Novel selective pi3k delta inhibitors
AssigneeRhizen Pharmaceuticals SA
InventorsSwaroop K. Vakkalanka, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
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Abstract
The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.
Claims30
-20. (canceled)
(S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]-pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one 4-methylbenzenesulfonate having an enantiomeric excess of at least 95%.
A method for the treatment of leukemia comprising administering to a subject in need thereof an effective amount of (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo└3,4-d┘pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one 4-methylbenzenesulfonate having an enantiomeric excess of at least 95%.
A method of treating chronic lymphocytic leukemia (CLL) in a human subject in need thereof comprising administering to the human subject an effective amount of (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo [3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one 4-methylbenzenesulfonate having an enantiomeric excess of at least 95%.
A method of treating diffuse large B-cell lymphoma (DLBCL) in a human subject in need thereof comprising administering to the human subject an effective amount of (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo [3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one 4-methylbenzenesulfonate having an enantiomeric excess of at least 95%.
A method of treating non-Hodgkin lymphoma (NHL) in a human subject in need thereof comprising administering to the human subject an effective amount of ((S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo [3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one 4-methylbenzenesulfonate having an enantiomeric excess of at least 95%.
A method for the treatment of lymphoid lineage, B-cell lymphoma, T-cell lymphoma, Hodgkin's lymphoma, hairy cell lymphoma or Burkett's lymphoma in a subject in need thereof, the method comprising administering to the subject an effective amount of (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one 4-methylbenzenesulfonate having an enantiomeric excess of at least 95%.
A method for the treatment of lymphoid lineage, B-cell lymphoma, T-cell lymphoma, Hodgkin's lymphoma, hairy cell lymphoma and Burkett's lymphoma, hematopoietic tumors of myeloid lineage, multiple myelomas, smoldering multiple myeloma, nonsecretory myeloma, osteosclerotic myeloma, plasma cell leukemia, solitary plasmacytoma, or extramedullary plasmacytoma in a subject in need thereof, the method comprising administering to the subject an effective amount of (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo [3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one 4-methylbenzenesulfonate having an enantiomeric excess of at least 95%.
A method for the treatment of Multiple Myeloma (MM), Small Lymphocytic Lymphoma (SLL), Indolent Non-Hodgkin's Lymphoma (I-NHL), mantle cell lymphoma (MCL), follicular lymphoma, Waldestrom's macroglobulinemia (WM), T-cell lymphoma or B-cell lymphoma in a subject in need thereof, the method comprising administering to the subject an effective amount of (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl) -1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one 4-methylbenzenesulfonate having an enantiomeric excess of at least 95%.
Dependencies are inferred from the claim text.