1. A compound represented by the following formula (I), a salt thereof, or a solvate thereof
in the formula,
R1 means a basic group which may have a substituent,
R2 means
hydrogen atom,
halogen atom,
carboxy group,
a group represented by the following formula
(in the formula, R21 and R22 each independently represents hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an aryl group having from 6 to 10 carbon atoms),
an alkyl group having from 1 to 6 carbon atoms,
an alkenyl group having from 2 to 6 carbon atoms,
an alkynyl group having from 2 to 6 carbon atoms,
an acyl group having from 2 to 7 carbon atoms,
an alkoxycarbonyl group having from 2 to 7 carbon atoms,
a cycloalkyl group having from 3 to 6 carbon atoms,
a cycloalkenyl group having 5 or 6 carbon atoms,
a cycloalkylalkyl group having from 4 to 12 carbon atoms,
an aryl group having from 6 to 10 carbon atoms,
an aralkyl group having from 7 to 12 carbon atoms,
a monocyclic, bicyclic or spiro cyclic heterocyclic group having from 2 to 10 carbon atoms (contains from 1 to 4 hetero atoms of 1 or more species selected from the group consisting of nitrogen atom, oxygen atom and sulfur atom),
a heteroaryl group having from 3 to 10 carbon atoms, or
a heteroarylalkyl group having from 3 to 12 carbon atoms,
wherein when R2 is an alkyl group, an alkenyl group, an alkynyl group, an acyl group or an alkoxycarbonyl group, these may have 1 or more groups of 1 or more species selected from substituent group 2-1 as the substituent;
substituent group 2-1:
halogen atom,
amino group,
imino group,
nitro group,
hydroxy group,
mercapto group,
carboxy group,
cyano group,
sulfo group,
a dialkyl phosphoryl group,
a group represented by the following formula
(in the formula, R211 and R221 each independently represents hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an aryl group having from 6 to 10 carbon atoms),
an alkoxy group having from 1 to 6 carbon atoms,
an alkylthio group having from 1 to 6 carbon atoms,
an acyl group having from 2 to 7 carbon atoms,
an alkoxycarbonyl group having from 2 to 7 carbon atoms,
a cycloalkyl group having from 3 to 6 carbon atoms,
an aryl group having from 6 to 10 carbon atoms, and
an arylthio group having from 6 to 10 carbon atoms
wherein amino group of the substituent group 2-1 may have 1 or 2 groups, as the substituent, selected from the group consisting of formyl group, an alkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, a mercaptoalkyl group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, an alkoxycarbonyl group having from 2 to 7 carbon atoms, a cycloalkyl group having from 3 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, an aromatic heterocyclic group, an alkylsulfonyl group having from 1 to 6 carbon atoms and an arylsulfonyl group having from 6 to 10 carbon atoms, in addition, when said amino group has 2 substituents, they may be bonded together to form a cyclic structure;
hydroxy group of the substituent group 2-1 or mercapto group of the substituent group 2-1 may have a substituent selected from the group consisting of an alkyl group having from 1 to 6 carbon atoms, an aminoalkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, a mercaptoalkyl group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, a cycloalkyl group having from 3 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms and an aromatic heterocyclic group;
when R2 is a cycloalkyl group, these may have 1 or more groups of 1 or more species selected from substituent group 2-2 as the substituent;
substituent group 2-2:
halogen atom,
amino group,
imino group,
nitro group,
hydroxy group,
mercapto group,
carboxy group,
cyano group,
sulfo group,
a group represented by the following formula
(in the formula, R212 and R222 each independently represents hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an aryl group having from 6 to 10 carbon atoms),
an alkoxy group having from 1 to 6 carbon atoms,
an alkylthio group having from 1 to 6 carbon atoms,
an acyl group having from 2 to 7 carbon atoms, and
an alkoxycarbonyl group having from 2 to 7 carbon atoms;
amino group of the substituent group 2-2 may have 1 or 2 groups, as the substituent, selected from the group consisting of formyl group, an alkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, a mercaptoalkyl group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, an alkoxycarbonyl group having from 2 to 7 carbon atoms, a cycloalkyl group having from 3 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, an aromatic heterocyclic group, an alkylsulfonyl group having from 1 to 6 carbon atoms and an arylsulfonyl group having from 6 to 10 carbon atoms, in addition, when said amino group has 2 substituents, they may be bonded together to form a cyclic structure;
when R2 is an aryl group, an aralkyl group, a heteroaryl group or a heteroarylalkyl group, these may have 1 or more groups of 1 or more species selected from substituent group 2-3 as the substituent;
substituent group 2-3:
halogen atom,
amino group,
imino group,
nitro group,
hydroxy group,
mercapto group,
carboxy group,
cyano group,
sulfo group,
a group represented by the following formula
