Novel physiologically active substances

1 . A compound represented by the formula (I):

(in the formula, R 3 , R 6 , R 7 and R 21 are the same as or different from one another and each represents

1) a hydroxyl group or an oxo group formed together with the carbon atom to which each of R 3 , R 6 , R 7 and R 21 is bound, provided that R 6 is limited to hydroxyl group,

2) an optionally substituted C 1-22 alkoxy group,

3) an optionally substituted unsaturated C 2-22 alkoxy group,

4) an optionally substituted C 7-22 aralkyloxy group,

5) an optionally substituted 5 to 14-membered heteroaralkyloxy group,

6) RCO—O— (wherein R represents

a) a hydrogen atom,

b) an optionally substituted C 1-22 alkyl group,

c) an optionally substituted unsaturated C 2-22 alkyl group,

d) an optionally substituted C 6-14 aryl group,

e) an optionally substituted 5 to 14-membered heteroaryl group,

f) an optionally substituted C 7-22 aralkyl group,

g) an optionally substituted 5 to 14-membered heteroaralkyl group,

h) an optionally substituted C 1-22 alkoxy group,

i) an optionally substituted unsaturated C 2-22 alkoxy group,

j) an optionally substituted C 6-14 aryloxy group or

k) an optionally substituted 5 to 14-membered heteroaryloxy group),

7) R S1 R S2 R S3 SiO— (wherein R S1 , R S2 and R S3 are the same as or different from one another and each represents

a) a C 1-6 alkyl group or

b) a C 6-14 aryl group),

8) a halogen atom,

9) R N1 R N2 N—R M — (wherein R M represents

a) a single bond,

b) —CO—O—,

c) —SO 2 —O—,

d) —CS—O— or

e) —CO—NR N3 — (wherein R N3 represents a hydrogen atom or an optionally substituted C 1-6 alkyl group), provided that each of the leftmost bond in b) to e) is bound to the nitrogen atom; and

 R N1 and R 12 are the same as or different from each other and each represents

a) a hydrogen atom,

b) an optionally substituted C 1-22 alkyl group,

c) an optionally substituted unsaturated C 2-22 alkyl group,

d) an optionally substituted aliphatic C 2-22 acyl group,

e) an optionally substituted aromatic C 7-15 acyl group,

f) an optionally substituted C 6-14 aryl group,

g) an optionally substituted 5 to 14-membered heteroaryl group,

h) an optionally substituted C 7-22 aralkyl group,

i) an optionally substituted C 1-22 alkylsulfonyl group,

j) an optionally substituted C 6-14 arylsulfonyl group,

k) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group formed by

 R N1 and R N2 together with the nitrogen atom to which R N1 and R N2 are bound, and the non-aromatic heterocyclic group may have substituents,

l) an optionally substituted 5 to 14-membered heteroaralkyl group,

m) an optionally substituted C 3-14 cycloalkyl group or

n) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group),

10) R N4 SO 2 —O— (wherein R N4 represents

a) an optionally substituted C 1-22 alkyl group,

b) an optionally substituted C 6-14 aryl group,

c) an optionally substituted C 1-22 alkoxy group,

d) an optionally substituted unsaturated C 2-22 alkoxy group,

e) an optionally substituted C 6-14 aryloxy group,

f) an optionally substituted 5 to 14-membered heteroaryloxy group,

g) an optionally substituted C 7-22 aralkyloxy group or

h) an optionally substituted 5 to 14-membered heteroaralkyloxy group),

11) (R N5 O) 2 PO—(wherein R N5 represents

a) an optionally substituted C 1-22 alkyl group,

b) an optionally substituted unsaturated C 2-22 alkyl group,

c) an optionally substituted C 6-14 aryl group,

d) an optionally substituted 5 to 14-membered heteroaryl group,

e) an optionally substituted C 7-22 aralkyl group or

f) an optionally substituted 5 to 14-membered heteroaralkyl group),

12) (R N1 R N2 N) 2 PO—O— (wherein R N1 and R N2 have the same meanings as defined above) or

13) (R N1 R N2 N)(R N5 O)PO—O— (wherein R N1 , R N2 and R N5 have the same meanings as defined above), provided that a compound in which R 3 , R 6 , R 7 and R 21 are all hydroxyl groups, and a compound in which R 3 , R 6 and R 21 are all hydroxyl groups and R 7 is an acetoxy group are excluded), a pharmacologically acceptable salt thereof or a hydrate of them.

