Abstract: The present invention provides a tricyclic compound represented by general formula (I), a pharmaceutical salt thereof, or a stereoisomer thereof exhibits excellent antibacterial activity against Gram-negative bacteria resistant bacteria thereof, and also being excellent in terms of safety. Furthermore, the present invention provides production processes, pharmaceutical compositions comprising a tricyclic compound, a pharmaceutically acceptable salt thereof, or a stereoisomer thereof as an active ingredient and use thereof as a pharmaceutical agent. The compounds of the present invention are useful for the treatment and/or prevention of disease such as complicated urinary tract infections (cUTIs), nosocomial pneumonia, intra-abdominal infections (IAIs) or bacteremia.

Abstract: The present invention provides a tricyclic compound represented by general formula (I), a pharmaceutical salt thereof, or a stereoisomer thereof exhibits excellent antibacterial activity against Gram-negative bacteria resistant bacteria thereof, and also being excellent in terms of safety. Furthermore, the present invention provides production processes, pharmaceutical compositions comprising a tricyclic compound, a pharmaceutically acceptable salt thereof, or a stereoisomer thereof as an active ingredient and use thereof as a pharmaceutical agent. The compounds of the present invention are useful for the treatment and/or prevention of disease such as complicated urinary tract infections (cUTIs), nosocomial pneumonia, intra-abdominal infections (IAIs) or bacteremia.

Abstract: Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): [wherein, Ar which is a partial structure in the general formula (1) represents a phenyl group or a naphthyl group; R1a and R1b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; R2a and R2b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; A represents a single bond, an oxygen atom, or the like; B represents a single bond, a C1-C4 alkanediyl group, or the like; Z represents a carboxyl group or a tetrazolyl group; and m represents an integer of 1 to 3] or a pharmacologically acceptable salt thereof.

Abstract: Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): [wherein, Ar which is a partial structure in the general formula (1) represents a phenyl group or a naphthyl group; R1a and R1b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; R2a and R2b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; A represents a single bond, an oxygen atom, or the like; B represents a single bond, a C1-C4 alkanediyl group, or the like; Z represents a carboxyl group or a tetrazolyl group; and m represents an integer of 1 to 3] or a pharmacologically acceptable salt thereof.

Abstract: Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): [wherein, Ar which is a partial structure in the general formula (1) represents a phenyl group or a naphthyl group; R1a and R1b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; R2a and R2b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; A represents a single bond, an oxygen atom, or the like; B represents a single bond, a C1-C4 alkanediyl group, or the like; Z represents a carboxyl group or a tetrazolyl group; and m represents an integer of 1 to 3] or a pharmacologically acceptable salt thereof.

Abstract: The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

Abstract: The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

Abstract: The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

Abstract: The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

Abstract: The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

Abstract: Pharmaceutical compositions and methods of treatment are provided for treating amyloidosis, containing, as an active ingredient, at least one nitrogen-containing heteroaryl compound represented by the following general formula or a pharmacologically permitted salt thereof; together with nitrogen-containing heteroaryl derivatives, and pharmacologically permitted salts thereof: where, R1, R2, Z1-Z5, and A are as defined herein.

Abstract: A compound of the formula (I): wherein R1 represents a C1-C6 alkyl, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and represent hydrogen or a C1-C6 alkyl; Ra represents hydrogen, C1-C6 alkyl or C2-C6 alkenyl or together with R2 represents a C1-C3 alkylene; Arom represents a heteroaryl; A represents a C1-C6 alkylene; E represents a single bond, oxygen, sulphur or R4NR4—, wherein R4 is hydrogen or C1-C7 alkenoyl; X1 and X2 both represent oxygen; X2 is attached at the 3-position or the 4-position; or a pharmacologically acceptable salt or ester thereof. The compound has superior acetylcholinesterase inhibitory action and selective serotonin reuptake inhibitory action, and is useful for treating Alzheimer's disease, depression, Huntington's chorea, Pick's disease, tardive dyskinesia, compulsive disorders or panic disorders.