(in the formula, R213 and R223 each independently represents hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an aryl group having from 6 to 10 carbon atoms), an alkoxy group having from 1 to 6 carbon atoms, an alkylthio group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, an alkoxycarbonyl group having from 2 to 7 carbon atoms, an aralkyloxy group having from 7 to 12 carbon atoms, an aralkyloxycarbonyl group having from 8 to 15 carbon atoms, an aryl group and a monocyclic, bicyclic or spiro cyclic heterocyclic group having from 2 to 10 carbon atoms (contains from 1 to 4 hetero atoms of 1 or more species selected from the group consisting of nitrogen atom, oxygen atom and sulfur atom);
amino group of the substituent group 2-3 may have 1 or 2 groups, as the substituent, selected from the group consisting of formyl group, an alkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, a mercaptoalkyl group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, an alkoxycarbonyl group having from 2 to 7 carbon atoms, a cycloalkyl group having from 3 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, an aromatic heterocyclic group, an alkylsulfonyl group having from 1 to 6 carbon atoms and an arylsulfonyl group having from 6 to 10 carbon atoms, in addition, when said amino group has 2 substituents, they may be bonded together to form a cyclic structure;
when R2 is a heterocyclic group, it may have 1 or 2 groups selected from the next substituent group 2-4 as the substituent;
substituent group 2-4:
halogen atom,
amino group,
hydroxy group,
mercapto group,
carboxy group,
sulfo group,
a group represented by the following formula
(in the formula, R214 and R224 each independently represents hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an aryl group having from 6 to 10 carbon atoms),
an alkyl group having from 1 to 6 carbon atoms,
an alkenyl group having from 2 to 6 carbon atoms,
an alkynyl group having from 2 to 6 carbon atoms,
an alkoxy group having from 1 to 6 carbon atoms,
an alkylthio group having from 1 to 6 carbon atoms,
a halogenoalkyl group having from 1 to 6 carbon atoms,
an acyl group having from 2 to 7 carbon atoms,
an alkoxycarbonyl group having from 2 to 7 carbon atoms, and
an aryl group having from 6 to 10 carbon atoms;
wherein amino group of the substituent group 2-4 may have 1 or 2 groups, as the substituent, selected from the group consisting of formyl group, an alkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, a mercaptoalkyl group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, an alkoxycarbonyl group having from 2 to 7 carbon atoms, a cycloalkyl group having from 3 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, a monocyclic, bicyclic or spiro cyclic heterocyclic group having from 2 to 10 carbon atoms (contains from 1 to 4 hetero atoms of 1 or more species selected from the group consisting of nitrogen atom, oxygen atom and sulfur atom), an aromatic heterocyclic group, an alkylsulfonyl group having from 1 to 6 carbon atoms and an arylsulfonyl group having from 6 to 10 carbon atoms, in addition, when said amino group has 2 substituents, they may be bonded together to form a cyclic structure;
in addition, R1 and R2 may together form a cyclic structure including the carbon atoms to which these are bonded, wherein this ring contains 1 or 2 hetero atoms of 1 or more species selected from the group consisting of nitrogen atom, oxygen atom and sulfur atom, and the structural moiety to be formed herein may be saturated or unsaturated;
R3 means
hydrogen atom,
halogen atom,
amino group,
hydroxy group,
mercapto group,
nitro group,
cyano group,
formyl group,
carboxy group,
a group represented by the following formula
(in the formula, R31 and R32 each independently represents hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an aryl group having from 6 to 10 carbon atoms),
an alkyl group having from 1 to 6 carbon atoms,
an alkenyl group having from 2 to 6 carbon atoms,
an alkynyl group having from 2 to 6 carbon atoms,
an alkoxy group having from 1 to 6 carbon atoms,
an alkylthio group having from 1 to 6 carbon atoms
an acyl group having from 2 to 5 carbon atoms,
an alkoxycarbonyl group having from 2 to 5 carbon atoms,
a cycloalkyl group having from 3 to 7 carbon atoms,
a cycloalkenyl group having from 4 to 7 carbon atoms,
an aryl group having from 6 to 10 carbon atoms,
an aralkyl group having from 7 to 12 carbon atoms,
a heteroaryl group having from 3 to 10 carbon atoms;
wherein said amino group, said hydroxy group or said mercapto group may be protected by a protecting group;
when R3 is an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an acyl group, an alkoxycarbonyl group, a cycloalkyl group, a cycloalkenyl group, an aryl group, an aralkyl group or a heteroaryl group, these may have 1 or more groups of 1 or more species selected from substituent group 3-1 as the substituent;
substituent group 3-1:
amino group,
hydroxy group,
mercapto group,
halogen atom,
an alkoxy group having from 1 to 6 carbon atoms,
an alkylthio group having from 1 to 6 carbon atoms,
an acyl group having from 2 to 5 carbon atoms, and
an alkoxycarbonyl group having from 2 to 5 carbon atoms;
amino group of the substituent group 3-1 may have 1 or 2 groups, as the substituent, selected from the group consisting of formyl group, an alkyl group having from 1 to 6 carbon atoms, a cycloalkyl group having from 3 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aromatic heterocyclic group, an acyl group having from 2 to 5 carbon atoms and an alkoxycarbonyl group having from 2 to 5 carbon atoms, wherein when said amino group has 2 substituents, they may be bonded together to form a cyclic structure;
