Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integraso inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

Abstract: The present invention is directed to a class of substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1H-pyrido[1,2-a]pyrrolo[1?,2?:3,4]imidazo[1,2-d]pyrazine-8-carboxamides useful as anti-HIV agents. The compounds have the formula (I-1-1): wherein ring A is an optionally substituted hexahydro-1H-pyrrolo[1,2-c]-imidazole; R14 and RX are independently hydrogen or optionally substituted lower alkyl; R3 is selected from various groups; R1 is hydrogen or lower alkyl; R is halogen; m is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to a substituted 2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2 -a]pyrido[1,2-d]pyrazine-5,7-dione useful as an anti-HIV agent, which has the formula: as well as pharmaceutically acceptable salts thereof, compostions thereof, and methods of use thereof.

Abstract: A compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent, of the formula: wherein R1, R2, R3, R4, B1 and B2 are defined in the specification.

Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.

Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

Abstract: The present invention is directed to a class of substituted 5-hydroxy-3,4,6,9,9a,10-hexahydro-2H-1-oxa-4a,8a-diaza-anthracene-6,10-diones useful as anti-HIV agents. The compounds have the formula: Z?O; R20, R21, R22, R23, R24 and R25 independently are hydrogen, C1-C8 alkyl, (C6-C14)aryl-(C1-C8)alkyl, C6-C14 aryl, or alkoxy; the stereochemistry of an asymmetric carbon represented by * shows R- or S-configuration, or a mixture thereof; RX is hydrogen; R14 is hydrogen or optionally substituted lower alkyl; R3 is hydrogen; R1 is hydrogen or lower alkyl; R is halogen; and m is 1, 2 or 3; or a pharmaceutically acceptable salt thereof.

Abstract: A compound having HIV Integrase Inhibitory activity of the formula: (wherein: R1 is optionally substituted aralkyl; R2 and R3 are each independently hydrogen, optionally substituted alkyl, optionally substituted amino, optionally substituted alkenyl or optionally substituted alkoxy (provided that each substituent for “optionally substituted” is a noncyclic group); R4 is hydrogen, optionally substituted carboxy, optionally substituted formylamino, optionally substituted carbamoyl, optionally substituted amino (provided that a substituent on amino in “optionally substituted formylamino”, “optionally substituted carbamoyl” and “optionally substituted amino” may form an optionally-substituted N-atom containing heterocyclic ring together with an adjacent N atom), optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl) or a salt thereof.

Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

Abstract: [Problems to be Solved] To provide a novel compound having antiviral activity, especially inhibitory activity against HIV integrase, a pharmaceutical composition, especially anti-HIV drug, containing the same.

Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.

Abstract: A heterocyclic compound of the formula (I): wherein B1 is —C(R2)? or —N?; R1? is H, etc.; one of R1 and R2 is -Z1-Z2-Z3-R5 wherein Z1 and Z3 are independently single bond, optionally substituted alkylene, etc.; Z2 is single bond, optionally substituted alkylene, etc.; R5 is optionally substituted aryl, optionally substituted heteroaryl, etc., and the other of R1 and R2 is H; -A1- is —C(—Y)?C(—RA)—C(—R3)?C(—R4)—, etc. wherein Y is OH, etc.; RA is —COR7 wherein R7 is OH, etc.; one of R3 and R4 is carboxy, etc., and the other of R1 and R2 is H, etc, a prodrug thereof, a pharmaceutically acceptable salt thereof, and a solvate thereof, having an antiviral activity, more particularly, an inhibitory activity against HIV integrase, and a pharmaceutical composition containing the same, especially an anti-HIV drug.

Abstract: A heterocyclic compound of the formula (I): wherein B1 is —C(R2)? or —N?; R1? is H, etc.; one of R1 and R2 is -Z1-Z2-Z3-R5 wherein Z1 and Z3 are independently single bond, optionally substituted alkylene, etc.; Z2 is single bond, optionally substituted alkylene, etc.; R5 is optionally substituted aryl, optionally substituted heteroaryl, etc., and the other of R1 and R2 is H; -A1- is —C(—Y)?C(—RA)—C(—R3)?C(—R4)—, etc. wherein Y is OH, etc.; RA is —COR7 wherein R7 is OH, etc.; one of R3 and R4 is carboxy, etc., and the other of R1 and R2 is H, etc, a prodrug thereof, a pharmaceutically acceptable salt thereof, and a solvate thereof, having an antiviral activity, more particularly, an inhibitory activity against HIV integrase, and a pharmaceutical composition containing the same, especially an anti-HIV drug.

Abstract: A heterocyclic compound of the formula (I): wherein B1 is —C(R2)? or —N?; R1? is H, etc.; one of R1 and R2 is -Z1-Z2-Z3-R5 wherein Z1 and Z3 are independently single bond, optionally substituted alkylene, etc.; Z2 is single bond, optionally substituted alkylene, etc.; R1 is optionally substituted aryl, optionally substituted heteroaryl, etc., and the other of R1 and R2 is H; -A1- is —C(—Y)?C(—RA)—C(—R3)?C(—R4)—, etc. wherein Y is OH, etc.; RA is —COR7 wherein R7 is OH, etc.; one of R3 and R4 is carboxy, etc., and the other of R1 and R2 is H, etc, a prodrug thereof, a pharmaceutically acceptable salt thereof, and a solvate thereof, having an antiviral activity, more particularly, an inhibitory activity against HIV integrase, and a pharmaceutical composition containing the same, especially an anti-HIV drug.

Abstract: A heterocyclic compound of the formula (I): wherein B1 is —C(R2)? or —N?; R1? is H, etc.; one of R1 and R2 is -Z1-Z2-Z3-R5 wherein Z1 and Z3 are independently single bond, optionally substituted alkylene, etc.; Z2 is single bond, optionally substituted alkylene, etc.; R5 is optionally substituted aryl, optionally substituted heteroaryl, etc., and the other of R1 and R2 is H; -A1- is —C(—Y)?C(—RA)—C(—R3)?C(—R4)—, etc. wherein Y is OH, etc.; RA is —COR7 wherein R7 is OH, etc.; one of R3 and R4 is carboxy, etc., and the other of R1 and R2 is H, etc, a prodrug thereof, a pharmaceutically acceptable salt thereof, and a solvate thereof, having an antiviral activity, more particularly, an inhibitory activity against HIV integrase, and a pharmaceutical composition containing the same, especially an anti-HIV drug.