Abstract: A compound represented by the general formula (I) given below or a pharmacologically acceptable salt thereof has been found to have a strong G9a inhibitory effect. The compound (I) or the pharmacologically acceptable salt thereof inhibits G9a and thereby has high usefulness for the treatment, prevention or suppression of various pathological conditions (proliferative disease such as cancer, ?-globin abnormality, fibrosis, pain, neurodegenerative disease, Prader-Willi syndrome, malaria, viral infection, myopathy, autism, etc.).

Abstract: Provided is a cell proliferation inhibitor comprising a compound of the formula (1) or a pharmacologically acceptable salt thereof: wherein J1 and J2 each represent CH or N, with the proviso that J1 and J2 are not simultaneously CH; r represents 0 to 4; each R101 is the same or different when r is 2 or more, and R101 represents a C1-6 alkyl group optionally substituted with a halogen atom or the like; s represents 0 to 5; each R102 is the same or different when s is 2 or more, and R102 represents a halogen atom or the like; R103 represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkyl C1-6 alkyl group; and R101 and R103 are optionally linked together to form a five- to seven-membered ring hetero ring when R101 is present at the 8-position.

Abstract: The present invention aims to provide a novel compound having a high mPTP-opening inhibitory activity and/or a useful therapeutic effect on various diseases. An aspect of the present invention relates to a mitochondrial permeability transition pore (mPTP)-opening inhibitor, a medicament or a pharmaceutical composition comprising a compound represented by formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are the same as defined in the specification and the claims, a stereoisomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, as an active ingredient. Another aspect of the present invention relates to a compound represented by formula (Ia), wherein R1a, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are the same as defined in the specification and the claims, a stereoisomer thereof, a prodrug thereof, or a salt thereof, or a solvate thereof.

Abstract: Provided are 2-(piperidin-1-yl)pyrimidin-4(3H)-ones or pharmaceutically acceptable salts thereof, each characterized by having a 1,8-diazaspiro[4.5]deca-3-ene, 1-oxa-8-azaspiro[4.5]deca-3-ene, 2,8-diazaspiro[4.5]deca-3-ene, 2-oxa-8-azaspiro[4.5]deca-3-ene, 2,9-diazaspiro[5.5]undeca-3-ene, 1-oxa-9-azaspiro[5.5]undeca-3-ene, 1,9-diazaspiro[5.5]undeca-4-ene, or 3,9-diazaspiro[5.

Abstract: Provided is a cell proliferation inhibitor comprising a compound of the formula (1) or a pharmacologically acceptable salt thereof: wherein J1 and J2 each represent CH or N, with the proviso that J1 and J2 are not simultaneously CH; r represents 0 to 4; each R101 is the same or different when r is 2 or more, and R101 represents a C1-6 alkyl group optionally substituted with a halogen atom or the like; s represents 0 to 5; each R102 is the same or different when s is 2 or more, and R102 represents a halogen atom or the like; R103 represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkyl C1-6 alkyl group; and R101 and R103 are optionally linked together to form a five- to seven-membered ring hetero ring when R101 is present at the 8-position.

Abstract: To provide an anticancer agent for preventing and/or treating cancer, comprising a tankyrase inhibitor containing a tankyrase inhibitory compound and a microtubule inhibitor containing a microtubule inhibitory compound as active ingredients.

Abstract: Provided are 2-(piperidin-1-yl)pyrimidin-4(3H)-ones or pharmaceutically acceptable salts thereof, each characterized by having a 1,8-diazaspiro[4.5]deca-3-ene, 1-oxa-8-azaspiro[4.5]deca-3-ene, 2,8-diazaspiro[4.5]deca-3-ene, 2-oxa-8-azaspiro[4.5]deca-3-ene, 2,9-diazaspiro[5.5]undeca-3-ene, 1-oxa-9-azaspiro[5.5]undeca-3-ene, 1,9-diazaspiro[5.5]undeca-4-ene, or 3,9-diazaspiro[5.

Abstract: On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. It was found that a nitrogen-containing bicyclic heterocyclic compound has an excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has an cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.

Abstract: On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. It was found that a nitrogen-containing bicyclic heterocyclic compound has an excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has an cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.

Abstract: [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.

Abstract: [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.

Abstract: This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof. More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC-related disease.

Abstract: A compound having the following formula (I): wherein —R1 is hydrogen, optionally substituted lower alkyl, cyclo(lower)alkyl, cyclo(higher)alkyl, optionally substituted aryl, optionally substituted heterocyclyl, or aryl-fused cyclo(lower)alkyl, R2 is hydrogen or halogen, Z is CH or N, X is formula (II) R3 is lower alkyl which may be substituted with —OH or optionally substituted aryl, or lower alkanoyl, R4 is hydrogen or lower alkyl, Y is optionally substituted lower alkylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.

Abstract: Compounds having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is pyrrolidinylene or piperidinylene, Y is pyridylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, and salts thereof are useful as a histone deacetylase inhibitors.

Abstract: Compounds having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is pyrrolidinylene or piperidinylene, Y is pyridylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, and salts thereof are useful as a histone deacetylase inhibitors.

Abstract: This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof. More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC-related disease.

Abstract: A compound having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is arylene, heterorarylene, cycloalkylene, heterocycloalkylene or aryl-fused cycloalkene, Y is arylene, heteroarylene, which may be substituted with one or more suitable substituent(s), Z lower alenylene, which may be substituted with lower alkyl or halogen, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.

Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.

Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.

Abstract: A compound having the following formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower) alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is arylene, heteroarylene, cycloalkylene, heterocycloalkylene or aryl-fused cycloalkylene, Y is arylene or heteroarylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.