in addition, R2 and R3 may together form a polymethylene chain structure and form a 5-membered or 6-membered cyclic structure by including the carbon atoms to which R2 and R3 are to be bonded, this polymethylene chain may contain 1 or 2 hetero atoms of 1 or more species selected from the group consisting of nitrogen atom, oxygen atom and sulfur atom, and the polymethylene chain formed herein may have 1 or more groups of 1 or more species selected from substituent group 3-2 as the substituent;
substituent group 3-2:
amino group,
hydroxy group,
mercapto group,
halogen atom,
an alkoxy group having from 1 to 6 carbon atoms,
an alkylthio group having from 1 to 6 carbon atoms,
an acyl group having from 2 to 5 carbon atoms, and
an alkoxycarbonyl group having from 2 to 5 carbon atoms;
amino group of the substituent group 3-2 may have 1 or 2 groups, as the substituent, selected from the group consisting of formyl group, an alkyl group having from 1 to 6 carbon atoms, a cycloalkyl group having from 1 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aromatic heterocyclic group, an acyl group having from 2 to 5 carbon atoms and an alkoxycarbonyl group having from 2 to 5 carbon atoms, wherein when said amino group has 2 substituents, they may be bonded together to form a cyclic structure; and
R4 means
hydrogen atom,
halogen atom,
amino group,
hydroxy group,
mercapto group,
nitro group,
cyano group,
formyl group,
carboxy group,
a group represented by the following formula
(in the formula, R31 and R32 each independently represents hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an aryl group having from 6 to 10 carbon atoms),
an alkyl group having from 1 to 4 carbon atoms,
an cyclic alkyl group having from 3 to 8 carbon atoms,
an aryl group having from 6 to 10 carbon atoms,
a heteroaryl group having from 5 to 9 carbon atoms,
an alkynyl group having from 2 to 6 carbon atoms, or
a group represented by
(in the formula, R41 and R42 each independently represents hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an alkoxy group having from 1 to 6 carbon atoms, or both may together form an exomethylene structure, and this exomethylene structure may further have an alkyl group having from 1 to 6 carbon atoms, an alkoxy group having from 1 to 6 carbon atoms or a halogenoalkyl group having from 1 to 6 carbon atoms, as a substituent, and
R43 means hydrogen atom, a halogen atom, hydroxy group, mercapto group, nitrile group, nitro group, carboxy group, an alkoxycarbonyl group having from 2 to 7 carbon atoms, an alkylaminocarbonyl group having from 2 to 7 carbon atoms, an arylaminocarbonyl group having from 7 to 11 carbon atoms, a cycloalkylaminocarbonyl group having from 4 to 7 carbon atoms, an aralkylaminocarbonyl group having from 8 to 12 carbon atoms, an alkyl group having from 1 to 6 carbon atoms, a halogenoalkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, an aminoalkyl group having from 1 to 6 carbon atoms, an alkoxy group having from 1 to 6 carbon atoms, a cycloalkyl group having from 3 to 8 carbon atoms, a cycloalkyloxy group having from 3 to 8 carbon atoms, an aralkyl group having from 7 to 11 carbon atoms, or an aralkyloxy group having from 7 to 11 carbon atoms);
when R4 is an alkyl group, a cyclic alkyl group, an aryl group or a heteroaryl group, and when R43 is an alkyl group, these may have 1 or more groups of 1 or more species selected from substituent group 4 as the substituent;
substituent group 4:
halogen atom,
amino group,
nitro group,
hydroxy group,
mercapto group,
carboxy group,
cyano group,
sulfo group,
a group represented by the following formula
(in the formula, R411 and R421 each independently mean hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an aryl group having from 6 to 10 carbon atoms),
an alkoxy group having from 1 to 6 carbon atoms,
an alkylthio group having from 1 to 6 carbon atoms,
an acyl group having from 2 to 7 carbon atoms,
an alkoxycarbonyl group having from 2 to 7 carbon atoms,
an aralkyloxy group having from 7 to 12 carbon atoms,
an aralkyloxycarbonyl group having from 8 to 15 carbon atoms,
an aryl group having from 6 to 10 carbon atoms, and
a monocyclic, bicyclic or Spiro cyclic heterocyclic group having from 2 to 10 carbon atoms (contains from 1 to 4 hetero atoms of 1 or more species selected from the group consisting of nitrogen atom, oxygen atom and sulfur atom);
amino group of the substituent group 4 may have 1 or 2 groups, as the substituent, selected from the group consisting of formyl group, an alkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, a mercaptoalkyl group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, an alkoxycarbonyl group having from 2 to 7 carbon atoms, a cycloalkyl group having from 3 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, an aromatic heterocyclic group, an alkylsulfonyl group having from 1 to 6 carbon atoms and an arylsulfonyl group having from 6 to 10 carbon atoms, wherein when said amino group has 2 substituents, they may be bonded together to form a cyclic structure;