2 . The compound according to claim 1 represented by the formula (I-a):

(in the formula, R 3a , R 6a , R 7a and R 21a are the same as or different from one another and each represents

1) a hydroxyl group or an oxo group formed together with the carbon atom to which each of R 3a , R 6a , R 7a and R 21a is bound, provided that R 6a is limited to a hydroxyl group,

2) an optionally substituted C 1-22 alkoxy group,

3) R a CO—O— (wherein R a represents

a) a hydrogen atom,

b) an optionally substituted C 1-22 alkyl group,

c) an optionally substituted unsaturated C 2-22 alkyl group,

d) an optionally substituted C 6-14 aryl group,

e) an optionally substituted 5 to 14-membered heteroaryl group,

f) an optionally substituted C 7-22 aralkyl group,

g) an optionally substituted 5 to 14-membered heteroaralkyl group,

h) an optionally substituted C 1-22 alkoxy group,

i) an optionally substituted unsaturated C 2-22 alkoxy group,

j) an optionally substituted C 6-14 aryloxy group or

k) an optionally substituted 5 to 14-membered heteroaryloxy group),

4) R aS1 R aS2 R aS3 SiO— (wherein R aS1 , R aS2 and R aS3 are the same as or different from one another and each represents

a) a C 1-6 alkyl group or

b) a C 6-14 aryl group),

5) a halogen atom or

6) R aN1 R aN2 N—R aM — (wherein R aM represents

a) a single bond,

b) —CO—O—,

c) —SO 2 —O—,

d) —CS—O— or

e) —CO—NR aN3 — (wherein R aN3 represents a hydrogen atom or an optionally substituted C 1-6 alkyl group, provided that each of the leftmost bond in b) to e) is bound to the nitrogen atom); and

R aN1 and R aN2 are the same as or different from each other and each represents

a) a hydrogen atom,

b) an optionally substituted C 1-22 alkyl group,

c) an optionally substituted unsaturated C 2-22 alkyl group,

d) an optionally substituted aliphatic C 2-22 acyl group,

e) an optionally substituted aromatic C 7-15 acyl group,

f) an optionally substituted C 6-14 aryl group,

g) an optionally substituted 5 to 14-membered heteroaryl group,

h) an optionally substituted C 7-22 aralkyl group,

i) an optionally substituted C 1-22 alkylsulfonyl group,

j) an optionally substituted C 6-14 arylsulfonyl group,

k) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group formed by R aN1 and R aN2 together with the nitrogen atom to which R aN1 and R aN2 are bound, and the non-aromatic heterocyclic group may have substituents,

l) an optionally substituted 5 to 14-membered heteroaralkyl group,

m) an optionally substituted C 3-1 4 cycloalkyl group or

n) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group)), a pharmacologically acceptable salt thereof or a hydrate of them.

3 . The compound according to claim 1 represented by the formula (I-b):

(in the formula, R 3b , R 6b , R 7b and R 21b are the same as or different from one another and each represents

1) a hydroxyl group or an oxo group formed together with the carbon atom to which each of R 3b , R 6b , R 7b and R 21b is bound, provided that R 6b is limited to a hydroxyl group,

2) an optionally substituted C 1-22 alkoxy group,

3) R b CO—O— (wherein R b represents

a) a hydrogen atom,

b) an optionally substituted C 1-22 alkyl group,

c) an optionally substituted unsaturated C 2-22 alkyl group,

d) an optionally substituted C 6-14 aryl group,

e) an optionally substituted 5 to 14-membered heteroaryl group,

f) an optionally substituted C 7-22 aralkyl group,

g) an optionally substituted 5 to 14-membered heteroaralkyl group,

h) an optionally substituted C 1-22 alkoxy group,

i) an optionally substituted unsaturated C 2-22 alkoxy group,

j) an optionally substituted C 6-14 aryloxy group or

k) an optionally substituted 5 to 14-membered heteroaryloxy group),

4) R bS1 R bS2 R bS3 SiO— (wherein R bS1 , R bS2 and R bS3 are the same as or different from one another and each represents

a) a C 1-6 alkyl group or

b) a C 6-14 aryl group) or

5) R bN1 R bN2 N—R bM — (wherein R bM represents

a) —CO—O— or

b) —CS—O—, provided that each of the leftmost bond in a) and b) is bound to the nitrogen atom; and

 R bN1 and R bN2 are the same as or different from each other and each represents

a) a hydrogen atom,

b) an optionally substituted C 1-22 alkyl group,

c) an optionally substituted unsaturated C 2-22 alkyl group,

d) an optionally substituted aliphatic C 2-22 acyl group,

e) an optionally substituted aromatic C 7-15 acyl group,

f) an optionally substituted C 6-14 aryl group,

g) an optionally substituted 5 to 14-membered heteroaryl group,

h) an optionally substituted C 7-22 aralkyl group,

i) an optionally substituted C 1-22 alkylsulfonyl group,

j) an optionally substituted C 6-14 arylsulfonyl group,

k) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group formed by R bN1 and R bN2 together with the nitrogen atom to which R bN1 and R bN2 are bound, and the non-aromatic heterocyclic group may have substituents,

l) an optionally substituted 5 to 14-membered heteroaralkyl group,

m) an optionally substituted C 3-14 cycloalkyl group or

n) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group)), a pharmacologically acceptable salt thereof or a hydrate of them.

