Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ßproduction, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ßproteins. A compound of Formula (I) wherein R3 is each independently alkyl optionally substituted with halogen, cyano, alkyloxy, haloalkyloxy or non-aromatic carbocyclyl, or the like; t is integer from 0 to 3; R5 is a hydrogen atom or halogen; R6 is selected from the group consisting of a hydrogen atom, halogen, and substituted or unsubstituted alkyl; ring B is a substituted or unsubstituted pyrazine or the like; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins.

Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ßproduction, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ßproteins. A compound of Formula (I) wherein R3 is each independently alkyl optionally substituted with halogen, cyano, alkyloxy, haloalkyloxy or non-aromatic carbocyclyl, or the like; t is integer from 0 to 3; R5 is a hydrogen atom or halogen; R6 is selected from the group consisting of a hydrogen atom, halogen, and substituted or unsubstituted alkyl; ring B is a substituted or unsubstituted pyrazine or the like; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a Sonogashira-Carbonylation reaction using two types of gas, as well as novel crystals which can control a heat of the said reaction and the process of producing the same. In addition, the present invention relates to a ligand (additive) to prevent the deactivation of a palladium catalyst.

Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins. A compound of the formula (I): wherein X is —C(R3a)(R3b)—, —C(R3a)(R3b)—C(R3c)(R3d)— or —C(R3a)?C(R3c)—, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R3a, R3b, R3c and R3d are each independently hydrogen, halogen or the like, R4 is hydrogen or halogen, Ring B is substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a Sonogashira-Carbonylation reaction using two types of gas, as well as novel crystals which can control a heat of the said reaction and the process of producing the same. In addition, the present invention relates to a ligand (additive) to prevent the deactivation of a palladium catalyst.

Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent, for diseases induced by production, secretion and/or deposition of amyloid ? proteins. A compound of the formula (I) wherein X is —S— or —O—, R3a is alkyl, haloalkyl or the like, R2a is H, halogen, alkyloxy, haloalkyloxy or the like, R2b is H or the like, R3b is H or alkyl, ring A and ring B is each independently a substituted or unsubstituted aromatic carbocycle, a substituted or unsubstituted aromatic heterocycle or the like, and R1 is substituted or unsubstituted alkyl or the like, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins. A compound of the formula (I): wherein X is —C(R3a)(R3b)—, —C(R3a)(R3b)—C(R3c)(R3d)— or —C(R3a)?C(R3c)—, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R3a, R3b, R3c and R3d are each independently hydrogen, halogen or the like, R4 is hydrogen or halogen, Ring B is substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins. A compound of the formula (I): wherein X is —C(R3a)(R3b)—, —C(R3a)(R3b)—C(R3c)(R3d)— or —C(R3a)?C(R3c)—, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R3a, R3b, R3c and R3d are each independently hydrogen, halogen or the like, R4 is hydrogen or halogen, Ring B is substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins. A compound of the formula (I): wherein X is —C(R3a)(R3b)—, —C(R3a)(R3b)—C(R3c)(R3d)— or —C(R3a)?C(R3c)—, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R3a, R3b, R3c and R3d are each independently hydrogen, halogen or the like, R4 is hydrogen or halogen, Ring B is substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2?X3 is CR5—CR6?CR7, N—CR6?CR7, CR5—N?CR7 or CR5—CR6?N, R1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R4a, R4b, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.

Abstract: The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2?X3 is CR5—CR6?CR7, N—CR6?CR7, CR5—N?CR7 or CR5—CR6?N, R1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R4a, R4b, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.

Abstract: Provided are a compound represented by general formula (1) and having a TTK inhibitory action and a medicine containing the compound. In formula (1), (X, Y, V, W) is (—N?, ?CR1—, ?N—, —CR7?), (—CR2?, ?N—, ?N—, —CR7?), etc.; A is an (un)substituted aromatic hydrocarbon ring, etc.; L is a single bond, —C(?O)—NRA—, etc.; Z is a group represented by the formula —NR3R4 or a group represented by the formula —OR5; R1 to R3, R6, and R7 each is a hydrogen atom, etc.; R4 and R5 each is an (un)substituted alkyl, etc.; and R8 is an (un)substituted cycloalkyl, etc.

Abstract: A compound represented by the general formula (I): wherein R1 is wherein R26 and R28 are each independently lower alkyloxy and the like; n1 is an integer of 0 to 3; Z is a optionally substituted C1-C5 alkynylene which may be interrupted with a substituent selected from Substituent group a and the like; A is a group represented by the formula: wherein R6 and R7 are each independently lower alkyl and the like; m and n are each independently 0, 1, or 2; R2 is a hydrogen atom and the like; R3 is optionally substituted lower alkyl and the like; R4 is a hydrogen atom; or R3 and R4 may be taken together with an adjacent carbon atom to from a ring; R5 is hydroxyl and the like, or an optically active isomer, a pharmaceutically acceptable salt or a solvate thereof.