hydroxy group or mercapto group of the substituent group 4 may have a substituent selected from the group consisting of an alkyl group having from 1 to 6 carbon atoms, an aminoalkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, a mercaptoalkyl group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, a cycloalkyl group having from 3 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms and an aromatic heterocyclic group, wherein when R4 is an alkynyl group, it may have an alkyl group having from 1 to 6 carbon atoms, an alkoxyalkyl group having from 1 to 6 carbon atoms, a halogenoalkyl group having from 1 to 6 carbon atoms or carboxy group as a substituent;
X1 and X2 each independently mean
nitrogen atom or
carbon atom which may be substituted with
a halogen atom,
an alkoxy group having from 1 to 6 carbon atoms,
an alkyl group having from 1 to 6 carbon atoms which may have a substituent,
an ester group, wherein either one of X1 and X2 is nitrogen atom;
wherein the substituent of alkyl group is 1 or 1 or more groups selected from the following group of substituents;
halogen atom,
amino group,
nitro group,
hydroxy group,
mercapto group,
carboxy group,
cyano group,
an alkoxy group having from 1 to 6 carbon atoms,
an alkylthio group having from 1 to 6 carbon atoms,
an acyl group having from 2 to 7 carbon atoms,
an alkoxycarbonyl group having from 2 to 7 carbon atoms,
a cycloalkyl group having from 3 to 6 carbon atoms, and
an aryl group having from 6 to 10 carbon atoms;
when the substituents on carbon atoms are esters, these may be
an alkyl ester having from 1 to 6 carbon atoms,
an aryl ester having from 6 to 10 carbon atoms,
or an aralkyl ester consisting of an alkyl group having from 1 to 6 carbon atoms and an aryl group having from 6 to 10 carbon atoms;
in addition, the aryl moiety of these aryl esters and aralkyl groups may be substituted with 1 or 1 or more groups selected from the following group of substituents;
halogen atom,
amino group,
nitro group,
hydroxy group,
mercapto group,
carboxy group,
cyano group,
an alkyl group having from 1 to 6 carbon atoms,
an alkoxy group having from 1 to 6 carbon atoms,
an alkylthio group having from 1 to 6 carbon atoms,
an acyl group having from 2 to 7 carbon atoms,
an alkoxycarbonyl group having from 2 to 7 carbon atoms,
a cycloalkyl group having from 3 to 6 carbon atoms, and
an aryl group having from 6 to 10 carbon atoms.
2. The compound, a salt thereof, or a solvate thereof described in claim 1, wherein the basic group of R1 is
(1) an amino substituted alkyl group having from 1 to 6 carbon atoms, which may have a substituent,
(2) an amino substituted cyclic alkyl group having from 3 to 6 carbon atoms, which may have a substituent,
(3) an aminocycloalkenyl group having from 3 to 6 carbon atoms, which may have a substituent,
(4) an amino substituted aralkyl group wherein the binding region with the bicyclic nucleus is an aromatic ring, which may have a substituent,
(5) an aminoalkyl substituted amino group having from 1 to 6 carbon atoms, which may have a substituent,
(6) an amino substituted cyclic alkylamino group having from 3 to 6 carbon atoms, which may have a substituent,
(7) an aminocycloalkenylamino group having from 3 to 6 carbon atoms, which may have a substituent,
(8) an amino substituted aralkylamino group wherein the binding region with the bicyclic nucleus is an aromatic ring, which may have a substituent, or
(9) a nitrogen-containing heterocyclic substituent, which may have a substituent;
wherein the amino group as the basic nature expressing group in the substituents of (1) to (8) may have 1 or 2 (may be the same or different when 2) of the substituents selected from the following substituent group 1-1;
substituent group 1-1:
an alkyl group having from 1 to 6 carbon atoms, an alkenyl group having from 2 to 6 carbon atoms, an alkynyl group having from 2 to 6 carbon atoms, an alkoxycarbonyl group having from 2 to 7 carbon atoms, a cycloalkyl group having from 3 to 10 carbon atoms, a cycloalkenyl group having from 4 to 10 carbon atoms, and a group derived from an amino acid, a dipeptide or a polypeptide consisting of 3 to 5 amino acids;
also, when the substituent selected from the substituent group 1-1 is an alkyl group, an alkenyl group, an alkynyl group, an alkoxycarbonyl group, a cycloalkyl group or a cycloalkenyl group, these may have 1 or more of 1 or more groups selected from substituent group 1-1-1;
substituent group 1-1-1: hydroxy group, mercapto group, a halogen atom, an alkoxy group having from 1 to 6 carbon atoms, an alkylthio group having from 1 to 6 carbon atoms and a cycloalkyl group having from 3 to 10 carbon atoms;
in addition, the nitrogen-containing heterocyclic substituent of (9) preferably uses a carbon atom as the binding position, is saturated or partially saturated, and is a monocyclic, bicyclic or spiro cyclic heterocyclic group having from 2 to 10 carbon atoms (contains from 1 to 4 hetero atoms of 1 or more species selected from the group consisting of nitrogen atom, oxygen atom and sulfur atom), and the substituent on this heterocyclic group may be selected from substituent group 1-2;
substituent group 1-2: a halogen atom, amino group, hydroxy group, oxo group, a group represented by the following formula