4 . The compound according to claim 1 represented by the formula (I-c):

(in the formula, R 3c , R 6c , R 7c and R 21c are the same as or different from one another and each represents

1) a hydroxyl group or an oxo group formed together with the carbon atom to which each of R 3c , R 6c , R 7c and R 21c is bound, provided that R 6c is limited to a hydroxyl group,

2) an optionally substituted C 1-22 alkoxy group,

3) R c CO—O— (wherein R c represents

a) an optionally substituted C 1-22 alkyl group,

b) an optionally substituted C 6-14 aryl group,

c) an optionally substituted C 7-22 aralkyl group or

d) an optionally substituted C 6-14 aryloxy group),

4) R cS1 R cS2 R cS3 SiO— (wherein R cS1 , R cS2 and R cS3 are the same as or different from one another and each represents

a) a C 1-6 alkyl group or

b) a C 6-14 aryl group) or

5) R cN1 R cN2 N—R cM — (wherein R cM represents

a) —CO—O— or

b) —CS—O—, provided that each of the leftmost bond in a) and b) is bound to the nitrogen atom; and

 R cN and R cN2 are the same as or different from each other and each represents

a) a hydrogen atom,

b) an optionally substituted C 1-22 alkyl group,

c) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group formed by R cN1 and R cN2 together with the nitrogen atom to which R cN1 and R cN2 are bound, and the non-aromatic heterocyclic group may have substituents,

d) an optionally substituted 5 to 14-membered heteroaralkyl group,

e) an optionally substituted C 3-14 cycloalkyl group or

f) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group)), a pharmacologically acceptable salt thereof or a hydrate of them.

5 . The compound according to claim 1 represented by the formula (I-d):

(in the formula, R 3d represents

1) a hydroxyl group or an oxo group formed together with the carbon atom to which R 3d is bound,

2) an optionally substituted C 1-22 alkoxy group,

3) an optionally substituted unsaturated C 2-22 alkoxy group,

4) an optionally substituted C 7-22 aralkyloxy group,

5) R d CO—O— (wherein R d represents

a) a hydrogen atom,

b) an optionally substituted C 1-22 alkyl group,

c) an optionally substituted unsaturated C 2-22 alkyl group,

d) an optionally substituted C 6-14 aryl group,

e) an optionally substituted 5 to 14-membered heteroaryl group,

f) an optionally substituted C 7-22 aralkyl group,

g) an optionally substituted 5 to 14-membered heteroaralkyl group,

h) an optionally substituted C 1-22 alkoxy group,

i) an optionally substituted unsaturated C 2-22 alkoxy group,

j) an optionally substituted C 6-14 aryloxy group or

k) an optionally substituted 5 to 14-membered heteroaryloxy group) or

6) R dN1 R dN2 N—CO—O— (wherein R dN1 and R dN2 are the same as or different from each other and each represents

a) a hydrogen atom,

b) an optionally substituted C 1-22 alkyl group,

c) an optionally substituted unsaturated C 2-22 alkyl group,

d) an optionally substituted C 6-14 aryl group,

e) an optionally substituted 5 to 14-membered heteroaryl group,

f) an optionally substituted C 7-22 aralkyl group,

g) an optionally substituted 5 to 14-membered heteroaralkyl group,

h) an optionally substituted C 3-14 cycloalkyl group,

i) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group or

j) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group formed by R dN1 and R dN2 together with the nitrogen atom to which R dN1 and R dN2 are bound, and the non-aromatic heterocyclic group may have substituents); and

 R 6d , R 7d and R 21d are the same as or different from one another and each represents

1) a hydroxyl group or an oxo group formed together with the carbon atom to which each of R 6d , R 7d and R 21d is bound, provided that R 6d is limited to a hydroxyl group,

2) an optionally substituted C 1-22 alkoxy group,

3) an optionally substituted unsaturated C 2-22 alkoxy group,

4) an optionally substituted C 7-22 aralkyloxy group,

5) R d CO—O— (wherein Rd has the same meaning as defined above),

6) R dN1 R dN2 N—CO—O— (wherein R dN1 and R dN2 have the same meanings as defined above),

7) R dN1 R dN2 N—SO 2 —O— (wherein R dN1 and R dN2 have the same meanings as defined above),

