Patent classifications
C07D215/42
Compounds for use as an anti-bacterial or anti-fungal agent and as a zinc sensor
The present invention relates to a compound, which can be used as an anti-bacterial and/or an anti-fungal agent as well as a zinc sensor. Moreover, the present invention relates to a pharmaceutical composition comprising said compound and methods for treating bacterial or fungal infections in mammals.
Compounds for use as an anti-bacterial or anti-fungal agent and as a zinc sensor
The present invention relates to a compound, which can be used as an anti-bacterial and/or an anti-fungal agent as well as a zinc sensor. Moreover, the present invention relates to a pharmaceutical composition comprising said compound and methods for treating bacterial or fungal infections in mammals.
Heterocyclic acyl hydrazone linkers, methods and uses thereof
The present application is directed to compounds of Formula (I): compounds of Formula (II): compounds of Formula (III): and compounds of Formula (IV): compositions comprising these compounds and their uses, for example as medicaments and/or diagnostics. Specifically claimed are: (1) compounds containing reactive functional groups (compound of formula I), compounds containing compounds to be linked together (compound of formula II) and compounds having a reactive functional group/a compound to be linked (compound of formula IV), (2) an antibody-drug conjugate (compound of formula III), wherein the antibody is covalently attached by a linker to one or more drugs, (3) pharmaceutical compositions comprising compounds of Formula (II) or Formula (III), (4) treatment/diagnosis of disease comprising compounds of Formula (II) or Formula (III), and (5) methods of preparing an ADC of Formula III. ##STR00001##
Heterocyclic acyl hydrazone linkers, methods and uses thereof
The present application is directed to compounds of Formula (I): compounds of Formula (II): compounds of Formula (III): and compounds of Formula (IV): compositions comprising these compounds and their uses, for example as medicaments and/or diagnostics. Specifically claimed are: (1) compounds containing reactive functional groups (compound of formula I), compounds containing compounds to be linked together (compound of formula II) and compounds having a reactive functional group/a compound to be linked (compound of formula IV), (2) an antibody-drug conjugate (compound of formula III), wherein the antibody is covalently attached by a linker to one or more drugs, (3) pharmaceutical compositions comprising compounds of Formula (II) or Formula (III), (4) treatment/diagnosis of disease comprising compounds of Formula (II) or Formula (III), and (5) methods of preparing an ADC of Formula III. ##STR00001##
2-QUINOLONE DERIVED INHIBITORS OF BCL6
The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: Formula I wherein X.sub.1, X.sub.2, X.sub.3, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.
##STR00001##
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##
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##
MECHANISM OF RESISTANCE TO BET BROMODOMAIN INHIBITORS
The present disclosure provides combination therapy comprising a BET inhibitor and a protein phosphatase 2A (PP2A) activator, a B-cell lymphoma-2 (Bcl-2) inhibitor, a B-cell lymphoma-extra large (Bcl-xl) inhibitor, a casein kinase 2 (CK2) inhibitor, and/or a mediator complex subunit 1 (MED1) for cancer. The combination therapy is expected to be synergistic in treating the cancer, compared to the monotherapy. Methods for identifying a subject having a cancer that is resistant to or at risk of developing resistance to bromodomain and extra terminal (BET) inhibitor therapy are also provided.
COMPOUNDS, COMPOSITIONS, METHODS FOR TREATING DISEASES, AND METHODS FOR PREPARING COMPOUNDS
Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)). Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer). Further embodiments include methods for making the inventive compounds. Additional embodiments of the invention are also discussed herein.
COMPOUNDS, COMPOSITIONS, METHODS FOR TREATING DISEASES, AND METHODS FOR PREPARING COMPOUNDS
Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)). Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer). Further embodiments include methods for making the inventive compounds. Additional embodiments of the invention are also discussed herein.