(in the formula, R111 and R121 each independently represents hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an aryl group having from 6 to 10 carbon atoms), an alkyl group having from 1 to 6 carbon atoms, an aminoalkyl group having from 1 to 8 carbon atoms, an aminocycloalkyl group having from 3 to 8 carbon atoms, an alkoxy group having from 1 to 6 carbon atoms, an alkylthio group having from 1 to 6 carbon atoms, a halogenoalkyl group having from 1 to 6 carbon atoms and an alkylamino group having from 1 to 6 carbon atoms;
wherein the alkyl moiety of the alkyl group, alkylamino group, cycloalkylamino group, alkoxy group, alkylthio group, halogenoalkyl group or aminoalkyl group of the substituent group 1-2 may have 1 or more groups of 1 or more species selected from substituent group 1-2-1;
substituent group 1-2-1: a halogen atom, hydroxy group, an alkyl group having from 1 to 6 carbon atoms, an alkoxy group having from 1 to 6 carbon atoms, an alkoxycarbonyl group having from 2 to 7 carbon atoms, an alkylcarbonylamino group having from 2 to 7 carbon atoms and an aryl group having from 6 to 10 carbon atoms;
wherein the amino group moiety of the amino group, aminoalkyl group, aminocycloalkyl group and alkylamino group of the substituent group 1-2 may be protected with a protecting group, and also may have 1 or 2 of alkyl groups having from 1 to 6 carbon atoms (may have 1 or more groups of 1 or more species selected from the group of groups consisting of hydroxy group, a halogen atom, and an alkoxy group and alkylthio group having from 1 to 6 carbon atoms) as the substituent, and also, an amino acid, a dipeptide or a polypeptide consisting of 3 to 5 amino acids may be bonded thereto.
3. The compound, a salt thereof, or a solvate thereof described in claim 2, wherein R1 is a nitrogen-containing heterocyclic group which may have a substituent.
4. The compound, a salt thereof, or a solvate thereof described in claim 3, wherein R1 is a nitrogen-containing heterocyclic group which may have a substituent, and said nitrogen-containing heterocyclic group is a saturate or partially saturated nitrogen-containing heterocyclic group.
5. The compound, a salt thereof or a solvate thereof described in claim 4, wherein R1 is a group represented by the following formula;
in the formula, Xa means oxygen atom, sulfur atom, a substituent or NR52,
R51 and R52 each independently means hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a halogenoalkyl group having from 1 to 6 carbon atoms or a cycloalkyl group having from 3 to 6 carbon atoms,
the substituent Q means a substituent represented by the following formula,
\u2014(CR71CR72)n2\u2014N(R61R62)\u2003\u2003Formula 75
b means an integer of 0, 1 or 2,
n1 means an integer of 0 or 1,
n2 means an integer of 0, 1 or 2,
R61 and R62 each independently means hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or a halogenoalkyl group having from 1 to 6 carbon atoms, or a group derived from an amino acid, a dipeptide or a polypeptide consisting of 3 to 5 amino acids,
R71 and R72 each independently means hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a halogenoalkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 3 to 6 carbon atoms, an aminoalkyl group having from 1 to 6 carbon atoms, an alkoxyalkyl group having from 2 to 12 carbon atoms, a cycloalkyl group having from 3 to 6 carbon atoms, a phenyl group which may have a substituent or a heteroaryl group having from 3 to 10 carbon atoms which may have a substituent,
and the dotted line means that said binding region may form a double bond.
6. The compound, a salt thereof, or a solvate thereof described in any one of claims 1 to 5, wherein R2 is an aryl group having from 6 to 10 carbon atoms, which may have a substituent, or a monocyclic, bicyclic or spiro cyclic heterocyclic group having from 2 to 10 carbon atoms (contains from 1 to 4 hetero atoms of 1 or more species selected from the group consisting of nitrogen atom, oxygen atom and sulfur atom).
7. The compound, a salt thereof, or a solvate thereof described in claim 6, wherein R2 is a group represented by the following formula;
(in the formula, Xb means oxygen atom, sulfur atom, a substituent or NR8, wherein R8 means hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or a halogenoalkyl group having from 1 to 6 carbon atoms, and the substituent Y1 has the same meaning as described in the aforementioned substituent group 2-2).
8. The compound, a salt thereof, or a solvate thereof described in claim 7, wherein R3 is a halogen atom, amino group, hydroxy group, mercapto group, an alkyl group having from 1 to 4 carbon atoms which may have a substituent, an alkoxy group having from 1 to 6 carbon atoms which may have a substituent, an alkylthio group having from 1 to 6 carbon atoms, an acyl group having from 2 to 5 carbon atoms or an alkoxycarbonyl group having from 2 to 5 carbon atoms;
wherein the amino group among them may have 1 or 2 groups, as the substituent, selected from the group consisting of formyl group, an alkyl group having from 1 to 6 carbon atoms, a cycloalkyl group having from 1 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, a heteroaryl group having from 3 to 10 carbon atoms, an acyl group having from 2 to 5 carbon atoms and an alkoxycarbonyl group having from 2 to 5 carbon atoms, and when said amino group has 2 substituents, they may be bonded together to form a cyclic structure.
