Fluorine-containing compound and anti-cancer medical use thereof
AssigneeAscentawits Pharmaceuticals, Ltd.
InventorsJianxin Duan, Anrong Li, Fanying Meng, Xiaohong Cai
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Abstract
Described is a fluorine-containing compound shown in Formula II/III and its anti-cancer medical use. The present application creatively introduced the fluorine-containing groups such as special trifluoromethyl groups, fluorine-substituted aryl groups, or heteroaryl groups at special positions (such as the position between the nitrobenzene ring and the phosphate amine group) in the structures of the above compounds. After this modification, it was found that all of the resulting compounds were solids (including waxes).
Claims17
A solid compound of formula II or III or a pharmaceutically acceptable salt, or a solvate thereof,
- wherein
- R1 is C6-C10 aryl or Z-substituted aryl, 4-15 membered heterocycle or Z-substituted heterocycle, 5-15 membered heteroaryl or Z-substituted heteroaryl, or a 7-15 membered fused ring or Z-substituted fused ring;
- R2 is hydrogen, a halogen atom, cyano or isocyano, hydroxy, sulfhydryl, amino, OTs, OLCMS, C1-C6 alkyl or Z-substituted alkyl, C2-C6 alkenyl or Z-substituted alkenyl, C2-C6 alkynyl or Z-substituted alkynyl, C3-C8 cycloalkyl or Z-substituted cycloalkyl, C6-C10 to aryl or Z-substituted aryl, 4-15 membered heterocycle or Z-substituted heterocycle, 5-15 membered heteroaryl or Z-substituted heteroaryl, ether having from 1 to 6 carbon atoms or Z-substituted alkoxy having from 1 to 6 carbon atoms, —CONR6R7, —SO2NR6R7, —SO2R6, —OCOO—R6, —COOR6, —NR6COR7, —OCOR6, —NR6SO2R7 or —NR6SO2NR6R7, or R2 together with the atom in the group R1 to which it is bonded to form a 7-15 membered fused ring or Z-substituted fused ring;
- R3 is hydrogen;
- R4 and R5 are each hydrogen;
- R6 and R7 are each independently hydrogen, cyano or isocyano, C1-C6 alkyl or Z-substituted alkyl, C2-C6 alkenyl or Z-substituted alkenyl, C2-C6 alkynyl or Z-substituted alkynyl, C3-C8 cycloalkyl or Z-substituted cycloalkyl, C6-C10 aryl or Z-substituted aryl, 4-15 membered heterocycle or Z-substituted heterocycle, 5-15 membered heteroaryl or Z-substituted heteroaryl, or C1-C6 alkoxy or Z-substituted C1-C6 alkoxy, or R6 and R7 together with the atom to which they are bonded to form 5-7 membered heterocyclyl or Z-substituted 5-7 membered heterocyclyl;
- R8 and R10 are each hydrogen;
- R9 is substituted C6-C10 aryl which is substituted with at least one fluorine atom or nitro group, substituted 4-15 membered heterocycle which is substituted with at least one fluorine atom or nitro group, or substituted 5-15 membered heteroaryl which is substituted with at least one fluorine atom or nitro group;
- the substituent Z is a halogen atom, cyano or isocyano, hydroxy, sulfhydryl, amino, OTs, OLCMS, C1-C3 alkyl or substituted alkyl, C1-C3 alkoxy or substituted alkoxy, C2-C3 alkenyl or substituted alkenyl, C2-C3 alkynyl or substituted alkynyl, C3-C8 cycloalkyl or substituted cycloalkyl, an aromatic ring, heterocycle, a heteroaromatic ring and fused ring or a substituted aromatic ring, heterocycle, or a heteroaromatic ring and fused ring, the pattern of substitution being mono- or geminal di-substitution;
- the substitution in the substituted C6-C10 aryl, substituted 4-15 membered heterocycle or substituted 5-15 membered heteroaryl in R9 is a halogen atom, nitro, cyano or isocyano, hydroxy, amino, C1-C3 alkyl or alkoxy, alkenyl, alkynyl, cycloalkyl or benzene ring, substituted benzene ring, C1-C3 alkoxy or halogen atom-substituted alkoxy.
A solid compound having the following formula:
Dependencies are inferred from the claim text.