45 results about "Narcotic Effects" patented technology

The invention provides N-diethylaminoacetyl-2,6-dimethylaniline derivatives, a preparation method and applications thereof. The structure of the derivatives is represented by the formula (I). The preparation method comprises the following steps: carrying out reactions between N-diethylaminoacetyl-2,6-dimethylaniline and halogenated compounds to obtain a corresponding quaternary ammonium salt intermediate, and then subjecting the quaternary ammonium salt intermediate to react with corresponding 2-methoxyl-4-subsituted phenol derivative raw material so as to obtain the N-diethylaminoacetyl-2,6-dimethylaniline derivatives. The derivatives can be used as a long-acting local anesthetic drug or a pain relieving drug capable of separating the motion and the feeling, can exert a reversible and lasting local anesthetic effect in organism bodies, do not affect motor function in a certain dosage range, and have an ideal retardant effect on separation of motion and feeling.

The invention discloses an application of an N-acetanilide cationic compound in preparation of a local nerve blocking drug. The cationic compound is a quaternary ammonium salt compound and has a structure as shown in a formula (I), wherein X is a halogen atom. When used alone, the compound has the characteristics of good safety performance, strong nerve blocking effect and the like, can take a reversible and durable local anaesthesia effect in vivo and can be used as a local anaesthesia drug or an analgesic drug which is long-acting and / or capable of realizing selective blocking. Particularly, a composition composed of the compound and other local anaesthesia drugs has the remarkable characteristics of high effect taking speed, strong effect, long acting time, little nerve injury and the like when used for nerve blocking.

The invention discloses a compound as shown in the formula I, or a stereisomer, or pharmaceutically acceptable salt, or a solvate, or a prodrug, or a metabolite, or a deuterated derivative thereof. The compound is an N-substituted imidazole formate derivative with a novel structure and belongs to the field of medicinal chemistry. The invention also discloses application of the N-substituted imidazole formate derivative in the preparation of medicines with sedative, hypnotic and / or anesthetic effects, and application in the preparation of medicines capable of controlling the status epilepticus.The compound has a good inhibitory effect on the central nervous system, and provides a new selection for clinical screening and / or preparation of medicines with the sedative, hypnotic and / or anesthetic effects and capable of controlling the status epilepticus.

The invention discloses a compound as shown in the formula I, or a stereisomer, or pharmaceutically acceptable salt, or a solvate, or a prodrug, or a metabolite, or a deuterated derivative thereof. The compound is an N-substituted imidazole formate derivative with a novel structure and belongs to the field of medicinal chemistry. The invention also discloses application of the N-substituted imidazole formate derivative in the preparation of medicines with sedative, hypnotic and / or anesthetic effects, and application in the preparation of medicines capable of controlling the status epilepticus.The compound has a good inhibitory effect on the central nervous system, and provides a new selection for clinical screening and / or preparation of medicines with the sedative, hypnotic and / or anesthetic effects and capable of controlling the status epilepticus.

The invention relates to a propofol ester derivative containing an amino carboxylic acid amide structure, its preparation method and its purpose. The derivative has a following formula (I), in the formula, M is H, NH4 or pharmaceutically acceptable alkali metal element or alkali earth metal element, n=1-3, m=1-7, x=1 / 2-1. 2,6-diisopropyl phenol (II) is taken as a raw material, reacted with diacid or the corresponding anhydride to obtain a 2,6-diisopropyl phenol monoester intermediate, and continuously reacted with amino carboxylic acid to obtain the corresponding product (I). The propofol ester derivative can be used for preparing injection type central inhibition medicaments for generating effects of calmness, hypnosis and / or anaesthesia on animals and human, and is capable of improving the water-solubility of propofol, reducing the toxic and side effects of original drug and analogous prodrug, increasing the stability of profrug in vitro and increasing the application scope. The preparation method is simple which has industrial application value.

