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247results about How to "Has inhibitory activity" patented technology

5-substituted methylpyrrolidine-2, 4-diketone compound and use thereof

The invention relates to a 5-substituted methylpyrrolidine-2, 4-diketone compound and the use thereof. The structure of the 5-substituted methylpyrrolidine-2, 4-diketone compound is shown in a general formula (I), wherein R1, R2 and R3 are defined as the specification. The compound with the structure shown in the general formula (I) belongs to the technical field of applying compound to pesticide and can be used for preparing phytocide.
Owner:NANJING AGRICULTURAL UNIVERSITY

Hydroxyl phosphate amino acid ester derivatives of Brefeldin A, preparation method thereof, and application thereof

The invention relates to hydroxyl phosphate amino acid ester derivatives of Brefeldin A, a preparation method thereof, and an application thereof. The invention relates to a fungal metabolite. The derivatives comprises (+)-Brefeldin A-4,7-dihydroxyl phosphate amino acid ester, (+)-Brefeldin A-4-hydroxyl phosphate amino acid ester, and (+)-Brefeldin A-7-hydroxyl phosphate amino acid ester. According to the invention, Brefeldin A hydroxyl phosphate amino acid ester derivatives with high bioactivity, good dissolubility, and good bioavailability are synthesized. The derivatives are simple to prepare, and the cost is low. The derivatives are advantaged in novel structure, relatively stable structure, and substantial inhibitive activities against tumor cell proliferation. Compared with the original medicine (+)-Brefeldin A, the derivatives are advantaged in good dissolubility and long half-life period. The Brefeldin A hydroxyl phosphate amino acid ester derivatives can be applied in the preparations of anticancer medicines.
Owner:TIANJIN LINMEI TECH

C17-hydroxy-steroid lactone antitumour medicine

An anticancer 17-hydroxy-steroid lactone medicine for treating lung cancer, breast cancer, liver cancer, leukemia, etc is disclosed. Its advantages are simple preparing process and high suppression activity to A-549, MCF-7, BEL-7402 and P388.
Owner:SHANGHAI INST OF ORGANIC CHEMISTRY - CHINESE ACAD OF SCI

Gallbladder wood leaf composition containing strictosamide and preparation thereof

InactiveCN102600268AHas the effect of treating coughProlonged cough incubation periodOrganic active ingredientsRespiratory disorderKaempferol-3-O-rutinosideAllergic asthma
The invention relates to a gallbladder wood leaf composition containing strictosamide and a preparation thereof. The gallbladder wood leaf composition containing the strictosamide is characterized in that the composition is applied in the preparation of medicament for clearing heat and eliminating phlegm and relieving cough and asthma, and or is applied in the preparation of medicines used for treating expectoration, cough with dyspnea and irritability asthma; the composition is composed of alkaloid and flavonoid extracted from gallbladder wood leaf through combination, and the alkaloid contains strictosamide, 10-hydroxy-strictosamide and short snakeroot glucoside; and the flavonoid contains kaempferol-3-O-rutinoside and rutin. The invention also discloses a preparation of the composition. The gallbladder wood leaf composition provided by the invention has the advantages that the active ingredient is definite, and the gallbladder wood leaf composition has notable curative effects.
Owner:江苏中康药物科技有限公司 +1

Substituted pyrimidin-4-one derivatives

A pyrimidone derivative represented by formula (I) or a salt thereof: wherein: Y represents two hydrogen atoms, a sulphur atom, an oxygen atom; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted by a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R3 represents a phenyl-group, a phenyl-CH2- group, a C1-6 alkyl-O-C(O)- group, a phenyl-C(O)- group, a 5-10 membered heterocyclic group, a phenyl-CH2-O-C(O)- group, a -C(O)-5-10 membered heterocyclic group, these groups being optionnally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-6 alkoxy group, a C1-2 perhalogenated alkoxy group, a C1-6 alkylsulfonyl group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group or a C2-12 dialkylamino-group, an acetoxy group, an aminosulfonyl group; R4 represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-6 alkyl group; m represents 0 to 2, in the form of a free base or of an addition salt with an acid.
Owner:MITSUBISHI TANABE PHARMA CORP +1

Preparing method and application of peroxy-ergosterol compound

The invention discloses a preparing method of a peroxy-ergosterol compound. The preparing method comprises the steps of smashing blocks of poria cocos, conducting reflux extraction 3-5 times, recycling an extracting solution to obtain extract, adding water to disperse the extract, and using ethyl acetate to conduct extraction 5-10 times to obtain a crude extract; using dynamic axial industrially-prepared chromatography to separate the crude extract to obtain a relatively pure product of peroxy-ergosterol; recrystallizing the obtained relatively pure product of peroxy-ergosterol to obtain peroxy-ergosterol of which the purity is larger than 98%. The invention further discloses application of the peroxy-ergosterol compound in preparing a drug for resisting herpes simple virus I. The multiplication of HSV-I in cells can be inhibited, the multiplication of the virus can be 100% inhibited when the concentration of peroxy-ergosterol is 40.12Mug / mL, and the selection index of peroxy-ergosterol in HSV-I is 7.5. As is shown, peroxy-ergosterol can be applied to preparing the drug for resisting the herpes simplex virus-I(HSV-I).
Owner:JIANGSU KANION PHARMA CO LTD
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