8) R dN1 R dN2 N—CS—O— (wherein R dN1 and R dN2 have the same meanings as defined above),

9) R dN3 SO 2 —O— (wherein R dN3 represents

a) an optionally substituted C 1-22 alkyl group,

b) an optionally substituted C 1-22 alkoxy group,

c) an optionally substituted unsaturated C 2-22 alkoxy group,

d) an optionally substituted C 6-14 aryl group,

e) an optionally substituted C 6-14 aryloxy group,

f) an optionally substituted 5 to 14-membered heteroaryloxy group,

g) an optionally substituted C 7-22 aralkyloxy group or

h) an optionally substituted 5 to 14-membered heteroaralkyloxy group),

10) (R dN5 O) 2 PO— (wherein R dN5 represents

a) an optionally substituted C 1-22 alkyl group,

b) an optionally substituted unsaturated C 2-22 alkyl group,

c) an optionally substituted C 6-14 aryl group,

d) an optionally substituted 5 to 14-membered heteroaryl group,

e) an optionally substituted C 7-22 aralkyl group or

f) an optionally substituted 5 to 14-membered heteroaralkyl group),

11) (R dN1 R dN2 N) 2 PO— (wherein R dN1 and R dN2 have the same meanings as defined above) or

12) (R dN1 R dN2 N)(R dN5 O)PO— (wherein R dN1 , R dN2 and R dN1 have the same meanings as defined above), provided that a compound in which R 3d , R 6d , R 7d and R 21d are all hydroxyl groups, and a compound in which R 3d , R 6d and R 21d are hydroxyl groups and R 7d is an acetoxy group are excluded), a pharmacologically acceptable salt thereof or a hydrate of them.

6 . The compound according to claim 1 , wherein R 6 and/or R 7 represents R N1 R N2 N—R M — (wherein R M represents

a) —CO—O— or

b) —CS—O—; and

R N1 and R N2 have the same meanings as defined above, provided that each of the leftmost bond in a) and b) is bound to the nitrogen atom), a pharmacologically acceptable salt thereof or a hydrate of them.

7 . The compound according to claim 1 , a pharmacologically acceptable salt thereof or a hydrate of them, wherein R 21 is an oxo group formed together with the carbon atom to which R 21 is bound.

8 . The compound according to claim 5 represented by the formula (I-e):

(in the formula, R 3e and R 21e are the same as or different from each other and each represents

1) a hydroxyl group or an oxo group formed together with the carbon atom to which each of R 3e and R 21e is bound,

2) an optionally substituted C 1-6 alkoxy group,

3) an optionally substituted unsaturated C 2-10 alkoxy group,

4) an optionally substituted C 7-10 aralkyloxy group,

5) an optionally substituted aliphatic C 2-6 acyloxy group or

6) R eN1 R eN2 N—CO—O— (wherein R eN1 and R eN2 are the same as or different from each other and each represents

A) a hydrogen atom or

B) an optionally substituted C 1-6 alkyl group); and

R 6e and R 7e are the same as or different from each other and each represents

1) a hydroxyl group or an oxo group formed together with the carbon atom to which each of R 6e and R 7e is bound, provided that R 6e is limited to a hydroxyl group,

2) an optionally substituted C 1-6 alkoxy group,

3) an optionally substituted unsaturated C 2-10 alkoxy group,

4) an optionally substituted C 7-10 aralkyloxy group,

5) an optionally substituted aliphatic C 2-6 acyloxy group or

6) R e C(═Y e )—O— (wherein Y e represents an oxygen atom or a sulfur atom; and R e represents

a) a hydrogen atom,

b) an optionally substituted C 1-6 alkyl group,

c) an optionally substituted C 7-10 aralkyl group,

d) an optionally substituted 5 to 14-membered heteroaralkyl group,

e) the formula (III):

(in the formula,

A) n represents an integer of 0 to 4;

X e represents

i) —CHR eN4 —,

ii) —NR eN5 —,

iii) —O—,

iv) —S—,

v) —SO— or

vi) —SO 2 —;

R eN1 represents

i) a hydrogen atom or

ii) a C 1-6 alkyl group;

R eN2 represents

i) a hydrogen atom or

ii) a C 1-6 alkyl group;

R eN3 and R eN4 are the same as or different from each other and each represents

i) a hydrogen atom,

ii) an optionally substituted C 1-6 alkyl group,

iii) an optionally substituted unsaturated C 2-10 alkyl group,

iv) an optionally substituted C 6-14 aryl group,

v) an optionally substituted 5 to 14-membered heteroaryl group,

vi) an optionally substituted C 7-10 aralkyl group,

vii) an optionally substituted C 3-8 cycloalkyl group,

viii) an optionally substituted C 4-9 cycloalkyl alkyl group,

ix) an optionally substituted 5 to 14-membered heteroaralkyl group,

x) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group,

xi) —NR eN6 R eN7 (wherein R eN6 and R eN7 are the same as or different from each other and each represents a hydrogen atom or an optionally substituted C 1-6 alkyl group) or

xii) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group formed by R eN3 and R eN4 together with the carbon atom to which R eN3 and R eN4 are bound, and the non-aromatic heterocyclic group may have substituents; and

