Abstract: The present invention provides an amine derivative having a DYRK-inhibiting activity and represented by formula (1): wherein A1, A2, L1, L2, X, Z, R1 and R4 are as defined in the description, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a 1,4-disubstituted imidazole derivative of formula (1?) wherein ring Q1 is optionally-substituted C6-10 aryl group, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is optionally-substituted C1-4 alkylene group; W2 is —NR3aC(O)— wherein R3a is hydrogen atom or C1-6 alkyl group, etc.; ring Q2 is 5- to 10-membered heteroaryl group, etc.; W3 is optionally-substituted C1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R4 is independently halogen atom, optionally-substituted C1-6 alkyl group, etc.; R5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.

Abstract: The present invention provides a compound that has an inhibitory effect on DYRK and that is represented by general formula (I): wherein Q, R1, R2 and R3 are as defined in the description.

Abstract: The present invention provides a 1,4-disubstituted imidazole derivative of formula (1?) wherein ring Q1 is optionally-substituted C6-10 aryl group, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is optionally-substituted C1-4 alkylene group; W2 is —NR3aC(O)— wherein R3a is hydrogen atom or C1-6 alkyl group, etc.; ring Q2 is 5- to 10-membered heteroaryl group, etc.; W3 is optionally-substituted C1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R4 is independently halogen atom, optionally-substituted C1-6 alkyl group, etc.; R5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.

Abstract: The present invention pertains to an imidazolylamide derivative represented by formula (1) that exhibits an exceptional suppressive effect on cancer cell sphere formation ability and that is useful as an antitumor agent that can be administered orally, or a pharmacologically acceptable salt thereof.

Abstract: The present invention provides a 1,4-disubstituted imidazole derivative of formula (1?) wherein ring Q1 is optionally-substituted C6-10 aryl group, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is optionally-substituted C1-4 alkylene group; W2 is —NR3aC(O)— wherein R3a is hydrogen atom or C1-6alkyl group, etc.; ring Q2 is 5- to 10-membered heteroaryl group, etc.; W3 is optionally-substituted C1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R4 is independently halogen atom, optionally-substituted C1-6 alkyl group, etc.; R5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.

Abstract: The present invention relates to a substituted purine derivative of formula (1) wherein R1 is alkoxy or the like, R2 is alkyl or the like, Ring Q1 is aryl or the like, W1 is alkylene or the like, Ring Q2 is aromatic carbocyclyl or the like, n is 1-4, R3 is hydrogen atom or the like, X1 is single bond or the like, W2 is alkylene or the like, and R4 is hydrogen atom or the like, or a pharmaceutically acceptable salt thereof, which has a potent inhibitory effect against TLR7, and thereby is useful for treating autoimmune disease.

Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R1 is optionally substituted heteroaryl etc.; R2 is hydrogen etc.; R3 and R4 are each independently hydrogen etc., R5 is the following group: (wherein Y is optionally substituted five membered heteroaryl etc., R9a is optionally substituted aryl etc., R9b and R9c are each dependently hydrogen etc., and m is the integral 0 etc.) etc.; R6 is hydrogen etc.; and R7 is hydrogen etc.

Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.

Abstract: The present invention relates to a substituted purine derivative of formula (1) wherein R1 is alkoxy or the like, R2 is alkyl or the like, Ring Q1 is aryl or the like, W1 is alkylene or the like, Ring Q2 is aromatic carbocyclyl or the like, n is 1-4, R3 is hydrogen atom or the like, X1 is single bond or the like, W2 is alkylene or the like, and R4 is hydrogen atom or the like, or a pharmaceutically acceptable salt thereof, which has a potent inhibitory effect against TLR7, and thereby is useful for treating autoimmune disease.

Abstract: The present invention pertains to an imidazolylamide derivative represented by formula (1) that exhibits an exceptional suppressive effect on cancer cell sphere formation ability and that is useful as an antitumor agent that can be administered orally, or a pharmacologically acceptable salt thereof.

Abstract: The present invention provides a 1,4-disubstituted imidazole derivative of formula (1?) wherein ring Q1 is optionally-substituted C6-10 aryl group, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is optionally-substituted C1-4 alkylene group; W2 is —NR3aC(O)— wherein R3a is hydrogen atom or C1-6alkyl group, etc.; ring Q2 is 5- to 10-membered heteroaryl group, etc.; W3 is optionally-substituted C1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R4 is independently halogen atom, optionally-substituted C1-6 alkyl group, etc.; R5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.

Abstract: The present invention provides a 1,4-disubstituted imidazole derivative of formula (1?) wherein ring Q1 is optionally-substituted C6-10 aryl group, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is optionally-substituted C1-4 alkylene group; W2 is —NR3aC(O)— wherein R3a is hydrogen atom or C1-6 alkyl group, etc.; ring Q2 is 5- to 10-membered heteroaryl group, etc.; W3 is optionally-substituted C1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R4 is independently halogen atom, optionally-substituted C1-6 alkyl group, etc.; R5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.

Abstract: The present invention provides a 1,4-disubstituted imidazole derivative of formula (1?) wherein ring Q1 is optionally-substituted C6-10 aryl group, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is optionally-substituted C1-4 alkylene group; W2 is —NR3aC(O)— wherein R3a is hydrogen atom or C1-6 alkyl group, etc.; ring Q2 is 5- to 10-membered heteroaryl group, etc.; W3 is optionally-substituted C1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R4 is independently halogen atom, optionally-substituted C1-6 alkyl group, etc.; R5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.

Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R1 is optionally substituted heteroaryl etc.; R2 is hydrogen etc.; R3 and R4 are each independently hydrogen etc., R5 is the following group: (wherein Y is optionally substituted five membered heteroaryl etc., R9a is optionally substituted aryl etc., R9b and R9c are each dependently hydrogen etc., and m is the integral 0 etc.) etc.; R6 is hydrogen etc.; and R7 is hydrogen etc.

Abstract: The invention provides compounds of Formula I as inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, wherein i.a. R2 is an optionally substituted heterocycle or optionally substituted aryl; and one of R4, R5, R6 and R7 is a substituted heterocycle or substituted aryl.

Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R1 is optionally substituted heteroaryl etc.; R2 is hydrogen etc.; R3 and R4 are each independently hydrogen etc., R5 is the following group: (wherein Y is optionally substituted five membered heteroaryl etc., R9a is optionally substituted aryl etc., R9b and R9c are each dependently hydrogen etc., and m is the integral 0 etc.) etc.; R6 is hydrogen etc.; and R7 is hydrogen etc.

Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R1 is optionally substituted heteroaryl etc.; R2 is hydrogen etc.; R3 and R4 are each independently hydrogen etc., R5 is the following group: (wherein Y is optionally substituted five membered heteroaryl etc., R9a is optionally substituted aryl etc., R9b and R9c are each dependently hydrogen etc., and m is the integral 0 etc.) etc.; R6 is hydrogen etc.; and R7 is hydrogen etc.

Abstract: The present invention provides compounds of formula (I): wherein Ra, Rb, Rc, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention provides compounds of formula (I) wherein R1, Y1, X1, Z1, X2, Y2, A, Y3, n, R and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.