C07D271/10

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

1,2,4-Oxadiazole and Thiadiazole Compounds as Immunomodulators

The present invention relates to 1,2,4-oxadiazole and thiadiazole compounds of formula (1) and their use to inhibit the programmed cell death 1 (PD1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.

1,2,4-Oxadiazole and Thiadiazole Compounds as Immunomodulators

The present invention relates to 1,2,4-oxadiazole and thiadiazole compounds of formula (1) and their use to inhibit the programmed cell death 1 (PD1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.

METABOLICALLY STABLE N-ACYLAMINOOXADIAZOLES USEFUL AS ANTIBACTERIAL AGENTS

The present invention is related to the development of therapeutics and prophylactics for the treatment and/or prevention of bacterial infections in humans and other mammals. A new class of small molecules is disclosed that inhibits the bacterial trans-translation/ribosome rescue mechanism and thus blocks infection of host cells by bacteria. Also disclosed are methods of using the small molecule inhibitors in the treatment/prevention of bacterial infections.

BENZOSULFONYL COMPOUNDS
20200354325 · 2020-11-12 ·

Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

BENZOSULFONYL COMPOUNDS
20200354325 · 2020-11-12 ·

Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

Aryl sulfonohydrazides

Compound of formula I: ##STR00001##
wherein: A is selected from: (i) ##STR00002##
where R.sup.F1 is H or F; (ii) ##STR00003## (iii) a N-containing C.sub.6 heteroaryl group; and B is ##STR00004##
where X.sup.1 is either CR.sup.F2 or N, where R.sup.F2 is H or F; X.sup.2 is either CR.sup.3 or N, where R.sup.3 is selected from H, Me, Cl, F OMe; X.sup.3 is either CH or N; X.sup.4 is either CR.sup.F3 or N, where R.sup.F3 is H or F; where only one or two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 may be N; and R.sup.4 is selected from I, optionally substituted phenyl, optionally substituted C.sub.5-6 heteroaryl; optionally substituted C.sub.1-6 alkyl and optionally substituted C.sub.1-6 alkoxy, which are useful in the treatment of a condition ameliorated by the inhibition of MOZ.

Aryl sulfonohydrazides

Compound of formula I: ##STR00001##
wherein: A is selected from: (i) ##STR00002##
where R.sup.F1 is H or F; (ii) ##STR00003## (iii) a N-containing C.sub.6 heteroaryl group; and B is ##STR00004##
where X.sup.1 is either CR.sup.F2 or N, where R.sup.F2 is H or F; X.sup.2 is either CR.sup.3 or N, where R.sup.3 is selected from H, Me, Cl, F OMe; X.sup.3 is either CH or N; X.sup.4 is either CR.sup.F3 or N, where R.sup.F3 is H or F; where only one or two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 may be N; and R.sup.4 is selected from I, optionally substituted phenyl, optionally substituted C.sub.5-6 heteroaryl; optionally substituted C.sub.1-6 alkyl and optionally substituted C.sub.1-6 alkoxy, which are useful in the treatment of a condition ameliorated by the inhibition of MOZ.

LSD1 INHIBITOR AND PREPARATION METHOD AND APPLICATION THEREOF

A cyclopropylamine compound as a lysine-specific demethylase 1 (LSD1) inhibitor. Particularly, the present invention relates to a compound represented by formula (I) and a pharmaceutically acceptable salt thereof. The present invention also provides an application of the same in preparing a drug for treating an LSD1-related disease.

##STR00001##

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.