C07D219/10

COMPOUNDS FOR INHIBITING LY6K AND METHODS OF USING SAME
20210009522 · 2021-01-14 ·

The present technology relates to compounds that inhibit human Ly6K and homologs thereof. Also disclosed are methods of using such compounds to: inhibit activity of a Ly6K protein in a cell; decrease migration, colony formation, and/or proliferation of a cell; modulate expression of a gene in a cell, reduce suppression of the immune response to cancer in a subject, decrease tumorigenic growth of a cancer in a subject, and treat or prevent in a subject a disorder mediated by Ly6K protein.

DIAZINYL AMINO ACRIDINES AND MEDICAL USES THEREOF

There is provided herein compounds of formula (I) and pharmaceutically-acceptable salts and/or detectably-labelled derivatives thereof, wherein R.sup.1 to R.sup.3, X, Y, n and m have meanings as provided in the description, together with formulations and products comprising the same. There is also provided the use of such compounds, formulations and products in the treatment of cancers characterised by increased MYC activity.

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Diazinyl amino acridines and medical uses thereof

There is provided herein compounds of formula (I) and pharmaceutically-acceptable salts and/or detectably-labelled derivatives thereof, wherein R.sup.1 to R.sup.3, X, Y, n and m have meanings as provided in the description, together with formulations and products comprising the same. There is also provided the use of such compounds, formulations and products in the treatment of cancers characterised by increased MYC activity. ##STR00001##

Compounds as modulators of a mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction

An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. The invention provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation F508-CFTR, or another mutation of class II.

Compounds as modulators of a mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction

An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. The invention provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation F508-CFTR, or another mutation of class II.

Fused-tricyclic inhibitors of KRAS and methods of use thereof

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):(I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A is a heterocyclic or heteroaryl ring, and R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, A, G.sup.1, G.sup.2, L.sup.1, L.sup.2, m.sup.1, m.sup.2, and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided. ##STR00001##

Fused-tricyclic inhibitors of KRAS and methods of use thereof

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):(I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A is a heterocyclic or heteroaryl ring, and R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, A, G.sup.1, G.sup.2, L.sup.1, L.sup.2, m.sup.1, m.sup.2, and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided. ##STR00001##

Compounds as modulators of a mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction

An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. The invention provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation F508-CFTR, or another mutation of class II.

Compounds as modulators of a mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction

An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. The invention provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation F508-CFTR, or another mutation of class II.

Compounds as modulators of a mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction

An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. An exemplary embodiment provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation F508-CFTR, or another mutation of class II.