Patent classifications
C07D401/14
Ink set
An ink set includes a first ink containing the compound represented by formula (y-1) or its salt, a second ink containing one or two or more of the compound represented by formula (m-1) or its salt, the compound represented by formula (m-2) or its salt, a compound represented by formula (m-3) or its salt, and the compound represented by formula (m-4) or its salt, and a third ink containing one or two or more of a compound represented by formula (c-1) or its salt, the compound represented by formula (c-2) or its salt, the compound represented by formula (c-3) or its salt, a compound represented by formula (c-4) or its salt, and the compound represented by formula (c-5) or its salt. ##STR00001##
Ink set
An ink set includes a first ink containing the compound represented by formula (y-1) or its salt, a second ink containing one or two or more of the compound represented by formula (m-1) or its salt, the compound represented by formula (m-2) or its salt, a compound represented by formula (m-3) or its salt, and the compound represented by formula (m-4) or its salt, and a third ink containing one or two or more of a compound represented by formula (c-1) or its salt, the compound represented by formula (c-2) or its salt, the compound represented by formula (c-3) or its salt, a compound represented by formula (c-4) or its salt, and the compound represented by formula (c-5) or its salt. ##STR00001##
KDM1A inhibitors for the treatment of disease
The present disclosure relates to compounds and methods which may be useful as inhibitors of KDM1A for the treatment or prevention of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation in cancer cells in a human or animal subject are also provided for treatment of disease such as acute myelogenous leukemia.
KDM1A inhibitors for the treatment of disease
The present disclosure relates to compounds and methods which may be useful as inhibitors of KDM1A for the treatment or prevention of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation in cancer cells in a human or animal subject are also provided for treatment of disease such as acute myelogenous leukemia.
Inhibitors of LRRK2 kinase
Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I): ##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R.sup.1a, R.sup.1b, R.sup.2, and L 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 LRRK2 kinase are also provided.
Inhibitors of LRRK2 kinase
Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I): ##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R.sup.1a, R.sup.1b, R.sup.2, and L 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 LRRK2 kinase are also provided.
Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use
The present application provides bifunctional compounds of Formula (X): ##STR00001##
or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for protein kinases. The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.
Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use
The present application provides bifunctional compounds of Formula (X): ##STR00001##
or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for protein kinases. The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.
Nitrogenous heterocyclic compound, preparation method, intermediate, composition, and application
A nitrogenous heterocyclic compound, a preparation method, an intermediate, a composition, and an application. The present invention provides a nitrogenous heterocyclic compound as represented by formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, diastereoisomers thereof, tautomers thereof, solvates thereof, metabolites thereof, or prodrugs thereof. The compound has high inhibitory activity against ErbB2 tyrosine kinase, has good inhibitory activity against human breast cancer cells BT-474, human gastric cancer cells NCI-N87 and the like with high expression of ErbB2, and in addition has relatively weak inhibitory activity against EGFR kinase, that is, the compound is an EGFR/ErbB2 double target inhibitor that attenuates EGFR kinase inhibitory activity or a small-molecule inhibitor having selectivity for an ErbB2 target. ##STR00001##
Solid forms comprising (S)-2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione and salts thereof, and compositions comprising and methods of using the same
Provided herein are formulations, processes, solid forms and methods of use relating to salts of and solid forms comprising free base or salts of (S)-2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione.