Claims for Patent: 8,987,441

Summary for Patent: 8,987,441

Title:	Substituted polycyclic carbamoyl pyridone derivative prodrug
Abstract:	The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
Inventor(s):	Takahashi; Chika (Toyonaka, JP), Mikamiyama; Hidenori (Toyonaka, JP), Akiyama; Toshiyuki (Toyonaka, JP), Tomita; Kenji (Toyonaka, JP), Taoda; Yoshiyuki (Toyonaka, JP), Kawai; Makoto (Toyonaka, JP), Anan; Kosuke (Toyonaka, JP), Miyagawa; Masayoshi (Toyonaka, JP), Suzuki; Naoyuki (Toyonaka, JP)
Assignee:	Shionogi & Co., Ltd. (Osaka, JP)
Application Number:	13/824,723
Patent Claims:	1. A compound represented by formula (I): ##STR01340## a pharmaceutically acceptable salt, or a solvate thereof: wherein: --C(.dbd.O)--P.sup.R0, a) --C(.dbd.O)--P.sup.R1, b) --C(.dbd.O)-L-P.sup.R1, c) --C(.dbd.O)-L-O--P.sup.R1, d) --C(.dbd.O)-L-O-L-O--P.sup.R1, e) --C(.dbd.O)-L-O--C(.dbd.O)--P.sup.R1, f) --C(.dbd.O)--O--P.sup.R2, g) --C(.dbd.O)--N(P.sup.R2).sub.2, h) --C(.dbd.O)--O-L-O--P.sup.R2, i) --CH.sub.2--O--P.sup.R3, j) --CH.sub.2--O-L-O--P.sup.R3, k) --CH.sub.2--O--C(.dbd.O)--P.sup.R3, l) --CH.sub.2--O--C(.dbd.O)--O--P.sup.R3, m) --CH(--CH.sub.3)--O--C(.dbd.O)--O--P.sup.R3, n) --CH.sub.2--O--C(.dbd.O)--N(--K)--P.sup.R3, o) --CH.sub.2--O--C(.dbd.O)--O-L-O--P.sup.R3, p) --CH.sub.2--O--C(.dbd.O)--O-L-N(P.sup.R3).sub.2, q) --CH.sub.2--O--C(.dbd.O)--N(--K)-L-O--P.sup.R3, r) --CH.sub.2--O--C(.dbd.O)--N(--K)-L-N(P.sup.R3).sub.2, s) --CH.sub.2--O--C(.dbd.O)--O-L-O-L-O--P.sup.R3, t) --CH.sub.2--O--C(.dbd.O)--O-L-N(--K)--C(.dbd.O)--P.sup.R3, u) --CH.sub.2-O--P(.dbd.O)(--OH).sub.2, v) --CH.sub.2--O--P(.dbd.O)(--OBn).sub.2, w) --CH.sub.2--PR.sup.4(except for a benzyl group), x) --C(.dbd.N.sup.+P.sup.R5.sub.2)(--NP.sup.R5.sub.2) y); (wherein L is straight or branched lower alkylene, or straight or branched lower alkenylene, K is hydrogen, or straight or branched lower alkylene, P.sup.R0 is lower alkyl optionally substituted by substituent group F, or lower alkenyl optionally substituted by substituent group F, P.sup.R1 is carbocyclic group optionally substituted by substituent group F, heterocyclic group optionally substituted by substituent group F, lower alkyl amino optionally substituted by substituent group F, or lower alkylthio optionally substituted by substituent group F, P.sup.R2 is lower alkyl optionally substituted by substituent group F, carbocyclic group optionally substituted by substituent group F, or heterocyclic group optionally substituted by substituent group F, P.sup.R3 is lower alkyl optionally substituted by substituent group F, carbocyclic group optionally substituted by substituent group F, heterocyclic group optionally substituted by substituent group F, lower alkyl amino optionally substituted by substituent group F, carbocycle lower alkyl optionally substituted by substituent group F, heterocycle lower alkyl optionally substituted by substituent group F, or lower alkylsilyl, and P.sup.R5 is lower alkyl optionally substituted by substituent group F; wherein Substituent group F is chosen from oxo, lower alkyl, hydroxy lower alkyl, amino, lower alkylamino, carbocycle lower alkyl, lower alkylcarbonyl, halogen, hydroxy, carboxy, lower alkylcarbonylamino, lower alkylcarbonyloxy, lower alkvloxycarbonyl, lower alkyloxy, cyano, and nitro); R.sup.1a is hydrogen, halogen, hydroxy, carboxy, cyano, formyl, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, lower alkyloxy optionally substituted by substituent group C, lower alkenyloxy optionally substituted by substituent group C, lower alkylcarbonyl optionally substituted by substituent group C, lower alkyloxycarbonyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, carbocycleoxy optionally substituted by substituent group C, carbocycleoxycarbonyl optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, heterocycleoxy optionally substituted by substituent group C, heterocycleoxycarbonyl optionally substituted by substituent group C, --Z--N(R.sup.A1)(R.sup.A2), --Z--N(R.sup.A3)--SO.sub.2--(R.sup.A4), --Z--C(.dbd.O)--N(R.sup.A5)--SO.sub.2--(R.sup.A6), --Z--N(R.sup.A7)--C(.dbd.O)--R.sup.A8, --Z--S--R.sup.A9, --Z--SO.sub.2--R.sup.A10, --Z--S(.dbd.O)--R.sup.A11, --Z--N(R.sup.A12)--C(.dbd.O)--O--R.sup.A13, --Z--N(R.sup.A14)--C(.dbd.O)--N(R.sup.A15)(R.sup.A16), --Z--C(.dbd.O)--N(R.sup.A17)--C(.dbd.O)--N(R.sup.A18)(R.sup.A19), --Z--N(R.sup.A20)--C(.dbd.O)--C(.dbd.O)--R.sup.A21, or --Z--B(--OR.sup.A22)(--OR.sup.A23); (wherein R.sup.A1, R.sup.A2, R.sup.A3, R.sup.A5, R.sup.A7, R.sup.A8, R.sup.A9, R.sup.A12, R.sup.A13, R.sup.A14, R.sup.A15, R.sup.A16, R.sup.A17, R.sup.A18, R.sup.A19, R.sup.A20, and R.sup.A21 are each independently selected from a substituent group consisting of hydrogen, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, and heterocycle lower alkyl optionally substituted by substituent group C, R.sup.A4, R.sup.A6, R.sup.A10, and R.sup.A11 are each independently selected from a substituent group consisting of lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, and heterocycle lower alkyl optionally substituted by substituent group C, R.sup.A1 and R.sup.A2, R.sup.A15 and R.sup.A16, and R.sup.A18 and R.sup.A19, each may be taken together with an adjacent atom to form heterocycle, R.sup.A22 and R.sup.A23 are each independently an hydrogen atom, lower alkyl optionally substituted by substituent group C, or R.sup.A22 and R.sup.A23 may be taken together with an adjacent atom to form heterocycle, and Z is a single bond or straight or branched lower alkylene); R.sup.2a is hydrogen, halogen, carboxy, cyano, formyl, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, lower alkyloxy optionally substituted by substituent group C, lower alkenyloxy optionally substituted by substituent group C, lower alkylcarbonyl optionally substituted by substituent group C, lower alkyloxycarbonyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, carbocyclecarbonyl optionally substituted by substituent group C, carbocycleoxy optionally substituted by substituent group C, carbocycleoxycarbonyl optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, heterocyclecarbonyl optionally substituted by substituent group C, heterocycleoxy optionally substituted by substituent group C, heterocycleoxycarbonyl optionally substituted by substituent group C, --Z--N(R.sup.B1)--SO.sub.2--R.sup.B2, --Z--N(R.sup.B3)--C(.dbd.O)--R.sup.B4, --Z--N(R.sup.B5)--C(.dbd.O)--O--R.sup.B6, --Z--C(.dbd.O)--N(R.sup.B7)(R.sup.B8), --Z--N(R.sup.B9)(R.sup.B10), or --Z--SO.sub.2--R.sup.B11 (wherein R.sup.B1, R.sup.B3, R.sup.B4, R.sup.B5, R.sup.B6, R.sup.B7, R.sup.B8, R.sup.B9, and R.sup.B10 are each independently selected from a substituent group consisting of hydrogen, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, and heterocycle lower alkyl optionally substituted by substituent group C, R.sup.B2 and R.sup.B11 are each independently selected from a substituent group consisting of lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, and heterocycle lower alkyl optionally substituted by substituent group C, R.sup.B7 and R.sup.B8, and R.sup.B9 and R.sup.B10 may be taken together with an adjacent atom to form heterocycle and Z is a single bond or straight or branched lower alkylene); R.sup.3a is hydrogen, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, carbocycleoxy lower alkyl optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, --Z--N(R.sup.C1)--SO.sub.2--R.sup.C2, --Z--N(R.sup.C3)--C(.dbd.O)--R.sup.C4, --Z--N(R.sup.C5)--C(.dbd.O)--O--R.sup.C6, --Z--C(.dbd.O)--N(R.sup.C7)(R.sup.C8), or --Z--N(R.sup.C9)(R.sup.C10), (wherein R.sup.C1, R.sup.C3, R.sup.C4, R.sup.C5, R.sup.C6, R.sup.C7, R.sup.C8, R.sup.C9, and R.sup.C10 are each independently selected from a substituent group consisting of hydrogen, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, and heterocycle lower alkyl optionally substituted by substituent group C, R.sup.C2 is independently selected from a substituent group consisting of lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, and heterocycle lower alkyl optionally substituted by substituent group C, R.sup.C7 and R.sup.C8, and R.sup.C9 and R.sup.C10 each may be taken together with an adjacent atom to form heterocycle, and Z is a single bond or straight or branched lower alkylene) and; B.sup.1 is NR.sup.7a and B.sup.2 is CR.sup.5aR.sup.6a; R.sup.5a, R.sup.6a, and R.sup.7a are each independently selected from a substituent group consisting of hydrogen, carboxy, cyano, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, lower alkyl carbonyl optionally substituted by substituent group C, lower alkyl oxycarbonyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, carbocycleoxy lower alkyl optionally substituted by substituent group C, carbocyclecarbonyl optionally substituted by substituent group C, carbocycleoxycarbonyl optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, heterocycleoxy lower alkyl optionally substituted by substituent group C, heterocyclecarbonyl optionally substituted by substituent group C, heterocycleoxycarbonyl optionally substituted by substituent group C, --Y--S--R.sup.D1, --Z--S(.dbd.O)--R.sup.D2, --Z--SO.sub.2--R.sup.D3, --C(.dbd.O)--C(.dbd.O)--R.sup.D4, --C(.dbd.O)--N(R.sup.D5)(R.sup.D6), --Z--C(R.sup.D7)(R.sup.D8)(R.sup.D9), --Z--CH.sub.2--R.sup.D10, --Z--N(R.sup.D11)--C(.dbd.O)--O--R.sup.D12, or --Z--N(R.sup.D13)--C(.dbd.O)--R.sup.D14, or R.sup.5a and R.sup.6a may be taken together to form heterocyclic group optionally substituted by substituent group C, (wherein R.sup.D1, R.sup.D4, R.sup.D5, R.sup.D6, R.sup.D9, R.sup.D11, R.sup.D12, R.sup.D13, and R.sup.D14 are each independently selected from a substituent group consisting of hydrogen, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, and heterocycle lower alkyl optionally substituted by substituent group C, R.sup.D2 and R.sup.D3 are each independently selected from a substituent group consisting of lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, and heterocycle lower alkyl optionally substituted by substituent group C, R.sup.D7, R.sup.D8, and R.sup.D10 are each independently carbocyclic group optionally substituted by substituent group C, or heterocyclic group optionally substituted by substituent group C, R.sup.D5 and R.sup.D6 may be taken together with an adjacent atom to form heterocycle, Y is straight or branched lower alkylene, and Z is a single bond or straight or branched lower alkylene), and R.sup.D5 and R.sup.D6 may be taken together with an adjacent atom to form carbocycle; R.sup.3a and R.sup.6a may be taken together with an adjacent atom to form heterocycle optionally substituted by substituent group D, with a proviso that the following c) is excluded c) R.sup.5a, R.sup.6a, and R.sup.7a are all hydrogens; wherein the substituent group C is chosen from halogen, cyano, hydroxy, carboxy, formyl, amino, oxo, nitro, lower alkyl, lower alkenyl, lower alkynyl, halogeno lower alkyl, lower alkyloxy, lower alkynyloxy, lower alkylthio, hydroxy lower alkyl, carbocyclic group, heterocyclic group, heterocyclic group substituted by oxo, carbocycle lower