13 results about "Benzodiazine" patented technology

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 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

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.

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.

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.

Compounds comprising pyrrolobenzodiazepine (PBD) conjugates and methods for using such conjugates are provided. In some embodiments, the conjugate is of formula (I), or a pharmaceutically acceptable salt, tautomer, solvate, or stereoisomer thereof, where each of rings A and B is independently one of the following formulas, namely formulas (IIa), (IIb), (IIc), (IId), (IIe), (IIf), and (IIg), and the remaining variable elements (e.g., linker, ring C, R) 1 , R 2 , R 3 , R 4 , R 5 The values ​​of m, n, and o are as described herein. TIFF2026514000000140.tif154165