Ena nucleic acid drugs modifying splicing in mrna precursor
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Abstract
Oligonucleotides having a nucleotide sequence complementary to nucleotide numbers such as 2571-2607, 2578-2592, 2571-2592, 2573-2592, 2578-2596, 2578-2601 or 2575-2592 of the dystrophin cDNA (Gene Bank accession No. NM_004006.1) and therapeutic agents for muscular dystrophy comprising such oligonucleotides.
-
Citations
111 Claims
-
1-59. -59. (canceled)
-
60. A method of treating muscular dystrophy in a patient in need thereof, said method comprising administering to the patient an effective amount of a pharmaceutical composition comprising an antisense oligonucleotide compound capable of inducing skipping of any one of the exons of the dystrophin gene or a pharmacologically acceptable salt thereof, provided that at least one of the nucleotides constituting the compound has a 2′
- -O, 4′
-C-alkylene group. - View Dependent Claims (61, 62)
-
61. The method according to claim 60, wherein muscular dystrophy is Duchenne muscular dystrophy.
-
62. The method according to claim 61, wherein the total number of amino acids in the open reading frame of the dystrophin gene in the patient will be a multiple of 3 when exon 19, 41, 45, 46, 44, 50, 55, 51 or 53 of the dystrophin gene has been skipped.
-
61. The method according to claim 60, wherein muscular dystrophy is Duchenne muscular dystrophy.
- -O, 4′
-
63. An antisense oligonucleotide compound complementary to a nucleotide sequence in any one of the region of the nucleotides Nos. 6691-6727, 7554-7757, 6921-6992, 6555-6673, 7447-7551, 7907-8068, 8275-8458, 2571-2601 or 6125-6161 of dystrophin cDNA (Gene Bank accession No. NM—
- 004006.1) or a pharmaceutically acceptable salt thereof, provided that at least one of the nucleotides constituting the compound complementary to a nucleotide sequence in the region of the nucleotides No. 2571-2601 of dystrophin cDNA (Gene Bank accession No. NM—
004006.1) has a 2′
-O, 4′
-C-alkylene group. - View Dependent Claims (64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111)
-
64. The compound according to claim 63 or a pharmacologically acceptable salt thereof, having the nucleotide sequence as shown in any one of SEQ ID NOS:
- 15, 14, 16, 17, 64, 56-63, 65, 66, 87, 88, 18-22, 30-39, 40-46, 67-78, 47-55, 2-7 or 10-13.
-
65. The compound according to claim 63 or a pharmacologically acceptable salt thereof, wherein at least one of the sugars and/or the phosphates constituting the oligonucleotide is modified.
-
66. The compound according to claim 65 or a pharmacologically acceptable salt thereof, wherein the sugar constituting the oligonucleotide is D-ribofuranose and the modification of the sugar is modification of the hydroxyl group at position 2′
- of D-ribofuranose.
-
67. The compound according to claim 66 or a pharmacologically acceptable salt thereof, wherein the modification of the sugar is 2′
- -O-alkylation and/or 2′
-O4′
-C-alkylenation of the D-ribofuranose.
- -O-alkylation and/or 2′
-
68. The compound according to claim 65 or a pharmacologically acceptable salt thereof, wherein the modification of the phosphate is thioation of the phosphate group.
-
69. The compound according to claim 63 which is represented by any one of formulae (III′
- ), (IV′
), (XV″
), (IX″
), (X″
), (XI″
), (XII″
), (XIII″
), (XIV″
), (V′
) (VI′
) (VII′
) (I″
), (II″
), (III″
), (IV″
), (V″
), (XVI″
), (XVII″
), (XVIII″
), (XIX″
), (XX″
), (XXI″
), (VI″
), (VII″
), (VIII″
), (I), (I′
) and (II′
), or a pharmacologically acceptable salt thereof,wherein said formulae are defined as follows;
BT′
3—
BM′
3—
BB′
3
(III′
)where BT′
3 is a group represented by any one of (3a′
) to (3c′
);
HO—
,
(3a′
)
HO-Bc-, or
(3b′
)
HO-Bg-Bc-
(3c′
)where Bg is a group represented by formula (G1) or (G2); and
Bc is a group represented by formula (C1) or (C2);
where X is individually and independently a group represented by formula (X1) or (X2);
Y is individually and independently a hydrogen atom, a hydroxyl group or an alkoxy group with 1-6 carbon atoms; and
Z is individually and independently a single bond or an alkylene group with 1-5 carbon atoms;
BM′
3 is a group represented by formula (3′
);
-Bc-Bg-Bc-Bt-Bg-Bc-Bc-Bc-Ba—
Ba—
(3′
)where Bg and Bc are as defined above;
Ba is a group represented by formula (A1) or (A2); and
Bt is a group represented by formula (U1) or (T2);
where X and Y are as defined above;
BB′
3 is a group represented by any one of (32a′
) to (32i′
);
—
CH2CH2OH,
(32a′
)
-Bt-CH2CH2OH,
(32b′
)
-Bt-Bg-CH2CH2OH,
(32c′
)
-Bt-Bg-Bc-CH2CH2OH,
(32d′
)
-Bt-Bg-Bc-Bc-CH2CH2OH,
(32e′
)
-Bt-Bg-Bc-Bc-Ba—
CH2CH2OH,
(32f′
)
-Bt-Bg-Bc-Bc-Ba-Bt-CH2CH2OH,
(32g′
)
-Bt-Bg-Bc-Bc-Ba-Bt-Bc-CH2CH2OH, or
(32h′
)
-Bt-Bg-Bc-Bc-Ba-Bt-Bc-Bc-CH2CH2OH,
(32i′
)where Bg, Ba, Bt and Bc are as described above;
provided that at least one of the nucleosides constituting the compound represented by formula (III′
) has a 2′
-O, 4′
-C-alkylene group;
BT′
4—
BM′
4—
BB′
4
(IV′
)where BT′
4 is a group represented by any one of (4a′
) to (4m′
);
HO—
,
(4a′
)
HO—
Ba—
,
(4b′
)
HO—
Ba—
Ba—
,
(4c′
)
HO-Bc-Ba—
Ba—
,
(4d′
)
HO—
Ba-Bc-Ba—
Ba—
,
(4e′
)
HO-Bg-Ba-Bc-Ba—
Ba—
,
(4f′
)
HO-Bt-Bg-Ba-Bc-Ba—
Ba—
,
(4g′
)
HO-Bc-Bt-Bg-Ba-Bc-Ba—
Ba—
,
(4h′
)
HO-Bt-Bc-Bt-Bg-Ba-Bc-Ba—
Ba—
,
(4j′
)
HO-Bt-Bt-Bc-Bt-Bg-Ba-Bc-Ba—
Ba—
,
(4k′
)
HO-Bg-Bt-Bt-Bc-Bt-Bg-Ba-Bc-Ba—
Ba—
, or
(4l′
)
HO-Bt-Bg-Bt-Bt-Bc-Bt-Bg-Ba-Bc-Ba—
Ba—
(4m′
)BM′
4 is a group represented by formula (4′
);
-Bc-Ba-Bg-Bt-Bt-Bt-Bg-
(4′
)BB′
4 is a group represented by any one of (42a′
) to (42l′
);
—
CH2CH2OH,
(42a′
)
-Bc-CH2CH2OH,
(42b′
)
-Bc-Bc-CH2CH2OH,
(42c′
)
-Bc-Bc-Bg-CH2CH2OH,
(42d′
)
-Bc-Bc-Bg-Bc-CH2CH2OH,
(42e′
)
-Bc-Bc-Bg-Bc-Bt-CH2CH2OH,
(42f′
)
-Bc-Bc-Bg-Bc-Bt-Bg-CH2CH2OH,
(42g′
)
-Bc-Bc-Bg-Bc-Bt-Bg-Bc-CH2CH2OH,
(42h′
)
-Bc-Bc-Bg-Bc-Bt-Bg-Bc-Bc-CH2CH2OH,
(42i′
)
-Bc-Bc-Bg-Bc-Bt-Bg-Bc-Bc-Bc-CH2CH2OH,
(42j′
)
-Bc-Bc-Bg-Bc-Bt-Bg-Bc-Bc-Bc-Ba—
CH2CH2OH, or
(42k′
)
-Bc-Bc-Bg-Bc-Bt-Bg-Bc-Bc-Bc-Ba—
Ba—
CH2CH2OH
(42l′
)where Bg, Ba, Bt and Bc are as described above;
provided that at least one of the nucleosides constituting the compound represented by formula (IV′
) has a 2′
-O, 4′
-C-alkylene group;
BT″
15—
BM″
15—
BB″
15
(XV′
)where BT″
15 is a group represented by any one of the following (15a″
) to (15j″
);
HO—
,
(15a″
)
HO-Bt-,
(15b″
)
HO-Bc-Bt-,
(15c″
)
HO-Bt-Bc-Bt-,
(15d″
)
HO-Bt-Bt-Bc-Bt-,
(15e″
)
HO-Bt-Bt-Bt-Bc-Bt-,
(15f″
)
HO—
Ba-Bt-Bt-Bt-Bc-Bt-,
(15g″
)
HO-Bc-Ba-Bt-Bt-Bt-Bc-Bt-,
(15h″
)
HO-Bg-Bc-Ba-Bt-Bt-Bt-Bc-Bt-, or
(15i″
)
HO-Bg-Bg-Bc-Ba-Bt-Bt-Bt-Bc-Bt-
(15j″
)BM″
15 is a group represented by formula (15″
);
—
Ba-Bg-Bt-Bt-Bt-Bg-Bg-Ba-Bg-
(15″
)BB″
15 is a group represented by any one of (115a″
) to (115j″
);
—
CH2CH2OH,
(115a″
)
—
Ba—
CH2CH2OH,
(115b″
)
—
Ba-Bt-CH2CH2OH,
(115c″
)
—
Ba-Bt-Bg-CH2CH2OH,
(115d″
)
—
Ba-Bt-Bg-Bg-CH2CH2OH,
(115e″
)
—
Ba-Bt-Bg-Bg-Bc-CH2CH2OH,
(115f″
)
—
Ba-Bt-Bg-Bg-Bc-Ba—
CH2CH2OH,
(115g″
)
—
Ba-Bt-Bg-Bg-Bc-Ba-Bg-CH2CH2OH,
(115h″
)
—
Ba-Bt-Bg-Bg-Bc-Ba-Bg-Bt-CH2CH2OH, or
(115i″
)
—
Ba-Bt-Bg-Bg-Bc-Ba-Bg-Bt-Bt-CH2CH2OH
(115j″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (XV″
) has 2″
-O, 4″
-C-alkylene group;
BT″
9—
BM″
9—
BB″
9
(IX″
)where BT″
9 is a group represented by any one of (9a″
) to (9n″
);
D-,
(9a″
)
D-Bg-,
(9b″
)
D-Ba-Bg-,
(9c″
)
D-Bg-Ba-Bg-,
(9d″
)
D-Ba-Bg-Ba-Bg-,
(9e″
)
D-Bc-Ba-Bg-Ba-Bg-,
(9f″
)
D-Bc-Bc-Ba-Bg-Ba-Bg-,
(9g″
)
D-Ba-Bc-Bc-Ba-Bg-Ba-Bg-,
(9h″
)
D-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-,
(9i″
)
D-Bt-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-,
(9j″
)
D-Bg-Bt-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-,
(9k″
)
D-Bt-Bg-Bt-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-,
(9l″
)
D-Bg-Bt-Bg-Bt-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-, or
(9m″
)
D-Bt-Bg-Bt-Bg-Bt-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-
(9n″
)BM″
9 is a group represented by formula (9″
);
-Bt-Ba—
Ba-Bc-Ba-Bg-Bt-
(9″
)BB″
9 is a group represented by any one of (109a″
) to (109l″
);
—
CH2CH2OH,
(109a″
)
-Bc-CH2CH2OH,
(109b″
)
-Bc-Bt-CH2CH2OH,
(109c″
)
-Bc-Bt-Bg-CH2CH2OH,
(109d″
)
-Bc-Bt-Bg-Ba—
CH2CH2OH,
(109e″
)
-Bc-Bt-Bg-Ba-Bg-CH2CH2OH,
(109f″
)
-Bc-Bt-Bg-Ba-Bg-Bt-CH2CH2OH,
(109g″
)
-Bc-Bt-Bg-Ba-Bg-Bt-Ba—
CH2CH2OH,
(109h″
)
-Bc-Bt-Bg-Ba-Bg-Bt-Ba-Bg-CH2CH2OH,
(109i″
)
-Bc-Bt-Bg-Ba-Bg-Bt-Ba-Bg-Bg-CH2CH2OH,
(109j″
)
-Bc-Bt-Bg-Ba-Bg-Bt-Ba-Bg-Bg-Ba—
CH2CH2OH, or
(109k″
)
