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US 12,734,164 B2Granted
Piperidine urea derivatives for cancer therapy
AssigneeNeuroPn Therapeutics, Inc.
InventorsIsh Khanna, Sivaram Pillarisetti, Hans Marcus Malkmus, Kathrin Christin Kortschak
Life of this patent
Estimating the term…
Abstract
Described herein are novel piperidine urea derived compounds and their pharmaceutical compositions for the treatment of cancer as a monotherapy or a combination therapy with chemotherapeutic agents and/or checkpoint inhibitors.
Claims24
A method of treating a cancer wherein the cancer includes one of brain cancer, breast cancer and melanoma, comprising:
- administering to a subject a therapeutic amount of at least one compound of Formula I:
- where
- R1 is selected from a group consisting of alkyl, hydrogen, haloalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl and wherein when R1 is aryl, heteroaryl or heterocycloalkyl, R1 is unsubstituted or substituted with alkyl, hydroxy, halogen, haloalkyl, hydroxyalkyl, alkoxyalkyl, alkoxy, amine, SO2NHR2, or COR3;
- R2 is selected from a group consisting of hydrogen, alkyl, haloalkyl, or cycloalkyl;
- R3 is selected from a group consisting of alkyl, cycloalkyl, hydroxy, amine, alkylamine or alkoxy;
- R4 is selected from a group consisting of hydrogen, alkyl, halogen, haloalkyl, hydroxy, amine, alkoxy, SO2R5, or COR3;
- R5 is selected from a group consisting of alkyl, haloalkyl, cycloalkyl, aryl or amine;
- R6 is selected from a group consisting of alkyl, cycloalkyl, aryl or heteroaryl;
- X is selected from O, (CH2)p, NH and p is from 0-2;
- Y1-Y2 are selected from CH—CH2, CH—O, or C═CH, however when Y1-Y2 is CH—O, X is selected from O or NH or R1 is not hydrogen;
- and
- Y3 is selected from H or Me,
- its stereoisomers or pharmaceutically acceptable salts thereof.
10 more elements
A method of treating a cancer comprising administrating to a subject a therapeutic amount of at least one compound of Formula I:
- wherein
- R1 is selected from a group consisting of alkyl, hydrogen, haloalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl and wherein when R1 is aryl, heteroaryl or heterocycloalkyl, R1 is unsubstituted or substituted with alkyl, hydroxy, halogen, haloalkyl, hydroxyalkyl, alkoxyalkyl, alkoxy, amine, SO2NHR2, or COR3;
- R2 is selected from a group consisting of hydrogen, alkyl, haloalkyl, or cycloalkyl;
- R3 is selected from a group consisting of alkyl, cycloalkyl, hydroxy, amine, alkylamine or alkoxy;
- R4 is selected from a group consisting of hydrogen, alkyl, halogen, haloalkyl, hydroxy, amine, alkoxy, SO2R5, or COR3;
- R5 is selected from a group consisting of alkyl, haloalkyl, cycloalkyl, aryl or amine;
- R6 is selected from a group consisting of alkyl, cycloalkyl, aryl or heteroaryl;
- X is selected from O, (CH2)p, NH and p is from 0-2, however when p=0, Y1-Y2 is not CH—CH2 or CH—O, and R1 is not aryl;
- Y1-Y2 are selected from CH—CH2, CH—O, or C═CH, however when Y1-Y2 is CH—O, X is selected from O or NH, and R1 is not hydrogen or alkyl;
- and
- Y3 is selected from H or Me,
- its stereoisomers or pharmaceutically acceptable salts thereof.
9 more elements
Dependencies are inferred from the claim text.