alkyloxy, carbocycleoxy lower alkyl, carbocycle lower alkyloxy lower alkyl, heterocycle lower alkyloxy, heterocycleoxy lower alkyl, heterocycle lower alkyloxy lower alkyl, halogeno lower alkyloxy, lower alkyloxy lower alkyl, lower alkyloxy lower alkyloxy, lower alkylcarbonyl, lower alkylcarbonyloxy, lower alkyloxycarbonyl, lower alkylamino, lower alkylcarbonylamino, halogeno lower alkyl carbonylamino, lower alkylaminocarbonyl, lower alkylsulfonyl, lower alkylsulfinyl, and lower alkylsulfonylamino; and wherein the substituent is chosen from halogen, cyano, hydroxy, carboxy, formyl, amino, oxo, nitro, lower alkyl, halogeno lower alkyl, lower alkyloxy, carbocycle lower alkyloxy, heterocycle lower alkyloxy, halogeno lower alkyloxy, lower alkyloxy lower alkyl, lower alkyloxy lower alkyloxy, lower alkylcarbonyl, lower alkyloxycarbonyl, lower alkylamino, lower alkylcarbonylamino, lower alkylaminocarbonyl, lower alkylsulfonyl, lower alkylsulfonylamino, carbocyclic group optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, and heterocycle lower alkyl optionally substituted by substituent group C. 2. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.1a is hydrogen, halogen, hydroxy, carboxy, cyano, formyl, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, lower alkyloxy optionally substituted by substituent group C, lower alkenyloxy optionally substituted by substituent group C, lower alkylcarbonyl optionally substituted by substituent group C, lower alkyloxycarbonyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, carbocycleoxy optionally substituted by substituent group C, carbocycleoxycarbonyl optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, heterocycleoxy optionally substituted by substituent group C, heterocycleoxycarbonyl optionally substituted by substituent group C, --Z--N(R.sup.A1)(R.sup.A2), --Z--N(R.sup.A3)--SO.sub.2--(R.sup.A4), --Z--N(R.sup.A7)--C(.dbd.O)--R.sup.A8, --Z--S--R.sup.A9, --Z--SO.sub.2--R.sup.A10, --Z--N(R.sup.A12)--C(.dbd.O)--O--R.sup.A13, --Z--N(R.sup.A20)--C(.dbd.O)--C(.dbd.O)--R.sup.A21, or --Z--B(--OR.sup.A22)(--OR.sup.A23) 3. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.1a is hydrogen, halogen, hydroxy, carboxy, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkyloxy optionally substituted by substituent group C, lower alkylcarbonyl optionally substituted by substituent group C, lower alkyloxycarbonyl optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, --Z--N(R.sup.A1)(R.sup.A2), --Z--N(R.sup.A7)--C(.dbd.O)--R.sup.A8, --Z--N(R.sup.A12)--C(.dbd.O)--O--R.sup.A13, or --Z--B(--OR.sup.A22)(--OR.sup.A23) 4. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.1a is hydrogen, halogen, hydroxy, carboxy, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkyloxy optionally substituted by substituent group C, lower alkylcarbonyl optionally substituted by substituent group C, lower alkyloxycarbonyl optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, or --Z--N(R.sup.A1)(R.sup.A2) 5. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.1a is hydrogen, or carboxy. 6. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.2a is hydrogen, lower alkyl optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, or) --Z--N(R.sup.B9)(R.sup.B10) 7. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.2a is hydrogen or lower alkyl optionally substituted by substituent group C 8. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.3a is hydrogen, lower alkyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C. 9. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.5a, R.sup.6a and R.sup.7a are each independently hydrogen, carboxy, cyano, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, lower alkyl carbonyl optionally substituted by substituent group C, lower alkyl oxycarbonyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, carbocycleoxy lower alkyl optionally substituted by substituent group C, carbocyclecarbonyl optionally substituted by substituent group C, carbocycleoxycarbonyl optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, heterocycleoxy lower alkyl optionally substituted by substituent group C, heterocyclecarbonyl optionally substituted by substituent group C, heterocycleoxycarbonyl optionally substituted by substituent group C, --Y--S--R.sup.D1, --Z--S(.dbd.O)--R.sup.D2, --Z--SO.sub.2--R.sup.D3, --C(.dbd.O)--C(.dbd.O)--R.sup.D4, --C(.dbd.O)--N(R.sup.D5)(R.sup.D6), --Z--C(R.sup.D7)(R.sup.D8)(R.sup.D9), --Z--N(R.sup.D11)--C(.dbd.O)--O--R.sup.D12, or --Z--N(R.sup.D13)--C(.dbd.O)--R.sup.D14 10. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.5a is hydrogen, R.sup.6a is hydrogen, or lower alkyl optionally substituted by substituent group C, and R.sup.7a is lower alkyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, carbocycleoxy lower alkyl optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, or --Z--C(R.sup.D7)(R.sup.D8)(R.sup.D9) 11. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.7a is a group shown below: ##STR01341## 12. The compound according to claim 1, or the pharmaceutically acceptable salt thereof or the solvate thereof, wherein R.sup.1a is hydrogen, or carboxy, R.sup.2a is hydrogen, R.sup.3a is lower alkyl optionally substituted by substituent group C, B.sup.1 is NR.sup.7a, and B.sup.2 is CH.sub.2, and R.sup.7a is a group shown below: ##STR01342## 13. The compound according to claim 1, or a pharmaceutically acceptable salt, or a solvate thereof: wherein, R.sup.1a is hydrogen, halogen, hydroxy, carboxy, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkyloxy optionally substituted by substituent group C, lower alkylcarbonyl optionally substituted by substituent group C, lower alkyloxycarbonyl optionally substituted by substituent group C, heterocyclic group optionally substituted by substituent group C, or --Z--N(R.sup.A1)(R.sup.A2), R.sup.2a is hydrogen, lower alkyl optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, or --Z--N(R.sup.B9)(R.sup.B10), R.sup.3a is hydrogen, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, carbocycleoxy lower alkyl optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, --Z--N(R.sup.C1)--SO.sub.2--R.sup.C2, --Z--N(R.sup.C3)--C(.dbd.O)--R.sup.C4, --Z--N(R.sup.C5)--C(.dbd.O)--O--R.sup.C6, --Z--C(.dbd.O)--N(R.sup.C7)(R.sup.C8), or --Z--N(R.sup.C9)(R.sup.C10), R.sup.3a and R.sup.6a may be taken together with an adjacent atom to form heterocycle optionally substituted by substituent group D, with a proviso that the following c) is excluded c) R.sup.5a, R.sup.6a, and R.sup.7a are all hydrogens. 14. The compound according to claim 1 or a pharmaceutically acceptable salt, or a solvate thereof: wherein, R.sup.1a is hydrogen or carboxy; R.sup.2a is hydrogen or lower alkyl optionally substituted by substituent group C; R.sup.3a is hydrogen, lower alkyl optionally substituted by substituent group C, lower alkenyl optionally substituted by substituent group C, lower alkynyl optionally substituted by substituent group C, carbocyclic group optionally substituted by substituent group C, carbocycle lower alkyl optionally substituted by substituent group C, carbocycleoxy lower alkyl optionally substituted by substituent group C, heterocycle lower alkyl optionally substituted by substituent group C, --Z--N(R.sup.C1)--SO.sub.2--R.sup.C2, --Z--N(R.sup.C3)--C(.dbd.O)--R.sup.C4, --Z--N(R.sup.C5)--C(.dbd.O)--O--R.sup.C6, --Z--C(.dbd.O)--N(R.sup.C7)(R.sup.C8), or --Z--N(R.sup.C9)(R.sup.C10), R.sup.3a and R.sup.6a may be taken together with an adjacent atom to form heterocycle optionally substituted by substituent group D, with a proviso that the following c) is excluded c) R.sup.5a, R.sup.6a, and R.sup.7a are all hydrogens. 