Abstract: A compound of the formula (I): wherein R1 is a C1-C6 alkyl, an amino, a (C1-C6 alkyl)amino, a di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and are a hydrogen or a C1-C6 alkyl; Arom is an unsubstituted or substituted aryl or an unsubstituted or substituted heteroaryl; wherein the substituted aryl is substituted at 1 to 5 positions and the substituted heteroaryl is substituted at 1 to 3 positions; wherein the heteroaryl is furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; and wherein the substituents of the substituted aryl and of the substituted heteroaryl are independently halogen, C1-C6 alkyl, halogeno C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C3 alkylenedioxy, C1-C7 alkanoyl, C2-C7 alkyloxycarbonyl, amino, C1-C7 alkanoylamino, hydroxyl, mercapto, cyano, nitro or carboxyl; A is an ethylene or propyle

Abstract: A compound of the formula (I): wherein R1 is a C1-C6 alkyl group, an amino group, a (C1-C6 alkyl)amino group, a di(C1-C6 alkyl)amino group or a nitrogen-containing saturated heterocyclic group; R3 is a hydrogen atom or a C1-C6 alkyl group; Arom is an unsubstituted or substituted aryl group or an unsubstituted or substituted heteroaryl group; wherein the substituted aryl group is substituted at 1 to 5 positions and the substituted heteroaryl group is substituted at 1 to 3 positions; and wherein the substituents of the aryl group and of the heteroaryl group are independently selected from the group consisting of halogen atom, C1-C6 alkyl, halogeno C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C3 alkylenedioxy, C1-C7 alkanoyl, C2-C7 alkyloxycarbonyl, amino, C1-C7 alkanoylamino, hydroxyl, mercapto, cyano, nitro and carboxyl; A is a C1-C6 alkylene group; Ra together with R2 is a C2-C3 alkylene group containing a double bond; E is a single bond, an oxygen atom, a sulfur atom or a group of the formula: —NR4—, w

Abstract: A compound of the formula (I): wherein R1 represents C1–C6 alkyl, amino(C1–C6 alkyl)amino, di(C1–C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and represent hydrogen or C1–C6 alkyl; Ra represents C1–C6 alkyl or C2–C6 alkenyl or together with R2 represents a C1–C3 alkylene; Arom represents aryl or heteroaryl; A represents a C1–C6 alkylene; E represents a single bond, oxygen, sulfur or R4NR4—, wherein R4 is hydrogen or C1–C7 alkenoyl; X1 and X2 are the same or different and represent oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof. The compound has superior acetylcholinesterase inhibitory action and selective serotonin reuptake inhibitory action, and is useful for treating or preventing Alzheimer's disease, depression, Huntington's chorea, Pick's disease, tardive dyskinesia, compulsive disorders or panic disorders.

Abstract: A compound of the formula (I): wherein R1 is C1-C6 alkyl, amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are hydrogen or C1-C6 alkyl; Arom is phenyl, idenyl, napthyl, phenanthrenyl, furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; A is C1-C6 alkylene; Ra is hydrogen, C1-C6 alkyl or C2-C6 alkenyl; E is a single bond, oxygen, sulfur or —NR4—, wherein R4 is hydrogen or C1-C7 alkanoyl; X1 and X2 are oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof.

Abstract: The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

Abstract: A compound of the formula (I): wherein R1 is a C1-C6 alkyl group, an amino group, a (C1-C6 alkyl)amino group, a di(C1-C6 alkyl)amino group or a nitrogen-containing saturated heterocyclic group; R3 is a hydrogen atom or a C1-C6 alkyl group; Arom is an unsubstituted or substituted aryl group or an unsubstituted or substituted heteroaryl group; wherein the substituted aryl group is substituted at 1 to 5 positions and the substituted heteroaryl group is substituted at 1 to 3 positions; and wherein the substituents of the aryl group and of the heteroaryl group are independently selected from the group consisting of halogen atom, C1-C6 alkyl, halogeno C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C3 alkylenedioxy, C1-C7 alkanoyl, C2-C7 alkyloxycarbonyl, amino, C1-C7 alkanoylamino, hydroxyl, mercapto, cyano, nitro and carboxyl; A is a C1-C6 alkylene group; Ra together with R2 is a C2-C3 alkylene group containing a double bond; E is a single bond, an oxygen atom, a sulfur atom or a group of the formula: —NR4—,

Abstract: A compound of the formula (1): wherein R1 is a C1-C6 alkyl, an amino, a (C1-C6 alkyl)amino, a di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and are a hydrogen or a C1-C6 alkyl; Arom is an unsubstituted or substituted aryl or an unsubstituted or substituted heteroaryl; wherein the substituted aryl is substituted at 1 to 5 positions and the substituted heteroaryl is substituted at 1 to 3 positions; wherein the heteroaryl is furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; and wherein the substituents of the substituted aryl and of the substituted heteroaryl are independently halogen, C1-C6 alkyl, halogeno C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C3 alkylenedioxy, C1-C7 alkanoyl, C2-C7 alkyloxycarbonyl, amino, C1-C7 alkanoylamino, hydroxyl, mercapto, cyano, nitro or carboxyl; A is an ethylene or propyl

Abstract: The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).