-Bc-Bt-Bg-Ba-Bg-Bt-Ba-Bg-Bg-Ba-Bg-CH2CH2OH
(109l″
)where Bg, Ba, Bt and Bc are as defined above; and
D is HO—
or Ph-wherein Ph- is a group represented by formula;
provided that at least one of the nucleosides constituting the compound represented by formula (IX″
) has 2″
-O, 4″
-C-alkylene group;
BT″
10—
BM″
10—
BB″
10
(X″
)where BT″
10 is a group represented by any one of (10a″
) to (10e″
);
D-,
(10a″
)
D-Bt-,
(10b″
)
D-Bg-Bt-,
(10c″
)
D-Bg-Bg-Bt-, or
(10d″
)
D-Ba-Bg-Bg-Bt-
(10e″
)BM″
10 is a group represented by formula (10″
);
-Bt-Bg-Bt-Bg-Bt-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-Bt-Ba—
Ba—
(10″
)BB″
10 is a group represented by any one of (110a″
) to (110e″
);
—
CH2CH2OH,
(110a″
)
-Bc-CH2CH2OH,
(110b″
)
-Bc-Ba—
CH2CH2OH,
(110c″
)
-Bc-Ba-Bg-CH2CH2OH, or
(110d″
)
-Bc-Ba-Bg-Bt-CH2CH2OH
(110e″
)where Bg, Ba, Bt, Bc and D are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (X″
) has 2″
-O, 4″
-C-alkylene group;
BT″
11—
BM″
11—
BB″
11
(XI″
)where BT″
11 is a group represented by any one of (11a″
) to (11j″
);
D-,
(11a″
)
D-Bc-,
(11b″
)
D-Ba-Bc-,
(11c″
)
D-Bc-Ba-Bc-,
(11d″
)
D-Bc-Bc-Ba-Bc-,
(11e″
)
D-Ba-Bc-Bc-Ba-Bc-,
(11f″
)
D-Ba—
Ba-Bc-Bc-Ba-Bc-,
(11g″
)
D-Bt-Ba—
Ba-Bc-Bc-Ba-Bc-,
(11h″
)
D-Bg-Bt-Ba—
Ba-Bc-Bc-Ba-Bc-, or
(11i″
)
D-Ba-Bg-Bt-Ba—
Ba-Bc-Bc-Ba-Bc-
(11j″
)BM″
11 is a group represented by formula (11″
);
—
Ba-Bg-Bg-Bt-Bt-Bg-Bt-Bg-Bt-Bc-Ba—
(11″
)BB″
11 is a group represented by any one of (111a″
) to (111j″
);
—
CH2CH2OH,
(111a″
)
-Bc-CH2CH2OH,
(111b″
)
-Bc-Bc-CH2CH2OH,
(111c″
)
-Bc-Bc-Ba—
CH2CH2OH,
(111d″
)
-Bc-Bc-Ba-Bg-CH2CH2OH,
(111e″
)
-Bc-Bc-Ba-Bg-Ba—
CH2CH2OH,
(111f″
)
-Bc-Bc-Ba-Bg-Ba-Bg-CH2CH2OH,
(111g″
)
-Bc-Bc-Ba-Bg-Ba-Bg-Bt-CH2CH2OH,
(111h″
)
-Bc-Bc-Ba-Bg-Ba-Bg-Bt-Ba—
CH2CH2OH, or
(111i″
)
-Bc-Bc-Ba-Bg-Ba-Bg-Bt-Ba—
Ba—
CH2CH2OH
(111j″
)where Bg, Ba, Bt, Bc and D are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (XI″
) has 2″
-O, 4″
-C-alkylene group;
BT″
12—
BM″
12—
BB″
12
(X()where BT″
12 is a group represented by any one of (12a″
) to (12j″
);
D-,
(12a″
)
D-Bt-,
(12b″
)
D-Ba-Bt-,
(12c″
)
D-Bc-Ba-Bt-,
(12d″
)
D-Bc-Bc-Ba-Bt-,
(12e″
)
D-Ba-Bc-Bc-Ba-Bt-,
(12f″
)
D-Bc-Ba-Bc-Bc-Ba-Bt-,
(12g″
)
D-Bc-Bc-Ba-Bc-Bc-Ba-Bt-,
(12h″
)
D-Bc-Bc-Bc-Ba-Bc-Bc-Ba-Bt-, or
(12i″
)
D-Ba-Bc-Bc-Bc-Ba-Bc-Bc-Ba-Bt-
(12j″
)BM″
12 is a group represented by formula (12″
);
-Bc-Ba-Bc-Bc-Bc-Bt-Bc-Bt-Bg-Bt-Bg-
(12″
)BB″
12 is a group represented by any one of (112a″
)˜
(112j″
);
—
CH2CH2OH,
(112a″
)
—
Ba—
CH2CH2OH,
(112b″
)
—
Ba-Bt-CH2CH2OH,
(112c″
)
—
Ba-Bt-Bt-CH2CH2OH,
(112d″
)
—
Ba-Bt-Bt-Bt-CH2CH2OH,
(112e″
)
—
Ba-Bt-Bt-Bt-Bt-CH2CH2OH,
(112f″
)
—
Ba-Bt-Bt-Bt-Bt-Ba—
CH2CH2OH,
(112g″
)
—
Ba-Bt-Bt-Bt-Bt-Ba-Bt-CH2CH2OH,
(112h″
)
—
Ba-Bt-Bt-Bt-Bt-Ba-Bt-Ba—
CH2CH2OH, or
(112i″
)
—
Ba-Bt-Bt-Bt-Bt-Ba-Bt-Ba—
Ba—
CH2CH2OH
(112j″
)where Bg, Ba, Bt, Bc and D are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (XII″
) has 2″
-O, 4″
-C-alkylene group;
BT″
13—
BM″
13—
BB″
13
(XIII″
)where BT″
13 is a group represented by any one of (13a″
) to (13k″
);
HO—
,
(13a″
)
HO-Bc-,
(13b″
)
HO-Bt-Bc-,
(13c″
)
HO-Bg-Bt-Bc-,
(13d″
)
HO-Bg-Bg-Bt-Bc-,
(13e″
)
HO—
Ba-Bg-Bg-Bt-Bc-,
(13f″
)
HO—
Ba—
Ba-Bg-Bg-Bt-Bc-,
(13g″
)
HO-Bc-Ba—
Ba-Bg-Bg-Bt-Bc-,
(13h″
)
HO-Bt-Bc-Ba—
Ba-Bg-Bg-Bt-Bc-,
(13i″
)
HO-Bc-Bt-Bc-Ba—
Ba-Bg-Bg-Bt-Bc-, or
(13j″
)
HO-Bc-Bc-Bt-Bc-Ba—
Ba-Bg-Bg-Bt-Bc-,
(13k″
)BM″
13 is a group represented by formula (13″
);
—
Ba-Bc-Bc-Bc-Ba-Bc-Bc-Ba-Bt-Bc-
(13″
)where Bg, Ba, Bt and Bc are as defined above;
BB″
13 is a group represented by (113a″
)
—
CH2CH2OH
(113a″
)provided that at least one of the nucleosides constituting the compound represented by formula (XIII″
) has 2″
-O, 4″
-C-alkylene group;
BT″
14—
BM″
14—
BB″
14
(XIV″
)where BT″
14 is a group represented by any one of (14a″
) to (14q″
);
HO—
,
(14a″
)
—
HO—
Ba—
,
(14b″
)
HO—
Ba—
Ba—
,
(14c″
)
HO-Bg-Ba—
Ba—
,
(14d″
)
HO—
Ba-Bg-Ba—
Ba—
,
(14e″
)
HO-Bg-Ba-Bg-Ba—
Ba—
,
(14f″
)
HO—
Ba-Bg-Ba-Bg-Ba—
Ba—
,
(14g″
)
HO-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
,
(14h″
)
HO-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
,
(14i″
)
HO—
Ba-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
,
(14j″
)
HO—
Ba—
Ba-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
,
(14k″
)
HO-Bc-Ba—
Ba-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
,
(14l″
)
HO-Bt-Bc-Ba—
Ba-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
,
(14m″
)
HO—
Ba-Bt-Bc-Ba—
Ba-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
,
(14n″
)
HO-Bg-Ba-Bt-Bc-Ba—
Ba-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
,
(14o″
)
HO-Bt-Bg-Ba-Bt-Bc-Ba—
Ba-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
, or
(14p″
)
HO-Bt-Bt-Bg-Ba-Bt-Bc-Ba—
Ba-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
(14q″
)BM″
14 is a group represented by formula (14″
);
—
Ba-Bg-Bc-Bc-
(14″
)BB″
14 is a group represented by any one of (114a″
) to (114o″
);
—
CH2CH2OH,
(114a″
)
—
Ba—
CH2CH2OH,
(114b″
)
—
Ba-Bg-CH2CH2OH,
(114c″
)
—
Ba-Bg-Bt-CH2CH2OH,
(114d″
)
—
Ba-Bg-Bt-Bc-CH2CH2OH,
(114e″
)
—
Ba-Bg-Bt-Bc-Bg-CH2CH2OH,
(114f″
)
—
Ba-Bg-Bt-Bc-Bg-Bg-CH2CH2OH,
(114g″
)
—
Ba-Bg-Bt-Bc-Bg-Bg-Bt-CH2CH2OH,
(114h″
)
—
Ba-Bg-Bt-Bc-Bg-Bg-Bt-Ba—
CH2CH2OH,
(114i″
)
—
Ba-Bg-Bt-Bc-Bg-Bg-Bt-Ba—
Ba—
CH2CH2OH,
(114j″
)
—
Ba-Bg-Bt-Bc-Bg-Bg-Bt-Ba—
Ba-Bg-CH2CH2OH,
(114k″
)
—
Ba-Bg-Bt-Bc-Bg-Bg-Bt-Ba—
Ba-Bg-Bt-CH2CH2OH,
(114l″
)
—
Ba-Bg-Bt-Bc-Bg-Bg-Bt-Ba—
Ba-Bg-Bt-Bt-CH2CH2OH,
(114m″
)
—
Ba-Bg-Bt-Bc-Bg-Bg-Bt-Ba—
Ba-Bg-Bt-Bt-Bc-CH2CH2OH, or
(114n″
)
—
Ba-Bg-Bt-Bc-Bg-Bg-Bt-Ba—
Ba-Bg-Bt-Bt-Bc-Bt-CH2CH2OH
(114o″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (XIV″
) has 2″
-O, 4″
-C-alkylene group;
BT′
5—
BM′
5—
BB′
5
(V′
)where BT′
5 is a group represented by any one of (5a′
) to (5g′
);
HO—
,
(5a′
)
HO-Bt-,
(5b′
)
HO-Bt-Bt-,
(5c′
)
HO-Bt-Bt-Bt-,
(5d′
)
HO-Bt-Bt-Bt-Bt-,
(5e′
)
HO-Bc-Bt-Bt-Bt-Bt-, or
(5f′
)
HO-Bg-Bc-Bt-Bt-Bt-Bt-
(5g′
)BM′
5 is a group represented by formula (5′
);
-Bc-Bt-Bt-Bt-Bt-Ba-Bg-Bt-Bt-Bg-Bc-Bt-Bg-Bc-
(5′
);
BB′
5 is a group represented by any one of (52a′
) to (52i′
);
—
CH2CH2OH,
(52a′
)
-Bt-CH2CH2OH,
(52b′
)
-Bt-Bc-CH2CH2OH,
(52c′
)
-Bt-Bc-Bt-CH2CH2OH,
(52d′
)
-Bt-Bc-Bt-Bt-CH2CH2OH,
(52e′
)
-Bt-Bc-Bt-Bt-Bt-CH2CH2OH,
(52f′
)
-Bt-Bc-Bt-Bt-Bt-Bt-CH2CH2OH,
(52g′
)
-Bt-Bc-Bt-Bt-Bt-Bt-Bc-CH2CH2OH, or
(52h′
)
-Bt-Bc-Bt-Bt-Bt-Bt-Bc-Bc-CH2CH2OH
(52i′
)where Bg, Ba, Bt and Bc are as described above;
provided that at least one of the nucleosides constituting the compound represented by formula (V′
) has a 2′
-O, 4′
-C-alkylene group;
BT′
6−
BM′
6—
BB′
6
(VI′
)where BT′
6 is a group represented by any one of (6a′
) to (6r′
);
HO—
,
(6a′
)
HO-Bc-,
(6b′
)
HO-Bt-Bc-,
(6c′
)
HO-Bc-Bt-Bc-,
(6d′
)
HO-Bg-Bc-Bt-Bc-,
(6e′
)
HO-Bt-Bg-Bc-Bt-Bc-,
(6f′
)
HO-Bc-Bt-Bg-Bc-Bt-Bc-,
(6g′
)
HO-Bg-Bc-Bt-Bg-Bc-Bt-Bc-,
(6h′
)
HO-Bt-Bg-Bc-Bt-Bg-Bc-Bt-Bc-,
(6j′
)
HO-Bt-Bt-Bg-Bc-Bt-Bg-Bc-Bt-Bc-,
(6k′
)
HO-Bg-Bt-Bt-Bg-Bc-Bt-Bg-Bc-Bt-Bc-,
(6l′
)
HO—
Ba-Bg-Bt-Bt-Bg-Bc-Bt-Bg-Bc-Bt-Bc-,
(6m′
)
HO-Bt-Ba-Bg-Bt-Bt-Bg-Bc-Bt-Bg-Bc-Bt-Bc-,
(6n′
)
HO-Bt-Bt-Ba-Bg-Bt-Bt-Bg-Bc-Bt-Bg-Bc-Bt-Bc-,
(6o′
)
HO-Bt-Bt-Bt-Ba-Bg-Bt-Bt-Bg-Bc-Bt-Bg-Bc-Bt-Bc-,
(6p′
)
HO-Bt-Bt-Bt-Bt-Ba-Bg-Bt-Bt-Bg-Bc-Bt-Bg-Bc-Bt-Bc-, or
(6q′
)
HO-Bc-Bt-Bt-Bt-Bt-Ba-Bg-Bt-Bt-Bg-Bc-Bt-Bg-Bc-Bt-Bc-
(6r′
)BM′
6 is a group represented by formula (6′
);
-Bt-Bt-Bt-Bt-Bc-Bc-
(6′
)BB′
6 is a group represented by any one of (62a′
) to (62m′
);
—
CH2CH2OH,
(62a′
)
—
Ba—
CH2CH2OH,
(62b′
)
—
Ba-Bg-CH2CH2OH,
(62c′
)
—
Ba-Bg-Bg-CH2CH2OH,
(62d′
)
—
Ba-Bg-Bg-Bt-CH2CH2OH,
(62e′
)
—
Ba-Bg-Bg-Bt-Bt-CH2CH2OH,
(62f′
)
—
Ba-Bg-Bg-Bt-Bt-Bc-CH2CH2OH,
(62g′
)
—
Ba-Bg-Bg-Bt-Bt-Bc-Ba—
CH2CH2OH,
(62h′
)
—
Ba-Bg-Bg-Bt-Bt-Bc-Ba—
Ba—
CH2CH2OH,
(62i′
)
—
Ba-Bg-Bg-Bt-Bt-Bc-Ba—
Ba-Bg-CH2CH2OH,
(62j′
)
—
Ba-Bg-Bg-Bt-Bt-Bc-Ba—
Ba-Bg-Bt-CH2CH2OH,
(62k′
)
—
Ba-Bg-Bg-Bt-Bt-Bc-Ba—
Ba-Bg-Bt-Bg-CH2CH2OH, or
(62l′
)
—
Ba-Bg-Bg-Bt-Bt-Bc-Ba—
Ba-Bg-Bt-Bg-Bg-CH2CH2OH
(62m′
)where Bg, Ba, Bt and Bc are as described above;
provided that at least one of the nucleosides constituting the compound represented by formula (VI′
) has a 2′
-O, ′
-C-alkylene group;
BT′
7—
BM′
7—
BB′
7
(VII′
)where BT′
7 is a group represented by any one of (7a′
) to (7f′
);
HO—
,
(7a′
)
HO-Bt-,
(7b′
)
HO—
Ba-Bt-,
(7c′
)
HO-Bt-Ba-Bt-,
(7d′
)
HO-Bt-Bt-Ba-Bt-, or
(7e′
)
HO-Bg-Bt-Bt-Ba-Bt-
(7f′
)BM′
7 is a group represented by formula (7′
);
-Bc-Bt-Bg-Bc-Bt-Bt-Bc-Bc-Bt-Bc-Bc-Ba—
Ba-Bc-Bc-
(7′
);
where Bg, Ba, Bt and Bc are as described above;
BB′
7 is a group represented by (72a′
);
—
CH2CH2OH
(72a′
)provided that at least one of the nucleosides constituting the compound represented by formula (VII′
) has a 2′
-O, 4′
-C-alkylene group;
BT″
1—
BM″
1—
BB″
1
(I″
)where BT″
1 is a group represented by any one of (1a″
) to (1m″
);
HO—
,
(1a″
)
HO-Bt-,
(1b″
)
HO-Bt-Bt-,
(1c″
)
HO-Bt-Bt-Bt-,
(1d″
)
HO—
Ba-Bt-Bt-Bt-,
(1e″
)
HO-Bt-Ba-Bt-Bt-Bt-,
(1f″
)
HO-Bg-Bt-Ba-Bt-Bt-Bt-,
(1g″
)
HO-Bt-Bg-Bt-Ba-Bt-Bt-Bt-,
(1h″
)
HO-Bt-Bt-Bg-Bt-Ba-Bt-Bt-Bt-,
(1i″
)
HO-Bt-Bt-Bt-Bg-Bt-Ba-Bt-Bt-Bt-,
(1j″
)
HO—
Ba-Bt-Bt-Bt-Bg-Bt-Ba-Bt-Bt-Bt-,
(1k″
)
HO-Bc-Ba-Bt-Bt-Bt-Bg-Bt-Ba-Bt-Bt-Bt-, or
(1l″
)
HO-Bc-Bc-Ba-Bt-Bt-Bt-Bg-Bt-Ba-Bt-Bt-Bt-,
(1m″
)BM″
1 is a group represented by formula (1″
);
—
Ba-Bg-Bc-Ba-Bt-Bg-
(1″
)BB″
1 is a group represented by any one of (101a″
) to (101m″
);
—
CH2CH2OH,
(101a″
)
-Bt-CH2CH2OH,
(101b″
)
-Bt-Bt-CH2CH2OH,
(10c″
)
-Bt-Bt-Bc-CH2CH2OH,
(101d″
)
-Bt-Bt-Bc-Bc-CH2CH2OH,
(101e″
)
-Bt-Bt-Bc-Bc-Bc-CH2CH2OH,
(101f″
)
-Bt-Bt-Bc-Bc-Bc-Ba—
CH2CH2OH,
(101g″
)
-Bt-Bt-Bc-Bc-Bc-Ba—
Ba—
CH2CH2OH,
(101h″
)
-Bt-Bt-Bc-Bc-Bc-Ba—
Ba-Bt-CH2CH2OH,
(101i″
)
-Bt-Bt-Bc-Bc-Bc-Ba—
Ba-Bt-Bt-CH2CH2OH,
(101j″
)
-Bt-Bt-Bc-Bc-Bc-Ba—
Ba-Bt-Bt-Bc-CH2CH2OH,
(101k″
)
-Bt-Bt-Bc-Bc-Bc-Ba—
Ba-Bt-Bt-Bc-Bt-CH2CH2OH, or
(101l″
)
-Bt-Bt-Bc-Bc-Bc-Ba—
Ba-Bt-Bt-Bc-Bt-Bc-CH2CH2OH,
(101m″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides, constituting the compound represented by formula (I″
) has 2″
-O, 4″
-C-alkylene group;
BT″
2—
BM″
2—
BB″
2
(II″
)where BT″
2 is a group represented by any one of (2a″
) to (2g″
);
HO—
,
(2a″
)
HO-Bg-,
(2b″
)
HO-Bt-Bg-,
(2c″
)
HO—
Ba-Bt-Bg-,
(2d″
)
HO-Bc-Ba-Bt-Bg-,
(2e″
)
HO-Bg-Bc-Ba-Bt-Bg-, or
(2f″
)
HO—
Ba-Bg-Bc-Ba-Bt-Bg-,
(2g″
)BM″
2 is a group represented by formula (2″
);
-Bt-Bt-Bc-Bc-Bc-Ba—
Ba-Bt-Bt-Bc-Bt-Bc-
(2″
)BB″
2 is a group represented by any one of (102a″
) to (102g″
);
—
CH2CH2OH,
(102a″
)
—
Ba—
CH2CH2OH,
(102b″
)
—
Ba-Bg-CH2CH2OH,
(102c″
)
—
Ba-Bg-Bg-CH2CH2OH,
(102d″
)
—
Ba-Bg-Bg-Ba—
CH2CH2OH,
(102e″
)
—
Ba-Bg-Bg-Ba—
Ba—
CH2CH2OH, or
(102f″
)
—
Ba-Bg-Bg-Ba—
Ba-Bt-CH2CH2OH,
(102g″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (II″
) has 2″
-O, 4″
-C-alkylene group;
BT″
3—
BM″
3—
BB″
3
(III″
)where BT″
3 is a group represented by any one of (3a″
) to (3m″
);
HO—
,
(3a″
)
HO-Bc-,
(3b″
)
HO—
Ba-Bc-,
(3c″
)
HO—
Ba—
Ba-Bc-,
(3d″
)
HO—
Ba—
Ba—
Ba-Bc-,
(3e″
)
HO—
Ba—
Ba—
Ba—
Ba-Bc-,
(3f″
)
HO-Bg-Ba—
Ba—
Ba—
Ba-Bc-,
(3g″
)
HO-Bt-Bg-Ba—
Ba—
Ba—
Ba-Bc-,
(3h″
)
HO—
Ba-Bt-Bg-Ba—
Ba—
Ba—
Ba-Bc-,
(3i″
)
HO—
Ba—
Ba-Bt-Bg-Ba—
Ba—
Ba—
Ba-Bc-,
(3j″
)
HO-Bt-Ba—
Ba-Bt-Bg-Ba—
Ba—
Ba—
Ba-Bc-,
(3k″
)
HO—
Ba-Bt-Ba—
Ba-Bt-Bg-Ba—
Ba—
Ba—
Ba-Bc-, or
(3l″
)
HO-Bc-Ba-Bt-Ba—
Ba-Bt-Bg-Ba—
Ba—
Ba—
Ba-Bc-
(3m″
)BM″
3 is a group represented by formula (3″
);
-Bg-Bc-Bc-Bg-Bc-Bc-
(3″
)BB″
3 is a group represented by any one of (103a″
) to (103m″
);
—
CH2CH2OH,
(103a″
)
—
Ba—
CH2CH2OH,
(103b″
)
—
Ba-Bt-CH2CH2OH,
(103c″
)
—
Ba-Bt-Bt-CH2CH2OH,
(103d″
)
—
Ba-Bt-Bt-Bt-CH2CH2OH,
(103e″
)
—
Ba-Bt-Bt-Bt-Bc-CH2CH2OH,
(103f″
)
—
Ba-Bt-Bt-Bt-Bc-Bt-CH2CH2OH,
(103g″
)
—
Ba-Bt-Bt-Bt-Bc-Bt-Bc-CH2CH2OH,
(103h″
)
—
Ba-Bt-Bt-Bt-Bc-Bt-Bc-Ba—
CH2CH2OH,
(103i″
)
—
Ba-Bt-Bt-Bt-Bc-Bt-Bc-Ba—
Ba—
CH2CH2OH,
(103j″
)
—
Ba-Bt-Bt-Bt-Bc-Bt-Bc-Ba—
Ba-Bc-CH2CH2OH,
(103k″
)
—
Ba-Bt-Bt-Bt-Bc-Bt-Bc-Ba—
Ba-Bc-Ba—
CH2CH2OH, or
(103l″
)
—
Ba-Bt-Bt-Bt-Bc-Bt-Bc-Ba—
Ba-Bc-Ba-Bg-CH2CH2OH
(103m″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (III″
) has 2″
-O, 4″
-C-alkylene group;
BT″
4—
BM″
4—
BB″
4
(IV″
)where BT″
4 is a group represented by any one of (4a″
) to (4j″
);
HO—
,
(4a″
)
HO—
Ba—
,
(4b″
)
HO-Bc-Ba—
,
(4c″
)
HO-Bt-Bc-Ba—
,
(4d″
)
HO-Bg-Bt-Bc-Ba—
,
(4e″
)
HO-Bg-Bg-Bt-Bc-Ba—
,
(4f″
)
HO—
Ba-Bg-Bg-Bt-Bc-Ba—
,
(4g″
)
HO-Bt-Ba-Bg-Bg-Bt-Bc-Ba—
,
(4h″
)
HO-Bc-Bt-Ba-Bg-Bg-Bt-Bc-Ba—
, or
(4i″
)
HO-Bg-Bc-Bt-Ba-Bg-Bg-Bt-Bc-Ba—
(4j″
)BM″
4 is a group represented by formula (4″
);
-Bg-Bg-Bc-Bt-Bg-Bc-Bt-Bt-Bt-
(4″
)BB″
4 is a group represented by any one of (104a″
) to (104j″
);
—
CH2CH2OH,
(104a″
)
-Bg-CH2CH2OH,
(104b″
)
-Bg-Bc-CH2CH2OH,
(104c″
)
-Bg-Bc-Bc-CH2CH2OH,
(104d″
)
-Bg-Bc-Bc-Bc-CH2CH2OH,
(104e″
)
-Bg-Bc-Bc-Bc-Bt-CH2CH2OH,
(104f″
)
-Bg-Bc-Bc-Bc-Bt-Bc-CH2CH2OH,
(104g″
)
-Bg-Bc-Bc-Bc-Bt-Bc-Ba—
CH2CH2OH,
(104h″
)
-Bg-Bc-Bc-Bc-Bt-Bc-Ba-Bg-CH2CH2OH, or
(104i″
)
-Bg-Bc-Bc-Bc-Bt-Bc-Ba-Bg-Bc-CH2CH2OH
(104j″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (IV″
) has 2″
-O, 4″
-C-alkylene group;
BT″
5—
BM″
5—
BB″
5
(V″
)where BT″
5 is a group represented by any one of (5a″
) to (5j″
);
HO—
,
(5a″
)
HO—
Ba—
,
(5b″
)
HO-Bg-Ba—
,
(5c″
)
HO-Bg-Bg-Ba—
,
(5d″
)
HO—
Ba-Bg-Bg-Ba—
,
(5e″
)
HO-Bc-Ba-Bg-Bg-Ba—
,
(5f″
)
HO-Bc-Bc-Ba-Bg-Bg-Ba—
,
(5g″
)
HO-Bt-Bc-Bc-Ba-Bg-Bg-Ba—
,
(5h″
)
HO-Bg-Bt-Bc-Bc-Ba-Bg-Bg-Ba—
, or
(5i″
)
HO—
Ba-Bg-Bt-Bc-Bc-Ba-Bg-Bg-Ba—
(5j″
)BM″
5 is a group represented by formula (5″
);
-Bg-Bc-Bt-Ba-Bg-Bg-Bt-Bc-Ba—
(5″
)BB″
5 is a group represented by any one of (105a″
) to (105j″
);
—
CH2CH2OH,
(105a″
)
-Bg-CH2CH2OH,
(105b″
)
-Bg-Bg-CH2CH2OH,
(105c″
)
-Bg-Bg-Bc-CH2CH2OH,
(105d′
)
-Bg-Bg-Bc-Bt-CH2CH2OH,
(105e″
)
-Bg-Bg-Bc-Bt-Bg-CH2CH2OH,
(105f″
)
-Bg-Bg-Bc-Bt-Bg-Bc-CH2CH2OH,
(105g″
)
-Bg-Bg-Bc-Bt-Bg-Bc-Bt-CH2CH2OH,
(105h″
)
-Bg-Bg-Bc-Bt-Bg-Bc-Bt-Bt-CH2CH2OH, or
(105i″
)
-Bg-Bg-Bc-Bt-Bg-Bc-Bt-Bt-Bt-CH2CH2OH
(105j″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (V″
) has 2″
-O, 4″
-C-alkylene group;
BT″
16—
BM″
16—
BB″
16
(XVI″
)where BT″
16 is a group represented by any one of (16a″
) to (16j″
);
HO—
,
(16a″
)
HO-Bg-,
(16b″
)
HO-Bt-Bg-,
(16c″
)
HO-Bg-Bt-Bg-,
(16d″
)
HO-Bg-Bg-Bt-Bg-,
(16e″
)
HO—
Ba-Bg-Bg-Bt-Bg-,
(16f″
)
HO—
Ba—
Ba-Bg-Bg-Bt-Bg-,
(16g″
)
HO-Bg-Ba—
Ba-Bg-Bg-Bt-Bg-,
(16h″
)
HO-Bt-Bg-Ba—
Ba-Bg-Bg-Bt-Bg-, or
(16i″
)
HO-Bc-Bt-Bg-Ba—
Ba-Bg-Bg-Bt-Bg-
(16j″
)BM″
16 is a group represented by formula (16″
)
-Bt-Bt-Bc-Bt-Bt-Bg-Bt-Ba-Bc-
(16″
)BB″
16 is a group represented by any one of (116a″
) to (116j″
);
—
CH2CH2OH,
(116a″
)
-Bt-CH2CH2OH,
(116b″
)
-Bt-Bt-CH2CH2OH,
(116c″
)
-Bt-Bt-Bc-CH2CH2OH,
(116d″
)
-Bt-Bt-Bc-Ba—
CH2CH2OH,
(116e″
)
-Bt-Bt-Bc-Ba-Bt-CH2CH2OH,
(116f″
)
-Bt-Bt-Bc-Ba-Bt-Bc-CH2CH2OH,
(116g″
)
-Bt-Bt-Bc-Ba-Bt-Bc-Bc-CH2CH2OH,
(116h″
)
-Bt-Bt-Bc-Ba-Bt-Bc-Bc-Bc-CH2CH2OH, or
(116i″
)
-Bt-Bt-Bc-Ba-Bt-Bc-Bc-Bc-Ba—
CH2CH2OH
(116j″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (XVI″
) has 2″
-O, 4″
-C-alkylene group;
BT″
17—
BM″
17—
BB″
17
(XVII″
)where BT″
17 is a group represented by any one of (17a″
) to (17j″
);
HO—
,
(17a″
)
HO-Bt-,
(17b″
)
HO-Bt-Bt-,
(17c″
)
HO-Bg-Bt-Bt-,
(17d″
)
HO-Bg-Bg-Bt-Bt-,
(17e″
)
HO-Bc-Bg-Bg-Bt-Bt-,
(17f″
)
HO-Bc-Bc-Bg-Bg-Bt-Bt-,
(17g″
)
HO-Bt-Bc-Bc-Bg-Bg-Bt-Bt-,
(17h″
)
HO-Bc-Bt-Bc-Bc-Bg-Bg-Bt-Bt-, or
(17i″
)
HO-Bc-Bc-Bt-Bc-Bc-Bg-Bg-Bt-Bt-
(17j″
)BM″
17 is a group represented by formula (17″
);
-Bc-Bt-Bg-Ba—
Ba-Bg-Bg-Bt-Bg-
(17″
)BB″
17 is a group represented by any one of (117a″
) to (117j″
);
—
CH2CH2OH,
(117a″
)
-Bt-CH2CH2OH,
(117b″
)
-Bt-Bt-CH2CH2OH,
(117c″
)
-Bt-Bt-Bc-CH2CH2OH,
(117d″
)
-Bt-Bt-Bc-Bt-CH2CH2OH,
(117e″
)
-Bt-Bt-Bc-Bt-Bt-CH2CH2OH,
(117f″
)
-Bt-Bt-Bc-Bt-Bt-Bg-CH2CH2OH,
(117g″
)
-Bt-Bt-Bc-Bt-Bt-Bg-Bt-CH2CH2OH,
(117h″
)
-Bt-Bt-Bc-Bt-Bt-Bg-Bt-Ba—
CH2CH2OH, or
(117i″
)
-Bt-Bt-Bc-Bt-Bt-Bg-Bt-Ba-Bc-CH2CH2OH
(117j″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (XVII″
) has 2″
-O, 4″
-C-alkylene group;
BT″
18—
BM″
18—
BB″
18
(XVIII″
)where BT″
18 is a group represented by any one of (18a″
) to (18j″
);
HO—
,
(18a″
)
HO-Bg-,
(18b″
)
HO-Bt-Bg-,
(18c″
)
HO-Bc-Bt-Bg-,
(18d″
)
HO-Bc-Bc-Bt-Bg-,
(18e″
)
HO—
Ba-Bc-Bc-Bt-Bg-,
(18f″
)
HO-Bg-Ba-Bc-Bc-Bt-Bg-,
(18g″
)
HO—
Ba-Bg-Ba-Bc-Bc-Bt-Bg-,
(18h″
)
HO—
Ba—
Ba-Bg-Ba-Bc-Bc-Bt-Bg-, or
(18i″
)
HO-Bt-Ba—
Ba-Bg-Ba-Bc-Bc-Bt-Bg-
(18j″
)BM″
18 is a group represented by formula (18″
)
-Bc-Bt-Bc-Ba-Bg-Bc-Bt-Bt-Bc-
(18″
)BB″
18 is a group represented by any one of (118a″
) to (118j″
);
—
CH2CH2OH,
(118a″
)
-Bt-CH2CH2OH,
(118b″
)
-Bt-Bt-CH2CH2OH,
(118c″
)
-Bt-Bt-Bc-CH2CH2OH,
(118d″
)
-Bt-Bt-Bc-Bc-CH2CH2OH,
(118e″
)
-Bt-Bt-Bc-Bc-Bt-CH2CH2OH,
(118f″
)
-Bt-Bt-Bc-Bc-Bt-Bt-CH2CH2OH,
(118g″
)
-Bt-Bt-Bc-Bc-Bt-Bt-Ba—
CH2CH2OH,
(118h″
)
-Bt-Bt-Bc-Bc-Bt-Bt-Ba-Bg-CH2CH2OH, or
(118i″
)
-Bt-Bt-Bc-Bc-Bt-Bt-Ba-Bg-Bc-CH2CH2OH
(118j″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (XVIII″
) has 2″
-O, 4″
-C-alkylene group;
BT″
19—
BM″
19—
BB″
19
(XIX″
)where BT″
19 is a group represented by any one of (19a″
) to (19j″
);
HO—
,
(19a″
)
HO-Bc-,
(19b″
)
HO-Bg-Bc-,
(19c″
)
HO—
Ba-Bg-Bc-,
(19d″
)
HO-Bt-Ba-Bg-Bc-,
(19e″
)
HO-Bt-Bt-Ba-Bg-Bc-,
(19f″
)
HO-Bc-Bt-Bt-Ba-Bg-Bc-,
(19g″
)
HO-Bc-Bc-Bt-Bt-Ba-Bg-Bc-,
(19h″
)
HO-Bt-Bc-Bc-Bt-Bt-Ba-Bg-Bc-, or
(19i″
)
HO-Bt-Bt-Bc-Bc-Bt-Bt-Ba-Bg-Bc-
(19j″
)BM″
19 is a group represented by formula (19″
);
-Bt-Bt-Bc-Bc-Ba-Bg-Bc-Bc-Ba—
(19″
)BB″
19 is a group represented by any one of (119a″
) to (119j″
);
—
CH2CH2OH,
(119a″
)
-Bt-CH2CH2OH,
(119b″
)
-Bt-Bt-CH2CH2OH,
(119c″
)
-Bt-Bt-Bg-CH2CH2OH,
(119d″
)
-Bt-Bt-Bg-Bt-CH2CH2OH,
(119e″
)
-Bt-Bt-Bg-Bt-Bg-CH2CH2OH,
(119f″
)
-Bt-Bt-Bg-Bt-Bg-Bt-CH2CH2OH,
(119g″
)
-Bt-Bt-Bg-Bt-Bg-Bt-Bt-CH2CH2OH,
(119h″
)
-Bt-Bt-Bg-Bt-Bg-Bt-Bt-Bg-CH2CH2OH, or
(119i″
)
-Bt-Bt-Bg-Bt-Bg-Bt-Bt-Bg-Ba—
CH2CH2OH
(11 9j″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (XIX″
) has 2″
-O, 4″
-C-alkylene group;
BT″
20—
BM″
20—
BB″
20
(XX″
)where BT″
20 is a group represented by any one of (20a″
) to (20j″
);
HO—
,
(20a″
)
HO-Bc-,
(20b″
)
HO-Bt-Bc-,
(20c″
)
HO-Bt-Bt-Bc-,
(20d″
)
HO-Bc-Bt-Bt-Bc-,
(20e″
)
HO-Bg-Bc-Bt-Bt-Bc-,
(20f″
)
HO—
Ba-Bg-Bc-Bt-Bt-Bc-,
(20g″
)
HO-Bc-Ba-Bg-Bc-Bt-Bt-Bc-,
(20h″
)
HO-Bt-Bc-Ba-Bg-Bc-Bt-Bt-Bc-, or
(20i″
)
HO-Bc-Bt-Bc-Ba-Bg-Bc-Bt-Bt-Bc-
(20j″
)BM″
20 is a group represented by formula (20″
);
-Bt-Bt-Bc-Bc-Bt-Bt-Ba-Bg-Bc-
(20″
)BB″
20 is a group represented by any one of (120a″
) to (120j″
);
—
CH2CH2OH,
(120a″
)
-Bt-CH2CH2OH,
(120b″
)
-Bt-Bt-CH2CH2OH,
(120c″
)
-Bt-Bt-Bc-CH2CH2OH,
(120d″
)
-Bt-Bt-Bc-Bc-CH2CH2OH,
(120e″
)
-Bt-Bt-Bc-Bc-Ba—
CH2CH2OH,
(120f″
)
-Bt-Bt-Bc-Bc-Ba-Bg-CH2CH2OH,
(120g″
)
-Bt-Bt-Bc-Bc-Ba-Bg-Bc-CH2CH2OH,
(120h″
)
-Bt-Bt-Bc-Bc-Ba-Bg-Bc-Bc-CH2CH2OH, or
(120i″
)
-Bt-Bt-Bc-Bc-Ba-Bg-Bc-Bc-Ba—
CH2CH2OH
(120j″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (XX″
) has 2″
-O, 4″
-C-alkylene group;
BT″
21—
BM″
21—
BB″
21
(XXI″
)where BT″
21 is a group represented by any one of (21a″
) to (21e″
);
HO—
,
(21a″
)
HO—
Ba—
,
(21b″
)
HO-Bc-Ba—
,
(21c″
)
HO-Bt-Bc-Ba—
, or
(21d″
)
HO-Bc-Bt-Bc-Ba—
(21e″
)BM″
21 is a group represented by formula (21″
);
-Bg-Bc-Bt-Bt-Bc-Bt-Bt-Bc-Bc-Bt-Bt-Ba-Bg-Bc-
(21″
);
BB″
21 is a group represented by any one of (121a″
) to (121e″
);
—
CH2CH2OH,
(121a″
)
-Bt-CH2CH2OH,
(121b″
)
-Bt-Bt-CH2CH2OH,
(121c″
)
-Bt-Bt-Bc-CH2CH2OH, or
(121d″
)
-Bt-Bt-Bc-Bc-CH2CH2OH
(121e″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (XXI″
) has 2″
-O, 4″
-C-alkylene group;
BT″
6—
BM″
6—
BB″
6
(VI″
)where BT″
6 is a group represented by any one of (6a″
) to (6j″
);
HO—
,
(6a″
)
HO—
Ba—
,
(6b″
)
HO—
Ba—
Ba—
,
(6c″
)
HO—
Ba—
Ba—
Ba—
,
(6d″
)
HO-Bc-Ba—
Ba—
Ba—
,
(6e″
)
HO-Bc-Bc-Ba—
Ba—
Ba—
,
(6f″
)
HO-Bt-Bc-Bc-Ba—
Ba—
Ba—
,
(6g″
)
HO-Bt-Bt-Bc-Bc-Ba—
Ba—
Ba—
,
(6h″
)
HO-Bc-Bt-Bt-Bc-Bc-Ba—
Ba—
Ba—
, or
(6i″
)
HO-Bt-Bc-Bt-Bt-Bc-Bc-Ba—
Ba—
Ba—
(6j″
)BM″
6 is a group represented by formula (6″
);
-Bg-Bc-Ba-Bg-Bc-Bc-Bt-Bc-Bt-
(6″
)BB″
6 is a group represented by any one of (106a″
) to (106j″
);
—
CH2CH2OH,
(106a″
)
-Bc-CH2CH2OH,
(106b″
)
-Bc-Bg-CH2CH2OH,
(106c″
)
-Bc-Bg-Bc-CH2CH2OH,
(106d″
)
-Bc-Bg-Bc-Bt-CH2CH2OH,
(106e″
)
-Bc-Bg-Bc-Bt-Bc-CH2CH2OH,
(106f″
)
-Bc-Bg-Bc-Bt-Bc-Ba—
CH2CH2OH,
(106g″
)
-Bc-Bg-Bc-Bt-Bc-Ba-Bc-CH2CH2OH,
(106h″
)
-Bc-Bg-Bc-Bt-Bc-Ba-Bc-Bt-CH2CH2OH, or
(106i″
)
-Bc-Bg-Bc-Bt-Bc-Ba-Bc-Bt-Bc-CH2CH2OH,
(106j″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (VI″
) has 2″
-O, 4″
-C-alkylene group;
BT″
7—
BM″
7—
BB″
7
(VII″
)where BT″
7 is a group represented by any one of (7a″
) to (7j″
);
HO—
,
(7a″
)
HO-Bt-,
(7b″
)
HO-Bt-Bt-,
(7c″
)
HO-Bg-Bt-Bt-,
(7d″
)
HO—
Ba-Bg-Bt-Bt-,
(7e″
)
HO-Bg-Ba-Bg-Bt-Bt-,
(7f″
)
HO-Bt-Bg-Ba-Bg-Bt-Bt-,
(7g″
)
HO—
Ba-Bt-Bg-Ba-Bg-Bt-Bt-,
(7h″
)
HO-Bt-Ba-Bt-Bg-Ba-Bg-Bt-Bt-, or
(7i″
)
HO-Bc-Bt-Ba-Bt-Bg-Ba-Bg-Bt-Bt-
(7j″
)BM″
7 is a group represented by formula (7″
);
-Bt-Bc-Bt-Bt-Bc-Bc-Ba—
Ba—
Ba—
(7″
)BB″
7 is a group represented by any one of (107a″
) to (107j″
);
—
CH2CH2OH,
(107a″
)
-Bg-CH2CH2OH,
(107b″
)
-Bg-Bc-CH2CH2OH,
(107c″
)
-Bg-Bc-Ba—
CH2CH2OH,
(107d″
)
-Bg-Bc-Ba-Bg-CH2CH2OH,
(107e″
)
-Bg-Bc-Ba-Bg-Bc-CH2CH2OH,
(107f″
)
-Bg-Bc-Ba-Bg-Bc-Bc-CH2CH2OH,
(107g″
)
-Bg-Bc-Ba-Bg-Bc-Bc-Bt-CH2CH2OH,
(107h″
)
-Bg-Bc-Ba-Bg-Bc-Bc-Bt-Bc-CH2CH2OH, or
(107i″
)
-Bg-Bc-Ba-Bg-Bc-Bc-Bt-Bc-Bt-CH2CH2OH
(107j″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (VII″
) has 2″
-O, 4″
-C-alkylene group;
BT″
8—
BM″
8—
BB″
8
(VIII″
)where BT″
8 is a group represented by any one of (8a″
) to (8n″
);
HO—
,
(8a″
)
HO-Bc-,
(8b″
)
HO-Bt-Bc-,
(8c″
)
HO—
Ba-Bt-Bc-,
(8d″
)
HO-Bc-Ba-Bt-Bc-,
(8e″
)
HO-Bt-Bc-Ba-Bt-Bc-,
(8f″
)
HO-Bt-Bt-Bc-Ba-Bt-Bc-,
(8g″
)
HO-Bt-Bt-Bt-Bc-Ba-Bt-Bc-,
(8h″
)
HO-Bg-Bt-Bt-Bt-Bc-Ba-Bt-Bc-,
(8i″
)
HO-Bt-Bg-Bt-Bt-Bt-Bc-Ba-Bt-Bc-,
(8j″
)
HO-Bt-Bt-Bg-Bt-Bt-Bt-Bc-Ba-Bt-Bc-,
(8k″
)
HO—
Ba-Bt-Bt-Bg-Bt-Bt-Bt-Bc-Ba-Bt-Bc-,
(8l″
)
HO-Bc-Ba-Bt-Bt-Bg-Bt-Bt-Bt-Bc-Ba-Bt-Bc-, or
(8m″
)
HO-Bc-Bc-Ba-Bt-Bt-Bg-Bt-Bt-Bt-Bc-Ba-Bt-Bc-
(8n″
)BM″
8 is a group represented by formula (8″
);
—
Ba-Bg-Bc-Bt-Bc-
(8″
)BB″
8 is a group represented by any one of (108a″
) to (108n″
)
—
CH2CH2OH,
(108a″
)
-Bt-CH2CH2OH,
(108b″
)
-Bt-Bt-CH2CH2OH,
(108c″
)
-Bt-Bt-Bt-CH2CH2OH,
(108d″
)
-Bt-Bt-Bt-Bt-CH2CH2OH,
(108e″
)
-Bt-Bt-Bt-Bt-Ba—
CH2CH2OH,
(108f″
)
-Bt-Bt-Bt-Bt-Ba-Bc-CH2CH2OH,
(108g″
)
-Bt-Bt-Bt-Bt-Ba-Bc-Bt-CH2CH2OH,
(108h″
)
-Bt-Bt-Bt-Bt-Ba-Bc-Bt-Bc-CH2CH2OH,
(108i″
)
-Bt-Bt-Bt-Bt-Ba-Bc-Bt-Bc-Bc-CH2CH2OH,
(108j″
)
-Bt-Bt-Bt-Bt-Ba-Bc-Bt-Bc-Bc-Bc-CH2CH2OH,
(108k″
)
-Bt-Bt-Bt-Bt-Ba-Bc-Bt-Bc-Bc-Bc-Bt-CH2CH2OH,
(108l″
)
-Bt-Bt-Bt-Bt-Ba-Bc-Bt-Bc-Bc-Bc-Bt-Bt-CH2CH2OH, or
(108m″
)
-Bt-Bt-Bt-Bt-Ba-Bc-Bt-Bc-Bc-Bc-Bt-Bt-Bg-CH2CH2OH
(108n″
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (VIII″
) has 2″
-O, 4″
-C-alkylene group;
BT—
BM—
BB
(I)where BT is a group represented by any one of (1a) to (1k);
HO—
,
(1a)
HO-Bt-,
(1b)
HO-Bc-Bt-,
(1c)
HO-Bg-Bc-Bt-,
(1d)
HO—
Ba-Bg-Bc-Bt-,
(1e)
HO-Bg-Ba-Bg-Bc-Bt-,
(1f)
HO-Bt-Bg-Ba-Bg-Bc-Bt-,
(1g)
HO-Bc-Bt-Bg-Ba-Bg-Bc-Bt-,
(1h)
HO-Bc-Bc-Bt-Bg-Ba-Bg-Bc-Bt-, or
(1j)
HO-Bg-Bc-Bc-Bt-Bg-Ba-Bg-Bc-Bt-;
(1k)BM is a group represented by formula (2);
-Bg-Ba-Bt-Bc-Bt-Bg-Bc-Bt-Bg-Bg-Bc-Ba-Bt-Bc-Bt-
(2)where Bg, Ba, Bt and Bc are as defined above;
BB is a group represented by any one of (2a) to (2h);
—
CH2CH2OH,
(2a)
-Bt-CH2CH2OH,
(2b)
-Bt-Bg-CH2CH2OH,
(2c)
-Bt-Bg-Bc-CH2CH2OH,
(2d)
-Bt-Bg-Bc-Ba—
CH2CH2OH,
(2e)
-Bt-Bg-Bc-Ba-Bg-CH2CH2OH,
(2f)
-Bt-Bg-Bc-Ba-Bg-Bt-CH2CH2OH, or
(2g)
-Bt-Bg-Bc-Ba-Bg-Bt-Bt-CH2CH2OH
(2h)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (I) has a 2′
-O, 4′
-C-alkylene group;
BT′
1—
BM′
1—
BB′
1
(I′
)where BT′
1 is a group represented by any one of (1a′
) to (1o′
);
HO—
,
(1a′
)
HO-Bg-,
(1b′
)
HO-Bc-Bg-,
(1c′
)
HO-Bt-Bc-Bg-,
(1d′
)
HO-Bt-Bt-Bc-Bg-,
(1e′
)
HO-Bc-Bt-Bt-Bc-Bg-,
(1f′
)
HO-Bt-Bc-Bt-Bt-Bc-Bg-,
(1g′
)
HO-Bg-Bt-Bc-Bt-Bt-Bc-Bg-,
(1h′
)
HO—
Ba-Bg-Bt-Bc-Bt-Bt-Bc-Bg-,
(1j′
)
HO-Bg-Ba-Bg-Bt-Bc-Bt-Bt-Bc-Bg-,
(1k′
)
HO-Bt-Bg-Ba-Bg-Bt-Bc-Bt-Bt-Bc-Bg-,
(1l′
)
HO-Bt-Bt-Bg-Ba-Bg-Bt-Bc-Bt-Bt-Bc-Bg-,
(1m′
)
HO-Bg-Bt-Bt-Bg-Ba-Bg-Bt-Bc-Bt-Bt-Bc-Bg-, or
(1n′
)
HO—
Ba-Bg-Bt-Bt-Bg-Ba-Bg-Bt-Bc-Bt-Bt-Bc-Bg-,
(1o′
)BM′
1 is a group represented by formula (1′
);
—
Ba—
Ba—
Ba-Bc-Bt-Bg-Ba—
(1′
)BB′
1 is a group represented by any one of (12a′
) to (121′
);
—
CH2CH2OH,
(12a′
)
-Bg-CH2CH2OH,
(12b′
)
-Bg-Bc-CH2CH2OH,
(12c′
)
-Bg-Bc-Ba—
CH2CH2OH,
(12d′
)
-Bg-Bc-Ba—
Ba—
CH2CH2OH,
(12e′
)
-Bg-Bc-Ba—
Ba—
Ba—
CH2CH2OH,
(12f′
)
-Bg-Bc-Ba—
Ba—
Ba-Bt-CH2CH2OH,
(12g′
)
-Bg-Bc-Ba—
Ba—
Ba-Bt-Bt-CH2CH2OH,
(12h′
)
-Bg-Bc-Ba—
Ba—
Ba-Bt-Bt-Bt-CH2CH2OH,
(12i′
)
-Bg-Bc-Ba—
Ba—
Ba-Bt-Bt-Bt-Bg-CH2CH2OH,
(12j′
)
-Bg-Bc-Ba—
Ba—
Ba-Bt-Bt-Bt-Bg-Bc-CH2CH2OH, or
(12k′
)
-Bg-Bc-Ba—
Ba—
Ba-Bt-Bt-Bt-Bg-Bc-Bt-CH2CH2OH,
(12l′
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (I′
) has a 2′
-O, 4′
-C-alkylene group;
BT′
2—
BM′
2—
BB′
2
(II′
)where BT′
2 is a group represented by any one of (2a′
) to (2j′
);
HO—
,
(2a′
)
HO-Bg-,
(2b′
)
HO—
Ba-Bg-,
(2c′
)
HO—
Ba—
Ba-Bg-,
(2d′
)
HO—
Ba—
Ba—
Ba-Bg-,
(2e′
)
HO-Bc-Ba—
Ba—
Ba-Bg-,
(2f′
)
HO-Bg-Bc-Ba—
Ba—
Ba-Bg-,
(2g′
)
HO-Bt-Bg-Bc-Ba—
Ba—
Ba-Bg-, or
(2h′
)
HO-Bg-Bt-Bg-Bc-Ba—
Ba—
Ba-Bg-
(2j′
)BM′
2 is a group represented by formula (21′
);
-Bt-Bt-Bg-Ba-Bg-Bt-Bc-Bt-Bt-Bc-
(2′
)BB′
2 is a group represented by any one of (22a′
) to (22i′
);
—
CH2CH2OH,
(22a′
)
—
Ba—
CH2CH2OH,
(22b′
)
—
Ba—
Ba—
CH2CH2OH,
(22c′
)
—
Ba—
Ba—
Ba—
CH2CH2OH,
(22d′
)
—
Ba—
Ba—
Ba—
Ba—
CH2CH2OH,
(22e′
)
—
Ba—
Ba—
Ba—
Ba-Bc-CH2CH2OH,
(22f′
)
—
Ba—
Ba—
Ba—
Ba-Bc-Bt-CH2CH2OH,
(22g′
)
—
Ba—
Ba—
Ba—
Ba-Bc-Bt-Bg-CH2CH2OH, or
(22h′
)
—
Ba—
Ba—
Ba—
Ba-Bc-Bt-Bg-Ba—
CH2CH2OH
(22i′
)where Bg, Ba, Bt and Bc are as defined above;
provided that at least one of the nucleosides constituting the compound represented by formula (II′
) has a 2′
-O, 4′
-C-alkylene group.
