51 results about "Benzodiazepine" patented technology

Disclosed in the present invention are a benzodiazepine compound, a pharmaceutical composition and the use thereof. Specifically provided is a compound represented by formula I, or a stereoisomer thereof, a deuterated compound thereof, or a pharmaceutically acceptable salt thereof. The compound provided in the present invention has one or more of the following advantageous effects: (1) the compound of the present invention exhibits good intravenous sedative and anesthetic effects; (2) the compound of the present invention exhibits low drug accumulation and a good tolerance; and (3) the compound of the present invention achieves an anesthetic effect with faster recovery.

The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.

Methods and compositions are provided for treating individuals exhibiting opioid withdrawal symptoms with opioid, benzodiazepine and other drugs of abuse by administering an opioid receptor antagonist agent together with a respiratory stimulant to reverse the effects of opioid withdrawal symptoms, including respiratory depression, sedation, and hypotension. Methods and compositions are also provided for treating stimulant overdose with a benzodiazepine and beta-adrenergic blocking agent. Methods and compositions are also provided for treating concurrent stimulant and opioid overdose comprising administering to a patient in need thereof a benzodiazepine and an opioid antagonist. Methods and compositions are also provided for treating individuals exhibiting opioid withdrawal symptoms or prophy tactically treating individuals for opioid withdrawal symptoms from opioid, benzodiazepine and other drugs of abuse by administering an opioid receptor antagonist agent together with a respiratory stimulant to reverse the effects of withdrawal, including respiratory depression, sedation, and hypotension.

The invention system is a wearable device that detects an impending or onset of cardio-respiratory arrest and remediates the condition by injecting an appropriate reversal drug depending upon the drug that triggered the arrest. It can detect and remediate arrests caused by drugs such as opioids, benzodiazepine or alcohol. Using self-test and other checks, it ensures that the system is operationally ready and that no near-expiration or expired drug is administered.

The present application relates to the technical field of copper-clad plate preparation, and particularly relates to a halogen-free flame-retardant BT resin-based copper-clad plate and a preparation method thereof. The present application adds 3,4-dihydroxybenzaldehyde, triethylamine, 7-chloro-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepine-2-thione and ethyl acetate to prepare an antibacterial monomer. Then, the Zn-MOF material, the antibacterial monomer and 9,10-dihydro-9-oxa-10-phosphaphenanthrene-10-oxide are used to prepare a flame retardant. Finally, the cyanate ester resin, the bismaleimide resin, the epoxy resin, the flame retardant, the solvent, the filler and the curing agent are added to prepare a resin glue solution. The glass fiber cloth is immersed in the resin glue solution, and then high-temperature curing, copper foil lamination and laminated molding are performed to prepare a finished product. The finished product prepared by the present application has good flame retardance and antibacterial property, and therefore has a wide application prospect in the technical field of copper-clad plate preparation.

Compositions for intranasal delivery of benzodiazepines, such as diazepam, midazolam, and lorazepam and methods for their use to treat and prevent seizures in pediatric subjects aged 2-5, inclusive. Compositions for rapid therapeutic onset with a decreased incidence and / or severity of adverse effects after administration and methods of improving patient compliance with a prescribed treatment regimen.

The invention discloses application of a selfheal compound in preparation of a medicine for adjusting an insomnia sleep structure. The selfheal compound comprises selfheal, rhizoma acori graminei, herba cepbalanoplosis segeti, semen boitae and caulis bambusae in taeniam. The selfheal compound can remarkably improve the sleep structure, and compared with a traditional benzodiazepine medicine (such as diazepam), the selfheal compound not only effectively recovers the physiological proportion of non-rapid eye movement sleep and rapid eye movement sleep, but also can reduce sleep fragmentation and rebuild sleep continuity.

This invention discloses an acylhydrazone-linked covalent organic framework material, its preparation method, and its application, belonging to the field of covalent organic framework material synthesis technology. The preparation method of the acylhydrazone-linked covalent organic framework material is as follows: benzo[1,2-b:3,4-b':5,6-b”]trithiophene-2,5,8-tricarboxaldehyde, benzodiazepine, o-dichlorobenzene, and n-butanol are mixed to obtain suspension A; trifluoroacetic acid is added to suspension A and mixed to obtain mixture A; mixture A is sequentially subjected to freeze degassing and heating treatment, followed by extraction to obtain the final product. This invention uses benzo[1,2-b:3,4-b':5,6-b”]trithiophene-2,5,8-tricarboxaldehyde and benzodiazepine with a specific structure as main raw materials, and by adjusting the concentration, type, and amount of catalyst, an acylhydrazone-linked covalent organic framework material with higher crystallinity and stability is prepared.

