C07D221/22

8-CARBOXAMIDO-2,6-METHANO-3-BENZAZOCINES
20170217977 · 2017-08-03 · ·

8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH.sub.2—OH, —CH.sub.2NH.sub.2, —NHSO.sub.2CH.sub.3,

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and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

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8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.

Spiroacridine-Triazine Hybrids and Applications for Electroluminescent Devices

The present invention relates to compounds of the formula (1), to the use thereof in electroluminescent devices, and particularly organic electroluminescence devices, comprising said compounds according to the invention.

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Spiroacridine-Triazine Hybrids and Applications for Electroluminescent Devices

The present invention relates to compounds of the formula (1), to the use thereof in electroluminescent devices, and particularly organic electroluminescence devices, comprising said compounds according to the invention.

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TARGETED NITROXIDE AGENTS

Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

TARGETED NITROXIDE AGENTS

Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

Compounds, compositions and methods for prevention and/or treatment of cancer

The present invention includes compounds, compositions and methods that are useful for preventing or treating melanoma or any other cancer in a subject, such as a GPCR-expressing cancer. In certain embodiments, the compounds comprise estrogen (including estrogen derivatives or analogues), a selective GPER agonist and/or another G-protein coupled receptor (GPCR) agonist that increases cancer cell differentiation.

BULLEYACONITINE D CRYSTAL AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
20220185781 · 2022-06-16 ·

Disclosed in the present invention are a bulleyaconitine D crystal and a preparation method therefor. FIG. 1 shows an X-ray powder diffraction spectrum of the crystal according to the present invention, the spectrum being measured with Cu—K alpha ray. The bulleyaconitine D crystal is prepared by an anti-solvent process with isopropanol, anisole, 1,4-dioxane or methylbenzene acting as a positive solvent and n-heptane as a negative solvent. The preparation process is simple, and the prepared crystal has a high purity. Upon characterization via XRD, DSC, TGA and .sup.1HNMR, the crystal is determined as D crystal type. Stability test shows that the prepared bulleyaconitine crystal is well stable to light, damp and heat.

BULLEYACONITINE D CRYSTAL AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
20220185781 · 2022-06-16 ·

Disclosed in the present invention are a bulleyaconitine D crystal and a preparation method therefor. FIG. 1 shows an X-ray powder diffraction spectrum of the crystal according to the present invention, the spectrum being measured with Cu—K alpha ray. The bulleyaconitine D crystal is prepared by an anti-solvent process with isopropanol, anisole, 1,4-dioxane or methylbenzene acting as a positive solvent and n-heptane as a negative solvent. The preparation process is simple, and the prepared crystal has a high purity. Upon characterization via XRD, DSC, TGA and .sup.1HNMR, the crystal is determined as D crystal type. Stability test shows that the prepared bulleyaconitine crystal is well stable to light, damp and heat.

CRYSTAL FORM E OF BULLEYACONITINE A, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
20220153704 · 2022-05-19 ·

Provided is a crystal form E of bulleyaconitine A and a preparation method for the crystal form E of bulleyaconitine A. An X-ray powder diffraction spectrum of the crystal form measured by Cu-Kα-ray is as shown in FIG. 1. The crystal form E of bulleyaconitine A is prepared by adding a mixed solution of alcohol and water to bulleyaconitine A, stirring to obtain a suspended solid, and centrifugally collecting the solid. The alcohol is methanol, ethanol or n-butanol. The preparation process is simple, and the obtained crystal form has high purity and is characterized by XRD, DSC, TGA, and .sup.1HNMR to be determined as the crystal form E. The obtained bulleyaconitine A crystal is an anhydrous crystal form, and stability test results show that the crystal has good light, humidity and heat stability.

CRYSTAL FORM E OF BULLEYACONITINE A, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
20220153704 · 2022-05-19 ·

Provided is a crystal form E of bulleyaconitine A and a preparation method for the crystal form E of bulleyaconitine A. An X-ray powder diffraction spectrum of the crystal form measured by Cu-Kα-ray is as shown in FIG. 1. The crystal form E of bulleyaconitine A is prepared by adding a mixed solution of alcohol and water to bulleyaconitine A, stirring to obtain a suspended solid, and centrifugally collecting the solid. The alcohol is methanol, ethanol or n-butanol. The preparation process is simple, and the obtained crystal form has high purity and is characterized by XRD, DSC, TGA, and .sup.1HNMR to be determined as the crystal form E. The obtained bulleyaconitine A crystal is an anhydrous crystal form, and stability test results show that the crystal has good light, humidity and heat stability.