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: 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: The present invention relates to a compound of the formula [I]: wherein (a), in which —Y—, R4, R5 and R6 are4 R5 each as defined in the description, etc., R1 is hydrogen, halogen, lower alkyl, hydroxy, etc., R2 is hydrogen, lower alkyl or hydroxy(lower)alkyl, R3 is hydrogen or an amino protective group, 20R7 is hydrogen, lower alkyl, cyclo(lower)alkyl, lower R9 alkenyl, —Z—R9 or (b), in which —Z— is —0—, —S—, R9 —SO— or —SO2—, and each R9 is independently hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R8 is -D-E-R10, in which -D- is —CONHSO2— or —S02NHCO—, E is bond or lower alkylene, and R10 is halogen, cyano, carboxy, etc., or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of ulcer, overactive bladder, and the like.

Abstract: The present invention relates to a compound formula[I]: wherein X is bond, —CH2—, —O— or —NH—, R1 and R12 are each independently hydrogen, halogen, lower alkyl, etc., R2 is hydrogen or optionally substituted lower alkyl, R3 is hydrogen or an amino protective group, R4, R5 and R6 are each independently hydrogen or optionally substituted lower alkyl, R7 is -Z-R13, in which Z is bond, etc., and R13 is carboxy, lower alkoxycarbonyl, (lower alkylsulfonyl)carbamoyl or lower alkanoylsulfamoyl, R8 is —Y—R9, in which Y is bond, —CH2—, —O—, —S—, etc., and R9 is hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R11 is hydrogen, lower alkyl, lower alkoxy, etc., or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

Abstract: The present invention relates to a compound of the formula [I]: wherein (a), in which —Y—, R4, R5 and R6 are4 R5 each as defined in the description, etc., R1 is hydrogen, halogen, lower alkyl, hydroxy, etc., R2 is hydrogen, lower alkyl or hydroxy(lower)alkyl, R3 is hydrogen or an amino protective group, 20R7 is hydrogen, lower alkyl, cyclo(lower)alkyl, lower R9 alkenyl, -Z-R9 or (b), in which -Z- is -0-, —S—, R9—SO— or —SO2—, and each R9 is independently hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R8 is -D-E-R?, in which -D- is —CONHSO2— or —S02NHCO—, E is bond or lower alkylene, and R10 is halogen, cyano, carboxy, etc., or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of ulcer, overactive bladder, and the like.

Abstract: Ornithine derivatives of the formula (I): wherein X is —CO— or —(CH2)k— (wherein k is 1, 2 or 3); Y is Z-(CH2)n—, and the like; {wherein Z is R1—CO—NR4—, and the like, (wherein R1 is aryl, and the like; and R4 is hydrogen, or lower alkyl); and n is 1, 2, 3, 4, 5 or 6}; R2 is aryl-(lower alkyl), and the like; R3 is -Q-R7, [wherein Q is —CO— or —SO2—, R is heterocyclyl], and the like; and R5 and R6 are independently hydrogen or lower alkyl; or a pharmaceutically acceptable salt thereof, which are useful as medicament.

Abstract: The present invention relates to a compound formula[I]: wherein X is bond, —CH2—, —O— or —NH—, R1 and R12 are each independently hydrogen, halogen, lower alkyl, etc., R2 is hydrogen or optionally substituted lower alkyl, R3 is hydrogen or an amino protective group, R4, R5 and R6 are each independently hydrogen or optionally substituted lower alkyl, R7 is -Z-R13, in which Z is bond, etc., and R13 is carboxy, lower alkoxycarbonyl, (lower alkylsulfonyl)carbamoyl or lower alkanoylsulfamoyl, R8 is —Y—R9, in which Y is bond, —CH2—, —O—, —S—, etc., and R9 is hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R11 is hydrogen, lower alkyl, lower alkoxy, etc., or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

