C07D417/14

SULFONYLUREA RING SUBSTITUTED MONOCYCLIC beta-LACTAM ANTIBIOTICS
20230037556 · 2023-02-09 ·

Sulfonylurea ring substituted monocyclic β-lactam antibiotics, and specifically relating to a compound represented by formula (I), a pharmaceutically acceptable salt or a stereoisomer thereof, and an application thereof in the preparation of medicaments for treating diseases related to bacterial infections.

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MODULATORS OF INTEGRATED STRESS RESPONSE PATHWAY

The present disclosure relates generally to therapeutic agents that may be useful as modulators of Integrated Stress Response (ISR) pathway.

AHR inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.

AHR inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.

HETEROCYCLIC TRPML1 AGONISTS

Disclosed is a compound of formula (I)

##STR00001## or a stereoisomer thereof, or a salt of any of the foregoing and to processes for its preparation. The compounds of formula (I) are useful in the treatment TRPML1-mediated disorders or diseases.

HETEROCYCLIC TRPML1 AGONISTS

Disclosed is a compound of formula (I)

##STR00001## or a stereoisomer thereof, or a salt of any of the foregoing and to processes for its preparation. The compounds of formula (I) are useful in the treatment TRPML1-mediated disorders or diseases.

A CONJUGATION LINKER CONTAINING 2,3-DIAMINOSUCCINYL GROUP

The present invention relates to a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (a dual-linker) containing a 2,3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.

A CONJUGATION LINKER CONTAINING 2,3-DIAMINOSUCCINYL GROUP

The present invention relates to a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (a dual-linker) containing a 2,3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.

COMPOUND COMPRISING EZH2 INHIBITOR AND E3 LIGASE BINDER AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING EZH2-ASSOCIATED DISEASE COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a compound comprising an EZH2 inhibitor and an E3 ligase binder, and a pharmaceutical composition for preventing or treating EZH2-associated disease and a pharmaceutical composition for selective protein degradation containing the same as an active ingredient. Since the compound of the present invention can selectively degrade EZH2, it can be effectively used for the treatment of EZH2-related diseases and cancers, particularly, cancers in which EZH2 is overexpressed, and can be usefully used for the selective degradation of EZH2.

WDR5 INHIBITORS AND MODULATORS

Isoquinolinone compounds and derivatives inhibit WDRS and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.