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AssigneeOncoethix GmbH
InventorHervé Dombret
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A method of treating acute myeloid leukemia or acute lymphoid leukemia in a mammal comprising the step of: administering a pharmaceutically acceptable amount of a thienotriazolodiazepine compound represented by the following Formula (1): wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; —NR5—(CH2)m—R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom; or —NR7—CO—(CH2)n—R8 wherein R7 is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R8 is phenyl or pyridyl optionally substituted by a halogen atom, and R4 is —(CH2)a—CO—NH—R9 wherein a is an integer of 1-4, and R9 is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or —(CH2)b—COOR10 wherein b is an integer of 1-4, and R10 is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof
1-32. (canceled)
A method of treating acute myeloid leukemia or acute lymphoid leukemia in a mammal comprising administering a pharmaceutically acceptable amount of a compound which is (S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,-4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide dihydrate, or (S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2, 4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide, or a pharmaceutically acceptable salt thereof wherein expression of HEXIM1 is upregulated after administration of the compound wherein the compound is formed as a solid dispersion comprising an amorphous compound and a pharmaceutically acceptable polymer which is hydroxypropylemethylcellulose acetate succinate (HPMCAS) having a compound to HPMCAS weight ratio of 1:3 to 1:1.
The method according to claim 32, wherein the acute myelogenous leukemia is a MLL-rearranged acute myelogenous leukemia.
The method according to claim 32, wherein the acute myelogenous leukemia is a NPM1-mutated acute myelogenous leukemia.
The method according to claim 32, wherein the acute myelogenous leukemia is BCR-ABL associated acute myeloic leukemia.
The method according to claim 32, wherein the acute lymphatic leukemia is BCR-ABL associated acute lymphatic leukemia.
The method according to claim 32, wherein the acute myelogenous leukemia harbors a PML-RARα fusion gene.
The method according to claim 32, wherein the acute myelogenous leukemia is a NRAS mutated acute myelogenous leukemia.
The method according to claim 32, wherein the acute myelogenous leukemia harbors a OP2-FGFR1 fusion gene.
Dependencies are inferred from the claim text.