This invention belongs to the fields of medicinal chemistry and pharmaceutical technology, and relates to 1,4-benzodiazepines and their use in the preparation of antitumor drugs, specifically the use of 1,4-benzodiazepines in the preparation of annexin A3 (ANXA3) degrading agents and in the preparation of drugs for treating cancer. In particular, it discloses the use of 1,4-benzodiazepines, or pharmaceutically acceptable salts thereof, or stereoisomers thereof, or compositions of drugs with these as active ingredients, in the preparation of drugs for the prevention and treatment of tumors. These compounds can bind to the ANXA3 protein, induce ANXA3 protein degradation, inhibit the proliferation, cloning, migration, and invasion of tumor cells, and exert antitumor therapeutic effects in vivo. They can be used to treat solid tumors and hematological malignancies, including breast cancer, cervical cancer, ovarian cancer, colorectal cancer, gastric cancer, pancreatic cancer, lung cancer, esophageal cancer, liver cancer, leukemia, and melanoma.

A conjugate obtained by binding a benzodiazepine to an antibody or an antigen-binding fragment thereof having immunological reactivity with MCEMP1 protein, the conjugate being an antibody-drug complex (ADC) having a strong anti-tumor effect and being useful for the treatment and / or prevention of cancer, particularly cancer expressing MCEMP1 protein on the cell surface.

The present disclosure relates to a pyrrolo benzodiazepine derivative and a conjugate, preparation method and use thereof. In particular, the present disclosure relates to a compound of formula (DL) and a antibody-drug conjugate thereof, a pharmaceutical composition containing same, and a use thereof in the preparation of a medicament for the treatment of cancer. The definitions of groups in the general formula (DL) are as defined in the description.

The present invention provides a pharmaceutical composition containing a benzodiazepine drug. [Solution] A drug solution for intranasal administration is provided, comprising: (a) a benzodiazepine drug; (b) one or more natural or synthetic tocopherols or tocotrienols, or any combination thereof, in an amount of about 30% to about 95% (w / w); (c) one or more alcohols or glycols, or any combination thereof, in an amount of about 10% to about 70% (w / w); and (d) an alkyl glycoside.

This invention discloses an AI-designed benzodiazepine derivative, a pharmaceutical composition, and its uses. The benzodiazepine derivative has the structure of Formula I: wherein R1 is any one of H, deuterium, halogen, or C1-C3 alkoxy group; A is a nitrogen-containing heterocyclic group; n is 0 or 1; and R2 and R3 are hydrogen, C1-C6 alkyl group, or C4-C6 alkyl group. 20 Any of the polycyclic cycloalkyl groups; or, R2 and R3 can form a C4-C4 group together with the N they are attached to. 20 The polycyclic heterocyclic group structure. The benzodiazepine derivative of this invention, as the active ingredient in drugs for preventing and / or inhibiting myopia progression, can significantly improve selectivity for M2 receptors and significantly reduce inhibitory effects on M3 receptors, with an M3 / M2 IC50 ratio. 50 The ratio increases significantly, enabling effective treatment of myopia without affecting pupil size, and helps improve the targeted nature of treatment and patient comfort.

