C07C2602/38

N-(3-(2-(4-CHLOROPHENOXY)ACETAMIDO)BICYCLO[1.1.1] PENTAN-1-YL)-2-CYCLOBUTANE-1- CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ATF4 INHIBITORS FOR TREATING CANCER AND OTHER DISEASES
20210145771 · 2021-05-20 ·

The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula I:

##STR00001##

wherein X, a, b, C, D, L.sup.2, L.sup.3, Y.sup.1, Y.sup.2, R.sup.2, R.sup.4, R.sup.5, R.sup.6, z.sup.2, z.sup.4, z.sup.5, and z.sup.6 are as defined herein, and salts thereof.

The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

COMPOUNDS, COMPOSITIONS AND METHODS

The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers or prodrug thereof, and methods of making and using thereof.

SSAO INHIBITORS AND USE THEREOF
20210147360 · 2021-05-20 ·

The application relates to a compound of Formula (I′) or (I):

##STR00001##

or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease in which SSAO plays a role.

Bicyclic compounds

Disclosed herein are compounds of Formulae (I) and (II), methods of synthesizing compounds of Formulae (I) and (II), and methods of using compounds of Formulae (I) and (II) as an analgesic.

MODULATORS OF EUKARYOTIC INITIATION FACTOR 2

The present disclosure relates generally to eukaryotic initiation factor 2B modulators of formula A, or a pharmaceutically acceptable salt, stereoisomer, or mixture of stereoisomers thereof and methods of making and using thereof.

##STR00001##

Chemical Compounds as ATF-4 Pathway Inhibitors

The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula IIIQ:

##STR00001##

wherein X.sup.6′, a, b, C.sup.8′, D.sup.8′, L.sup.82′, L.sup.83′, R.sup.81′, R.sup.82′, R.sup.83′, R.sup.84′, R.sup.85′, R.sup.86′, z.sup.82′, z.sup.84′, z.sup.85′, and z.sup.86′ are as defined herein; or salts thereof.

The compounds of the invention are inhibitors of the ATF4 pathway. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

CONTINUOUS FLOW PROCESSES FOR MAKING BICYCLIC COMPOUNDS

Processes for making bicyclic compounds and precursors thereof, and particularly for making [1.1.1]propellane and bicyclo[1.1.1]pentane and derivatives thereof, utilize continuous flow reaction methods and conditions. A continuous process for making [1.1.1]propellane can be conducted under reaction conditions that advantageously minimize clogging of a continuous flow reactor. A continuous flow process can be used to make precursors of [1.1.1]propellane.

TRNA SYNTHETASE INHIBITORS
20210053997 · 2021-02-25 ·

Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.

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.

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.