- ), (IV′
-
70. The compound according to claims 69 which is selected from the group consisting of compounds (i′
- ) to (xiii′
), or a pharmacologically acceptable salt thereof;
(i′
) a compound represented by formula (i′
);
HO—
Ba-Bg-Bt-Bt-Bg-Ba-Bg-Bt-Bc-Bt-Bt-Bc-Bg-Ba—
Ba—
Ba-Bc-Bt-Bg-Ba-Bg-Bc-Ba—
CH2CH2OH
(i′
)(ii′
) a compound represented by formula (ii′
);
HO—
Ba—
Ba—
Ba-Bc-Bt-Bg-Ba-Bg-Bc-Ba—
Ba—
Ba-Bt-Bt-Bt-Bg-Bc-Bt-CH2CH2OH
(ii′
)(iii′
) a compound represented by formula (iii′
);
HO-Bt-Bt-Bg-Ba-Bg-Bt-Bc-Bt-Bt-Bc-Ba—
Ba—
Ba—
Ba-Bc-Bt-Bg-Ba—
CH2CH2OH
(iii′
)(iv′
) a compound represented by formula (iv′
);
HO-Bg-Bt-Bg-Bc-Ba—
Ba—
Ba-Bg-Bt-Bt-Bg-Ba-Bg-Bt-Bc-Bt-Bt-Bc-CH2CH2OH
(iv′
)(v′
) a compound represented by formula (v′
);
HO-Bg-Bc-Bc-Bg-Bc-Bt-Bg-Bc-Bc-Bc-Ba—
Ba-Bt-Bg-Bc-CH2CH2OH
(v′
)(vi′
) a compound represented by formula (vi′
);
HO-Bc-Bg-Bc-Bt-Bg-Bc-Bc-Bc-Ba—
Ba-Bt-Bg-Bc-Bc-Ba-Bt-Bc-Bc-CH2CH2OH
(vi′
)(vii′
) a compound represented by formula (vii′
);
HO-Bc-Ba-Bg-Bt-Bt-Bt-Bg-Bc-Bc-Bg-Bc-Bt-Bg-Bc-Bc-Bc-Ba—
Ba—
CH2CH2OH
(vii′
)(viii′
) a compound represented by formula (viii′
);
HO-Bt-Bg-Bt-Bt-Bc-Bt-Bg-Ba-Bc-Ba—
Ba-Bc-Ba-Bg-Bt-Bt-Bt-Bg-CH2CH2OH
(viii′
)(ix′
) a compound represented by formula (ix′
);
HO-Bg-Bc-Bt-Bt-Bt-Bt-Bc-Bt-Bt-Bt-Bt-Ba-Bg-Bt-Bt-Bg-Bc-Bt-Bg-Bc-CH2CH2OH
(ix′
)(x′
) a compound represented by formula (x′
);
HO-Bc-Bt-Bt-Bt-Bt-Ba-Bg-Bt-Bt-Bg-Bc-Bt-Bg-Bc-Bt-Bc-Bt-Bt-Bt-Bt-Bc-Bc -CH2CH2OH
(x′
)(xi′
) a compound represented by formula (xi′
);
HO-Bt-Bt-Bt-Bt-Bc-Bc-Ba-Bg-Bg-Bt-Bt-Bc-Ba—
Ba-Bg-Bt-Bg-Bg-CH2CH2OH
(xi′
)(xii′
) a compound represented by formula (xii′
);
HO-Bc-Bt-Bg-Bc-Bt-Bt-Bc-Bc-Bt-Bc-Bc-Ba—
Ba-Bc-Bc-CH2CH2OH
(xii′
)(xiii′
) a compound represented by formula (xiii′
);
HO-Bg-Bt-Bt-Ba-Bt-Bc-Bt-Bg-Bc-Bt-Bt-Bc-Bc-Bt-Bc-Bc-Ba—
Ba-Bc-Bc-CH2CH2OH
(xiii′
)where Bg is a group represented by formula (G1) or (G2);
Ba is a group represented by formula (A1) or (A2);
Bc is a group represented by formula (C1) or (C2); and
Bt is a group represented by formula (U1) or (T2);
where X is individually and independently a group represented by formula (X1) or (X2);
Y is individually and independently a hydrogen atom, a hydroxyl group or an alkoxy group with 1-6 carbon atoms; and
Z is individually and independently a single bond or an alkylene group with 1-5 carbon atoms.
- ) to (xiii′
-
71. The compound according to claim 69 which is represented by any one of compounds (I′
- 1) to (I′
20), or a pharmacologically acceptable salt thereof;
HO—
Ba**-Bg**-Bt**-Bt**-Bg**-Ba*-Bg*-Bt*-Bc*-Bt*-Bt*-Bc*-Bg*-Ba*—
Ba*—
Ba*-Bc*-Bt*-Bg**-Ba**-Bg**-Bc**-Ba**—
CH2CH2OH
(I′
1)
HO—
Ba**-Bg**-Bt**-Bt**-Bg**-Ba**-Bg**-Bt**-Bc*-Bt*-Bt*-Bc*-Bg*-Ba*—
Ba*—
Ba**-Bc**-Bt**-Bg**-Ba**-Bg**-Bc**-Ba**—
CH2CH2OH
(I′
2)
HO—
Ba**—
Ba**—
Ba**-Bc**-Bt**-Bg*-Ba*-Bg*-Bc*-Ba*—
Ba*—
Ba*-Bt*-Bt**-Bt**-Bg**-Bc**-Bt**-CH2CH2OH
(I′
3)
HO-Bt**-Bt**-Bg**-Ba**-Bg**-Bt*-Bc*-Bt*-Bt*-Bc*-Ba*—
Ba*—
Ba*—
Ba**-Bc**-Bt**-Bg**-Ba**—
CH2CH2OH
(I′
4)
HO-Bg**-Bt**-Bg**-Bc**-Ba**—
Ba*—
Ba*-Bg*-Bt*-Bt*-Bg*-Ba*-Bg*-Bt**-Bc**-Bt**-Bt**-Bc**-CH2CH2OH
(I′
5)
HO-Bt**-Bt**-Bg*-Ba*-Bg*-Bt**-Bc**-Bt**-Bt**-Bc**-Ba*—
Ba*—
Ba*—
Ba*-Bc**-Bt**-Bg*-Ba*—
CH2CH2OH
(I′
6)
HO-Bg*-Bt**-Bg*-Bc**-Ba*—
Ba*—
Ba*-Bg*-Bt**-Bt**-Bg*-Ba*-Bg*-Bt**-Bc**-Bt**-Bt**-Bc**-CH2CH2OH
(I′
7)
HO-Bg**-Bc**-Bc**-Bg**-Bc**-Bt*-Bg*-Bc*-Bc*-Bc*-Ba**—
Ba**-Bt**-Bg**-Bc**-CH2CH2OH
(I′
8)
HO-Bc**-Bg*-Bc**-Bt**-Bg*-Bc*-Bc**-Bc**-Ba*—
Ba*-Bt**-Bg*-Bc**-Bc**-Ba*-Bt*-Bc**-Bc**-CH2CH2OH
(I′
9)
HO-Bc**-Ba*-Bg*-Bt**-Bt**-Bt*-Bg*-Bc**-Bc**-Bg*-Bc**-Bt**-Bg*-Bc**-Bc**-Bc**-Ba*—
Ba*—
CH2CH2OH
(I′
10)
HO-Bt**-Bg*-Bt**-Bt**-Bc**-Bt**-Bg*-Ba*-Bc**-Ba*—
Ba*-Bc**-Ba*-Bg*-Bt**-Bt**-Bt**-Bg*-CH2CH2OH
(I′
11)
HO-Bc**-Bg*-Bc**-Bt**-Bg*-Bc*-Bc**-Bc**-Ba*—
Ba*-Bt**-Bg*-Bc**-Bc**-Ba*-Bt*-Bc**-Bc**-CH2CH2OH
(I′
12)
HO-Bg**-Bc**-Bt**-Bt**-Bt**-Bt*-Bc*-Bt*-Bt*-Bt*-Ba*-Bg*-Bt*-Bt*-Bg**-Bc**-Bt**-Bg**-Bc**-CH2CH2OH
(I′
13)
HO-Bc*-Bt*-Bt*-Bt*-Bt*-Ba**-Bg**-Bt**-Bt**-Bg**-Bc**-Bt**-Bg**-Bc**-Bt**-Bc**-Bt**-Bt*-Bt*-Bt*-Bc*-Bc*-CH2CH2OH
(I′
14)
HO-Bc**-Bt**-Bg**-Bc**-Bt**-Bt*-Bc*-Bc*-Bt*-Bc*-Bc**-Ba**—
Ba**-Bc**-Bc**-CH2CH2OH
(I′
15)
HO-Bg**-Bt**-Bt**-Ba**-Bt**-Bc*-Bt*-Bg*-Bc*-Bt*-Bt*-Bc*-Bc*-Bt*-Bc*-Bc**-Ba**—
Ba**-Bc**-Bc**-CH2CH2OH
(I′
16)
HO-Bc**-Bt**-Bt**-Bt**-Bt**-Ba*-Bg*-Bt*-Bt*-Bg*-Bc*-Bt*-Bg*-Bc*-Bt*-Bc*-Bt*-Bt**-Bt**-Bt**-Bc**-Bc**-CH2CH2OH
(I′
17)
HO-Bt**-Bt**-Bt**-Bt**-Bc**-Bc*-Ba*-Bg*-Bg*-Bt*-Bt*-Bc*-Ba*—
Ba**-Bg**-Bt**-Bg**-Bg**-CH2CH2OH
(I′
18)
HO-Bc**-Bt*-Bg*-Bc**-Bt*-Bt*-Bc**-Bc**-Bt*-Bc**-Bc**-Ba*—
Ba*-Bc**-Bc**-CH2CH2OH
(I′
19)
HO-Bc**-Bt**-Bg*-Bc**-Bt**-Bc*-Bc**-Bt*-Bc*-Bc**-Ba*—
Ba*-Bc**-Bc**-CH2CH2OH
(I′
20)where Bg* is a group represented by formula (G1a);
Ba* is a group represented by formula (A1a);
Bc* is a group represented by formula (C1a);
Bt* is a group represented by formula (U1a);
Bg** is a group represented by formula (G2);
Ba** is a group represented by formula (A2);
Bc** is a group represented by formula (C2); and
Bt** is a group represented by formula (T2);
where X is individually and independently a group represented by formula (X1) or (X2);
R1 is individually and independently an alkyl group with 1-6 carbon atoms; and
Z is individually and independently a single bond or an alkylene group with 1-5 carbon atoms;
- 1) to (I′
-
72. The compound according to claim 71 which is represented by any one of formulae (I′
- 1-a) to (I′
20-b), or a pharmacologically acceptable salt thereof;
- 1-a) to (I′
-
73. The compound according to claim 69 which is selected from the group consisting of compounds (i″
- ) to (xlix″
), or a pharmacologically acceptable salt thereof;
(i″
) a compound represented by formula (i″
);
HO-Bg-Ba—
Ba—
Ba—
Ba-Bc-Bg-Bc-Bc-Bg-Bc-Bc-Ba-Bt-Bt-Bt-Bc-Bt-CH2CH2OH
(i″
)(ii″
) a compound represented by formula (ii″
);
HO-Bc-Bt-Bg-Bt-Bt-Ba-Bg-Bc-Bc-Ba-Bc-Bt-Bg-Ba-Bt-Bt-Ba—
Ba—
CH2CH2OH
(ii″
)(iii″
) a compound represented by formula (iii″
);
HO-Bt-Bg-Ba-Bg-Ba—
Ba—
Ba-Bc-Bt-Bg-Bt-Bt-Bc-Ba-Bg-Bc-Bt-Bt-CH2CH2OH
(iii″
)(iv″
) a compound represented by formula (iv″
);
HO-Bc-Ba-Bg-Bg-Ba—
Ba-Bt-Bt-Bt-Bg-Bt-Bg-Bt-Bc-Bt-Bt-Bt-Bc-CH2CH2OH
(iv″
)(v″
) a compound represented by formula (v″
);
HO-Bg-Bt-Ba-Bt-Bt-Bt-Ba-Bg-Bc-Ba-Bt-Bg-Bt-Bt-Bc-Bc-Bc-Ba—
CH2CH2OH
(v″
)(vi″
) a compound represented by formula (vi″
);
HO—
Ba-Bg-Bc-Ba-Bt-Bg-Bt-Bt-Bc-Bc-Bc-Ba—
Ba-Bt-Bt-Bc-Bt-Bc-CH2CH2OH
(vi″
)(vii″
) a compound represented by formula (vii″
);
HO-Bg-Bc-Bc-Bg-Bc-Bc-Ba-Bt-Bt-Bt-Bc-Bt-Bc-Ba—
Ba-Bc-Ba-Bg-CH2CH2OH
(vii″
)(viii″
) a compound represented by formula (viii″
);
HO-Bc-Ba-Bt-Ba—
Ba-Bt-Bg-Ba—
Ba—
Ba—
Ba-Bc-Bg-Bc-Bc-Bg-Bc-Bc-CH2CH2OH
(viii″
)(ix″
) a compound represented by formula (ix″
);
HO-Bt-Bt-Bc-Bc-Bc-Ba—
Ba-Bt-Bt-Bc-Bt-Bc-Ba-Bg-Bg-Ba—
Ba-Bt-CH2CH2OH
(ix″
)(x″
) a compound represented by formula (x″
);
HO-Bc-Bc-Ba-Bt-Bt-Bt-Bg-Bt-Ba-Bt-Bt-Bt-Ba-Bg-Bc-Ba-Bt-Bg-CH2CH2OH
(x″
)(xi″
) a compound represented by formula (xi″
);
HO-Bc-Bt-Bc-Ba-Bg-Ba-Bt-Bc-Bt-Bt-Bc-Bt-Ba—
Ba-Bc-Bt-Bt-Bc-CH2CH2OH
(xi″
)(xii″
) a compound represented by formula (xii″
);
HO—
Ba-Bc-Bc-Bg-Bc-Bc-Bt-Bt-Bc-Bc-Ba-Bc-Bt-Bc-Ba-Bg-Ba-Bg-CH2CH2OH
(xii″
)(xiii″
) a compound represented by formula (xiii″
);
HO-Bt-Bc-Bt-Bt-Bg-Ba—
Ba-Bg-Bt-Ba—
Ba—
Ba-Bc-Bg-Bg-Bt-Bt-Bt-CH2CH2OH
(xiii″
)(xiv″
) a compound represented by formula (xiv″
);
HO-Bg-Bg-Bc-Bt-Bg-Bc-Bt-Bt-Bt-Bg-Bc-Bc-Bc-Bt-Bc-Ba-Bg-Bc-CH2CH2OH
(xiv″
)(xv″
) a compound represented by formula (xv″
);
HO—
Ba-Bg-Bt-Bc-Bc-Ba-Bg-Bg-Ba-Bg-Bc-Bt-Ba-Bg-Bg-Bt-Bc-Ba—
CH2CH2OH
(xv″
)(xvi″
) a compound represented by formula (xvi″
);
HO-Bg-Bc-Bt-Bc-Bc-Ba—
Ba-Bt-Ba-Bg-Bt-Bg-Bg-Bt-Bc-Ba-Bg-Bt-CH2CH2OH
(xvi″
)(xvii″
) a compound represented by formula (xvii″
);
HO-Bg-Bc-Bt-Ba-Bg-Bg-Bt-Bc-Ba-Bg-Bg-Bc-Bt-Bg-Bc-Bt-Bt-Bt-CH2CH2OH
(xvii″
)(xviii″
) a compound represented by formula (xviii″
);
HO-Bg-Bc-Ba-Bg-Bc-Bc-Bt-Bc-Bt-Bc-Bg-Bc-Bt-Bc-Ba-Bc-Bt-Bc-CH2CH2OH
(xviii″
)(xix″
) a compound represented by formula (xix″
);
HO-Bt-Bc-Bt-Bt-Bc-Bc-Ba—
Ba—
Ba-Bg-Bc-Ba-Bg-Bc-Bc-Bt-Bc-Bt-CH2CH2OH
(xix″
)(xx″
) a compound represented by formula (xx″
);
HO-Bt-Bg-Bc-Ba-Bg-Bt-Ba—
Ba-Bt-Bc-Bt-Ba-Bt-Bg-Ba-Bg-Bt-Bt-CH2CH2OH
(xx″
)(xxi″
) a compound represented by formula (xxi″
);
HO-Bg-Bt-Bt-Bt-Bc-Ba-Bg-Bc-Bt-Bt-Bc-Bt-Bg-Bt-Ba—
Ba-Bg-Bc-CH2CH2OH
(xxi″
)(xxii″
) a compound represented by formula (xxii″
);
HO-Bt-Bg-Bt-Ba-Bg-Bg-Ba-Bc-Ba-Bt-Bt-Bg-Bg-Bc-Ba-Bg-Bt-Bt-CH2CH2OH
(xxii″
)(xxiii″
) a compound represented by formula (xxiii″
);
HO-Bt-Bc-Bc-Bt-Bt-Ba-Bc-Bg-Bg-Bg-Bt-Ba-Bg-Bc-Ba-Bt-Bc-Bc-CH2CH2OH
(xxiii″
)(xxiv″
) a compound represented by formula (xxiv″
);
HO—
Ba-Bg-Bc-Bt-Bc-Bt-Bt-Bt-Bt-Ba-Bc-Bt-Bc-Bc-Bc-Bt-Bt-Bg-CH2CH2OH
(xxiv″
)(xxv″
) a compound represented by formula (xxv″
);
HO-Bc-Bc-Ba-Bt-Bt-Bg-Bt-Bt-Bt-Bc-Ba-Bt-Bc-Ba-Bg-Bc-Bt-Bc-CH2CH2OH
(xxv″
)(xxvi″
) a compound represented by formula (xxvi″
);
HO-Bc-Bt-Ba-Bt-Bg-Ba-Bg-Bt-Bt-Bt-Bc-Bt-Bt-Bc-Bc-Ba—
Ba—
Ba—
CH2CH2OH
(xxvi″
)(xxvii″
) a compound represented by formula (xxvii″
);
D-Bt-Bg-Bt-Bg-Bt-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-Bt-Ba—
Ba-Bc-Ba-Bg-Bt-CH2CH2OH
(xxvii″
)(xxviii″
) a compound represented by formula (xxviii″
);
D-Ba-Bg-Bg-Bt-Bt-Bg-Bt-Bg-Bt-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-Bt-Ba—
Ba—
CH2CH2OH
(xxviii″
)(xxix″
) a compound represented by formula (xxix″
);
D-Ba-Bg-Bt-Ba—
Ba-Bc-Bc-Ba-Bc-Ba-Bg-Bg-Bt-Bt-Bg-Bt-Bg-Bt-Bc-Ba—
CH2CH2OH
(xxix″
)(xxx″
) a compound represented by formula (xxx″
);
D-Bt-Bt-Bg-Ba-Bt-Bc-Ba—
Ba-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
Ba-Bg-Bc-Bc-CH2CH2OH
(xxx″
)(xxxi″
