologically acceptable salt as well as a pharmaceutical composition comprising the derivative. The pharmacodynamic test proves that the compound provided by the invention has high inhibition activityon beta-lactamase, in particular the compounds 46 and 50 have the most excellent inhibition activity which is obviously better than that of the currently reported beta-lactamase micromolecular inhibitors such as captopril. The substituted aryl bisphosphonate derivative has specific medicine effect and provides new pharmacy choice for the clinic.

The present invention pertains to the field of medical technology, and particularly relates to a heterocyclic substituted pyrimidine compound represented by General Formula (I) and its pharmaceutically acceptable salt thereof, wherein R¹, R², R³, R⁴ and R⁵ are as defined in the description, the present invention also relates to a preparation method of the compound, a pharmaceutical composition containing the compound, and a use of the compound and the pharmaceutical composition in preparation of a medicine for enhancing a cGMP signal transduction function or a medicine for treating or preventing sexual dysfunction and diseases with lower urinary tract symptoms.

The invention provides a 1H-indazole-3-aminobiphenyl compound as well as a preparation method and an application thereof. the 1H-indazole-3-aminobiphenyl compound takes 1H-indazole-3-aminobiphenyl as a skeleton and has a structural formula as shown in the specification, wherein single substitution or bis substitution is carried out on a benzene ring, R is halogen, alkyl or alkoxy, and R1 is chain or cyclic aliphatic diamino. The 1H-indazole-3-aminobiphenyl compound is prepared by organic synthesis reaction with five steps, has the advantages of simpleness in operation of reaction process, easiness in raw material acquisition, mild reaction conditions, cheap used reagent and the like, is suitable for mass production of pharmaceutical enterprises, has very good inhibition activity to Bcr-Abl kinase, is capable of inhibiting proliferative activity of tumor cells, can be used for preparing antitumor drugs and drugs for inhibiting the activity of the Bcr-Abl kinase and has good application prospect and scientific value.

The invention provides a cyclomalonamide compound with antitumor activity, and a preparation method and application thereof. The compound has a structural formula as described in the specification. In the structural formula, R1 is a halogen group; and R2 is a halogen group or a group as described in the specification, or a group formed by R1 and R2 together. The compound provided by the invention has good inhibitory activity to VEGFR-2 kinase, so a signal channel induced by the VEGFR-2 kinase can be blocked through inhibition of the activity of the VEGFR-2 kinase, and proliferation and migration of tumor cells are inhibited; thus, the compound can be applied in preparation of antitumor drugs. Meanwhile, the preparation method for the compound has the following advantages: raw materials are easily available; reaction conditions are mild; the process of reaction is simple to operate; and used reagents are cheap.

The invention discloses a diarylurea PI3Kalpha/mTOR double-target inhibitor as well as a pharmaceutical composition, and application of the diarylurea PI3K alpha/mTOR double-target inhibitor and the pharmaceutical composition. The diarylurea PI3Kalpha/mTOR double-target inhibitor comprises a substituted triazine compound with a general formula (I) described in the specification, and a stereoisomer, a hydrate or a pharmaceutically acceptable salt thereof. The diarylurea PI3Kalpha/mTOR double-target inhibitor provided by the invention and the pharmaceutical composition containing the diarylurea PI3K alpha/mTOR double-target inhibitor can be used for inhibiting PI3Kalpha/mTOR double kinase and proliferative diseases caused by the PI3Kalpha/mTOR double kinase, and an inhibitor with better effectiveness and selectivity can be provided for treatment of the PI3Kalpha/mTOR double-kinase-induced proliferative diseases.

The invention discloses an alpha-glucosidase inhibitor, and a synthesis method and application thereof. The invention aims to provide the alpha-glucosidase inhibitor with a relatively good hypoglycemic effect. The structural formula of the alpha-glucosidase inhibitor is shown in the specification, wherein R1 is selected from H or CH3, and R2 is selected from the groups shown in the specification.The invention belongs to the technical field of medicines.

The present invention relates to a vine polyphenol and its preparation method and application. The preparation method comprises the following steps: pulverizing the vine polyphenol, and then sieving to collect the fine powder; extracting the fine powder with ethanol, and then filtering to collect the filtrate; The filtrate is concentrated until the ethanol is completely volatilized to obtain crude polyphenols; the crude polyphenols are dissolved in an aqueous ethanol solution with a volume fraction of 70%, and then loaded on an AB-8 macroporous resin column, and then the volume fraction is 50%- 80% ethanol aqueous solution was used for elution, and the eluate was collected; the eluate was concentrated to dryness under reduced pressure to obtain the polyphenols of Echinaceae. The present invention adopts the method of alcohol extraction to extract the vine polyphenols, and the prepared vine polyphenols have the advantages of high stability and good therapeutic effect on eczema caused by microbial infection, and can be applied to the preparation of prevention and/or treatment of eczema, especially microbial infection Caused by eczema medications.

