71 results about "Benzodiazepine" patented technology

The disclosure provides methods for treating a patient in need thereof comprising co-administering to the patient a therapeutically-effective dose of psilocybin and one or more benzodiazepines. The present disclosure also provides methods to reduce the SSRI washout period in patients prior to administration of psilocybin therapy.

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

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 present invention relates to antibody conjugates which are particularly suitable for targeting cells expressing PTK7, in particular tumor cells. An antibody conjugate according to the present invention has structure (1): AB-[(L6) b-{Z-L-D} x] y (1) wherein AB is an antibody capable of targeting a tumor expressing PTK7; l is a joint connecting Z to D; z is a linking group; l6 is-GlcNAc (Fuc) w-(G) j-S-(L7) w '-wherein G is a monosaccharide, j is an integer in the range of 0 to 10, S is a sugar or a sugar derivative, GlcNAc is N-acetylglucosamine, and Fuc is fucose, w is 0 or 1, w' is 0, 1 or 2, and L7 is-N (H) C (O) CH2-,-N (H) C (O) CF2-or-CH2-; d is selected from the group consisting of an anthracycline, a camptothecin, a tubulysin, an endiyne, an amanitine, a duocarmycin, a maytansinoid, an aurestatin, eribulin, a BCL-XL inhibitor, a miscanthus semiaquilaria, a KSP inhibitor, a TLR agonist, an indolo-benzodiazepine dimer or a pyrrolo-benzodiazepine dimer (PBD), and an analog or prodrug thereof; b is 0 or 1; x is 1 or 2; and y is 1, 2, 3 or 4. The invention further relates to a method for preparing said antibody conjugate of structure (1) and to the use of said antibody conjugate of structure (1).

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 invention discloses a deuterated compound of benzodiazepine and application thereof, the deuterated compound of benzodiazepine has the following general formula: in the formula, R1 and R2 are independently selected from ethyl or deuterated ethyl, R3 to R18 are independently selected from H group or deuterated group, and R1 to R18 at least contain one deuterated group. The deuterated compound of benzodiazepine or the pharmaceutically acceptable salt, hydrate or solvent compound thereof provided by the invention has a muscarinic M2 receptor antagonism effect, and compared with a known selective M2 receptor inhibitor, the compound provided by the invention has better inhibitory activity and pharmacodynamic performance, has little influence on the activity of an M3 receptor, and can be used for preparing a novel compound of benzodiazepine or a pharmaceutically acceptable salt, hydrate or solvent compound of benzodiazepine. The side effect of pupil dilation (mydriasis) is avoided, and the composition has a good development prospect in clinical application of treating myopia, preventing myopia and / or inhibiting myopia development.

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

The present disclosure provides compounds, pharmaceutical compositions, and methods useful for treating parasitic worms. The compound is a benzodiazepine type structure substituted at C3 according to Formula I, Formula II, Formula III, Formula IV, or Formula V. In various aspects, the presently described treatment can advantageously provide anthelmintic effects with reduced sedative qualities.

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).

Disclosed are a deuterated compound of benzodiazepine, and a use thereof. The deuterated compound of benzodiazepine has the following general formula (I), R1 and R2 being independently selected from ethyl or deuterated ethyl, R3-R18 being independently selected from hydrogen or deuterium, and R1-R18 containing at least one deuterium. The deuterated compound of benzodiazepine provided by the present invention, or a pharmaceutically acceptable salt, hydrate or solvate thereof, has antagonistic activity against muscarinic M2 receptors. Compared with known selective M2 receptor inhibitors, the compound of the present invention has better inhibitory activity and pharmacodynamic properties, and has minimal activity on M3 receptors, thereby avoiding the side effect of pupil dilation (mydriasis). It has promising prospects for clinical applications in treating myopia, preventing myopia, and / or inhibiting the progression of myopia.

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 invention provides benzodiazepine derivatives, radioactive probes and their applications, belonging to the field of biomedicine technology. The present invention modifies the benzodiazepine derivatives and introduces hydrophilic or lipophilic side chains. The prepared benzodiazepine derivatives can be used as precursors targeting V2R, which can achieve specific targeting of V2R and provide new molecular tools for the subsequent diagnosis and treatment of V2R-positive tumors. 68 The Ga-labeled radioactive probe of the present invention exhibits good tumor imaging effects and can achieve PET imaging of V2R-positive tumors, which helps to improve the accuracy of tumor diagnosis. It can also be used to evaluate treatment effects, has a high "target / non-target" ratio, and can better display the distribution of V2R receptors throughout the body. It has many applications in the diagnosis and treatment of cancer.

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.