R eN5 represents

i) a hydrogen atom,

ii) an optionally substituted C 1-6 alkyl group,

iii) an optionally substituted unsaturated C 2-10 alkyl group,

iv) an optionally substituted C 6-14 aryl group,

v) an optionally substituted 5 to 14-membered heteroaryl group,

vi) an optionally substituted C 7-10 aralkyl group,

vii) an optionally substituted C 3-8 cycloalkyl group,

viii) an optionally substituted C 4-9 cycloalkyl alkyl group,

ix) an optionally substituted 5 to 14-membered heteroaralkyl group,

x) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group or

xi) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group formed by R eN3 and R eN5 together with the nitrogen atom to which R eN3 and R eN5 are bound, and the non-aromatic heterocyclic group may have substituents,

B) X e , n, R eN3 , R eN4 and R eN5 each represents the group as defined above; and R eN1 and R eN2 together form an optionally substituted 5 to 14-membered non-aromatic heterocyclic group,

C) X e , n, R eN2 , R eN4 and R eNn5 each represents the group as defined above; and R eN1 and R eN3 together form an optionally substituted 5 to 14-membered non-aromatic heterocyclic group or

D) X e , n, R eN1 , R eN4 and R eN5 each represents the group as defined above; and R eN2 and R eN3 together form an optionally substituted 5 to 14-membered non-aromatic heterocyclic group) or

f) the formula (IV):

(in the formula, R eN8 and R eN9 are the same as or different from each other and each represents

i) a hydrogen atom,

ii) an optionally substituted C 1-6 alkyl group,

iii) an optionally substituted C 6-14 aryl group,

iv) an optionally substituted 5 to 14-membered heteroaryl group,

v) an optionally substituted C 7-10 aralkyl group or

vi) an optionally substituted 5 to 14-membered heteroaralkyl group))), a pharmacologically acceptable salt thereof or a hydrate of them.

9 . The compound according to claim 5 , wherein R 6d and/or R 7d represents R d1 C(═Y d1 )—O— (wherein Y d1 represents an oxygen atom or a sulfur atom; and R d1 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted C 7-10 aralkyl group or

4) an optionally substituted 5 to 14-membered heteroaralkyl group), a pharmacologically acceptable salt thereof or a hydrate of them.

10 . The compound according to claim 5 , wherein R 6d and/or R 7d represents R d2 C(═Y d2 )—O— (wherein Y d2 represents an oxygen atom or sulfur atom; and R d2 represents the formula (III′):

(in the formula, n represents an integer of 0 to 4; X 1 represents

1) —CHR dN7 —,

2) NR dN8 —,

3) —O—,

4) —S—,

5) —SO— or

6) —SO 2 —;

R dN4 and R dN5 are the same as or different from each other and each represents

1) a hydrogen atom or

2) a C 1-6 alkyl group;

R dN6 and R dN7 are the same as or different from each other and each represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted unsaturated C 2-10 alkyl group,

4) an optionally substituted C 6-14 aryl group,

5) an optionally substituted 5 to 14-membered heteroaryl group,

6) an optionally substituted C 7-10 aralkyl group,

7) an optionally substituted C 3-8 cycloalkyl group,

8) an optionally substituted C 4-9 cycloalkyl alkyl group,

9) an optionally substituted 5 to 14-membered heteroaralkyl group,

10) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group,

11) —NR dN9 R dN10 (wherein R dN9 and R dN10 are the same as or different from each other and each represents a hydrogen atom or an optionally substituted C 1-6 alkyl group) or

12) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group formed together by R dN6 and R dN7 , and the non-aromatic heterocyclic group may have substituents; and

R dN8 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted unsaturated C 2-10 alkyl group,

4) an optionally substituted C 6-14 aryl group,

5) an optionally substituted 5 to 14-membered heteroaryl group,

6) an optionally substituted C 7-10 aralkyl group,

7) an optionally substituted C 3-8 cycloalkyl group,

8) an optionally substituted C 4-9 cycloalkyl alkyl group,

9) an optionally substituted 5 to 14-membered heteroaralkyl group,

10) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group,

11) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group formed by R dN4 , d dN5 or R dN6 together with the nitrogen atom to which each of R dN4 , R dN5 and R dN5 is bound, and the non-aromatic heterocyclic group may have substituents or

12) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group formed by two substituents selected from the group consisting of R dN4 , R dN5 and R dN6 together with the nitrogen atom to which it is bound, and the non-aromatic heterocyclic group may have substituents)), a pharmacologically acceptable salt thereof or a hydrate of them.