15. The compound according to claim 1, or a pharmaceutically acceptable salt, or a solvate thereof; wherein, R.sup.1a is hydrogen or carboxy; R.sup.2a is hydrogen or lower alkyl optionally substituted by substituent group C; R.sup.3a is hydrogen or lower alkyl optionally substituted by substituent group C; R.sup.3a and R.sup.6a may be taken together with an adjacent atom to form heterocycle optionally substituted by substituent group D; with a proviso that the following c) is excluded c) R.sup.5a, R.sup.6a, and R.sup.7a are all hydrogens. 16. The compound according to claim 1, or a pharmaceutically acceptable salt, or a solvate thereof: wherein, R.sup.1a is hydrogen or carboxy; R.sup.2a is hydrogen or lower alkyl optionally substituted by substituent group C; R.sup.3a is hydrogen or lower alkyl optionally substituted by substituent group C; B.sup.1 is NR.sup.7a and B.sup.2 is CHR.sup.6a (wherein, R.sup.7a is carbocyclic group optionally substituted by substituent group C or heterocyclic group optionally substituted by substituent group C) R.sup.3a and R.sup.6a may be taken together with an adjacent atom to form heterocycle optionally substituted by substituent group D. 17. The compound according to claim 1, or a pharmaceutically acceptable salt, or a solvate thereof: wherein, R.sup.1a is hydrogen or carboxy; R.sup.2a is hydrogen; R.sup.3a is hydrogen or lower alkyl optionally substituted by halogen; B.sup.1 is NR.sup.7a and B.sup.2 is CHR.sup.6a; wherein, R.sup.7a is carbocyclic group optionally substituted by substituent group C or heterocyclic group optionally substituted by substituent group C; and Substituent group C: halogen, cyano, hydroxy, carboxy, formyl, amino, oxo, nitro, lower alkyl, lower alkynyl, halogeno lower alkyl, lower alkyloxy, lower alkyamino, halogeno lower alkyloxy, carbocyclic group; and R.sup.3a and R.sup.6a may be taken together with an adjacent atom to form heterocycle. 18. The compound according to claim 13, or a pharmaceutically acceptable salt, or a solvate thereof, wherein R.sup.7a is a tricyclic heterocyclic group optionally substituted by substituent group C; and Substituent group C; halogen, cyano, hydroxy, carboxy, formyl, amino, oxo, nitro, lower alkyl, lower alkynyl, halogeno lower alkyl, lower alkyloxy, lower alkyamino, halogeno lower alkyloxy, carbocyclic group. 19. The compound according to claim 13, or a pharmaceutically acceptable salt, or a solvate thereof wherein R.sup.7a is a tricyclic heterocyclic group optionally substituted by substituent group C; and Substituent group C: halogen, lower alkyl, halogeno lower alkyl, lower alkyloxy. 20. The compound according to claim 13, or a pharmaceutically acceptable salt, or a solvate thereof wherein R.sup.7a is the following group: ##STR01343## wherein R.sup.E6 is independently halogen, cyano, hydroxy, carboxy, formyl, amino, oxo, nitro, lower alkyl, lower alkynyl, halogeno lower alkyl, lower alkyloxy, lower alkyl amino, halogeno lower alkyloxy, carbocyclic group; and m is an integer from 0 to 6. 21. The compound according to claim 20, or a pharmaceutically acceptable salt, or a solvate thereof wherein R.sup.E6 is independently halogen or lower alkyloxy; and m is an integer from 0 to 2. 22. The compound according to claim 13, or a pharmaceutically acceptable salt, or a solvate thereof, wherein, R.sup.6a is hydrogen. 