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

    公开(公告)号:US11161828B2

    公开(公告)日:2021-11-02

    申请号:US17044158

    申请日:2019-07-24

    IPC分类号: C07D295/15 A61P21/02

    摘要: 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═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.

    N-substituted imidazole carboxylate compound, preparation method and use

    公开(公告)号:US11208385B2

    公开(公告)日:2021-12-28

    申请号:US16488484

    申请日:2018-01-31

    IPC分类号: C07D233/90

    摘要: An N-substituted imidazole carboxylate compound is of formula (I). In formula (I), C* is an R-type chiral carbon atom, R1 and R2 are independently selected from H, methyl, ethyl, cyclopropyl, cyclobutyl or isopropyl, or R1 and R2 form a C2˜5 alkylenyl group; R3 is a substituted or unsubstituted C1-18 saturated 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 carboxylic ester chiral compound containing an ether side chain, its preparation and application

    公开(公告)号:US09969695B2

    公开(公告)日:2018-05-15

    申请号:US15107415

    申请日:2014-10-30

    CPC分类号: C07D233/90 C07B2200/07

    摘要: 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.