C07D215/28

PREPARATION METHOD FOR AROMATIC ETHER COMPOUND
20230219928 · 2023-07-13 ·

A preparation method for an aromatic ether compound. The preparation method comprises the following step: c) in a solvent, in the presence of a catalyst and alkali, a compound V reacts with a compound 6 to obtain a compound VII,

##STR00001## wherein the solvent is a solvent system having two or more elements selected from water, tetrahydrofuran, 2-methyltetrahydrofuran, ethyl acetate, and dioxane. According to the preparation method for the aromatic ether compound in the present invention, the conversion rate of the reaction can be greatly improved, and thus the yield of the step and the total yield of the whole reaction route are improved; post-treatment and purification operations for preparing the compound VII are greatly simplified, and the compound VII having high purity can be obtained only be simply filtering a reaction solution and washing and drying a filter cake. The preparation method is suitable for industrial scale-up production.

PREPARATION METHOD FOR AROMATIC ETHER COMPOUND
20230219928 · 2023-07-13 ·

A preparation method for an aromatic ether compound. The preparation method comprises the following step: c) in a solvent, in the presence of a catalyst and alkali, a compound V reacts with a compound 6 to obtain a compound VII,

##STR00001## wherein the solvent is a solvent system having two or more elements selected from water, tetrahydrofuran, 2-methyltetrahydrofuran, ethyl acetate, and dioxane. According to the preparation method for the aromatic ether compound in the present invention, the conversion rate of the reaction can be greatly improved, and thus the yield of the step and the total yield of the whole reaction route are improved; post-treatment and purification operations for preparing the compound VII are greatly simplified, and the compound VII having high purity can be obtained only be simply filtering a reaction solution and washing and drying a filter cake. The preparation method is suitable for industrial scale-up production.

SMALL-MOLECULE INHIBITORS OF THE FRS2-FGFR INTERACTION AND THEIR USE IN MEDICINE, IN THE PREVENTION AND TREATMENT OF CANCER

The present invention relates to small-molecule inhibitors of the FRS2-FGFR interaction. The present invention relates the small-molecule inhibitors for use as a medicament and for use in cancer or metastasis treatment or prevention.

Substituted N-Benzhydrylacetamide Inhibitors of Jamanji Domain Histone Demethylases for the Treatment of Cancer
20230108479 · 2023-04-06 ·

Provided herein are compounds for inhibiting Wnt signaling and methods of treating cancer. The compounds include any compound having a structure according to Formula II. The method includes administering one or more compounds according to Formula I and/or Formula II to a subject in need thereof.

Formulations of Methionine Aminopeptidase Inhibitors for Treating Infectious Diseases
20170304288 · 2017-10-26 · ·

Provided herein are formulations and co-solvent formulations and methods for treating an infectious disease utilizing the same. The formulations and co-solvent formulations may comprise a hydroxyquinoline analog or its pharmaceutically acceptable salt, a solvent and at least two surfactants. Also provided are methods of quantitating a hydroxyquinoline analog in a sample via chromatographic/spectrometric measurements.

Luminescent polydentate polycyclic compounds for metal ions

Polydentate polycyclic compounds of various formulas are disclosed herein. The compounds are useful for ratiometric luminescence. Significantly, the compounds will luminesce at different wavelengths/colors, depending on the analyte (metal ion, acid, or boron-containing compound) it is combined with. Thus, a single compound can provide different luminescent outputs based on the analyte, rather than requiring an entire set of structurally different compounds to detect each analyte or to generate a desired color output.

Luminescent polydentate polycyclic compounds for metal ions

Polydentate polycyclic compounds of various formulas are disclosed herein. The compounds are useful for ratiometric luminescence. Significantly, the compounds will luminesce at different wavelengths/colors, depending on the analyte (metal ion, acid, or boron-containing compound) it is combined with. Thus, a single compound can provide different luminescent outputs based on the analyte, rather than requiring an entire set of structurally different compounds to detect each analyte or to generate a desired color output.

NOVEL THYROMIMETICS WITH A BIPHENYLMETHANE SCAFFOLD AND THEIR USE

The invention concerns a compound of Formula (I) or a salt thereof, wherein R.sub.1 is H, (C.sub.1-C.sub.3)alkyl or CF.sub.3; R.sub.2 is H, (C.sub.1-C.sub.3)alkyl or CF.sub.3; A is CH.sub.2COOH, XCH.sub.2COOCH.sub.2CH.sub.3, XCH.sub.2COOH, XCH.sub.2CH.sub.2NH.sub.2, where X is nitrogen or oxygen atom; Ar is an aromatic fragment selected from the group consisting of (Ar1), (Ar2) and (Ar3); where R.sub.3 is H, —CH.sub.3, —CH.sub.2CH.sub.3 or CH.sub.3CO—, R.sub.4 is H or —CH.sub.3, R5 is H or —CH.sub.3, and R.sub.6 is H or —CH.sub.3. The compounds of Formula (I) can be used in the treatment of diseases modulated by thyroid hormone receptor-beta (TRb or TRβ).

NOVEL THYROMIMETICS WITH A BIPHENYLMETHANE SCAFFOLD AND THEIR USE

The invention concerns a compound of Formula (I) or a salt thereof, wherein R.sub.1 is H, (C.sub.1-C.sub.3)alkyl or CF.sub.3; R.sub.2 is H, (C.sub.1-C.sub.3)alkyl or CF.sub.3; A is CH.sub.2COOH, XCH.sub.2COOCH.sub.2CH.sub.3, XCH.sub.2COOH, XCH.sub.2CH.sub.2NH.sub.2, where X is nitrogen or oxygen atom; Ar is an aromatic fragment selected from the group consisting of (Ar1), (Ar2) and (Ar3); where R.sub.3 is H, —CH.sub.3, —CH.sub.2CH.sub.3 or CH.sub.3CO—, R.sub.4 is H or —CH.sub.3, R5 is H or —CH.sub.3, and R.sub.6 is H or —CH.sub.3. The compounds of Formula (I) can be used in the treatment of diseases modulated by thyroid hormone receptor-beta (TRb or TRβ).

NITROXOLINE PRODRUG AND USE THEREOF
20210363165 · 2021-11-25 ·

Provided are a nitroxoline prodrug and a use thereof. Specifically, provided are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, a composition containing the compound, and a use thereof in the preparation of anti-infective and antitumor drugs, and definitions of groups in formula (I) are as stated in the specification. The compound represented by formula (I) has better pharmacokinetic parameters such as solubility, blood medicine concentration, or half-life period than nitroxoline. The compound represented by formula (I) can reduce the frequency of drug administration, and has potential for application in other fields other than the field of urinary tracts.

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