Patent classifications
C07D215/233
QUINAZOLINE AND QUINOLINE COMPOUNDS AND USES THEREOF
This invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein T, J, R, R.sup.4, R.sup.q, o, R.sup.A, W and R.sup.B and subsets thereof are as described in the specification. The compounds are inhibitors of NAMPT and are thus useful for treating cancer, inflammatory conditions, and/or T-cell mediated autoimmune disease.
##STR00001##
METHODS OF USING 4(1H)-QUINOLONE DERIVATIVES
Provided herein are compounds of Formula (I). The disclosure provides new compounds, compositions, and methods for treating, delaying, and/or preventing the adverse effects of proliferative diseases, such as cancers including, for example, lung cancer, breast cancer, ovarian cancer, prostate cancer, head cancer, neck cancer, head and neck cancer, or leukemia (e.g., cancer resistant to treatment by one or more microtubule-targeting agents (e.g., cancer resistant to multiple drugs associated with P-glycoprotein (P-gp) overexpression)). Provided are methods of inhibiting polymerization of a cancer cell microtubule in a subject in need thereof or a cell, tissue, or biological sample, binding β-tubulin, inhibiting microtubule assembly and, inducing apoptosis in a cancer cell resistant to multiple drugs in a tissue, biological sample, or subject. Also provided in the present disclosure are pharmaceutical compositions, kits, and methods of using the compounds for treating any of the target diseases described herein.
##STR00001##
METHODS OF USING 4(1H)-QUINOLONE DERIVATIVES
Provided herein are compounds of Formula (I). The disclosure provides new compounds, compositions, and methods for treating, delaying, and/or preventing the adverse effects of proliferative diseases, such as cancers including, for example, lung cancer, breast cancer, ovarian cancer, prostate cancer, head cancer, neck cancer, head and neck cancer, or leukemia (e.g., cancer resistant to treatment by one or more microtubule-targeting agents (e.g., cancer resistant to multiple drugs associated with P-glycoprotein (P-gp) overexpression)). Provided are methods of inhibiting polymerization of a cancer cell microtubule in a subject in need thereof or a cell, tissue, or biological sample, binding β-tubulin, inhibiting microtubule assembly and, inducing apoptosis in a cancer cell resistant to multiple drugs in a tissue, biological sample, or subject. Also provided in the present disclosure are pharmaceutical compositions, kits, and methods of using the compounds for treating any of the target diseases described herein.
##STR00001##
PHARMACEUTOCAL COMPOSITION CONTAINING N-(4-(6,7-DIMETHOXYQUINOLIN-4-YLOXY)PHENYL)-N?-(4-FLUOROPHENLY)CYCLOPROPANE-1,1-DICARBOXAMIDE, (2S)-HYDROXYBUTANEDIOATE
The present invention relates to a pharmaceutical composition comprising N-(4-(6,7-dimethoxy quinolin-4-yloxy)phenyl)-N′-(4-fluoro phenyl) cyclopropane-1,1-dicarboxamide, (2S)-hydroxy butanedioate of formula-1
##STR00001##
and a pharmaceutically acceptable carrier wherein the said pharmaceutical composition has a dimer impurity of formula-2 less than about 2.0% as measured by HPLC.
PHARMACEUTOCAL COMPOSITION CONTAINING N-(4-(6,7-DIMETHOXYQUINOLIN-4-YLOXY)PHENYL)-N?-(4-FLUOROPHENLY)CYCLOPROPANE-1,1-DICARBOXAMIDE, (2S)-HYDROXYBUTANEDIOATE
The present invention relates to a pharmaceutical composition comprising N-(4-(6,7-dimethoxy quinolin-4-yloxy)phenyl)-N′-(4-fluoro phenyl) cyclopropane-1,1-dicarboxamide, (2S)-hydroxy butanedioate of formula-1
##STR00001##
and a pharmaceutically acceptable carrier wherein the said pharmaceutical composition has a dimer impurity of formula-2 less than about 2.0% as measured by HPLC.
IMINO SULFANONE INHIBITORS OF ENPP1
The present disclosure relates generally to inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions thereof, and methods of using said compounds and compositions thereof. More specifically, the present disclosure relates to sulfoximine-based inhibitors of ENPP1 and methods of their use for treating disease mediated by ENPP1.
IMINO SULFANONE INHIBITORS OF ENPP1
The present disclosure relates generally to inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions thereof, and methods of using said compounds and compositions thereof. More specifically, the present disclosure relates to sulfoximine-based inhibitors of ENPP1 and methods of their use for treating disease mediated by ENPP1.
Bicyclic compounds as kinase modulators, methods and uses thereof
The present disclosure relates to derivatives of bicyclic compounds and their uses in therapy. In particular, the present disclosure relates to derivatives of bicyclic compounds for use in modulating kinase enzymatic activity and accordingly modulating kinase-dependent diseases and conditions such as cancer and in specific embodiments, hepatocellular carcinoma (HCC). The present disclosure also relates to methods of synthesizing these compounds.
Bicyclic compounds as kinase modulators, methods and uses thereof
The present disclosure relates to derivatives of bicyclic compounds and their uses in therapy. In particular, the present disclosure relates to derivatives of bicyclic compounds for use in modulating kinase enzymatic activity and accordingly modulating kinase-dependent diseases and conditions such as cancer and in specific embodiments, hepatocellular carcinoma (HCC). The present disclosure also relates to methods of synthesizing these compounds.
SMALL-MOLECULE INHIBITORS OF THE FRS2-FGFR INTERACTION
The present invention relates to small-molecule inhibitors of the FRS2-FGFR interaction. The present invention relates the small-molecule inhibitors for use as a medicament and for use in cancer treatment or prevention.