C07D207/48

NEW SELECTIVE MODULATORS OF INSECT NICOTINIC ACETYLCHOLINE RECEPTORS

The present invention relates to a compound having the following formula (I): wherein:—A is a (hetero)aryl radical comprising from 5 to 10 carbon atoms, possibly substituted by at least one substituent chosen from the group consisting of: halogen atoms, amino, azido, cyano, nitro, hydroxyl, formyl, carboxyl, amido, (C.sub.1-C.sub.6)alkyl groups, halo(C.sub.1-C.sub.6)alkyl groups, (C.sub.1-C.sub.6)alkoxy groups, alkenyl groups, cycloalkenyl groups, and alkynyl groups, and—R is H, CN or CF.sub.3, or their pharmaceutically acceptable salts, racemates, diastereomers or enantiomers.

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INHIBITORS OF INTEGRIN ALPHA 2 BETA 1 AND METHODS OF USE
20210387986 · 2021-12-16 ·

Disclosed herein, inter alia, are inhibitors of integrin alpha 2 beta 1 and methods of using the same.

INHIBITORS OF INTEGRIN ALPHA 2 BETA 1 AND METHODS OF USE
20210387986 · 2021-12-16 ·

Disclosed herein, inter alia, are inhibitors of integrin alpha 2 beta 1 and methods of using the same.

STABILIZATION OF AMYLOIDOGENIC IMMUNOGLOBULIN LIGHT CHAINS

In immunoglobulin light chain amyloidosis (AL), the unique antibody light chain (LC) protein that is secreted by monoclonal plasma cells in each patient misfolds and/or aggregates, a process leading to organ degeneration. For treating AL patients, such as those with substantial cardiac involvement who have difficulty tolerating existing chemotherapy regimens, provided herein are small molecule compounds of Formula Ia, Formula Ib, and Formula II that are kinetic stabilizers of the native dimeric structure of full-length LCs, which compounds can slow or stop the amyloidogenicity cascade at its origin.

STABILIZATION OF AMYLOIDOGENIC IMMUNOGLOBULIN LIGHT CHAINS

In immunoglobulin light chain amyloidosis (AL), the unique antibody light chain (LC) protein that is secreted by monoclonal plasma cells in each patient misfolds and/or aggregates, a process leading to organ degeneration. For treating AL patients, such as those with substantial cardiac involvement who have difficulty tolerating existing chemotherapy regimens, provided herein are small molecule compounds of Formula Ia, Formula Ib, and Formula II that are kinetic stabilizers of the native dimeric structure of full-length LCs, which compounds can slow or stop the amyloidogenicity cascade at its origin.

NOVEL SULFONAMIDEUREA COMPOUNDS

The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R.sup.1 and R.sup.3 are each independently hydrogen or an optionally substituted hydrocarbyl group, or R.sup.1 and R.sup.3 together with the nitrogen atom to which they are attached may form a 3- to 12-membered optionally substituted cyclic group; and R.sup.2 is a cyclic group substituted at the position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

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NOVEL SULFONAMIDEUREA COMPOUNDS

The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R.sup.1 and R.sup.3 are each independently hydrogen or an optionally substituted hydrocarbyl group, or R.sup.1 and R.sup.3 together with the nitrogen atom to which they are attached may form a 3- to 12-membered optionally substituted cyclic group; and R.sup.2 is a cyclic group substituted at the position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

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HBV INHIBITOR AND ITS USE
20220184035 · 2022-06-16 ·

The present invention provides anti-HBV compounds, pharmaceutically acceptable compounds or stereoisomers thereof, and preparation methods and uses for treating, eradicating or inhibiting HBV infection or for alleviating liver injury caused by HBV infection, and so on.

SMALL MOLECULES FOR CANCER THERAPY THAT REDUCE THE EXPRESSION OF TRANSCRIPTION FACTORS KLF5 AND EGR-1

The present disclosure provides compounds of formula (I), as described herein, their pharmaceutically acceptable salts, and their pharmaceutical compositions, which are effective in reducing the expression level of KLF5 or EGR1 in a living cell, and for the treatment of tumors and colorectal cancer in a human patient.

SMALL MOLECULES FOR CANCER THERAPY THAT REDUCE THE EXPRESSION OF TRANSCRIPTION FACTORS KLF5 AND EGR-1

The present disclosure provides compounds of formula (I), as described herein, their pharmaceutically acceptable salts, and their pharmaceutical compositions, which are effective in reducing the expression level of KLF5 or EGR1 in a living cell, and for the treatment of tumors and colorectal cancer in a human patient.