31 results about "Benzodiazine" 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.

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.

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.

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.

The present invention provides a novel pyrrolobenzodiazepine derivative compound with significantly reduced side effects such as toxicity, and a conjugate thereof with its ligand. It also provides a pharmaceutical composition for the prevention or treatment of proliferative disorders, containing the compound or its ligand conjugate as an active ingredient. Furthermore, the present invention provides a method for preventing or treating proliferative disorders by administering the compound or its ligand conjugate to an individual. [Solution] Specifically, for example, the following compound is shown. JPEG2026086866000188.jpg35136

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

Provided are compounds comprising pyrrolobenzodiazepine (PBD) conjugates and methods of using such conjugates. In some embodiments, a conjugate is of Formula (I):or a pharmaceutically acceptable salt, tautomer, solvate, or stereoisomer thereof, wherein each of ring A and ring B is, independently, one of the following formulas:and values for the remaining variables (e.g., Linker, ring C, R1, R2, R3, R4, R5, m, n, o) are as described herein.

The present invention relates to Orally Inhaled and Nasal Drug Product (OINDP) comprising a benzodiazepine, in particular remimazolam.

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 discloses a method for detecting dimethyl methylphosphonate at room temperature by using a surface modified transition metal disulfide nano material, and belongs to the technical field of biochemical safety monitoring. According to the technical scheme, the method comprises the following steps: 1) raw material pretreatment: adding 4-(hexafluoro-2-hydroxy isopropyl) aniline and water into a reaction bottle, and carrying out ultrasonic treatment; 2) acidification reaction: dropwise adding fluoboric acid into the system; 3) performing low-temperature diazotization: dropwise adding sodium nitrite into the reaction bottle; (4) crystallizing and purifying to obtain white powdery 4-hexafluoroisopropanol benzodiazepine tetrafluoroborate; 5) preparation of an activation solution: dissolving 4-hexafluoroisopropanol benzodiazepine tetrafluoroborate and potassium iodide in water; and 6) surface modification: immersing the two-dimensional transition metal dichalcogenide in the activation solution to obtain the surface-modified transition metal dichalcogenide nano material. According to the method, the specific adsorption capacity on dimethyl methylphosphonate is remarkably enhanced, and the detection limit reaches ppb level.

The present invention relates to a pyrrolobenzodiazepine dimer prodrug and a ligand-linker conjugate compound thereof, a composition containing these, and therapeutic use thereof particularly as an anticancer drug. The stability of the compounds themselves and the stability thereof in plasma are excellent and the compounds are advantageous in terms of manifestation of toxicity, and thus the compounds are industrially useful in that it is possible to target proliferative diseases such as cancer, to perform a specific treatment, to maximize the drug efficacy, and to minimize the occurrence of side effects.

Provided herein are benzodiazepine analogs that are modified at the 7-position on the benzodiazepine ring to include a moiety selected from C2-C4 alkynyl, C3-C6 cycloalkyl, d(5)-cyclopropyl, methyl alkynyl, alkynyl-CD3, and alkynyl-CF3. Also provided are methods of use of the compounds in treating cancer, sensitizing a tumor to radiation, sensitizing a tumor to immunotherapy or chemotherapy, and treating neurological conditions associated with Type-A GABA neurotransmitter receptor function. Pharmaceutical compositions including the compounds are also provided.

To provide a novel antibody-drug conjugate having strong antitumor activity.SOLUTION: The present invention provides a novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, and a novel CLDN6 and / or CLDN9 antibody.SELECTED DRAWING: Figure 1

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.

Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; R3 is H, C1-C6 alkyl or —NHR8; either (i), a, c and c are all bonds, with, b, d and f absent; or b, d, and f are all bonds, with a, c, and c absent; R4 is H or a group selected from C1-C6 alkyl, C3-C6 cycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; R5 is H or halo; R6 is —OR8, —NR8R9 or —R8; R7 is H or halo; each of R8 and R9 is independently H or a group selected from C1-C6 alkyl, C3-C6 cycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; n is 1 or 2; and one of V, W and X is N or CH and the other two are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

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 benzodiazepine pyrazolo carboxamides and pharmaceutically acceptable salts thereof as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of invention inhibit the activity RSV N-proteins and may be useful in the treatment, prevention, suppression, and amelioration of viral infections such as RSV.