The invention discloses a compound shown in a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt of the compound, or a solvate of the compound, or a prodrug of the compound, or a metabolite of the compound, or a deuterated derivative of the compound. The compound is a substituted pyrazole formate derivative with a novel structure and belongs to the field of pharmaceuticalchemistry. The invention also discloses an application of the substituted pyrazole formate derivative in preparing medicines with sedative, hypnotic and / or anaesthesia effects and in preparing medicines capable of controlling a continuous epilepsy state. The compound has a good inhibiting effect on central nervous system, and provides a new choice for clinically screening and / or preparing medicines which have sedative, hypnotic and / or anaesthesia effects and can control a continuous epilepsy state.

The invention discloses a compound as shown in the formula I, or a stereisomer, or pharmaceutically acceptable salt, or a solvate, or a prodrug, or a metabolite, or a deuterated derivative thereof. The compound is an N-substituted imidazole formate derivative with a novel structure and belongs to the field of medicinal chemistry. The invention also discloses application of the N-substituted imidazole formate derivative in the preparation of medicines with sedative, hypnotic and / or anesthetic effects, and application in the preparation of medicines capable of controlling the status epilepticus.The compound has a good inhibitory effect on the central nervous system, and provides a new selection for clinical screening and / or preparation of medicines with the sedative, hypnotic and / or anesthetic effects and capable of controlling the status epilepticus.

N-diethylaminoacetyl-2,6-dimethylaniline derivative, preparation method and use. The structure of said derivative is shown in formula (I). During preparation, the corresponding quaternary ammonium salt intermediate compound can be prepared from N-diethylaminoacetyl-2,6-dimethylaniline and halogenated compounds first, and then the corresponding 2-methoxy-4-substituted phenol derivative It is obtained after the reaction of similar raw materials. The derivative can be used as a local anesthetic or analgesic drug with long-acting and motor-sensory separation, can exert a reversible and long-lasting local anesthetic effect in the living body, and has no effect on motor function within a certain dose range, and has ideal movement and sensation Detached blocking effect.

The invention discloses a compound as shown in the formula I, or a stereisomer, or pharmaceutically acceptable salt, or a solvate, or a prodrug, or a metabolite, or a deuterated derivative thereof. The compound is an N-substituted imidazole formate derivative with a novel structure and belongs to the field of medicinal chemistry. The invention also discloses application of the N-substituted imidazole formate derivative in the preparation of medicines with sedative, hypnotic and / or anesthetic effects, and application in the preparation of medicines capable of controlling the status epilepticus.The compound has a good inhibitory effect on the central nervous system, and provides a new selection for clinical screening and / or preparation of medicines with the sedative, hypnotic and / or anesthetic effects and capable of controlling the status epilepticus.

The invention relates to a propofol ester derivative containing an amino carboxylic acid amide structure, its preparation method and its purpose. The derivative has a following formula (I), in the formula, M is H, NH4 or pharmaceutically acceptable alkali metal element or alkali earth metal element, n=1-3, m=1-7, x=1 / 2-1. 2,6-diisopropyl phenol (II) is taken as a raw material, reacted with diacid or the corresponding anhydride to obtain a 2,6-diisopropyl phenol monoester intermediate, and continuously reacted with amino carboxylic acid to obtain the corresponding product (I). The propofol ester derivative can be used for preparing injection type central inhibition medicaments for generating effects of calmness, hypnosis and / or anaesthesia on animals and human, and is capable of improving the water-solubility of propofol, reducing the toxic and side effects of original drug and analogous prodrug, increasing the stability of profrug in vitro and increasing the application scope. The preparation method is simple which has industrial application value.

Long-chain amine-substituted dimethylanilinium compounds, preparation, self-assembly structure and use. This type of compound can have super long-acting anesthetic effect and low neuropathological damage. It is a kind of long-chain amine-substituted N-diethylaminoacetyl-2,6-dimethylanilinium compound, and its structure is shown in formula (I) , and salts of such compounds, the structure of which is shown in formula (II). The compound can self-assemble in aqueous solvents to form microscopic particles including spherical micelles, Janus micelles and vesicles, and can exert long-term local anesthesia in vivo, and the local anesthesia and / or analgesic time can exceed 120 hours, neuropathological damage is low, and the safety is much higher than that of the published long-acting local anesthetic compounds.