) a compound represented by formula (xxxi″
);
D-Bc-Ba-Bc-Bc-Bc-Bt-Bc-Bt-Bg-Bt-Bg-Ba-Bt-Bt-Bt-Bt-Ba-Bt-Ba—
Ba—
CH2CH2OH
(xxxi″
)(xxxii″
) a compound represented by formula (xxxii″
);
D-Ba-Bc-Bc-Bc-Ba-Bc-Bc-Ba-Bt-Bc-Ba-Bc-Bc-Bc-Bt-Bc-Bt-Bg-Bt-Bg-CH2CH2OH
(xxxii″
)(xxxiii″
) a compound represented by formula (xxxiii″
);
D-Bc-Bc-Bt-Bc-Ba—
Ba-Bg-Bg-Bt-Bc-Ba-Bc-Bc-Bc-Ba-Bc-Bc-Ba-Bt-Bc-CH2CH2OH
(xxxiii″
)(xxxiv″
) a compound represented by formula (xxxiv″
);
HO-Bt-Ba—
Ba-Bc-Ba-Bg-Bt-Bc-Bt-Bg-Ba-Bg-Bt-Ba-Bg-Bg-Ba-Bg-CH2CH2OH
(xxxiv″
)(xxxv″
) a compound represented by formula (xxxv″
);
HO-Bg-Bg-Bc-Ba-Bt-Bt-Bt-Bc-Bt-Ba-Bg-Bt-Bt-Bt-Bg-Bg-Ba-Bg-CH2CH2OH
(xxxv″
)(xxxvi″
) a compound represented by formula (xxxvi″
);
HO—
Ba-Bg-Bc-Bc-Ba-Bg-Bt-Bc-Bg-Bg-Bt-Ba—
Ba-Bg-Bt-Bt-Bc-Bt-CH2CH2OH
(xxxvi″
)(xxxvii″
) a compound represented by formula (xxxvii″
);
HO—
Ba-Bg-Bt-Bt-Bt-Bg-Bg-Ba-Bg-Ba-Bt-Bg-Bg-Bc-Ba-Bg-Bt-Bt-CH2CH2OH
(xxxvii″
)(xxxviii″
) a compound represented by formula (xxxviii″
);
HO-Bc-Bt-Bg-Ba-Bt-Bt-Bc-Bt-Bg-Ba—
Ba-Bt-Bt-Bc-Bt-Bt-Bt-Bc-CH2CH2OH
(xxxviii″
)(xxxix″
) a compound represented by formula (xxxix″
);
HO-Bt-Bt-Bc-Bt-Bt-Bg-Bt-Ba-Bc-Bt-Bt-Bc-Ba-Bt-Bc-Bc-Bc-Ba—
CH2CH2OH
(xxxix″
)(xl″
) a compound represented by formula (xl″
);
HO-Bc-Bc-Bt-Bc-Bc-Bg-Bg-Bt-Bt-Bc-Bt-Bg-Ba—
Ba-Bg-Bg-Bt-Bg-CH2CH2OH
(xl″
)(xli″
) a compound represented by formula (xli″
);
HO-Bc-Ba-Bt-Bt-Bt-Bc-Ba-Bt-Bt-Bc-Ba—
Ba-Bc-Bt-Bg-Bt-Bt-Bg-CH2CH2OH
(xli″
)(xlii″
) a compound represented by formula (xlii″
);
HO-Bt-Bt-Bc-Bc-Bt-Bt-Ba-Bg-Bc-Bt-Bt-Bc-Bc-Ba-Bg-Bc-Bc-Ba—
CH2CH2OH
(xlii″
)(xliii″
) a compound represented by formula (xliii″
);
HO-Bt-Ba—
Ba-Bg-Ba-Bc-Bc-Bt-Bg-Bc-Bt-Bc-Ba-Bg-Bc-Bt-Bt-Bc-CH2CH2OH
(xliii″
)(xliv″
) a compound represented by formula (xliv″
);
HO-Bc-Bt-Bt-Bg-Bg-Bc-Bt-Bc-Bt-Bg-Bg-Bc-Bc-Bt-Bg-Bt-Bc-Bc-CH2CH2OH
(xliv″
)(xlv″
) a compound represented by formula (xlv″
);
HO-Bc-Bt-Bc-Bc-Bt-Bt-Bc-Bc-Ba-Bt-Bg-Ba-Bc-Bt-Bc-Ba—
Ba-Bg-CH2CH2OH
(xlv″
)(xlvi″
) a compound represented by formula (xlvi″
);
HO-Bc-Bt-Bg-Ba—
Ba-Bg-Bg-Bt-Bg-Bt-Bt-Bc-Bt-Bt-Bg-Bt-Ba-Bc-CH2CH2OH
(xlvi″
)(xlvii″
) a compound represented by formula (xlvii″
);
HO-Bt-Bt-Bc-Bc-Ba-Bg-Bc-Bc-Ba-Bt-Bt-Bg-Bt-Bg-Bt-Bt-Bg-Ba—
CH2CH2OH
(xlvii″
)(xlviii″
) a compound represented by formula (xlviii″
);
HO-Bc-Bt-Bc-Ba-Bg-Bc-Bt-Bt-Bc-Bt-Bt-Bc-Bc-Bt-Bt-Ba-Bg-Bc-CH2CH2OH
(xlviii″
)(xlix″
) a compound represented by formula (xlix″
);
HO-Bg-Bc-Bt-Bt-Bc-Bt-Bt-Bc-Bc-Bt-Bt-Ba-Bg-Bc-Bt-Bt-Bc-Bc-CH2CH2OH
(xlix″
)where Bg is a group represented by formula (G1) or (G2);
Ba is a group represented by formula (A1) or (A2);
Bc is a group represented by formula (C1) or (C2);
Bt is a group represented by formula (U1) or (T2); and
D is HO—
or Ph- wherein Ph- is a group represented by first formula;
where X is individually and independently a group represented by formula (X1) or (X2);
Y is individually and independently a hydrogen atom, a hydroxyl group or an alkoxy group with 1-6 carbon atoms; and
Z is individually and independently a single bond or an alkylene group with 1-5 carbon atoms.
- ) to (xlix″
-
74. The compound according to claim 69 which is selected from the group consisting of compounds (i″
- -a) to (1i″
-a), or a pharmacologically acceptable salt thereof;
(i″
-a) a compound represented by formula (i″
-a);
HO-Bg-Ba—
Ba—
Ba—
Ba-Bc-Bg-Bc-Bc-Bg-Bc-Bc-Ba-B′
t-B′
u-B′
u-Bc-B′
t-CH2CH2OH
(i″
-a)(ii″
-a) a compound represented by formula (ii″
-a);
HO-Bc-B′
t-Bg-B′
u-B′
t-Ba-Bg-Bc-Bc-Ba-Bc-B′
t-Bg-Ba-B′
t-B′
t-Ba—
Ba—
CH2CH2OH
(ii″
-a)(iii″
-a) a compound represented by formula (iii″
-a);
HO-B′
t-Bg-Ba-Bg-Ba—
Ba—
Ba-Bc-B′
t-Bg-B′
t-B′
u-Bc-Ba-Bg-Bc-B′
u-B′
t-CH2CH2OH
(iii″
-a)(iv″
-a) a compound represented by formula (iv″
-a);
HO-Bc-Ba-Bg-Bg-Ba—
Ba-B′
t-B′
t-B′
u-Bg-B′
t-Bg-B′
u-Bc-B′
u-B′
u-B′
t-Bc-CH2CH2OH
(iv″
-a)(v″
-a) a compound represented by formula (v″
-a);
HO-Bg-B′
t-Ba-B′
u-B′
t-B′
t-Ba-Bg-Bc-Ba-B′
t-Bg-B′
u-B′
t-Bc-Bc-Bc-Ba—
CH2CH2OH
(v″
-a)(vi″
-a) a compound represented by formula (vi″
-a);
HO—
Ba-Bg-Bc-Ba-B′
t-Bg-B′
t-B′
t-Bc-Bc-Bc-Ba—
Ba-B′
t-B′
u-Bc-B′
t-Bc-CH2CH2OH
(vi″
-a)(vii″
-a) a compound represented by formula (vii″
-a);
HO-Bg-Bc-Bc-Bg-Bc-Bc-Ba-B′
t-B′
u-B′
u-Bc-B′
u-Bc-Ba—
Ba-Bc-Ba-Bg-CH2CH2OH
(vii″
-a)(viii″
-a) a compound represented by formula (viii″
-a);
HO-Bc-Ba-B′
t-Ba—
Ba-B′
t-Bg-Ba—
Ba—
Ba—
Ba-Bc-Bg-Bc-Bc-Bg-Bc-Bc-CH2CH2OH
(viii″
-a)(ix″
-a) a compound represented by formula (ix″
-a);
HO-B′
t-B′
u-Bc-Bc-Bc-Ba—
Ba-B′
t-B′
u-Bc-B′
t-Bc-Ba-Bg-Bg-Ba—
Ba-B′
t-CH2CH2OH
(ix″
-a)(x″
-a) a compound represented by formula (x″
-a);
HO-Bc-Bc-Ba-B′
u-B′
t-B′
u-Bg-B′
t-Ba-B′
u-B′
t-B′
t-Ba-Bg-Bc-Ba-B′
t-Bg-CH2CH2OH
(x″
-a)(xi″
-a) a compound represented by formula (xi″
-a);
HO-Bc-B′
t-Bc-Ba-Bg-Ba-B′
t-Bc-B′
-u-B′
u-Bc-B′
t-Ba—
Ba-Bc-B′
u-B′
u-Bc-CH2CH2OH
(xi″
-a)(xii″
-a) a compound represented by formula (xii″
-a);
HO—
Ba-Bc-Bc-Bg-Bc-Bc-B′
t-B′
u-Bc-Bc-Ba-Bc-B′
t-Bc-Ba-Bg-Ba-Bg-CH2CH2OH
(xii″
-a)(xiii″
-a) a compound represented by formula (xiii″
-a);
HO-B′
t-Bc-B′
t-B′
t-Bg-Ba—
Ba-Bg-B′
t-Ba—
Ba—
Ba-Bc-Bg-Bg-B′
t-B′
u-B′
t-CH2CH2OH
(xiii″
-a)(xiv″
-a) a compound represented by formula (xiv″
-a);
HO-Bg-Bg-Bc-B′
t-Bg-Bc-B′
t-B′
t-B′
u-Bg-Bc-Bc-Bc-B′
t-Bc-Ba-Bg-Bc-CH2CH2OH
(xiv″
-a)(xv″
-a) a compound represented by formula (xv″
-a);
HO—
Ba-Bg-B′
t-Bc-Bc-Ba-Bg-Bg-Ba-Bg-Bc-B′
t-Ba-Bg-Bg-B′
t-Bc-Ba—
CH2CH2OH
(xv″
-a)(xvi″
-a) a compound represented by formula (xvi″
-a);
HO-Bg-Bc-B′
t-Bc-Bc-Ba—
Ba-B′
t-Ba-Bg-B′
t-Bg-Bg-B′
t-Bc-Ba-Bg-B′
t-CH2CH2OH
(xvi″
-a)(xvii″
-a) a compound represented by formula (xvii″
-a);
HO-Bg-Bc-B′
t-Ba-Bg-Bg-B′
t-Bc-Ba-Bg-Bg-Bc-B′
t-Bg-Bc-B′
t-B′
t-B′
u-CH2CH2OH
(xvii″
-a)(xviii″
-a) a compound represented by formula (xviii″
-a);
HO-Bg-Bc-Ba-Bg-Bc-Bc-B′
u-Bc-B′
t-Bc-Bg-Bc-B′
t-Bc-Ba-Bc-B′
t-Bc-CH2CH2OH
(xviii″
-a)(xix″
-a) a compound represented by formula (xix″
-a);
HO-B′
t-Bc-B′
u-B′
u-Bc-Bc-Ba—
Ba—
Ba-Bg-Bc-Ba-Bg-Bc-Bc-B′
u-Bc-B′
t-CH2CH2OH
(xix″
-a)(xx″
-a) a compound represented-by formula (xx″
-a);
HO-B′
t-Bg-Bc-Ba-Bg-B′
t-Ba—
Ba-B′
t-Bc-B′
u-Ba-B′
t-Bg-Ba-Bg-B′
t-B′
t-CH2CH2OH
(xx″
-a)(xxi″
-a) a compound represented by formula (xxi″
-a);
HO-Bg-B′
t-B′
t-B′
u-Bc-Ba-Bg-Bc-B′
u-B′
t-Bc-B′
t-Bg-B′
t-Ba—
Ba-Bg-Bc-CH2CH2OH
(xxi″
-a)(xxii″
-a) a compound represented by formula (xxii″
-a);
HO-B′
t-Bg-B′
t-Ba-Bg-Bg-Ba-Bc-Ba-B′
t-B′
t-Bg-Bg-Bc-Ba-Bg-B′
t-B′
t-CH2CH2OH
(xxii″
-a)(xxiii″
-a) a compound represented by formula (xxiii″
-a)
HO-B′
t-Bc-Bc-B′
t-B′
t-Ba-Bc-Bg-Bg-Bg-B′
t-Ba-Bg-Bc-Ba-B′
u-Bc-Bc-CH2CH2OH
(xxiii″
-a)(xxiv″
-a) a compound represented by formula (xxiv″
-a);
HO—
Ba-Bg-Bc-B′
t-Bc-B′
u-B′
t-B′
u-B′
t-Ba-Bc-B′
t-Bc-Bc-Bc-B′
t-B′
t-Bg-CH2CH2OH
(xxiv″
-a)(xxv″
-a) a compound represented by formula (xxv″
-a);
HO-Bc-Bc-Ba-B′
u-B′
t-Bg-B′
u-B′
t-B′
u-Bc-Ba-B′
u-Bc-Ba-Bg-Bc-B′
t-Bc-CH2CH2OH
(xxv″
-a)(xxvi″
-a) a compound represented by formula (xxvi″
-a);
HO-Bc-B′
t-Ba B′
t-Bg-Ba-Bg-B′
t-B′
t-B′
t-Bc-B′
t-B′
t-Bc-Bc-Ba—
Ba—
Ba—
CH2CH2OH
(xxvi″
-a)(xxvii″
-a) a compound represented by formula (xxvii″
-a);
D-B′
t-Bg-B′
t-Bg-B′
t-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-B′
u-Ba—
Ba-Bc-Ba-Bg-B′
t-CH2CH2OH
(xxvii″
-a)(xxviii″
-a) a compound represented by formula (xxviii″
-a);
D-Ba-Bg-Bg-B′
t-B′
t-Bg-B′
u-Bg-B′
u-Bc-Ba-Bc-Bc-Ba-Bg-Ba-Bg-B′
t-Ba—
Ba—
CH2CH2OH
(xxviii″
-a)(xxix″
-a) a compound represented by formula (xxix″
-a);
D-Ba-Bg-B′
t-Ba—
Ba-Bc-Bc-Ba-Bc-Ba-Bg-Bg-B′
u-B′
u-Bg-B′
t-Bg-B′
t-Bc-Ba—
CH2CH2OH
(xxix″
-a)(xxx″
-a) a compound represented by formula (xxx″
-a);
D-B′
t-B′
t-Bg-Ba-B′
t-Bc-Ba—
Ba-Bg-Bc-Ba-Bg-Ba-Bg-Ba—
Ba—
Ba-Bg-Bc-Bc-CH2CH2OH
(xxx″
-a)(xxxi″
-a) a compound represented by formula (xxxi″
-a);
D-Bc-Ba-Bc-Bc-Bc-B′
u-Bc-B′
u-Bg-B′
u-Bg-Ba-B′
u-B′
u-B′
u-B′
t-Ba-B′
t-Ba—
Ba—
CH2CH2OH
(xxxi″
-a)(xxxii″
-a) a compound represented by formula (xxxii″
-a);
D-Ba-Bc-Bc-Bc-Ba-Bc-Bc-Ba-B′
u-Bc-Ba-Bc-Bc-Bc-B′
u-Bc-B′
t-Bg-B′
t-Bg-CH2CH2OH
(xxxii″
-a)(xxxiii″
-a) a compound represented by formula (xxxiii″
-a);
D-Bc-Bc-B′
t-Bc-Ba—
Ba-Bg-Bg-B′
u-Bc-Ba-Bc-Bc-Bc-Ba-Bc-Bc-Ba-B′
t-Bc-CH2CH2OH
(xxxiii″
-a)(xxxiv″
-a) a compound represented by formula (xxxiv″
-a);
HO-B′
t-Ba—
Ba-Bc-Ba-Bg-B′
u-Bc-B′
u-Bg-Ba-Bg-B′
u-Ba-Bg-Bg-Ba-Bg-CH2CH2OH
(xxxiv″
-a)(xxxv″
-a) a compound represented by formula (xxxv″
-a);
HO-Bg-Bg-Bc-Ba-B′
t-B′
u-B′
u-Bc-B′
u-Ba-Bg-B′
u-B′
u-B′
t-Bg-Bg-Ba-Bg-CH2CH2OH
(xxxv″
-a)(xxxvi″
-a) a compound represented by formula (xxxvi″
-a);
HO—
Ba-Bg-Bc-Bc-Ba-Bg-B′
u-Bc-Bg-Bg-B′
u-Ba—
Ba-Bg-B′
t-B′
t-Bc-B′
t-CH2CH2OH
(xxxvi″
-a)(xxxvii″
-a) a compound represented by formula (xxxvii″
-a);
HO—
Ba-Bg-B′
t-B′
t-B′
t-Bg-Bg-Ba-Bg-Ba-B′
u-Bg-Bg-Bc-Ba-Bg-B′
t-B′
t-CH2CH2OH
(xxxvii″
-a)(xxxviii″
-a) a compound represented by formula (xxxviii″
-a);
HO-Bc-B′
t-Bg-Ba-B′
t-B′
t-Bc-B′
t-Bg-Ba—
Ba-B′
t-B′
t-Bc-B′
u-B′
u-B′
t-Bc-CH2CH2OH
(xxxviii″
-a)(xxxix″
-a) a compound represented by formula (xxxix″
-a);
HO-B′
t-B′
t-Bc-B′
t-B′
t-Bg-B′
t-Ba-Bc-B′
t-B′
t-Bc-Ba-B′
t-Bc-Bc-Bc-Ba—
CH2CH2OH
(xxxix″
-a)(xl″
-a) a compound represented by formula (xl″
-a);
HO-Bc-Bc-B′
t-Bc-Bc-Bg-Bg-B′
t-B′
t-Bc-B′
t-Bg-Ba—
Ba-Bg-Bg-B′
t-Bg-CH2CH2OH
(xl″
-a)(xli″
-a) a compound represented by formula (xli″
-a);
HO-Bc-Ba-B′
t-B′
t-B′
t-Bc-Ba-B′
u-B′
t-Bc-Ba—
Ba-Bc-B′
t-Bg-B′
t-B′
t-Bg-CH2CH2OH
(xli″
-a)(xlii″
-a) a compound represented by formula (xlii″
-a);
HO-B′
t-B′
t-Bc-Bc-B′
t-B′
t-Ba-Bg-Bc-B′
t-B′
u-Bc-Bc-Ba-Bg-Bc-Bc-Ba—
CH2CH2OH
(xlii″
-a)(xliii″
-a) a compound represented by formula (xliii″
-a);
HO-B′
t-Ba—
Ba-Bg-Ba-Bc-Bc-B′
t-Bg-Bc-B′
t-Bc-Ba-Bg-Bc-B′
u-B′