The invention relates to benzodiazepine pyrazolo carboxamidesand pharmaceutically acceptable salts thereof as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of invention inhibit the activity RSV N-proteins and may be useful in the treatment, prevention, suppression, and amelioration of viral infections such as RSV.

The invention is applicable to the technical field of medicine, and provides application of spinosin in preparation of medicine for promoting non-rapid eye movement sleep, spinosin shortens the sleep latency period of mice, increases NREM sleep duration and reduces wakefulness; different from benzodiazepine drugs, spinosin does not change the EEG power spectrum density and does not affect the exercise performance in a rotating bar test, which indicates that spinosin is suitable for treating insomnia. The invention solves the problems of adverse reaction and reduction of sleep quality of the existing hypnotics, and is suitable for treating insomnia, especially insomnia accompanied with anxiety and neurological disorders.

The present invention concerns antibody-conjugates which are especially suitable for the targeting of PTK7-expressing cells, in particular tumour cells. The antibody-conjugates according to the invention have structure (1):Herein, AB is an antibody capable of targeting PTK7-expressing tumours; L is a linker that links Z to D; Z is a connecting group; L6 is -GlcNAc(Fuc)w-(G)j-S-(L7)w′-, wherein G is a monosaccharide, j is an integer in the range of 0-10, 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 anthracyclines, camptothecins, tubulysins, enediynes, amanitins, duocarmycins, maytansinoids, auristatins, eribulins, BCL-XL inhibitors, hemiasterlins, KSP inhibitors, TLR agonists, indolinobenzodiazepine dimers or pyrrolobenzodiazepine dimers (PBDs), and analogues or prodrugs thereof; b is 0 or 1; x is 1 or 2; and y is 1, 2, 3 or 4. The invention further concerns a method for preparing the antibody-conjugates of structure (1) and application of the antibody-conjugates of structure (1).

The application belongs to the field of environmental sample detection, and discloses a method for simultaneously detecting 20 kinds of benzene amphetamine, piperazine and benzodiazepine psychoactive substances in water bodies. The method simultaneously extracts and detects 20 kinds of benzene amphetamine, piperazine and benzodiazepine psychoactive substances in water bodies by using dispersion liquid liquid microextraction and high performance liquid chromatography mass spectrometry. The average recovery rate of the 20 target compounds is 71.5% to 108%, the standard deviation is 0.7% to 4.8%, the detection limit is 1.5 to 10.5 ng / L, and the quantitative limit is 6.0 to 42.2 ng / L. The method has high recovery rate, high sensitivity and good repeatability, and can be used for detecting benzene amphetamine, piperazine and benzodiazepine psychoactive substances in water bodies.

A benzodiazepine compound represented by formula I, or a salt thereof has an intravenous sedative anesthesia effect. The recovery quality of the compound is significantly improved compared with remimazolam in rat and mouse caudal venous anesthesia models. During anesthetization, the compound has a rapid onset, a short duration, a quick recovery and a good tolerance, can be used for anesthesia induction, anesthesia maintenance and day surgery anesthesia.

The present disclosure relates in some aspects to methods for modulating and improving the subjective experience of N,N-dimethyltryptamine (DMT) by administering DMT after a long-acting tryptamine such as psilacetin, and in some embodiments, together with a benzodiazepine and / or ketamine, or in some further embodiments, together with a second long-acting psychedelic. In some aspects, disclosed methods are useful for treating medical conditions, such as mental health disorders and neurodegenerative disorders. In some aspects, disclosed methods are useful for improving health and wellbeing, such as in healthy people.