Benzodiazepine derivatives of formula (Ie) 1 and R 2 is a benzodiazepinyl-containing group of formula (II), and R 8 is H or halo, and R 1 and R 2 The other is H, C3-C6 cycloalkyl, halo, -NHR 9 , benzyl, phenyl, 4-10 membered heterocyclyl and 4-10 membered heteroaryl, where phenyl, heterocyclyl and heteroaryl are unsubstituted or 4-10 membered heterocyclyl (unsubstituted or substituted with OR), as well as C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, halo, -OR, -(CH2) m OR, -NR2, -(CH2) m NR2, -NHR'', -SO m NR2, -SO m R, -SR, nitro, -CO2R, -CN, -CONR2, -NHCOR, -CH2NR 10 R 11 and -NR 10 R 11 each R is independently H or C1-C6 alkyl; R" is C3-C6 cycloalkyl; m is 1 or 2; and R 9 is selected from phenyl and 4- to 10-membered heteroaryl, wherein phenyl and heteroaryl are unsubstituted or substituted with halo; R 10 and R 11 are each independently H or C1-C6 alkyl, or R 10 and R 11together with the N atom to which they are attached form either (a) a morpholine ring optionally bridged by a —CH— group connecting two ring carbon atoms positioned para to each other, or (b) a spiro group of formula (b) below, wherein ring A is one of the rings of the following structural formulas (I-1), (I-2) and (I-3), wherein Y is selected from O, S, SO and NR, R is as defined above, and R 2 ~R 7 each independently represents H, C1-C6 alkyl, C1-C6 hydroxyalkyl, C3-C6 cycloalkyl, halo, -OR, -CH2OR, -NR2, -CH2NR 12 R 13 , -NRCOOR, -CH2OR, -SO m NR2, -SO m R, -CHSO m R, nitro, -COR, -CN, -CONR, or -NHCOR, R and m are as defined above, and R 12 and R 13 are each independently H, C1-C6 alkyl, benzyl, 4- to 10-membered heterocyclyl, or R 12 and R 13 are taken together with the N atom to which they are attached to form an unsubstituted 4-10 membered heteroaryl or a 4-10 membered heterocyclyl (unsubstituted or substituted with C1-C6 alkyl or halo), or R 2 ~R 7 any two of which form a spiro ring selected from a C3-C6 cycloalkyl spiro ring and a spirooxetane ring of the following structure] and pharmaceutically acceptable salts thereof are inhibitors of RSV and therefore can be used to treat or prevent RSV infection. [Case 1] TIFF2023539985000299.tif4467 [C2] TIFF2023539985000300.tif6375 [3] TIFF2023539985000301.tif4630 [C4] TIFF2023539985000302.tif53147 [Chemical 5] TIFF2023539985000303.tif2630

To provide application of RO 5-3335 in anti-aging.SOLUTION: RO 5-3335 is a core binding factor (CBF) leukemia inhibitor, the RO 5-3335 is a benzodiazepine compound, and the RO 5-3335 is applied to anti-aging drugs. The invention applies the core binding factor (CBF) leukemia inhibitor to delaying, preventing and / or treating senescence, provides a new treatment choice for relieving senescence, and has important practical application value in the fields of medicine and anti-senescence.SELECTED DRAWING: None

A conjugate of an antibody or a fragment thereof linked to benzodiazepine, which bas immunological reactivity with a CAPRIN-1 protein having an amino acid sequence represented by any of even-numbered SEQ ID NOs among SEQ ID NOs: 2 to 30 or an amino acid sequence having 80% or more sequence identity to the amino acid sequence, is useful as an antibody-drug conjugate (ADC).

The invention relates to a crystal form of hydrochloride of a benzodiazepine derivative with the following formula I, wherein R is ethyl. The invention also relates to a pharmaceutical composition containing the crystal form, and application and a preparation method thereof. Formula I

The present application belongs to the field of chemiluminescence detection, and particularly relates to a preparation method and application method of an electrochemiluminescence sensor for detecting benzodiazepine 2-chlordiazepoxide. Technical points are as follows: the electrochemiluminescence sensor is obtained by modifying the surface of a glassy carbon electrode with a Cu3(HHTP)2 / PTCA-COF composite material; the Cu3(HHTP)2 / PTCA-COF composite material modification is formed by the adsorption of PTCA-COF on Cu3(HHTP)2. Through the mechanism of the quenching of the ECL signal intensity of the system by 2-chlordiazepoxide, sensitive detection of 2-chlordiazepoxide is realized, the sensing platform can specifically recognize and detect 2-chlordiazepoxide, has high selectivity, and is simple to operate, good in selectivity, low in detection cost, and high in sensitivity.

The invention relates to the technical field of research and development of original drugs, and discloses a sleep-aiding traditional Chinese medicine stir-fried and scorched incense and a preparation method of the sleep-aiding traditional Chinese medicine stir-fried and scorched incense. 15 to 30 parts of brown malt; 5 to 15 parts of fructus momordicae; 3-8 parts of an adhesive; and 40 to 150 parts of purified water. Long-term insomnia obviously affects health, the risk of cardiovascular diseases is easily increased, and many problems such as metabolic disorder, cognitive impairment and immunity decline are caused, benzodiazepine drugs are commonly used for sedation and hypnosis, and tolerance and dependency are easily generated after long-term use of the benzodiazepine drugs. According to the invention, the scorched fragrance emitted by the traditional Chinese medicine fried to be scorched is developed into the sleep-aiding incense, the scorched fragrance of the traditional Chinese medicine fried to be scorched is creatively prepared, collected and applied by adopting a low-temperature drying and incense nourishing method, and meanwhile, the health management APP is matched to strengthen the self sleep management consciousness of a patient through the functions of incense reminding, symptom recording, voice guidance and the like, so that the sleep-aiding effect of the patient is improved. Identification and mechanism research of scorch aroma substances are carried out, and clinical random control tests and animal model experiments are combined.

