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公开(公告)号:US11697639B2
公开(公告)日:2023-07-11
申请号:US16969005
申请日:2019-01-31
发明人: Jin Liu , Bowen Ke , Wensheng Zhang , Jun Yang , Lei Tang
IPC分类号: C07D207/02 , C07D211/60 , C07C231/12 , C07C237/04 , C07D205/04 , C07D207/16 , C07D223/06 , C07D225/02
CPC分类号: C07D211/60 , C07C231/12 , C07C237/04 , C07D205/04 , C07D207/16 , C07D223/06 , C07D225/02
摘要: 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.
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公开(公告)号:US11161828B2
公开(公告)日:2021-11-02
申请号:US17044158
申请日:2019-07-24
发明人: Jun Yang , Jin Liu , Weiyi Zhang , Wensheng Zhang , Cheng Zhou , Bowen Ke , Lei Tang
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.
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公开(公告)号:US10011562B2
公开(公告)日:2018-07-03
申请号:US15327962
申请日:2015-07-22
发明人: Lei Tang , Jin Liu , Wensheng Zhang , Jun Yang , Bowen Ke , Qinqin Yin
IPC分类号: C07C237/04 , C07C237/16 , C07C231/12
CPC分类号: C07C237/04 , A61K31/167 , C07C219/04 , C07C231/12 , C07C237/16 , C07C237/20
摘要: 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.
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公开(公告)号:US11459298B2
公开(公告)日:2022-10-04
申请号:US17044520
申请日:2019-07-24
发明人: Jin Liu , Jun Yang , Wensheng Zhang , Bowen Ke , Weiyi Zhang , Cheng Zhou , Lei Tang
IPC分类号: C07D211/38 , C07D295/15 , C07D307/52 , C07D333/20 , C07D407/12 , C07D409/12
摘要: 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.
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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.
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公开(公告)号:US09969695B2
公开(公告)日:2018-05-15
申请号:US15107415
申请日:2014-10-30
发明人: Wensheng Zhang , Jun Yang , Jin Liu , Lei Tang , Bowen Ke
IPC分类号: C07D233/90 , A61P25/20 , A61P23/00
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.
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