C07D277/82

WDR5-MYC INHIBITORS

Substituted N-heteroaryl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject such as cancer cell proliferation.

Antibacterial compounds

The present invention relates to certain compounds of formula (I) wherein—Ar is (Ar1) or (Ar2) and to their uses as antibacterial agents. The invention further relates to methods of treatment of bacterial infection with such compounds, optionally in combination with other antimicrobials and to compositions and pharmaceutical formulations containing such compounds. The invention additionally relates to coatings containing such compounds and to items having such coatings. ##STR00001##

AGENT FOR REDUCING VISCERAL FAT WEIGHT
20230019803 · 2023-01-19 · ·

An FGF21 production promoting agent containing, as an active ingredient, a compound represented by the following formula (1):

##STR00001##

wherein each of R.sup.1 and R.sup.2, which may be identical to or different from each other, represents, for example, a hydrogen atom; each of R.sup.3a, R.sup.3b, R.sup.4a, and R.sup.4b, which may be identical to or different from one another, represents, for example, a hydrogen atom or a halogen atom, or R.sup.3a and R.sup.3b or R.sup.4a and R.sup.4b may bond together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R.sup.5 (R.sup.5 represents, for example, a hydrogen atom or a C.sub.1-4 alkyl group); Y represents, for example, an oxygen atom, an S(O).sub.l group (l is a number of from 0 to 2), or a carbonyl group; Z represents CH or N; n is a number of from 1 to 6; and m is a number from 2 to 6, a salt of the compound, or a solvate of the compound or the salt.

AGENT FOR REDUCING VISCERAL FAT WEIGHT
20230019803 · 2023-01-19 · ·

An FGF21 production promoting agent containing, as an active ingredient, a compound represented by the following formula (1):

##STR00001##

wherein each of R.sup.1 and R.sup.2, which may be identical to or different from each other, represents, for example, a hydrogen atom; each of R.sup.3a, R.sup.3b, R.sup.4a, and R.sup.4b, which may be identical to or different from one another, represents, for example, a hydrogen atom or a halogen atom, or R.sup.3a and R.sup.3b or R.sup.4a and R.sup.4b may bond together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R.sup.5 (R.sup.5 represents, for example, a hydrogen atom or a C.sub.1-4 alkyl group); Y represents, for example, an oxygen atom, an S(O).sub.l group (l is a number of from 0 to 2), or a carbonyl group; Z represents CH or N; n is a number of from 1 to 6; and m is a number from 2 to 6, a salt of the compound, or a solvate of the compound or the salt.

RILUZOLE PRODRUGS AND THEIR USE

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

RILUZOLE PRODRUGS AND THEIR USE

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

BENZOTHIAZOLE DERIVATIVES AND USES THEREOF

A compound represented by general formula (I) or stereoisomers thereof and pharmaceutically acceptable salts, solvates or prodrugs thereof, a preparation method therefor and a pharmaceutical composition containing the compound. An application of the compound of general formula (I) in preparation of drugs for treating and/or preventing she-mediated diseases, especially an application in preparation of drugs for treating inflammatory diseases, cardiovascular and cerebrovascular diseases, diabetes, diabetes complications, diabetes-related diseases, fibrotic diseases, neurological and mental diseases, pain, and ulcer diseases, etc.

##STR00001##

BENZOTHIAZOLE DERIVATIVES AND USES THEREOF

A compound represented by general formula (I) or stereoisomers thereof and pharmaceutically acceptable salts, solvates or prodrugs thereof, a preparation method therefor and a pharmaceutical composition containing the compound. An application of the compound of general formula (I) in preparation of drugs for treating and/or preventing she-mediated diseases, especially an application in preparation of drugs for treating inflammatory diseases, cardiovascular and cerebrovascular diseases, diabetes, diabetes complications, diabetes-related diseases, fibrotic diseases, neurological and mental diseases, pain, and ulcer diseases, etc.

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