Abstract: The present invention belongs to the medical field, and relates to novel ?-lactamase inhibitors, for the treatment of bacterial infections in combination with ?-lactam antibiotics, including infection caused by drug resistant organisms and especially multi-drug resistant organisms. The present invention includes compounds according to formula (I): or pharmaceutically acceptable salts thereof, wherein M and R are as defined herein.

Abstract: An application of N1-dihydrocaffeoyl-N10-caffeoylspermidine in preparation of a drug, health product or functional food is disclosed. It belongs to the technical field of pharmaceutical chemistry. In the dose range of 2-100 mg/kg given to experimental animals, N1-dihydrocaffeoyl-N10-caffeoylspermidine can significantly reduce the number of activities, shorten the sleep latency and prolong the sleep duration of mice with insomnia, and at the same time, it can significantly regulate back the indicator levels of neurotransmitters such as 5-HT, 5-HIAA, GABA and Glu in the brain tissues of mice with insomnia. All of the above confirm that N1-dihydrocaffeoyl-N10-caffeoylspermidine have a sedative hypnotic effect and can be applied for the prevention and treatment of psychiatric disorders such as insomnia, anxiety and depression.

Abstract: ?-lactamase inhibitors, pharmaceutical compositions including the same, methods of preparing the same, and methods of treating bacterial infections in combination with ?-lactam antibiotics, including infection caused by drug resistant organisms and especially multi-drug resistant organisms. The present invention includes compounds according to formula (I) or pharmaceutically acceptable salts thereof, wherein M and R are as defined herein.

Abstract: A monobactam compound of formula (I), a preparation thereof, and a use thereof as antibiotic agents for the treatment of bacterial infections are provided. In the formula (I), M is hydrogen or a pharmaceutically acceptable salt forming cation, R1 and R2 represent independently of one another hydrogen or methyl, W represents a bond or O, X represents CR4 or N, R4 represents halogen, R3 represents hydrogen, amino, hydroxy, (C1-C6)-alkyl, or a 4-, 5- or 6-membered nitrogen-containing heterocycle.

Abstract: A N-heterocyclic five-membered ring-containing capsid protein assembly inhibitor, and a pharmaceutical composition and use thereof, specifically relating to a compound as represented by formula I, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a medical use thereof. The medical use comprises the use in treating diseases benefiting from the capsid protein assembly inhibitor, and in particular, diseases caused by hepatitis B virus infection.

Abstract: Provided are ?-lactam compounds of formula (I), their preparation and use as antibiotic agents for the treatment of bacterial infections: Wherein X, W, R1, R2 and R3 are defined herein.

Abstract: A N-heterocyclic five-membered ring-containing capsid protein assembly inhibitor, and a pharmaceutical composition and use thereof, specifically relating to a compound as represented by formula I, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a medical use thereof. The medical use comprises the use in treating diseases benefiting from the capsid protein assembly inhibitor, and in particular, diseases caused by hepatitis B virus infection.

Abstract: Provided is a compound of formula I or II, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and the medical uses thereof in treating diseases benefiting from the capsid protein assembly inhibitor, particularly diseases caused by hepatitis B virus infection.

Abstract: A N-heterocyclic five-membered ring-containing capsid protein assembly inhibitor, and a pharmaceutical composition and use thereof, specifically relating to a compound as represented by formula I, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a medical use thereof. The medical use comprises the use in treating diseases benefiting from the capsid protein assembly inhibitor, and in particular, diseases caused by hepatitis B virus infection.

Abstract: Hydroxypropyl-sulfobutyl-&bgr;-cyclodextrin, the preparation method, analytical method, and the pharmaceutical application thereof. The hydroxypropyl-sulfobutyl-&bgr;-cyclodextrin is a derivate of cyclodextrin which is substituted by hydroxypropyl group and sulfobutyl group: n-(2,3,6-O-2-hydroxypropyl)-m-(2,3,6-O-sulfobutyl)-&bgr;-cyclodextrin. The number of substituent groups per mole cyclodextrin is n hydroxypropyl groups and m sulfobutyl groups. “n” represents the average substituent degree of hydroxypropyl groups; “m” represents the average substituent degree of sulfobutyl groups; “n+m=z” is the gross average substituent degree, in which n is a random integer chosen from 1,2,3,4,5,6,7,8,9; m is a random integer chosen from 1,2,3,4,5,6,7,8,9; and the gross average substituent degree z is a random integer chosen from 2,3,4,5,6,7,8,9,10. The present invention shows low haemolysis and low toxicity.

Abstract: Hydroxypropyl-sulfobutyl-&bgr;-cyclodextrin, the preparation method, analytical method, and the pharmaceutical application thereof. The hydroxypropyl-sulfobutyl-&bgr;-cyclodextrin is a derivate of cyclodextrin which is substituted by hydroxypropyl group and sulfobutyl group: n-(2,3,6-O-2-hydroxypropyl)-m-(2,3,6-O-sulfobutyl)-&bgr;-cyclodextrin. The number of substituent groups per mole cyclodextrin is n hydroxypropyl groups and m sulfobutyl groups. “n” represents the average substituent degree of hydroxypropyl groups; “m” represents the average substituent degree of sulfobutyl groups; “n+m=z” is the gross average substituent degree, in which n is a random integer chosen from 1, 2, 3, 4, 5, 6, 7, 8, 9; m is a random integer chosen from 1, 2, 3, 4, 5, 6, 7, 8, 9; and the gross average substituent degree z is a random integer chosen from 2, 3, 4, 5, 6, 7, 8, 9, 10. The present invention shows low haemolysis and low toxicity.