Sichuan University

Yichang Humanwell Pharmaceutical Co., Ltd.

Jin Liu

Jun Luo

Jun Yang

Wensheng Zhang

Bowen Ke

Lei Tang

Weiyi Zhang

Cheng Zhou

Qinqin Yin

Hongzhe Shi

Zhengzheng Xiang

Lu Rong

Pu Yuan

Shaogang Qu

Baochun Yang

Hua Long

Lisi Lu

Xianzhi Yang

Shujie Zhao

Xiaocong Yu

Hongjun Zhang

A benzodiazepine compound represented by formula I, or a salt thereof has an intravenous sedative anesthesia effect. The recovery quality of the compound is significantly improved compared with remimazolam in rat and mouse caudal venous anesthesia models. During anesthetization, the compound has a rapid onset, a short duration, a quick recovery and a good tolerance, can be used for anesthesia induction, anesthesia maintenance and day surgery anesthesia.

Benzodiazepine compound, preparation method therefor, and use thereof in medicine

A nitrogen-containing derivative of substituted phenol hydroxyl acid ester is represented by formula (I). A salt of the compound of formula (I) has good water solubility, and in vivo, can rapidly and completely release substituted phenols having a pharmacological effect, which can improve the water solubility of substituted phenols, rapidly exert the pharmacological effects of substituted phenols in vivo, and has good safety. The method for preparing the above-mentioned compound is provided. This compound can also be used in the preparation of drugs that produce anaesthesia and/or sedative and hypnotic effects on humans and animals.

Nitrogen-containing derivative of substituted phenol hydroxy acid ester, and preparation and use thereof

A quaternary ammonium salt compound of formula I is fast-acting and has a long-term local anaesthetic effect after a single administration, the sensory nerve block time being longer than the motor nerve block time, has both a long-acting local anaesthetic effect and a selective local anaesthetic effect, and also significantly reduces the side effects of quaternary ammonium salt compounds with the structural features of surfactants and is highly safe; thus, the compound of formula I and the pharmaceutically acceptable salt thereof can be used for the preparation of saft drugs having a long-term local anaesthetic effect and a selective local anaesthetic effect

Quaternary ammonium salt compound, preparation method therefor and use thereof

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.

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. 

N-substituted imidazole carboxylic ester chiral compound containing an ether side chain, its preparation and application

Hydroxy acid compound of substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), Y&#x2550;Cstraight carbon chain. The compound can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has sedative, hypnotic and/or anesthetic effect. By protecting the hydroxyl group of 2, 6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2, 6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis, and/or anesthesia. 

Hydroxy acid ester compound of substituted phenol, preparation method and medical use thereof

Phosphate ester compound of hydroxy acid substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), in which Y&#x2550;Cstraight carbon chain, Mand/or M=H, alkali metal ion, protonated amine or protonated amino acid. The compound has good water solubility and high stability in its aqueous solution, and it can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has the effects of sedation, hypnosis and/or anesthesia. By protecting hydroxyl of 2,6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2,6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis and/or anesthesia. 

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Sichuan, China

Jin Liu