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US 11,298,358 B2Granted
Combination therapy using ascochlorin derivative
AssigneeTatsuo Hoshino
InventorsTatsuo Hoshino, Shinji Kagaya, Nobuo Shimma, Tsutomu Kawaguchi
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Abstract
An object of the present invention is to provide a measure for treating or preventing a disease or condition that involves AMPK dysregulation, particularly a cancer. The present invention provides a combination therapy using a compound presented by formula (I), a pharmaceutically acceptable salt or a solvate thereof with an immune checkpoint inhibitor.
Claims13
A method for treating or preventing a cancer, comprising administrating to a subject in need thereof a therapeutically effective amount of a compound represented by formula (I):
- wherein
- R1 is formyl, or —CH═N—O—Y, in which Y is a hydrogen atom or C1-6 alkyl;
- R2 is C1-6 alkyl that may be substituted with 1 to 5 fluorine atoms;
- R3 is a hydrogen atom or C1-6 alkyl;
- R4 is hydroxy, C1-6 alkylamino, C3-7 cycloalkylamino, or 3- to 7-membered heterocycloalkylamino which contains —O—, —S—, —NR6—, —SO— or —SO2— as a ring atom, or
- R3 and R4 together with the carbon atom to which they are attached form >C═N—O—Z;
- Z is a hydrogen atom, C1-6 alkyl, —CO(CH2)n—R5 or —(CH2)n—R5;
- n is an integer selected from 1 to 4;
- R5 is —CO2R6, —CONH2, —CONR7R8, —OCONR7R8, —SO2NR7R8, —SO2R9, hydroxy, —NHSO2R9, or —NR7R8;
- R6, R7 and R8 are each independently selected from a group consisting of a hydrogen atom, C1-6 alkyl, and C3-7 cycloalkyl;
- or R7 and R8 together with the nitrogen atom to which they are attached form a nitrogen-containing 3- to 7-membered heterocyclic ring which may further contain —O—, —S—, —NR6—, —SO— or —SO2— as a ring atom, in which the heterocyclic ring may be substituted with one or more substituents selected from hydroxy and C1-6 alkyl;
- R9 is C1-6 alkyl, or C3-7 cycloalkyl;
- a pharmaceutically acceptable salt or a solvate thereof,
- in combination with administration of an immune checkpoint inhibitor.
11 more elements
Dependencies are inferred from the claim text.