11 . The compound according to claim 10 , a pharmacologically acceptable salt thereof or a hydrate of them, wherein X 1 represents —NR dN8 — (wherein NR dN8 has the same meanings as defined above).

12 . The compound according to claim 5 represented by the formula (I-f):

(in the formula, R 7f represents R f C(═Y f )—O— (wherein Y f represents an oxygen atom or a sulfur atom; and R f represents the formula (V):

(wherein n represents an integer of 0 to 4;

R fN1 represents

1) a hydrogen atom,

2) a methyl group or

3) an ethyl group; and

R fN2 represents

1) a hydrogen atom,

2) a methylamino group,

3) a dimethylamino group,

4) an ethylamino group,

5) a diethylamino group,

6) an ethylmethylamino group,

7) a pyridinyl group,

8) a pyrrolidin-1-yl group,

9) a piperidin-1-yl group,

10) a morpholin-4-yl group or

11) a 4-methylpiperazin-1-yl group))), a pharmacologically acceptable salt thereof or a hydrate of them.

13 . The compound according to claim 5 , wherein R 6d and/or R 7d represents R d3 CO—O— (wherein R d3 represents the formula (VI):

(wherein n 1 and n 2 are the same as or different from each other and each represents an integer of 0 to 4;

X 2 represents

1) —CHR dN13 —,

2) —NR dN14 —,

3) —O—,

4) —S—,

5) —SO— or

6) —SO 2 —;

R dN11 represents

1) a hydrogen atom or

2) an optionally substituted C 1-6 alkyl group;

R dN12 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted C 6-14 aryl group or

4) an optionally substituted C 7-10 aralkyl group;

R dN13 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted unsaturated C 2-10 alkyl group,

4) an optionally substituted C 6-14 aryl group,

5) an optionally substituted 5 to 14-membered heteroaryl group,

6) an optionally substituted C 7-10 aralkyl group,

7) an optionally substituted C 3-8 cycloalkyl group,

8) an optionally substituted C 4-9 cycloalkyl alkyl group,

9) an optionally substituted 5 to 14-membered heteroaralkyl group,

10) —NR dN15 R dN16 (wherein R dN15 and R dN16 are the same as or different from each other and each represents a hydrogen atom or an optionally substituted C 1-6 alkyl group) or

11) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group; and

R dN14 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted unsaturated C 2-10 alkyl group,

4) an optionally substituted C 6-14 aryl group,

5) an optionally substituted 5 to 14-membered heteroaryl group,

6) an optionally substituted C 7-10 aralkyl group,

7) an optionally substituted C 3-8 cycloalkyl group,

8) an optionally substituted C 4-9 cycloalkyl alkyl group,

9) an optionally substituted 5 to 14-membered heteroaralkyl group or

10) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group)), a pharmacologically acceptable salt thereof or a hydrate of them.

14 . The compound according to claim 5 represented by the formula (I-g):

(in the formula, R 7g represents R g CO—O— (wherein R g represents the formula (VII):

(wherein n 3 represents 1 or 2;

R dN17 represents

1) a hydrogen atom,

2) a methyl group or

3) an ethyl group; and

R dN18 represents

1) a hydrogen atom,

2) a methyl group or

3) an ethyl group))), a pharmacologically acceptable salt thereof or a hydrate of them.

15 . The compound according to claim 5 , wherein R 6d and/or R 7d represents R d4 CO—O— (wherein R d4 represents the formula (VIII):

(wherein n 1 and n 2 are the same as or different from each other and each represents an integer of 0 to 4;

X 3 represents

1) —CHR dN21 ,

2) NR dN22 —,

3) —O—,

4) —S—,

5) —SO— or

6) —SO 2 —;

R dN19 represents

1) a hydrogen atom or

2) a C 1-6 alkyl group;

R dN20 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted C 6-14 aryl group or

4) an optionally substituted C 7-10 aralkyl group;

R dN21 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted unsaturated C 2-10 alkyl group,

4) an optionally substituted C 1-6 alkoxy group,

5) an optionally substituted C 6-14 aryl group,

6) an optionally substituted 5 to 14-membered heteroaryl group,

7) an optionally substituted C 7-10 aralkyl group,

8) an optionally substituted C 3-8 cycloalkyl group,

9) an optionally substituted C 4-9 cycloalkyl alkyl group,

10) an optionally substituted 5 to 14-membered heteroaralkyl group,

11) —NR dN23 R dN24 (wherein R dN23 and R dN24 are the same as or different from each other and each represents a hydrogen atom or an optionally substituted C 1-6 alkyl group) or

12) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group; and

R dN22 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted unsaturated C 2-10 alkyl group,

4) an optionally substituted C 6-14 aryl group,

5) an optionally substituted 5 to 14-membered heteroaryl group,

6) an optionally substituted C 7-10 aralkyl group,

7) an optionally substituted C 3-8 cycloalkyl group,

8) an optionally substituted C 4-9 cycloalkyl alkyl group,

9) an optionally substituted 5 to 14-membered heteroaralkyl group or

10) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group)), a pharmacologically acceptable salt thereof or a hydrate of them.

16 . The compound according to claim 5 represented by the formula (I-h):

(in the formula, R 7h represents R h CO—O— (wherein R h represents the formula (IX):

(wherein n 4 represents an integer of 1 to 3; and

R dN25 represents

1) an amino group,

2) a methylamino group,

3) a dimethylamino group,

4) a pyrrolidin-1-yl group,

5) a piperidin-1-yl group or

6) a morpholin-4-yl group))), a pharmacologically acceptable salt thereof or a hydrate of them.

17 . The compound according to claim 5 represented by the formula (I-i):

(in the formula, R 7i represents R i CO—O— (wherein R i represents the formula (X):

(wherein n 4 represents an integer of 1 to 3;

R dN26 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted C 6-14 aryl group or

4) an optionally substituted C 7-10 aralkyl group; and

R dN27 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted C 3-8 cycloalkyl group,

4) an optionally substituted 3 to 8-membered non-aromatic heterocyclic group,

5) an optionally substituted C 6-14 aryl group,

6) an optionally substituted 5 to 14-membered heteroaryl group,

7) an optionally substituted C 7-10 aralkyl group,

8) an optionally substituted 5 to 14-membered heteroaralkyl group or

9) an optionally substituted C 4-9 cycloalkyl alkyl group))), a pharmacologically acceptable salt thereof or a hydrate of them.

18 . The compound according to claim 5 represented by the formula (I-j):

(in the formula, R 7j represents R j CO—O— (wherein R j represents the formula (XI):

(wherein n 4 represents an integer of 1 to 3; and

R dN28 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) a C 3-8 cycloalkyl group,

4) a C 4-9 cycloalkyl alkyl group,

5) a C 7-10 aralkyl group,

6) a pyridinyl group or

7) a tetrahydropyranyl group))), a pharmacologically acceptable salt thereof or a hydrate of them.

19 . The compound according to claim 5 represented by the formula (I-k):

(in the formula, R 7k represents R k CO—O— (wherein R k represents the formula (XII):

(wherein m 1 , m 2 , m 3 and m 4 are the same as or different from one another and each represents 0 or 1;

n 4 represents an integer of 1 to 3; and

R dN29 represents

1) a hydrogen atom,

2) an optionally substituted C 1-6 alkyl group,

3) an optionally substituted unsaturated C 2-10 alkyl group,

4) an optionally substituted C 6-14 aryl group,

5) an optionally substituted 5 to 14-membered heteroaryl group,

6) an optionally substituted C 7-10 aralkyl group,

7) an optionally substituted C 3-8 cycloalkyl group,

8) an optionally substituted C 4-9 cycloalkyl alkyl group,

9) an optionally substituted 5 to 14-membered heteroaralkyl group or

10) an optionally substituted 5 to 14-membered non-aromatic heterocyclic group))), a pharmacologically acceptable salt thereof or a hydrate of them.

20 . The compound according to claim 5 represented by the formula (I-m):

(in the formula, R 7m represents R m CO—O— (wherein R m represents the formula (XIII):

(wherein m 5 represents an integer of 1 to 3; and n 5 represents 2 or 3))), a pharmacologically acceptable salt thereof or a hydrate of them.

21 . The compound according to claim 5 represented by the formula (I-n):

(in the formula, R 7n represents R n CO—O— (wherein R n is a group represented by the formula (XIV):

a pharmacologically acceptable salt thereof or a hydrate of them.