The invention discloses a ketone-substituted heterocyclic compound and its anesthetic effect. Specifically provided are compounds represented by formula I, or pharmaceutically acceptable salts thereof, or stereoisomers thereof, or deuterated derivatives thereof. The ketone-substituted heterocyclic compound provided by the present invention has a good inhibitory effect on the central nervous system, can produce sedative, hypnotic and / or general anesthesia, and can control status epilepticus; the ketone-substituted heterocyclic compound maintains excellent anesthetic activity At the same time, it also has the characteristics of rapid onset and rapid recovery; at the same time, the ketone-substituted heterocyclic compound has almost no inhibitory effect on the function of the adrenal cortex, and has little side effects, which solves the technical problems in this field. Or the preparation of drugs for sedation, hypnosis and / or general anesthesia and drugs for controlling status epilepticus provides a new option.

The invention discloses a quaternary ammonium salt compound, a preparation method and application thereof, and belongs to the field of chemical medicine. The present invention provides a compound represented by formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or a solvate thereof, or a prodrug thereof, or a metabolite thereof. The compound has quick onset, long-term local anesthesia effect after a single administration, sensory nerve block time longer than motor nerve block time, both long-acting local anesthesia effect and selective local anesthesia effect, and significantly reduces The side effects of the quaternary ammonium salt compound with surfactant structural characteristics have good safety, that is, the compound of formula I of the present invention and its pharmaceutically acceptable salt can be used to prepare safe, long-term local anesthesia and selective local Drugs with anesthesia effect have the advantages of long local anesthesia effect time, good local anesthesia selectivity and high safety.

Disclosed are a propofol hydroxy acid ester compound with an ester constitutional terminal, a preparation method for the same and application thereof. As shown in the constitutional formula (I) of the compound, Y refers to a C1-4 linear carbon chain, and R refers to acetyl or propiono. The propofol hydroxy acid ester compound can be prepared by utilizing corresponding propofol hydroxy acid ester as raw materials and is obtained by means of esterification reaction with corresponding acid anhydride. As experiments show, the compound is stable in vitro but capable of quickly releasing propofol with sedation and hypnogenesis and / or narcotism in blood plasma. Since hydroxy in propofol hydroxy butyric ester molecules is protected by means of shielding, heat stability of the propofol hydroxy acid ester compound is improved, and self-decomposition of the propofol hydroxy acid ester compound caused by lactonization is reduced.

The invention discloses a pure traditional Chinese medicine narcotic drug formula, and relates to the field of narcotic drugs; according to the pure traditional Chinese medicine narcotic drug formula, radix angelicae, ligusticum wallichii, raw radix aconite and galangal are used as raw materials; fresh ginger and honeysuckle are cooperatively used with the raw radix aconite, and mangnolia officinalis, angelica sinensis and cortex cassiae are cooperatively used with galangal, so the narcotic effect of the narcotic drug is effectively improved, the aching feeling of a user is alleviated, and the side effects are small.

The present invention describes a new propofol-containing anesthetic pharmaceutical composition for parenteral administration, in the form of an oil-in-water microemulsion in which the oily phase is constituted by propofol in the form of particles with size comprised between 1 and 100 nm using a single surfactant selected from the group consisting of polyethylene glycol stearates with general formula C17H35COO. (OCH2CH2)nH or C17H35COO. (OCH2CH2)n.COOC17H35. The anesthetic pharmaceutical composition of the present invention is more potent for induction of hypnosis and anesthesia, has a ready-to-use presentation and highly stable particle size, presenting improved physicochemical properties, and preventing the potential risks of undesirable effects encountered in the state-of-the-art propofol formulations.

Disclosed are an N-substituted imidazole carboxylate compound with the structure of formula (I), a preparation method and the use of the same. In the formula, 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 anaesthetic effects on humans or animals, and can produce rapid and reversible anaesthetic 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, the incidence of muscle tremors is low after administration, and after the drug withdrawal, waking-up is rapid.