t-Bc-CH2CH2OH
(xliii″
-a)(xliv″
-a) a compound represented by formula (xliv″
-a);
HO-Bc-B′
t-B′
t-Bg-Bg-Bc-B′
t-Bc-B′
t-Bg-Bg-Bc-Bc-B′
t-Bg-B′
u-Bc-Bc-CH2CH2OH
(xliv″
-a)(xlv″
-a) a compound represented by formula (xlv″
-a);
HO-Bc-B′
t-Bc-Bc-B′
t-B′
u-Bc-Bc-Ba-B′
t-Bg-Ba-Bc-B′
t-Bc-Ba—
Ba-Bg-CH2CH2OH
(xlv″
-a)(xlvi″
-a) a compound represented by formula (xlvi″
-a);
HO-Bc-B′
t-Bg-Ba—
Ba-Bg-Bg-B′
t-Bg-B′
t-B′
t-Bc-B′
t-B′
t-Bg-B′
t-Ba-Bc-CH2CH2OH
(xlvi″
-a)(xlvii″
-a) a compound represented by formula (xlvii″
-a);
HO-B′
t-B′
t-Bc-Bc-Ba-Bg-Bc-Bc-Ba-B′
t-B′
t-Bg-B′
t-Bg-B′
t-B′
t-Bg-Ba—
CH2CH2OH
(xlvii″
-a)(xlviii″
-a) a compound represented by formula (xlviii″
-a);
HO-Bc-B′
t-Bc-Ba-Bg-Bc-B′
t-B′
u-Bc-B′
t-B′
t-Bc-Bc-B′
t-B′
t-Ba-Bg-Bc-CH2CH2OH
(xlviii″
-a)(xlix″
-a) a compound represented by formula (xlix″
-a);
HO-Bg-Bc-B′
t-B′
t-Bc-B′
u-B′
t-Bc-Bc-B′
u-B′
t-Ba-Bg-Bc-B′
u-B′
t-Bc-Bc-CH2CH2OH
(xlix″
-a)(1″
-a) a compound represented by formula (1″
-a);
HO-Bg-Bg-Bc-Ba-B′
t-B′
t-B′
u-Bc-B′
t-Ba-Bg-B′
u-B′
t-B′
t-Bg-Bg-Ba-Bg-CH2CH2OH
(1″
-a)(1i″
-a) a compound represented by formula (1i″
-a);
HO—
Ba-Bg-B′
t-B′
u-B′
t-Bg-Bg-Ba-Bg-Ba-B′
t-Bg-Bg-Bc-Ba-Bg-B′
t-B′
t-CH2CH2OH
(1i″
-a)where Bg is a group represented by formula (G1) or (G2);
Ba is a group represented by formula (A1) or (A2);
Bc is a group represented by formula (C1) or (C2);
B′
t is a group represented by formula (T2);
B′
u is a formula represented by formula (U1); and
D is HO—
or Ph- wherein Ph- is a group represented by first formula;
where X is individually and independently a group represented by formula (X1) or (X2);
Y is individually and independently a hydrogen atom, a hydroxyl group or an alkoxy group with 1-6 carbon atoms; and
Z is individually and independently a single bond or an alkylene group with 1-5 carbon atoms.
- -a) to (1i″
-
75. The compound according to claim 69 which is represented by any one of formulae (I″
- 1) to (I″
51), or a pharmacologically acceptable salt thereof;
HO-Bg*-Ba**—
Ba*—
Ba*—
Ba*-Bc**-Bg*-Bc**-Bc**-Bg*-Bc*-Bc**-Ba*-Bt**-Bu*-Bu*-Bc**-Bt**-CH2CH2OH
(I″
1 )
HO-Bc**-Bt**-Bg*-Bu*-Bt**-Ba*-Bg*-Bc**-Bc*-Ba*-Bc**-Bt**-Bg*-Ba*-Bt**-Bt**-Ba*—
Ba*—
CH2CH2OH
( I″
2)
HO-Bt**-Bg*-Ba*-Bg*-Ba**—
Ba*—
Ba*-Bc**-Bt**-Bg*-Bt**-Bu*-Bc**-Ba*-Bg*-Bc**-Bu*-Bt**-CH2CH2OH
(I″
3)
HO-Bc**-Ba*-Bg*-Bg*-Ba**—
Ba*-Bt**-Bt**-Bu*-Bg*-Bt**-Bg*-Bu*-Bc**-Bu*-Bu*-Bt**-Bc**-CH2CH2OH
(I″
4)
HO-Bg*-Bt**-Ba*-Bu*-Bt**-Bt**-Ba*-Bg*-Bc**-Ba*-Bt**-Bg*-Bu*-Bt**-Bc*-Bc**-Bc**-Ba*—
CH2CH2OH
(I″
5)
HO—
Ba*-Bg*-Bc**-Ba*-Bt**-Bg*-Bt**-Bt**-Bc*-Bc*-Bc**-Ba*-Ba*-Bt**-Bu*-Bc*-Bt**-Bc**-CH2CH2OH
(I″
6)
HO-Bg*-Bc**-Bc**-Bg*-Bc**-Bc*-Ba*-Bt**-Bu*-Bu*-Bc**-Bu*-Bc**-Ba*—
Ba*-Bc**-Ba**-Bg*-CH2CH2OH
(I″
7)
HO-Bc**-Ba*-Bt**-Ba*—
Ba*-Bt**-Bg*-Ba*—
Ba**—
Ba*—
Ba*-Bc**-Bg*-Bc*-Bc**-Bg*-Bc**-Bc**-CH2CH2OH
(I″
8)
HO-Bt**-Bu*-Bc**-Bc*-Bc**-Ba*—
Ba*-Bt**-Bu*-Bc*-Bt**-Bc**-Ba*-Bg*-Bg*-Ba*—
Ba*-Bt**-CH2CH2OH
(I″
9)
HO-Bc**-Bc**-Ba*-Bu*-Bt**-Bu*-Bg*-Bt**-Ba*-Bu*-Bt**-Bt**-Ba*-Bg*-Bc**-Ba*-Bt**-Bg*-CH2CH2OH
(I″
10)
HO-Bc*-Bt**-Bc**-Ba*-Bg*-Ba*-Bt**-Bc**-Bu*-Bu*-Bc**-Bt**-Ba*—
Ba*-Bc**-Bu*-Bu*-Bc**-CH2CH2OH
(I″
11)
HO—
Ba*-Bc**-Bc**-Bg*-Bc*-Bc**-Bt**-Bu*-Bc*-Bc**-Ba*-Bc*-Bt**-Bc**-Ba*-Bg*-Ba**-Bg*-CH2CH2OH
(I″
12)
HO-Bt**-Bc*-Bt**-Bt**-Bg*-Ba*—
Ba*-Bg*-Bt**-Ba*—
Ba**—
Ba*-Bc**-Bg*-Bg*-Bt**-Bu*-Bt**-CH2CH2OH
(I″
13)
HO-Bg*-Bg*-Bc**-Bt**-Bg*-Bc*-Bt**-Bt**-Bu*-Bg*-Bc**-Bc*-Bc*-Bt**-Bc**-Ba*-Bg*-Bc**-CH2CH2OH
(I″
14)
HO—
Ba*-Bg*-Bt**-Bc**-Bc**-Ba*-Bg*-Bg*-Ba**-Bg*-Bc**-Bt**-Ba*-Bg*-Bg*-Bt**-Bc**-Ba*—
CH2CH2OH
(I″
15)
HO-Bg*-Bc**-Bt**-Bc*-Bc**-Ba*—
Ba*-Bt**-Ba*-Bg*-Bt**-Bg*-Bg*-Bt**-Bc**-Ba*-Bg*-Bt**-CH2CH2OH
(I″
16)
HO-Bg*-Bc**-Bt**-Ba*-Bg*-Bg*-Bt**-Bc**-Ba*-Bg*-Bg*-Bc**-Bt**-Bg*-Bc*-Bt**-Bt**-Bu*-CH2CH2OH
(I″
17)
HO-Bg*-Bc**-Ba*-Bg*-Bc**-Bc**-Bu*-Bc*-Bt**-Bc*-Bg*-Bc**-Bt**-Bc*-Ba*-Bc**-Bt**-Bc*-CH2CH2OH
(I″
18)
HO-Bt**-Bc**-Bu*-Bu*-Bc**-Bc**-Ba*—
Ba*—
Ba*-Bg*-Bc**-Ba*-Bg*-Bc**-Bc*-Bu*-Bc**-Bt**-CH2CH2OH
(I″
19)
HO-Bt**-Bg*-Bc**-Ba*-Bg*-Bt**-Ba*—
Ba*-Bt**-Bc**-Bu*-Ba*-Bt**-Bg*-Ba*-Bg*-Bt**-Bt**-CH2CH2OH
(I″
20)
HO-Bg*-Bt**-Bt**-Bu*-Bc**-Ba*-Bg*-Bc**-Bu*-Bt**-Bc*-Bt**-Bg*-Bt**-Ba*—
Ba*-Bg*-Bc**-CH2CH2OH
(I″
21)
HO-Bt**-Bg*-Bt**-Ba*-Bg*-Bg*-Ba*-Bc**-Ba*-Bt**-Bt**-Bg*-Bg*-Bc**-Ba*-Bg*-Bt**-Bt**-CH2CH2OH
(I″
22)
HO-Bt**-Bc*-Bc*-Bt**-Bt**-Ba*-Bc**-Bg*-Bg*-Bg*-Bt**-Ba*-Bg*-Bc**-Ba*-Bu*-Bc**-Bc**-CH2CH2OH
(I″
23)
HO—
Ba*-Bg*-Bc**-Bt**-Bc*-Bu*-Bt**-Bu*-Bt**-Ba*-Bc*-Bt**-Bc**-Bc*-Bc*-Bt**-Bt**-Bg*-CH2CH2OH
(I″
24)
HO-Bc**-Bc**-Ba*-Bu*-Bt**-Bg*-Bu*-Bt**-Bu*-Bc**-Ba*-Bu*-Bc**-Ba*-Bg*-Bc*-Bt**-Bc**-CH2CH2OH
(I″
25)
HO-Bc*-Bt**-Bt**-Bg*-Ba*-Bg*-Bt**-Bt**-Bt**-Bc*-Bt**-Bt**-Bc*-Bc*-Ba*—
Ba**—
Ba*—
CH2CH2OH
(I″
26)
Ph-Bt**-Bg**-Bt**-Bg**-Bt**-Bc*-Ba*-Bc*-Bc*-Ba*-Bg*-Ba*-Bg*-Bu*-Ba*—
Ba**-Bc**-Ba**-Bg**-Bt**-CH2CH2OH
(I″
27)
Ph-Ba**-Bg**-Bg**-Bt**-Bt**-Bg*-Bu*-Bg*-Bu*-Bc*-Ba*-Bc*-Bc*-Ba*-Bg*-Ba**-Bg**-Bt**-Ba**—
Ba**—
CH2CH2OH
(I″
28)
Ph-Ba**-Bg**-Bt**-Ba**—
Ba**-Bc*-Bc*-Ba*-Bc*-Ba*-Bg*-Bg*-Bu*-Bu*-Bg*-Bt**-Bg**-Bt**-Bc**-Ba**—
CH2CH2OH
(I″
29)
Ph-Bt**-Bt**-Bg**-Ba**-Bt**-Bc*-Ba*—
Ba*-Bg*-Bc*-Ba*-Bg*-Ba*-Bg*-Ba*—
Ba**—
Ba**-Bg**-Bc**-Bc**-CH2CH2OH
(I″
30)
Ph-Bc**-Ba**-Bc**-Bc**-Bc**-Bu*-Bc*-Bu*-Bg*-Bu*-Bg*-Ba*-Bu*-Bu*-Bu*-Bt**-Ba**-Bt**-Ba**—
Ba**—
CH2CH2OH
(I″
31)
Ph-Ba**-Bc**-Bc**-Bc**-Ba**-Bc*-Bc*-Ba*-Bu*-Bc*-Ba*-Bc*-Bc*-Bc*-Bu*-Bc**-Bt**-Bg**-Bt**-Bg**-CH2CH2OH
(I″
32)
Ph-Bc**-Bc**-Bt**-Bc**-Ba**—
Ba*-Bg*-Bg*-Bu*-Bc*-Bc*-Bc*-Ba*-Bc**-Bc**-Ba**-Bt**-Bc**-CH2CH2OH
(I″
33)
HO-Bt**-Ba**—
Ba**-Bc**-Ba**-Bg*-Bu*-Bc*-Bu*-Bg*-Ba*-Bg*-Bu*-Ba**-Bg**-Bg**-Ba**-Bg**-CH2CH2OH
(I″
34)
HO-Bg**-Bg**-Bc**-Ba**-Bt**-Bu*-Bu*-Bc*-Bu*-Ba*-Bg*-Bu*-Bu*-Bt**-Bg**-Bg**-Ba**-Bg**-CH2CH2OH
(I″
35)
HO—
Ba**-Bg**-Bc**-Bc**-Ba**-Bg*-Bu*-Bc*-Bg*-Bg*-Bu*-Ba*—
Ba*-Bg**-Bt**-Bt**-Bc**-Bt**-CH2CH2OH
(I″
36)
HO—
Ba**-Bg**-Bt**-Bt**-Bt**-Bg*-Bg*-Ba*-Bg*-Ba*-Bu*-Bg*-Bg*-Bc**-Ba**-Bg**-Bt**-Bt**-CH2CH2OH
(I″
37)
HO-Bc**-Bt**-Bg*-Ba*-Bt**-Bt**-Bc*-Bt**-Bg*-Ba*—
Ba*-Bt**-Bt**-Bc**-Bu*-Bu*-Bt**-Bc**-CH2CH2OH
(I″
38)
HO-Bt**-Bt**-Bc*-Bt**-Bt**-Bg*-Bt**-Ba*-Bc*-Bt**-Bt**-Bc*-Ba*-Bt**-Bc*-Bc**-Bc**-Ba*—
CH2CH2OH
(I″
39)
HO-Bc**-Bc**-Bu*-Bc**-Bc**-Bg*-Bg*-Bt**-Bt**-Bc**-Bt**-Bg*-Ba*-Ba*-Bg*-Bg*-Bt**-Bg*-CH2CH2OH
(I″
40)
HO-Bc**-Ba*-Bt**-Bt**-Bu*-Bc**-Ba*-Bu*-Bt**-Bc**-Ba*—
Ba*-Bc**-Bt*-Bg*-Bt**-Bt**-Bg*-CH2CH2OH
(I″
41)
HO-Bt**-Bt**-Bc*-Bc*-Bt**-Bt*-Ba*-Bg*-Bc**-Bt**-Bu*-Bc*-Bc**-Ba*-Bg*-Bc**-Bc**-Ba*—
CH2CH2OH
(I″
42)
HO-Bt*-Ba*—
Ba*-Bg*-Ba*-Bc**-Bt**-Bg*-Bc**-Bt**-Bc**-Ba*-Bg*-Bc**-Bu*-Bt*-Bc*-CH2CH2OH
(I″
43)
HO-Bc**-Bt**-Bt**-Bg*-Bg*-Bc**-Bt**-Bc*-Bt**-Bg*-Bg*-Bc*-Bc**-Bt**-Bg*-Bu*-Bc**-Bc**-CH2CH2OH
(I″
44)
HO-Bc**-Bt**-Bc*-Bc**-Bt**-Bu*-Bc**-Bc**-Ba*-Bt**-Bg*-Ba*-Bc**-Bt**-Bc**-Ba*—
Ba*-Bg*-CH2CH2OH
(I″
45)
HO-Bc**-Bt**-Bg*-Ba*—
Ba*-Bg*-Bg*-Bt**-Bg*-Bt**-Bt**-Bc**-Bt**-Bt**-Bg*-Bt**-Ba*-Bc**-CH2CH2OH
(I″
46)
HO-Bt**-Bt**-Bc*-Bc**-Ba*-Bg*-Bc**-Bc**-Ba*-Bt**-Bt**-Bg*-Bt**-Bg*-Bt**-Bt**-Bg*-Ba*—
CH2CH2OH
(I″
47)
HO-Bc**-Bt**-Bc**-Ba*-Bg*-Bc**-Bt**-Bu*-Bc*-Bt**-Bt**-Bc*-Bc*-Bt**-Bt**-Ba*-Bg*-Bc**-CH2CH2OH
(I″
48)
HO-Bg*-Bc**-Bt**-Bt**-Bc*-Bu*-Bt**-Bc**-Bc*-Bu*-Bt**-Ba*-Bg*-Bc**-Bu*-Bt**-Bc**-Bc**-CH2CH2OH
(I″
49)
HO-Bg*-Bg*-Bc**-Ba*-Bt**-Bt**-Bu*-Bc**-Bt**-Ba*-Bg*-Bu*-Bt**-Bt**-Bg*-Bg*-Ba**-Bg*-CH2CH2OH
(I″
50)
HO—
Ba**-Bg*-Bt**-Bu*-Bt**-Bg*-Bg*-Ba**-Bg*-Ba*-Bt**-Bg*-Bg*-Bc*-Ba**-Bg*-Bt**-Bt**-CH2CH2OH
(I″
51)where Bg* is a group represented by formula (G1a), Ba* is a group represented by formula (A1a);
Bc* is a group represented by formula (C1a);
Bu* is a group represented by formula (U1a);
Bg** is a group represented by formula (G2);
Ba** is a group represented by formula (A2);
Bc** is a group represented by formula (C2);
Bt** is a group represented by formula (T2); and
Ph- is a group represented by first formula;
where X is individually and independently a group represented by the following formula (X1) or (X2);
R1 is individually and independently an alkyl group with 1-6 carbon atoms; and
Z is individually and independently a single bond or an alkylene group with 1-5 carbon atoms;
- 1) to (I″
-
76. The compound according to claim 75 which is represented by any one of formulae (I″
- 50-a) to (I″
51-b), or a salt thereof;
- 50-a) to (I″
-
77. The compound according to claim 69 which is selected from the group consisting of compounds (I1) to (I7), or a pharmacologically acceptable salt thereof:
HO-Bg**-Bc**-Bc**-Bt**-Bg**-Ba*-Bg*-Bc*-Bt*-Bg*-Ba*-Bt*-Bc*-Bt*-Bg*-Bc*-Bt*-Bg*-Bg*-Bc*-Ba*-Bt*-Bc*-Bt*-Bt*-Bg*-Bc**-Ba**-Bg**-Bt**-Bt** -CH2CH2OH
(I1)
HO-Bg**-Ba**-Bt**-Bc**-Bt**-Bg*-Bc*-Bt*-Bg*-Bg*-Bc**-Ba**-Bt**-Bc**-Bt**-CH2CH2OH
(I2)
HO-Bg**-Ba**-Bt**-Bc**-Bt**-Bg*-Bc*-Bt*-Bg*-Bg*-Bc*-Ba*-Bt*-Bc*-Bt*-Bt*-Bg*-Bc**-Ba**-Bg**-Bt**-Bt**-CH2CH2OH
(I3)
HO—
Ba*-Bg**-Bc**-Bt**-Bg**-Ba*-Bt**-Bc*-Bt*-Bg*-Bc*-Bt*-Bg*-Bg**-Bc**-Ba*-Bt**-Bc**-Bt**-CH2CH2OH
(I4)
HO-Bg**-Bc**-Bc**-Bt**-Bg**-Ba*-Bg*-Bc*-Bt*-Bg*-Ba*-Bt*-Bc*-Bt*-Bg*-Bc*-Bt*-Bg*-Bg**-Bc**-Ba*-Bt**-Bc**-Bt**-CH2CH2OH
(I5)
HO-Bg**-Ba*-Bt**-Bc**-Bt**-Bg**-Bc*-Bt*-Bg*-Bg*-Bc*-Ba*-Bt*-Bc*-Bt**-Bt**-Bg**-Bc**-Ba*-Bg**-CH2CH2OH
(I6)
HO—
Ba**-Bg**-Bc**-Bt**-Bg**-Ba**-Bt**-Bc**-Bt**-Bg**-Bc**-Bt**-Bg**-Bg**-Bc**-Ba**-Bt**-Bc**-Bt**-CH2CH2OH
(I7)
HO-Bg**-Ba**-Bt**-Bc**-Bt**-Bg*-Bc*-Bt*-Bg*-Bg*-Bc*-Ba*-Bt*-Bc**-Bt**-Bt**-Bg**-Bc**-CH2CH2OH
(I8)
HO-Bg**-Ba**-Bt**-Bc**-Bt**-Bg**-Bc**-Bt**-Bg**-Bg**-Bc**-Ba**-Bt**-Bc**-Bt**-CH2CH2OH
(I9)where Bg* is a group represented by formula (G1a), Ba* is a group represented by formula (A1a);
Bc* is a group represented by formula (C1a);
Bt* is a group represented by formula (U1a);
Bg** is a group represented by formula (G2) ;
Ba** is a group represented by formula (A2);