Abstract: A compound of the formula (I): wherein X1 is bond or —OCH2—; X2 is —(CH2)n—, in which n is 1, 2 or 3; X3 is bond, —O—, —S—, —OCH2—, or —NH—; R1 is phenyl or pyridyl each of which may have one or two substituent(s) selected from the group consisting of hydroxy, halogen, etc.; R2 is hydrogen, (lower)alkoxycarbonyl, etc.; R3 is hydroxy(lower)alkyl; halo(lower)alkyl, etc.; R4 is aryl or unsaturated heterocyclic group, each of which may have one or two substituent(s) selected from the group consisting of lower alkyl, hydroxy, carbamoyl, halogen, lower alkoxy, etc.; and a salt thereof which is useful as a medicament.

Abstract: The present invention relates to a compound formula (I) wherein X1 is bond or —O—CH2—, (II) or (III) R1 is hydrogen or an amino protective group, a is phenyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s), and B is hydrogen; halogen; lower alkyl; lower alkoxycarbonyl; cyclo(lower)alkyl; or a heterocyclic group, naphthyl, 1,2,3,4-tetrahydronaphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s), or a salt thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiures or urinary incontinence.

Abstract: The present invention relates to a compound formula wherein R1 is phenyl, pyridyl, etc., each of which may be substituted with one or two substituent(s); R2 is hydrogen, an amino protective group, etc.; R3 and R4 are each independently hydrogen, lower alkyl or hydroxy(lower)alkyl; R5 is aryl, ar(lower)alkyl, etc., each of which may be substituted with one, two or three substituent(s); R8 is hydrogen or halogen, X is a single bond or O—CH2—, and n is 0, 1 or 2, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

Abstract: The present invention relates to a compound formula (I) wherein X1 is bond or —O—CH2—, (II) or (III) R1 is hydrogen or an amino protective group, a is phenyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s), and B is hydrogen; halogen; lower alkyl; lower alkoxycarbonyl; cyclo(lower)alkyl; or a heterocyclic group, naphthyl, 1,2,3,4-tetrahydronaphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s), or a salt thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiures or urinary incontinence.

Abstract: A compound of the formula (I) wherein X1 ? is bond or —O(CH2)m— (in which m is an integral number of 1, 2 or 3); X2 is bond, —(CH2)n—, etc. (in which n is an integral number of 1, 2 or 3); R1 is hydrogen or amino protective group; R2 is hydroxy(lower)alkyl or (lower)alkoxy(lower)alkyl; A is phenyl, pyridyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, lower alkyl, etc.; and B is phenyl or pyridyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, nitro, etc.; and a pharmaceutically acceptable salt thereof which is useful as a medicament.

Abstract: A compound of the formula [Ig]; wherein R1 is hydrogen or an amino protective group, R2 is hydrogen or hydroxy, and R3 and R4 are independently N-methyl-methoxycarbonylamino, N-ethyl-methoxycarbonylamino, N-propyl-methoxycarbonylamino or 3-ethylureid, or R3 and R4 are both methoxycarbonylamino substituted at a meta position of the benzene rings, or a salt thereof, and (2S)-1-phenoxy-3-[3,3-bis[4-methoxycarbonylamino)-phenyl]propylamino]-2-propanol sulfate (2:1) and some crystal forms thereof as &bgr;3adrenergic receptor agonists.

Abstract: A compound of the formula (I): 1

Abstract: Preparation of optically active 3-substituted azetidinones of the formula (I) ##STR1## in which R.sup.1 is a hydroxy-protective group wherein an allylic alcohol of the formula (II) ##STR2## is acylated, then subjected to asymmetric enzymatic hydrolysis yielding the R-allylic alcohol. The hydroxyl group is protected and then stereoselectively reacted with an amine which is subsequently cyclized to yield the desired 3-substituted azetidinone. Two new species of microorganisms have been isolated, Pimelobacter sp. No. 1254 and Bacillus megaterium No. 1253 which exhibit stereoselective esterase activity.