9. The compound, a salt thereof, or a solvate thereof described in claim 7, wherein R3 is a group represented by the following formula;
(in the formula, R9 means hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a cycloalkyl group having from 3 to 7 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms or an aromatic heterocyclic group, and the substituent Y2 means amino group, hydroxy group, mercapto group, a halogen atom, an alkoxy group having from 1 to 6 carbon atoms, an alkylthio group having from 1 to 6 carbon atoms, an acyl group having from 2 to 5 carbon atoms or an alkoxycarbonyl group having from 2 to 5 carbon atoms, wherein the amino group among them may have 1 or 2 groups, as the substituent, selected from the group consisting of formyl group, an alkyl group having from 1 to 6 carbon atoms, a cycloalkyl group having from 1 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aromatic heterocyclic group, an acyl group having from 2 to 5 carbon atoms and an alkoxycarbonyl group having from 2 to 5 carbon atoms, and when said amino group has 2 substituents, they may be bonded together to form a cyclic structure).
10. The compound, a salt thereof, or a solvate thereof described in claim 7, wherein R3 is a group represented by the following formula;
(in the formula, R9 means hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a cycloalkyl group having from 3 to 7 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms or an aromatic heterocyclic group, and the substituent Y2 means amino group, hydroxy group, mercapto group, a halogen atom, an alkoxy group having from 1 to 6 carbon atoms, an alkylthio group having from 1 to 6 carbon atoms, an acyl group having from 2 to 5 carbon atoms or an alkoxycarbonyl group having from 2 to 5 carbon atoms, wherein the amino group among them may have 1 or 2 groups, as the substituent, selected from the group consisting of formyl group, an alkyl group having from 1 to 6 carbon atoms, a cycloalkyl group having from 1 to 6 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aromatic heterocyclic group, an acyl group having from 2 to 5 carbon atoms and an alkoxycarbonyl group having from 2 to 5 carbon atoms, and when said amino group has 2 substituents, they may be bonded together to form a cyclic structure).
11. The compound, a salt thereof, or a solvate thereof described in claim 9 or 10, wherein Y2 is a halogen atom, alkoxy group having from 1 to 6 carbon atoms, hydroxy group or amino group, and R9 is hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a cycloalkyl group having from 3 to 7 carbon atoms, an aryl group having from 6 to 10 carbon atoms or an aralkyl group having from 7 to 12 carbon atoms.
12. The compound described in claim 9 or 10, wherein Y2 is fluorine atom, chlorine atom, methoxy group or hydroxy group, and R9 is hydrogen atom, methyl group, ethyl group or isopropyl group.
13. The compound, a salt thereof, or a solvate thereof described in any one of claims 1 to 12, wherein R4 is an alkyl group having from 1 to 4 carbon atoms which may have a substituent, or a compound represented by the following formula;
(R41, R42 and R43 are as defined in the foregoing).
14. The compound, a salt thereof, or a solvate thereof described in any one of claims 1 to 12, wherein R4 is a substituent having a structure represented by the following formula;
(R41, R42 and R43 are as defined in the foregoing).
15. A compound, a salt thereof, or a solvate thereof, which is a compound represented by the formula (I) having a combination in which
R2 is an aryl group;
R1 is a cyclic substituent having a saturated or partially saturated substituent;
R3 is an alkyl group having from 1 to 3 carbon atoms;
R4 is a substituent selected from the group consisting of (1) an alkyl or alkylene group having from 2 to 5 carbon atoms which may take a branched chain form, (2) a cyclic alkyl group having 3 or 4 carbon atoms, (3) an alkyl group having from 2 to 5 carbon atoms having fluorine atom or chlorine atom, which may take a branched chain form, (4) an alkoxyalkyl group having from 2 to 5 carbon atoms, and (6) a substituted benzyloxyethyl group which may have 1 or 2 methyl groups on the ethyl group.
16. A compound, a salt thereof, or a solvate thereof, which is a compound represented by the formula (I) having a combination in which
R2 is an aryl group;
R1 is a saturated or partially saturated nitrogen-containing heterocyclic group substituted with amino group, an alkylamino group or a dialkylamino group;
R3 is an alkyl group having from 1 to 3 carbon atoms;
R4 is a substituent selected from the group consisting of (1) an alkyl or alkylene group having from 2 to 5 carbon atoms which may take a branched chain form, (2) a cyclic alkyl group having 3 or 4 carbon atoms, (3) an alkyl group having from 2 to 5 carbon atoms having fluorine atom or chlorine atom, which may take a branched chain form, (4) an alkoxyalkyl group having from 2 to 5 carbon atoms, and (6) a substituted benzyloxyethyl group which may have 1 or 2 methyl groups on the ethyl group.