Bc** is a group represented by formula (C2); and
Bt** is a group represented by formula (T2);
where X is individually and independently a group represented by formula (X1) or (X2);
and R1 is individually and independently an alkyl group with 1-6 carbon atoms.
-
78. The compound according to claim 77 which is represented by any one of formulae (I1-a), (I2-a), (I3-a), (I4-a), (I5-a), (I6-a), (I7-a), (I8-a) and (I9-a), or a pharmacologically acceptable salt thereof:
-
79. The compound according to claim 69 where X in formulas (G1a), (A1a), (C1a) and (U1a) is a group represented by formula (X2) and X in formulae (G2), (A2), (C2) and (T2) is a group represented by formula (X1), or a pharmacologically acceptable salt thereof.
-
80. The compound according to claim 69 where X in all the formulae (G1a), (A1a), (C1a), (U1a), (G2), (A2), (C2) and (T2) is a group represented by formula (X2), or a pharmacologically acceptable salt thereof.
-
81. The compound according to claim 69 where Y in formulae (G1), (A1), (C1) and (U1) is a methoxy group and Z in formulae (G2), (A2), (C2) and (T2) is an ethylene group, or a pharmacologically acceptable salt thereof.
-
82. The compound according to claim 70 where X in formulas (G1a), (A1a), (C1a) and (U1a) is a group represented by formula (X2) and X in formulae (G2), (A2), (C2) and (T2) is a group represented by formula (X1), or a pharmacologically acceptable salt thereof.
-
83. The compound according to claim 70 where X in all the formulae (G1a), (A1a), (C1a), (U1a), (G2), (A2), (C2) and (T2) is a group represented by formula (X2), or a pharmacologically acceptable salt thereof.
-
84. The compound according to claim 70 where Y in formulae (G1), (A1), (C1) and (U1) is a methoxy group and Z in formulae (G2), (A2), (C2) and (T2) is an ethylene group, or a pharmacologically acceptable salt thereof.
-
85. The compound according to claim 71 where X in formulas (G1a), (A1a), (C1a) and (U1a) is a group represented by formula (X2) and X in formulae (G2), (A2), (C2) and (T2) is a group represented by formula (X1), or a pharmacologically acceptable salt thereof.
-
86. The compound according to claim 71 where X in all the formulae (G1a), (A1a), (C1a), (U1a), (G2), (A2), (C2) and (T2) is a group represented by formula (X2), or a pharmacologically acceptable salt thereof.
-
87. The compound according to claim 71 where Y in formulae (G1), (A1), (C1) and (U1) is a methoxy group and Z in formulae (G2), (A2), (C2) and (T2) is an ethylene group, or a pharmacologically acceptable salt thereof.
-
88. The compound according to claim 72 where X in formulas (G1a), (A1a), (C1a) and (U1a) is a group represented by formula (X2) and X in formulae (G2), (A2), (C2) and (T2) is a group represented by formula (X1), or a pharmacologically acceptable salt thereof.
-
89. The compound according to claim 72 where X in all the formulae (G1a), (A1a), (C1a), (U1a), (G2), (A2), (C2) and (T2) is a group represented by formula (X2), or a pharmacologically acceptable salt thereof.
-
90. The compound according to claim 72 where Y in formulae (G1), (A1), (C1) and (U1) is a methoxy group and Z in formulae (G2), (A2), (C2) and (T2) is an ethylene group, or a pharmacologically acceptable salt thereof.
-
91. The compound according to claim 73 where X in formulas (G1a), (A1a), (C1a) and (U1a) is a group represented by formula (X2) and X in formulae (G2), (A2), (C2) and (T2) is a group represented by formula (X1), or a pharmacologically acceptable salt thereof.
-
92. The compound according to claim 73 where X in all the formulae (G1a), (A1a), (C1a), (U1a), (G2), (A2), (C2) and (T2) is a group represented by formula (X2), or a pharmacologically acceptable salt thereof.
-
93. The compound according to claim 73 where Y in formulae (G1), (A1), (C1) and (U1) is a methoxy group and Z in formulae (G2), (A2), (C2) and (T2) is an ethylene group, or a pharmacologically acceptable salt thereof.
-
94. The compound according to claim 74 where X in formulas (G1a), (A1a), (C1a) and (U1a) is a group represented by formula (X2) and X in formulae (G2), (A2), (C2) and (T2) is a group represented by formula (X1), or a pharmacologically acceptable salt thereof.
-
95. The compound according-to claim 74 where X in all the formulae (G1a), (A1a), (C1a), (U1a), (G2), (A2), (C2), and (T2) is a group represented by formula (X2), or a pharmacologically acceptable salt thereof.
-
96. The compound according to claim 74 where Y in (G1), formulae (G1), (A1), (C1) and (U1) is a methoxy group and Z in formulae (G2), (A2), (C2) and (T2) is an ethylene group, or a pharmacologically acceptable salt thereof.
-
97. The compound according to claim 75 where X in formulas (G1a), (A1a), (C1a) and (U1a) is a group represented by formula (X2) and X in formulae (G2), (A2), (C2) and (T2) is a group represented by formula (X1), or a pharmacologically acceptable salt thereof.
-
98. The compound according to claim 75 where X in all the formulae (G1a), (A1a), (C1a), (U1a), (G2), (A2), (C2) and (T2) is a group represented by formula (X2), or a pharmacologically acceptable salt thereof.
-
99. The compound according to claim 75 where Y in formulae (G1), (A1), (C1) and (U1) is a methoxy group and Z in formulae (G2), (A2), (C2) and (T2) is an ethylene group, or a pharmacologically acceptable salt thereof.
-
100. The compound according to claim 76 where X in formulas (G1a), (A1a), (C1a) and (U1a) is a group represented by formula (X2) and X in formulae (G2), (A2), (C2) and (T2) is a group represented by formula (X1), or a pharmacologically acceptable salt thereof.
-
101. The compound according to claim 76 where X in all the formulae (G1a), (A1a), (C1a), (U1a), (G2), (A2), (C2) and (T2) is a group represented by formula (X2), or a pharmacologically acceptable salt thereof.
-
102. The compound according to claim 76 where Y in formulae (G1), (A1), (C1) and (U1) is a methoxy group and Z in formulae (G2), (A2), (C2) and (T2) is an ethylene group, or a pharmacologically acceptable salt thereof.
-
103. The compound according to claim 77 where X in formulas (G1a), (A1a), (C1a) and (U1a) is a group represented by formula (X2) and X in formulae (G2), (A2), (C2) and (T2) is a group represented by formula (X1), or a pharmacologically acceptable salt thereof.
-
104. The compound according to claim 77 where X in all the formulae (G1a), (A1a), (C1a), (U1a), (G2), (A2), (C2) and (T2) is a group represented by formula (X2), or a pharmacologically acceptable salt thereof.
-
105. The compound according to claim 77 where Y in formulae (G1), (A1), (C1) and (U1) is a methoxy group and Z in formulae (G2), (A2), (C2) and (T2) is an ethylene group, or a pharmacologically acceptable salt thereof.
-
106. The compound according to claim 78 where X in formulas (G1a), (A1a), (C1a) and (U1a) is a group represented by formula (X2) and X in formulae (G2), (A2), (C2) and (T2) is a group represented by formula (X1), or a pharmacologically acceptable salt thereof.
-
107. The compound according to claim 78 where X in all the formulae (G1a), (A1a), (C1a), (U1a), (G2), (A2), (C2) and (T2) is a group represented by formula (X2), or a pharmacologically acceptable salt thereof.
-
108. The compound according to claim 78 where Y in formulae (G1), (A1), (C1) and (U1) is a methoxy group and Z in formulae (G2), (A2), (C2) and (T2) is an ethylene group, or a pharmacologically acceptable salt thereof.
-
109. A method of treating muscular dystrophy in a patient in need thereof, said method comprising administering to the patient an effective amount of a pharmaceutical composition comprising the compound of claim 63 or a pharmacologically acceptable salt thereof.
-
110. The method according to claim 109, wherein muscular dystrophy is Duchenne muscular dystrophy.
-
111. The method according to claim 110, wherein the total number of the amino acids in the open reading frame of the dystrophin gene in the patient will be a multiple of 3 when exon 19, 41, 45, 46, 44, 50, 55, 51 or 53 of the dystrophin gene has been skipped.
-
64. The compound according to claim 63 or a pharmacologically acceptable salt thereof, having the nucleotide sequence as shown in any one of SEQ ID NOS:
- 004006.1) or a pharmaceutically acceptable salt thereof, provided that at least one of the nucleotides constituting the compound complementary to a nucleotide sequence in the region of the nucleotides No. 2571-2601 of dystrophin cDNA (Gene Bank accession No. NM—
Specification
-
- Resources
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Current AssigneeDaiichi Sankyo Company Limited
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Original AssigneeMasafumi Matsuo, Nonpro ORG Trans RES ORG of DUCH MUSC DYS, Yasuhiro Takeshima
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InventorsKoizumi, Makoto, Matsuo, Masafumi, Takeshima, Yasuhiro
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Granted Patent
-
Time in Patent OfficeDays
-
Field of Search
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US Class Current514/44.R
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CPC Class CodesA61K 38/00 Medicinal preparations cont...A61K 48/00 Medicinal preparations cont...A61P 21/00 Drugs for disorders of the ...A61P 21/04 for myasthenia gravisC07H 21/04 with deoxyribosyl as saccha...C12N 15/113 Non-coding nucleic acids mo...C12N 2310/11 AntisenseC12N 2310/3231 having an additional ring, ...C12N 2320/33 Alteration of splicing