The invention belongs to the field of traditional Chinese medicine modernization, and relates to traditional Chinese medicine grub glucan and application thereof. The molecular weight of the traditional Chinese medicine grub glucan is 1-4*10<4>Da, the composition of monosaccharide is glucose, and the sugar content is greater than 90%. The traditional Chinese medicine grub glucan has strong specificity affinity with ALDOA and can inhibit the activity of ALDOA, so that the traditional Chinese medicine grub glucan has remarkable effects of preventing or treating cancers, diabetes and complications thereof, obesity and related metabolic diseases thereof, viral meningitis, arthritis and myocardial hypertrophy.

Novel 4-phenylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I):

formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of pigmentary disorders, or for preventing and/or treating signs of skin aging, and/or for body or hair hygiene.

Novel 4-heteroarylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I):

formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of pigmentary disorders, or for preventing and/or treating signs of skin aging, and/or for body or hair hygiene.

Provided is a compound represented by formula (I) or a pharmacologically acceptable salt thereof:

wherein L¹ is an optionally substituted C_1-6 alkylene group or the like, L² is a single bond or the like, L³ is a single bond or the like, R¹, R², and R³ are each independently an optionally substituted C_1-4 alkyl group or the like, R⁴ is a hydrogen atom or the like, and R⁵ is a hydrogen atom or the like.

The invention belongs to the technical field of medicine, and particularly relates to use of bromophenol-pyrazoline compounds in the treatment of porcine coronavirus diseases. Through the research in the invention, it is found that the bromophenol-pyrazoline compounds inhibit replication of porcine coronaviruses at a cellular level, and can treat porcine coronavirus diseases (such as PEDV and TGEV) in clinical trials, greatly improving the survival rate of infected piglets, so the compounds can be used to prepare drugs for treating porcine coronavirus diseases.

The invention discloses a purine-ring-containing benzene sulfonamide chalcone derivative and preparation and application methods thereof. The purine-ring-containing benzene sulfonamide chalcone derivative has a formula (I) shown as below, in which R1 is 4-oxymethyl, 4-tert-butyl, 4-methyl, 4-flouride, 4-bromide, 2-methyl, 2-fluoride, 2-chloride, 2-bromide and hydrogen atom and R2 is methyl, ethyland benzyl. The purine-ring-containing benzene sulfonamide chalcone derivative can inhibit tobacco mosaic virus, cucumber mosaic virus, potato Y virus and southern rice black-streaked dwarf virus.

The present invention addresses the problem of providing an inhibitor which has an excellent inhibitory activity on a p21-activated kinase. The present invention, by which has been solved the above-mentioned problem, is a p21-activated kinase 1 inhibitor containing, as an active ingredient, one or more compounds selected from the group consisting of dehydrokawain compounds, derivatives of dehydrokawain compounds, mimosine, derivatives of mimosine, and cucurbitacin compounds.

The present invention provides a pharmaceutical composition for preventing or treating atopic dermatitis comprising 2-amino-1,9-dimethylpurin-6-one or its pharmaceutically acceptable salt as an active ingredient. And also, the present invention provides a cosmetic composition for improving atopic dermatitis comprising 2-amino-1,9-dimethylpurin-6-one or its pharmaceutically acceptable salt; and a food (i.e., a functional food) for preventing or improving atopic dermatitis comprising 2-amino-1,9-dimethylpurin-6-one or its pharmaceutically acceptable salt.

A composition for preventing, ameliorating or treating breast cancer, the composition containing a 2,3,5-substituted thiophene compound according to one embodiment of the present disclosure has an excellent activity of inhibiting the proliferation of breast cancers, particularly triple-negative breast cancer and Herceptin-resistant breast cancer, which have high mortality because there has yet been no effective therapeutic method therefor. Thus, the composition may be advantageously used for the prevention, amelioration or treatment of breast cancer.

The invention discloses a novel nitrogen and sulfur-contained benzotricycloheterocycle compound having anti-inflammation and antifungal activities, namely 2, 3, 3a, 4-tetrahydrothiochromeno pyrazole compound. In the invention, aiming at the existing research and development condition of few antifungal drug and high toxicity in the prior art, the novel 2, 3, 3a, 4-tetrahydrothiochromeno pyrazole compound is designed and synthesized, fungi experiments are carried out and results from the experiments indicate that the compound has favorable antifungal activity. The novel benzotricycloheterocycle compound of the invention has the advantages of simple synthesis method and easily obtained raw materials, and the specifications show the synthesis method in detail. The products of the invention can be used for anti-inflammation and antifungal drugs.

A nitrogenous heterocyclic compound, a preparation method, an intermediate, a composition, and an application. The present invention provides a nitrogenous heterocyclic compound as represented by formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, diastereoisomers thereof, tautomers thereof, solvates thereof, metabolites thereof, or prodrugs thereof. The compound has high inhibitory activity against ErbB2 tyrosine kinase, has good inhibitory activity against human breast cancer cells BT-474, human gastric cancer cells NCI-N87 and the like with high expression of ErbB2, and in addition has relatively weak inhibitory activity against EGFR kinase, that is, the compound is an EGFR/ErbB2 double target inhibitor that attenuates EGFR kinase inhibitory activity or a small-molecule inhibitor having selectivity for an ErbB2 target. (I)