22 . The compound according to claim 1 , which is selected from:

(8E,12E,14E)-7-(N-(2-(N′,N′-Dimethylamino)ethyl)-N-methylcarbamoyloxy)-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-7-((4-methylhomopiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-7-((4-methylpiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Butylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Ethylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-7-((4-propylpiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Cyclohexylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-(Cyclopropylmethyl)piperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-6,10,12,16,20-pentamethyl-7-((4-propylhomopiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-(Cyclopropylmethyl)homopiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Cyclopentylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-7-((4-isopropylpiperazin-1-yl)carbonyl)oxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-(N-(2-(N′,N′-Diethylamino)ethyl)-N-methylcarbamoyloxy)-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-Tetrahydroxy-7-((4-isobutylhomopiperazin-1-yl)carbonyl)oxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Ethylhomopiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Butylhomopiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,16,21-Trihydroxy-6-methoxy-6,10,12,16,20-pentamethyl-7-((4-methylpiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,16,21-Trihydroxy-6-methoxy-6,10,12,16,20-pentamethyl-7-((4-(piperidin-1-yl)piperidin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-(2,2-Dimethylpropyl)homopiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; and (8E,12E,14E)-3,6,16-Trihydroxy-21-methoxy-6,10,12,16,20-pentamethyl-7-((4-methylpiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide.

23 . The compound according to claim 1 , which is selected from:

(8E,12E,14E)-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-7-((4-methylhomopiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-7-(4-methylhomopiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-7-((4-methylpiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-cyclohexylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-3,6,16,21-tetrahydroxy-7-((4-isopropylpiperazin-1-yl)carbonyl)oxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; (8E,12E,14E)-7-((4-Cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide; and (8E,12E,14E)-7-(N-(2-(N′,N′-Diethylamino)ethyl)-N-methylcarbamoyloxy)-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide.

24 . A medicament comprising the compound according to claim 1 , a pharmacologically acceptable salt thereof or a hydrate of them as an active ingredient.

25 . A pharmaceutical composition comprising the compound according to claim 1 , a pharmacologically acceptable salt thereof or a hydrate of them as an active ingredient.

26 . The medicament according to claim 24 , which is an agent for preventing or treating a disease against which a regulation of gene expression is efficacious.

27 . The medicament according to claim 24 , which is an agent for preventing or treating a diseases against which suppression of VEGF production is efficacious.

28 . The medicament according to claim 24 , which is an agent for preventing or treating a disease against which an antiangiogenic effect is efficacious.

29 . The medicament according to claim 24 , which is an angiogenesis inhibitor.

30 . The medicament according to claim 24 , which is an antitumor agent.

31 . The medicament according to claim 24 , as a therapeutic agent for treating angioma.

32 . The medicament according to claim 24 , which is cancer metastasis inhibitor.

33 . The medicament according to claim 24 , which is a therapeutic agent for treating retinal neovascularization or diabetic retinopathy.

34 . The medicament according to claim 24 , which is a therapeutic agent for treating inflammatory disease.

35 . The medicament according to claim 24 , which is a therapeutic agent for treating inflammatory diseases consisting of deformans arthritis, rheumatoid arthritis, psoriasis and delayed hypersensitivity reaction.

36 . The medicament according to claim 24 , which is a therapeutic agent for treating atherosclerosis.

37 . The medicament according to claim 24 , which is a therapeutic agent for treating solid cancer.

38 . The medicament according to claim 37 , wherein the solid cancer is lung cancer, brain tumor, breast cancer, prostate cancer, ovarian cancer, colon cancer or melanoma.

39 . The medicament according to claim 24 , which is a therapeutic agent for treating leukemia.

40 . The medicament according to claim 24 , which is an antitumor agent based on a regulation of gene expression.

41 . The medicament according to claim 24 , which is an antitumor agent based on suppression of VEGF production.

42 . The medicament according to claim 24 , which is an antitumor agent based on an effect of angiogenesis inhibition.

43 . A method for preventing or treating a disease against which a regulation of gene expression is efficacious, which comprises administering a pharmacologically effective dose of the medicament according to claim 24 to a patient.

44 . A method for preventing or treating a disease against which suppression of VEGF production is efficacious, which comprises administering a pharmacologically effective dose of the medicament according to claim 24 to a patient.

45 . A method for preventing or treating a disease against which an angiogenesis inhibition is efficacious, which comprises administering a pharmacologically effective dose of the medicament according to claim 24 to a patient.

46 . Use of the compound according to claim 1 , a pharmacologically acceptable salt thereof or a hydrate of them, for manufacturing an agent for preventing or treating a disease against which a regulation of gene expression is efficacious.

47 . Use of the compound according to claim 1 , a pharmacologically acceptable salt thereof or a hydrate of them, for manufacturing an agent for preventing or treating a disease against which suppression of VEGF production is efficacious.

48 . Use of the compound according to claim 1 , a pharmacologically acceptable salt thereof or a hydrate of them, for manufacturing an agent for preventing or treating a disease against which an angiogenesis inhibition is efficacious.

49 . Use of the compound according to claim 1 , a pharmacologically acceptable salt thereof or a hydrate of them, for manufacturing an agent for preventing or treating solid cancers.