Sichuan University

Lei Tang

Wensheng Zhang

Jun Yang

Jin Liu

Bowen Ke

Weiyi Zhang

Cheng Zhou

Bin Wang

Qinqin Yin

A compound is shown in formula I and can be in the form of a pharmaceutically acceptable salt, or a stereoisomer, or a solvate, or a prodrug, or a metabolite. The compound takes effect rapidly and has a long-time local anesthetic effect following a single dose, with the sensory nerve blocking time being greater than the motor nerve blocking time, has both a long-acting local anesthetic effect and a selective local anesthetic effect, significantly reduces side effects of the compositions QX314 and QX314 and a quaternary ammonium salt compound with surfactant structural characteristics, and is safer. The compound of formula I of the present invention and a pharmaceutically acceptable salt thereof can be used for preparing drugs that have a long-time local anesthetic effect and a selective local anesthetic effect.

Quaternary ammonium salt compound, preparation method therefor and use thereof

A dication compound represented by formula (I), stereoisomers having the structure of formula (I) or a mixture of the stereoisomers, a pharmaceutically acceptable salt, a solvate, or a eutectic crystal, and a composition thereof, and use of a composition, are capable of producing neuromuscular junction retardation, formed of same with a pharmaceutically acceptable carrier in the field of preparation of a medicament for muscular flaccidity.

Class of dicationic compounds as well as the preparative method and the use thereof

An N-substituted imidazole carboxylate compound is of formula (I). In formula (I), C* is an R-type chiral carbon atom, Rand Rare independently selected from H, methyl, ethyl, cyclopropyl, cyclobutyl or isopropyl, or Rand Rform a Calkylenyl group; Ris a substituted or unsubstituted Csaturated or unsaturated aliphatic hydrocarbon or aromatic hydrocarbon, in which the aliphatic hydrocarbon comprises a straight chain, branched chain or cyclic aliphatic hydrocarbyl. The compound or pharmaceutically acceptable salts thereof can be used to prepare central inhibitory drugs that exert sedative, hypnotic and/or anesthetic effects on humans or animals, and can produce rapid and reversible anesthetic effects, and can be rapidly metabolized into an inactive etomidate acid, and after drug withdrawal, the wake-up quality is good; and the body's corticosteroid function can be rapidly recovered after a single administration or continuous administration. 

N-substituted imidazole carboxylate compound, preparation method and use

A two-quaternary ammonium compound has a structural formula of formula (I). L1 is a C1 to C8 alkylene group; L2 is a C1 to C8 alkylene group; Z1 is nitro group or a halogen or methoxy group; Z2 is nitro group or a halogen or methoxy group; Z3 is nitro group or a halogen or methoxy group; R&#x2550;H or a C1 to C6 alkyl group; a, b, and c are independently an integer from 0-5; and M is a pharmaceutically acceptable anion, such as a bromine ion, chlorine ion, sulfonate radical, etc. A stereoisomer or mixture of stereoisomers, or a pharmaceutically acceptable salt or solvate or eutectic of the compound of formula (I) forms a composition with a pharmaceutically acceptable carrier, or forms a compounded prescription with other active components, and the composition or compounded prescription may be used in the preparation of a muscle relaxant.

Class of bisquaternary ammonium compound as well as the preparative method and the use thereof

The present invention relates to long-chain dimethylaniline derivative compounds, their preparation methods, self-assembled texture, and uses thereof. Said compounds show ultralong acting anaesthetic effect, and belong to N-diethylaminoacetyl-2,6-dimethylaniline compounds, having a structure according to formula (I). Said compounds may self-assemble into micelle or gel in an aqueous solvent, and exert an in vivo elongated local anesthetic actions. Local anesthesia and/or analgesic activity can last more than 72 hours. The biomaterials can self-assemble into micelles or gels in water and have local anesthetic effect, as well as can further be used as the coating of medicinal bioactive molecules for treatment of pain, itching and the like and/or the drug carriers, together with as pharmaceutical adjuvants for delivery system. Thus, said materials have a favorable perspective. 

Long-chain dimethylaniline derivative compounds, their preparation methods, self-assembled textures, and uses thereof

The present invention relates to an N-substituted imidazole carboxylic ester chiral compound containing an ether side chain and to its preparation and application. The structure of this compound is represented by Formula (I). This compound can induce a rapid and reversible general anesthesia effect. Animal experiments show that this compound has rapid and short-acting pharmacological characteristics, so that it can be used as a rapid and short-acting general anesthesia medicine. Compared with etomidate, this compound can reduce the inhibition on the synthesis of adrenal cortical hormone, with an advantage of rapid and full recovery of the post-operative patient. The only chiral carbon in the compound structure belongs to the R form. This imidazole ring in the compound structure has acidifiable N atoms, so that this compound or its related pharmaceutically-acceptable salts can be used in preparation of the central inhibitory medicines, which can produce sedative, hypnotic and/or anesthetic effects on animals or human beings via their intravenous or non-intravenous administration. 

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Sichuan, China

Lei Tang