C07C317/34

Small molecule compounds having naphthylamine structure and application thereof

The present application discloses small molecule compounds having a naphthylamine structure and an application thereof. In the present application, the structure of a compound having a structure as shown in general formula (I) is as shown in the drawing. The compound and the pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof that are provided by the present application or the pharmaceutical composition provided by the present application can selectively induce autophagy in damaged mitochondria without affecting or only weakly affecting normal mitochondria, and further have superior metabolic stability and pharmacokinetic properties, lower toxicity, and better druggability. ##STR00001##

PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
20240366595 · 2024-11-07 ·

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof,

##STR00001##

wherein: the group XY is NHSO.sub.2 or SO.sub.2NH; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, Cl and alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl.

Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (Ia) and (Ib).

Aryl ethers and uses thereof

The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

Aryl ethers and uses thereof

The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

Aryl ethers and uses thereof

The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

Benzamide compounds and related methods of use

Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.

Benzamide compounds and related methods of use

Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.

Process for the synthesis of Dapsone and its intermediates

A process for the synthesis of Dapsone and intermediates thereof are described.

Process for the synthesis of Dapsone and its intermediates

A process for the synthesis of Dapsone and intermediates thereof are described.

ARYL ETHERS AND USES THEREOF

The present disclosure relates to HIF-2 inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2 scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.