US2013012708A1PendingUtilityA1

Heterocyclic compounds and thrombopoietin receptor activators

Assignee: NISSAN CHEMICAL IND LTDPriority: Jun 6, 2003Filed: Sep 13, 2012Published: Jan 10, 2013
Est. expiryJun 6, 2023(expired)· nominal 20-yr term from priority
A61P 7/02A61P 7/00A61P 7/04A61P 43/00A61P 9/00A61P 9/10A61P 35/00A61P 7/06C07D 231/18C07D 403/12C07D 409/12C07D 333/32C07D 295/192C07D 417/12C07D 333/38A61P 1/06
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Claims

Abstract

A compound represented by the formula (1): wherein A is a nitrogen atom or CR 4 , B is an oxygen atom, a sulfur atom or NR 9 (provided that when A is a nitrogen atom, B is not NH), R 1 is a C 2-14 aryl group, L 1 is a bond, CR 10 R 11 , an oxygen atom, a sulfur atom or NR 12 , X is OR 13 , SR 13 or NR 14 NR 15 , R 2 is a hydrogen atom, a formyl group, a C 1-10 alkyl group or the like, L 2 is a bond or the like, L 3 is a bond, CR 17 R 18 , an oxygen atom, a sulfur atom or NR 19 , L 4 is a bond, CR 20 R 21 , an oxygen atom, a sulfur atom or NR 22 , Y is an oxygen atom, a sulfur atom or NR 23 , and R 3 is a C 2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

Claims

exact text as granted — not AI-modified
1 . A compound represented by the formula (1) 
       
         
           
           
               
               
           
         
       
