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US 8,940,725 B2Granted
Purinone derivative
AssigneeOno Pharmaceutical Co., Ltd.
InventorsShingo Yamamoto, Toshio Yoshizawa
Life of this patent
Estimating the term…
Abstract
Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.
Claims11
A compound represented by general formula (I)
- (in the formula,
- L represents (1) —O—, (2) —S—, (3) —SO—, (4) —SO2— (5) —NH—, (6) —C(O)—, (7) —CH2—O—, (8) —O—CH2—, (9) —CH2—, or (10) —CH(OH)—;
- R1 represents (1) a halogen atom, (2) a C1-4 alkyl group, (3) a C1-4 alkoxy group, (4) a C1-4 haloalkyl group, or (5) a C1-4 haloalkoxy group;
- ring1 represents a benzene, cyclohexane, or pyridine ring, which may be substituted by from one to five substituents each independently selected from the group consisting of (1) halogen atoms, (2) C1-4 alkyl groups, (3) C1-4 alkoxy groups, (4) nitrile, (5) C1-4 haloalkyl groups, and (6) C1-4 haloalkoxy groups, wherein when two or more substituents are present on ring1, these substituents may form a 4- to 7-membered cyclic group together with the atoms in ring1 to which these substituents are bound;
- ring2 represents a 4- to 6-membered nitrogenous saturated heterocycle, which is substituted by from one to three —K—R2;
- K represents C(O), (wherein the bond on the left is bound to the ring2);
- R2 represents (1) a C1-4 alkyl, (2) a C2-4 alkenyl, or (3) a C2-4 alkynyl group, each of which may be substituted by from one to five substituents each independently selected from the group consisting of (1) NR3R4, (2) halogen atoms, (3) CONR5R6, (4) CO2R7, and (5) OR8;
- R3 and R4 each independently represent (1) a hydrogen atom, or (2) a C1-4 alkyl group which may be substituted by OR9 or CONR10R11;
- R3 and R4 may, together with the nitrogen atom to which they are bound, form a 4- to 7-membered nitrogenous saturated heterocycle, which may be substituted by an oxo group or a hydroxyl group;
- R5 and R6 each independently represent (1) a hydrogen atom, (2) a C1-4 alkyl group, or (3) a phenyl group;
- R7 represents (1) a hydrogen atom or (2) a C1-4 alkyl group;
- R8 represents (1) a hydrogen atom, (2) a C1-4 alkyl group, (3) a phenyl group, or (4) a benzotriazolyl group;
- R9 represents (1) a hydrogen atom or (2) a C1-4 alkyl group;
- R10 and R11 each independently represent (1) a hydrogen atom or (2) a C1-4 alkyl group;
- n represents an integer from 0 to 4;
- m represents an integer from 0 to 2;
- and
- when n is two or more, the R1's may be the same as each other or may differ from one another),
- an optical isomer thereof or their mixture, a salt thereof, a solvate thereof, or an N-oxide thereof.
16 more elements
Dependencies are inferred from the claim text.