This invention belongs to the fields of biopharmaceutical and biochemical technologies, specifically a method for the enzyme-catalyzed synthesis of baconin. This invention uses inexpensive and readily available androstened 4-ene-3,17-dione as a substrate, via a 3-sterone-Δ... 1 The synthesis of 3-sterones via a cascade reaction catalyzed by β-dehydrogenase and 17β-hydroxydehydrogenase. This invention relates to 3-sterone-Δ 1 -Dehydrogenase mutants and their encoding genes, obtaining mutants, containing 3-sterone-Δ 1 Recombinant expression vectors and recombinant expression transformants of β-dehydrogenase gene and 17β-hydroxydehydrogenase gene, 3-sterone-Δ 1 The amino acid sequences of β-dehydrogenase and its mutants are shown in SEQ ID NO.1, SEQ ID NO.2, SEQ ID NO.3 and SEQ ID NO.4, and the amino acid sequence of 17β-hydroxydehydrogenase is shown in SEQ ID NO.5. This invention simplifies the synthesis steps of steroidal drugs, significantly improves catalytic selectivity and yield, and features high substrate concentration, mild reaction conditions, low cost, and environmental friendliness.

The invention relates to besylate salts of the compound of formula (I):Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.

The invention relates to a preparation method of a quinazoline [3, 2-a] [1, 4]-benzodiazepine natural product. Aiming at the defects of an existing synthesis strategy and an existing synthesis route, on the basis of a large number of experiments, a carbonylation synthesis strategy and a novel synthesis route are innovatively adopted, the novel preparation method of the novel, simple and reliable quinazoline [3, 2-a] [1, 4]-benzodiazepine compound is developed, and through adjustment of reagents used in related reactions, the yield of the quinazoline [3, 2-a] [1, 4]-benzodiazepine compound is increased, and the yield of the quinazoline [3, 2-a] [1, 4]-benzodiazepine compound is increased. A series of quinazoline [3, 2-a] [1, 4]-benzodiazepine alkaloids can be more conveniently synthesized, so that the structure-function relationship or related biological research of the quinazoline [3, 2-a] [1, 4]-benzodiazepine alkaloids is facilitated.

This invention belongs to the field of medicinal chemistry, specifically relating to a benzodiazepine compound, its preparation method, and its application. The benzodiazepine compound provided by this invention is a compound represented by Formula I or a pharmaceutically acceptable salt thereof. This invention introduces a hydrogen, benzyl, propargyl, or acyl group at the 10-position of benzodiazepine, and simultaneously introduces an aliphatic amine, aromatic amine, aromatic heteroamine, aliphatic hydrazine, or acyl hydrazine group at the 4-position of benzodiazepine. The resulting compound has a novel skeleton, and experiments have confirmed that this type of compound exhibits good inhibitory activity against LSD1. It can provide a novel structural skeleton for the development of highly effective LSD1-targeted inhibitors or antitumor drugs, and also provide a new direction for the development of LSD1-targeted inhibitory drugs, demonstrating its application potential in the field of LSD1-targeted drugs.

The present application relates to the field of medicinal chemistry, in particular to a new heterocyclic system, namely 1,5-benzodiazepine derivatives and preparation method and use thereof.The benzodiazepine derivative has the activity of anti-solid tumor such as colon cancer, pancreatic cancer, cervical cancer, gastric cancer, liver cancer, etc.; the benzodiazepine derivative has good selectivity to colon cancer cells, can inhibit the proliferation and migration of colon cancer cells, and promote the apoptosis of colon cancer cells; pharmacodynamic experiments show that the effect of the benzodiazepine derivative in treating colon cancer is better than that of the clinical drug 5-Fu, and the toxicity to normal intestinal epithelial cells HIEC is smaller; in addition, the benzodiazepine derivative T0 also has good cytotoxicity to pancreatic cancer cells PANC-1, cervical cancer cells Hela, gastric cancer cells AGS and liver cancer cells HepG-2, and can also be used as a potential broad-spectrum anticancer drug, and has good application prospect.

The invention belongs to the field of medicinal chemistry, and relates to a benzodiazepine compound as well as a pharmaceutical composition and application thereof. Specifically, the invention relates to a compound as shown in a formula (I), or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound as shown in the formula (I). The compound and the pharmaceutical composition thereof can inhibit RSV virus replication, achieve the anti-RSV virus effect, have good druggability and pharmacokinetic characteristics, and are very suitable for protection, treatment, treatment or alleviation of diseases caused by RSV infection of patients.