C07D209/38

Aurora kinase inhibitors

The invention provides compounds of the formula: ##STR00001##
and salts thereof that are useful as intermediates for preparing corresponding compounds of formula I: ##STR00002##
that are useful for treating conditions associated with Aurora B kinase activity (e.g. cancer).

INDOLINE ANALOGS AND USES THEREOF
20170283420 · 2017-10-05 ·

Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

INDOLINE ANALOGS AND USES THEREOF
20170283420 · 2017-10-05 ·

Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

Targeting of EWS-FLI1 as anti-tumor therapy

Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.

Targeting of EWS-FLI1 as anti-tumor therapy

Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.

Histone acetyltransferase activators and uses thereof

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

Histone acetyltransferase activators and uses thereof

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

METHODS AND COMPOSITIONS RELATING TO INHIBITION OF ALDEHYDE DEHYDROGENASES FOR TREATMENT OF CANCER

Disclosed are compositions and methods for inhibiting aldehyde dehydrogenases. In further aspects, treatment of cancers by inhibiting aldehyde dehydrogenases with the disclosed compositions are also disclosed.

PRODUCTION METHOD OF QUINOLINECARBOXAMIDE DERIVATIVE OR PRODUCTION INTERMEDIATE THEREOF

Provided is a method for industrially advantageously synthesizing a production intermediate of a quinolinecarboxamide derivative or a salt thereof. The present invention provides a method for producing a quinolinecarboxylic acid derivative of formula (4) or a salt thereof, including reacting an aniline of the following formula (1), in the presence of boron trifluoride-tetrahydrofuran complex or boron trifluoride-diethyl ether complex, with an aldehyde of formula (2) and subsequently reacting the resulting compound with an α-keto acid of formula (3), wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represent a hydrogen atom, a halogen atom, a lower alkyl group, or the like, R.sup.5 represents a hydrogen atom, a lower alkyl group, or the like, and R.sup.6 represents a hydrogen atom, a lower alkyl group, or the like.

##STR00001##

PRODUCTION METHOD OF QUINOLINECARBOXAMIDE DERIVATIVE OR PRODUCTION INTERMEDIATE THEREOF

Provided is a method for industrially advantageously synthesizing a production intermediate of a quinolinecarboxamide derivative or a salt thereof. The present invention provides a method for producing a quinolinecarboxylic acid derivative of formula (4) or a salt thereof, including reacting an aniline of the following formula (1), in the presence of boron trifluoride-tetrahydrofuran complex or boron trifluoride-diethyl ether complex, with an aldehyde of formula (2) and subsequently reacting the resulting compound with an α-keto acid of formula (3), wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represent a hydrogen atom, a halogen atom, a lower alkyl group, or the like, R.sup.5 represents a hydrogen atom, a lower alkyl group, or the like, and R.sup.6 represents a hydrogen atom, a lower alkyl group, or the like.

##STR00001##