17. A compound, a salt thereof, or a solvate thereof, which is a compound represented by the formula (I) having a combination in which
R2 is phenyl group;
R1 is pyrrolidinyl group substituted with amino group, an alkylamino group or a dialkylamino group;
R3 is methyl group;
R4 is a substituent selected from the group consisting of ethyl group, isopropyl group, normal butyl group, tertiary butyl group, cyclopropyl group, propylen-2-yl group, methoxymethyl group, fluoromethyl group, 2-chloroethyl group, 2-hydroxyethyl group, 1,1-dimethyl-2-hydroxyethyl group, 2-benzyloxyethyl group, 2-benzyloxy-1,1-dimethyl-ethyl group and 2-(4-fluorophenylmethyl)oxyethyl group.
18. (canceled)
19. A medicine which comprises the compound, a salt thereof, or a solvate thereof described in any one of claims 1 to 17.
20. An infection treating agent which comprises the compound, a salt thereof, or a solvate thereof described in any one of claims 1 to 17.
21. An antifungal agent which comprises the compound, a salt thereof, or a solvate thereof described in any one of claims 1 to 17.
22. A method for treating an infection, which uses the compound, a salt thereof, or a solvate thereof described in any one of claims 1 to 17.
23. Use of the compound, a salt thereof or a solvate thereof described in any one of claims 1 to 17 for infection treatment.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
1. A filtration device comprising:
a first fabric layer suitable for adsorbing a liquid hydrocarbon, said first fabric layer comprising:
a plurality of relatively shorter hydrophobic and lipophilic synthetic fibers, said relatively shorter hydrophobic and lipophilic synthetic fibers having rough, delustered surfaces, wherein said plurality of relatively shorter hydrophobic and lipophilic synthetic fibers comprises a mixture of polyester fibers and nylon fibers;
a plurality of relatively longer hydrophobic and lipophilic synthetic fibers, said relatively longer hydrophobic and lipophilic synthetic fibers having rough, delustered surfaces, said relatively longer hydrophobic and lipophilic synthetic fibers and said rough delustered surfaces binding said plurality of relatively shorter hydrophobic and lipophilic synthetic fibers and said plurality of relatively longer hydrophobic and lipophilic fibers into a wadded mass, said wadded mass including a plurality of interstitial spaces, wherein said plurality of relatively longer hydrophobic and lipophilic synthetic fibers comprises a mixture of polyester fibers and nylon fibers; and
a second fabric layer joined to said first fabric layer; and
a granular component embedded between said first and second layers, said granular component having desirable adsorbent, absorbent, filtering or treatment characteristics, said granular component being a treatment component chosen from the group of treatment components consisting of:
inorganic elements, compounds and mixtures;
mined ores, including clays, metal bearing and organic humates;
organic compounds; and
organometallic compounds and organic immobilized compounds on an organic or inorganic substrate.
2. The device of claim 1, wherein said granular component is adhered to at least one of said first and second layers.
3. The device of claim 1, wherein said second layer is composed of material identical to said first layer.
4. The device of claim 1, wherein said second layer is composed of synthetic fibers different from those of said first layer.
5. The device of claim 4, wherein said second layer is composed of polyester.
6. The device of claim 1, wherein said granular component comprises activated carbon.
7. The device of claim 1, wherein said granular component comprises zeolite.
8. A filtration device suitable for adsorbing a liquid hydrocarbon product, said filtration device comprising at least two fabric layers, at least one of said fabric layers comprising:
a plurality of relatively shorter hydrophobic and lipophilic synthetic fibers, a majority of said plurality of relatively shorter hydrophobic and lipophilic synthetic fibers having lengths ranging from about 10 mm to about 20 mm, wherein said plurality of relatively shorter hydrophobic and lipophilic synthetic fibers comprises a mixture of polyester fibers and nylon fibers; and
a plurality of relatively longer hydrophobic and lipophilic synthetic fibers, a majority of said plurality of relatively longer hydrophobic and lipophilic synthetic fibers having lengths ranging from about 70 mm to about 90 mm, said relatively longer hydrophobic and lipophilic synthetic fibers binding said plurality of relatively shorter hydrophobic and lipophilic synthetic fibers and said plurality of relatively longer hydrophobic and lipophilic fibers, wherein said plurality of relatively longer hydrophobic and lipophilic synthetic fibers comprises a mixture of polyester fibers and nylon fibers; and
a granular component embedded between said two fabric layers, said granular component having desirable adsorbent, absorbent, filtering or treatment characteristics, said granular component being a treatment component chosen from the group of treatment components consisting of:
inorganic elements, compounds and mixtures;
mined ores, including clays, metal bearing and organic humates;
organic compounds; and
organometallic compounds and organic immobilized compounds on an organic or inorganic substrate.
9. The device of claim 8, wherein said granular component is adhered to at least one of said fabric layers.
10. The device of claim 8, wherein said two layers are composed of identical material.
11. The device of claim 1, wherein one said fabric layer is composed of synthetic fibers different from said other fabric layer.
12. The device of claim 11, wherein said synthetic fibers are polyester.
13. The device of claim 8, wherein said granular component comprises activated carbon.
14. The device of claim 8, wherein said granular component comprises zeolite.
15. The device of claim 8, wherein each mixture of polyester fibers and nylon fibers comprises substantially more polyester than nylon.