       wherein A is a nitrogen atom or CR 4  (wherein R 4  is a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted with a C 2-6  alkenyl group or a C 2-6  alkynyl group), a thiol group (the thiol group may be substituted with a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group or a C 1-10  alkylcarbonyl group), an amino group (the amino group may be substituted with one or two C 2-6  alkenyl groups or one or two C 2-6  alkynyl groups), a formyl group, a halogen atom, a nitro group, a cyano group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkylcarbonylamino group, a mono- or di-C 1-10  alkylamino group, a C 1-10  alkoxy group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkylcarbonylamino group, the mono- or di-C 1-10  alkylamino group and the C 1-10  alkoxy group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono-di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group), a C 2-14  aryloxy group (the C 2-14  aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, C 2-14  aryl group and a C 2-14  aryloxy group), SO 2 R 5 , SOR 5  or COR 5  (wherein R 5  is a hydroxyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group and the C 1-10  alkoxy group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group), a C 2-14  aryloxy group (the C 2-14  aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C oi- 1 alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-24  aryl group and a C 2-14  aryloxy group) or NR 6 R 7  (wherein each of R 6  and R 7  is independently a hydrogen atom, a hydroxyl group, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkoxycarbonyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14 , aryl group and a C 2-14  aryloxy group), or R 6  and R 7  mean, together with each other, —(CH 2 ) m1 -E-(CH 2 ) m2 — (wherein E is an oxygen atom, sulfur-atom, CR 26 R 27  (wherein each of R 26  and R 27  is independently a hydrogen atom, a C 1-10  alkyl group, a C 2-14  aryl group, a C 1-10  alkoxy group, a C 2-14  aryloxy groUp, a hydroxyl group or a protected hydroxyl group) or NR 8  (wherein R 8  is a hydrogen atom, a hydroxyl group, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkoxycarbonyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)), and each of m1 and m2 is independently an integer of from 0 to 5 provided that m1+m2 is 3, 4 or 5)))),
 B is an oxygen atom, a sulfur atom or NR 9  (wherein R 9  is a hydrogen atom, a hydroxyl group, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkoxycarbonyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group) or a C 2-14  aryloxy group (the C 2-14  aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)) (provided that when A is a nitrogen atom, B is not NH), 
 R 1  is a C 2-14  aryl group (the C 2-14  aryl group may be substituted with one or more substituents selected from the group consisting of: a halogen atom, a carboxyl group, a nitro group, OCHO, a cyano group, a hydroxyl group, a protected hydroxyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyl group, the C 1-10  alkylcarbonyloxy group and the C 1-10  alkoxycarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group), a thiol group and an amino group (the thiol group and the amino group may be optionally substituted with one or two substituents selected from the group consisting of: a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group and a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)))), 
 L 1  is a bond, CR 10 R 11  (wherein each of R 10  and R 11  is independently a hydrogen atom or a C 1-6  alkyl group (the C 1-6  alkyl group may be substituted with one or more halogen atoms)), an oxygen atom, a sulfur atom or NR 12  (wherein R 12  is a hydrogen atom, a hydroxyl group, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkoxycarbonyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)), 
 X is OR 13 , SR 13  or NR 14 R 15  (wherein R 13  is a hydrogen atom, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group or a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)), and each of R 14  and R 15  is independently a hydrogen atom, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substittited with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)), 
 R 2  is a hydrogen atom, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonyloxy group, (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkoxycarbonyl group, the C 1-10  alkylcarbonyloxy group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-24  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group), 
 L 2  is a bond, CR 34 R 35  (wherein each of R 34  and R 35  is independently a hydrogen atom or a C 1-6  alkyl group (the C 1-6  alkyl group may be substituted with one or more halogen atoms)), an oxygen atom, a sulfur atom or NR 15  (wherein R 16  is a hydrogen atom, a hydroxyl group, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-30  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkoxycarbonyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-24  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-34  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)), 
 L 3  is a bond, CR 17 R 18  (wherein each of R 17  and R 18  is independently a hydrogen atom, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group (the C 2-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a c 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkyloarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)), an oxygen atom, a sulfur atom or NR 19  (wherein R 19  is a hydrogen atom, a hydroxyl group, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkoxycarbonyl group, the C 1-10  alkoxy group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)), 
 L 4  is a bond, CR 20 R 21  (wherein each of R 20  and R 21  is independently a hydrogen atom, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)), an oxygen atom, a sulfur atom or NR 22  (wherein R 22  is a hydrogen atom, a hydroxyl group, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkyldarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkoxycarbonyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)), 
 Y is an oxygen atom, a sulfur atom or NR 23  (wherein R 23  is a hydrogen atom, a hydroxyl group, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkoxycarbonyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino is group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)), and 
 R 3  is a C 2-14  aryl group (the C 2-14  aryl group may be substituted with one or more substituents independently represented by —W 1  (CW 2 W 3 ) m W 4  (wherein W 1  is (CR 24 R 25 ) n  (wherein each of R 24  and R 25  is independently a hydrogen atom or a C 1-6  alkyl group, (the C 1-6  alkyl group may be substituted with one or more halogen atoms), and n is 0, 1, 2 or 3), an oxygen atom, a sulfur atom or NR 36  (wherein R 36  is a hydrogen atom, a C 1-6  alkyl group, formyl group or a C 1-6  alkylcarbonyl group), each of W 2  and W 3  is independently a hydrogen atom or a C 1-3  alkyl group (the C 1-3  alkyl group may be substituted with one or more halogen atoms), m is 0, 1, 2 or 3, and W 4  is a hydroxyl group, a thiol group, an amino group, a formyl group, a halogen atom, a nitro group, a cyano group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkylcarbonylamino group, a mono- or di-C 1-10  alkylamino group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkylcarbonylamino group and the mono- or di-C 1-10  alkylamino group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, a amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-34  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a thiol group, a phosphonic acid group, a sulfonic acid group, a tetrazole group, a C 2-14  aryl group and a C 2-14  aryloxy group), SO 2 R 28 , SOR 28 , COR 28  (wherein R 28  is a hydroxyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group and the C 1-10  alkoxy group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)), a C 2-14  aryl group, a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group) or NR 29 R 30  (wherein each of R 29  and R 30  is independently a hydrogen atom, a hydroxyl group, a formyl group, a cyano group, a C 1-10  alkyl group, a C 2-6  alkenyl group, a C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkoxycarbonyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group), or R 29  and R 30 , together with each other means —(CH 2 ) m3 -G-(CH 2 ) m4 — (wherein G is an oxygen atom, a sulfur atom, a CR 31 R 32  (wherein each of R 31  and R 32  is independently a hydrogen atom, a C 1-10  alkyl group, a C 2-14  aryl group, a C 1-10  alkoxy group, a C 2-14  aryloxy group, hydroxyl group or a protected hydroxyl group) or NR 33  (wherein R 33  is a hydrogen atom, a hydroxyl group, a formyl group, a C 1-10  alkyl group, a C 2-6  alkenyl group, C 2-6  alkynyl group, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonyl group (the C 1-10  alkyl group, the C 2-6  alkenyl group, the C 2-6  alkynyl group, the C 1-10  alkoxy group, the C 1-10  alkylcarbonyloxy group, the C 1-10  alkoxycarbonyl group and the C 1-10  alkylcarbonyl group may be optionally substituted with one or more substituents selected from the group consisting of: a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group (the C 2-14  aryl group and the C 2-14  aryloxy group may be substituted with one or more C 1-6  alkyl groups (the C 1-6  alkyl group may be substituted with one or more halogen atoms) or one or more halogen atoms)) or a C 2-14  aryl group (the C 2-14  aryl group may be optionally substituted with one or more substituents selected from the group consisting of: a C 1-10  alkyl group (the C 1-10  alkyl group may be substituted with one or more halogen atoms), a C 2-6  alkenyl group, a C 2-6  alkynyl group, a carboxyl group, a nitro group, a cyano group, a halogen atom, a C 1-10  alkoxy group, a C 1-10  alkylcarbonyl group, a C 1-10  alkylcarbonyloxy group, a C 1-10  alkoxycarbonyl group, a C 1-10  alkylcarbonylamino group, an amino group, a mono- or di-C 1-10  alkylamino group, a hydroxyl group, a protected hydroxyl group, a C 2-14  aryl group and a C 2-14  aryloxy group)), and each of m3 and m4 is independently an integer of from 0 to 5, provided that m3+m4 is 3, 4 or 5))), a tetrazole group, or a phosphonic acid group)), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

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