23. The compound according to claim 13, or a pharmaceutically acceptable salt, or a solvate thereof, wherein, R.sup.3a and R.sup.6a are taken together with an adjacent atom to form heterocycle optionally substituted by substituent group D. 24. The compound according to claim 13, or a pharmaceutically acceptable salt, or a solvate thereof, wherein, R.sup.3a and R.sup.6a are taken together with an adjacent atom to form 5- to 7-membered heterocycle optionally substituted by substituent group D. 25. The compound according to claim 23, or a pharmaceutically acceptable salt, or a solvate thereof: wherein P.sup.R is a group selected from the following: --C(.dbd.O)--P.sup.R0, a) --C(.dbd.O)--P.sup.R1, b) --C(.dbd.O)--O--P.sup.R2, g) --C(.dbd.O)--O-L-O--P.sup.R2, i) --CH.sub.2--O--P.sup.R3, j) --CH.sub.2--O-L-O--P.sup.R3, k) --CH.sub.2--O--C(.dbd.O)--P.sup.R3, l) --CH.sub.2--O--C(.dbd.O)--O--P.sup.R3, m) --CH(--CH.sub.3)--O--C(.dbd.O)--O--P.sup.R3, n) --CH.sub.2--O--C(.dbd.O)--N(--K)--P.sup.R3, o) 26. The compound according to claim 13, or a pharmaceutically acceptable salt, or a solvate thereof: wherein P.sup.R is a group selected from the following: --C(.dbd.O)--P.sup.R0, a) --C(.dbd.O)--P.sup.R1, b) --CH.sub.2--O--C(.dbd.O)--P.sup.R3, l) --CH.sub.2--O--C(.dbd.O)--O--P.sup.R3. m) 27. The compound according to claim 13, or a pharmaceutically acceptable salt, or a solvate thereof: wherein P.sup.R is a group selected from the following: --C(.dbd.O)--P.sup.R0, a) --C(.dbd.O)--P.sup.R1, b) --CH.sub.2--O--C(.dbd.O)--P.sup.R3, l) --CH.sub.2--O--C(.dbd.O)--O--P.sup.R3, m) wherein: P.sup.R0 is lower alkyl; P.sup.R1 is carbocyclic group or heterocyclic group; and P.sup.R3 is lower alkyl, carbocyclic group or heterocyclic group. 28. The compound according to claim 1, or a pharmaceutically acceptable salt, or a solvate thereof: wherein: P.sup.R is a group selected from the following: --C(.dbd.O)--P.sup.R0, a) --C(.dbd.O)--P.sup.R1, b) --CH.sub.2--O--C(.dbd.O)--P.sup.R3, l) --CH.sub.2--O--C(.dbd.O)--O--P.sup.R3, m) wherein: P.sup.R0 is lower alkyl; P.sup.R1 is carbocyclic group or heterocyclic group; P.sup.R3 is lower alkyl, carbocyclic group or heterocyclic group; R.sup.1a is hydrogen or carboxy; R.sup.2a is hydrogen or lower alkyl optionally substituted by substituent group C; R.sup.3a is hydrogen or lower alkyl optionally substituted by substituent group C; B.sup.1 is NR.sup.7a and B.sup.2 is CHR.sup.6a wherein, R.sup.7a is carbocyclic group optionally substituted by substituent group C or heterocyclic group optionally substituted by substituent group C; wherein substituent group C is chosen from halogen, cyano, hydroxy, carboxy, formyl, amino, oxo, nitro, lower alkyl, lower alkynyl, halogeno lower alkyl, lower alkyloxy, lower alkyamino, halogeno lower alkyloxy, carbocyclic group; wherein R.sup.3a and R.sup.6a may be taken together with an adjacent atom to form heterocycle optionally substituted by substituent group D; and 29. The compound according to claim 28, or a pharmaceutically acceptable salt, or a solvate thereof: wherein R.sup.7a is the following group: ##STR01344## wherein, R.sup.E6 is independently halogen, cyano, hydroxy, carboxy, formyl, amino, oxo, nitro, lower alkyl, lower alkynyl, halogeno lower alkyl, lower alkyloxy, lower alkyl amino, halogeno lower alkyloxy, carbocyclic group; and m is an integer from 0 to 6. 30. A pharmaceutical composition containing a compound according to any one of claims 1-8, 10, 11, 12 and 16-29, or a pharmaceutically acceptable salt thereof or a solvate thereof. 31. The pharmaceutical composition according to claim 30 which exhibits anti influenza activity. 32. The pharmaceutical composition according to claim 30 which exhibits cap-dependent endonuclease inhibitory activity.