16. The device of claim 15, wherein a ratio of polyester fibers to nylon fibers ranges from about 2:1 to about 4:1.
17. The device of claim 8, wherein said plurality of relatively shorter hydrophobic and lipophilic fibers and said plurality of relatively longer hydrophobic and lipophilic fibers have rough, delustered surfaces, said rough, delustered surfaces providing fiber-to-fiber traction that enhances a cohesiveness of said wadded mass, said rough, delustered surfaces further enhancing a volume of interstitial space within said wadded mass, said interstitial space enabling said sorbent mass to also absorb said liquid hydrocarbon, the absorption occurring within said interstitial spaces.
18. The device of claim 8, wherein said relatively shorter hydrophobic and lipophilic fibers and said relatively longer hydrophobic and lipophilic fibers comprise fibers ranging in length from about 5 mm to about 100 mm.
19. The device of claim 8, wherein said wadded mass is capable of adsorbing an amount of liquid hydrocarbon up to about 25 times a weight of said wadded mass.
20. A filtration device comprising at least two fabric layers, at least one of said fabric layers comprising a delustered fiber sorbent suitable for adsorbing an organic liquid, said delustered fiber sorbent comprising:
a plurality of relatively shorter delustered hydrophobic and lipophilic synthetic fibers, wherein said plurality of relatively shorter delustered hydrophobic and lipophilic synthetic fibers comprises a mixture of polyester fibers and nylon fibers, and
a plurality of relatively longer delustered hydrophobic and lipophilic synthetic fibers, wherein said plurality of relatively longer delustered hydrophobic and lipophilic synthetic fibers comprises a mixture of polyester fibers and nylon fibers; and
a granular component embedded between said two fabric layers, said granular component having desirable adsorbent, absorbent, filtering or treatment characteristics, said granular component being a treatment component chosen from the group of treatment components consisting of:
inorganic elements, compounds and mixtures;
mined ores, including clays, metal bearing and organic humates;
organic compounds; and
organometallic compounds and organic immobilized compounds on an organic or inorganic substrate.
21. The device of claim 20, wherein:
said plurality of relatively shorter hydrophobic and lipophilic synthetic fibers includes a majority of relatively shorter hydrophobic and lipophilic synthetic fibers having lengths ranging from about 10 mm to about 20 mm; and
said plurality of relatively longer hydrophobic and lipophilic synthetic fibers includes a majority of relatively longer hydrophobic and lipophilic synthetic fibers having lengths ranging from about 70 mm to about 90 mm, said relatively longer hydrophobic and lipophilic synthetic fibers binding said plurality of relatively shorter hydrophobic and lipophilic synthetic fibers and said plurality of relatively longer hydrophobic and lipophilic synthetic fibers into a wadded mass.
22. The device of claim 20, wherein said plurality of delustered hydrophobic and lipophilic synthetic fibers comprises:
a majority of relatively shorter hydrophobic and lipophilic synthetic fibers; and
a minority of relatively longer hydrophobic and lipophilic synthetic fibers.
23. The device of claim 20, further comprising a plurality of hydrophilic fibers, such that said delustered fiber sorbent comprises substantially more delustered hydrophobic and lipophilic synthetic fibers than hydrophilic fibers.
24. The device of claim 20, wherein said granular component comprises activated carbon.
25. The device of claim 20, wherein said granular component comprises zeolite.
26. A delustered fiber filter suitable for removing an organic liquid from a mass of water, said delustered fiber filter comprising at least two fabric layers, at least on of said layers comprising a plurality of delustered hydrophobic and lipophilic synthetic fibers, wherein said plurality of delustered hydrophobic and lipophilic synthetic fibers comprises a mixture of polyester fibers and nylon fibers and a mixture of relatively shorter fibers and relatively longer fibers; and
a granular component embedded between said two layers, said granular component having desirable adsorbent, absorbent, filtering or treatment characteristics, said granular component being a treatment component chosen from the group of treatment components consisting of:
inorganic elements, compounds and mixtures;
mined ores, including clays, metal bearing and organic humates;
organic compounds; and
organometallic compounds and organic immobilized compounds on an organic or inorganic substrate.
27. The delustered fiber filter of claim 26, wherein said plurality of delustered hydrophobic and lipophilic synthetic fibers further comprises a majority of relatively shorter hydrophobic and lipophilic synthetic fibers and a minority of relatively longer hydrophobic and lipophilic synthetic fibers.
28. The delustered fiber filter of claim 26, further comprising a plurality of hydrophilic fibers, such that said delustered fiber filter comprises substantially more delustered hydrophobic and lipophilic synthetic fibers than hydrophilic fibers.
29. The delustered fiber filter of claim 26, wherein said delustered fiber filter does not substantially impede a flow of water through said delustered fiber filter.
30. The device of claim 26, wherein said granular component comprises activated carbon.
31. The device of claim 26, wherein said granular component comprises zeolite.