| US 7,550,503 B2 | ||
| Physiologically active substances | ||
| Yoshihiko Kotake, Ibaraki (Japan); Jun Niijima, Ibaraki (Japan); Yoshio Fukuda, Ibaraki (Japan); Mitsuo Nagai, Ibaraki (Japan); Regina Mikie Kanada, Ibaraki (Japan); Takashi Nakashima, Shizuoka (Japan); Masahi Yoshida, Shizuoka (Japan); and Toshio Tsuchida, Shizuoka (Japan) | ||
| Assigned to Eisai R& D Management Co., Ltd., Tokyo (Japan); and Merican Corporation, Tokyo (Japan) | ||
| Filed on Jun. 23, 2006, as Appl. No. 11/473,201. | ||
| Application 11/473201 is a continuation of application No. 10/515647, filed on Jul. 20, 2005, abandoned. | ||
| Prior Publication US 2006/0241171 A1, Oct. 26, 2006 | ||
| Int. Cl. A01N 43/02 (2006.01); A61K 31/335 (2006.01); C07D 313/00 (2006.01); C07D 313/04 (2006.01) | ||
| U.S. Cl. 514—450 [549/266; 549/271] | 26 Claims |
1. A compound represented by the formula (I):
 1) a hydroxyl group or an oxo group formed together with the carbon atom to which each of R3, R6, R7 and R21 is bound, provided that R6 is limited to hydroxyl group,
2) an optionally substituted C1-22 alkoxy group,
3) an optionally substituted unsaturated C2-22 alkoxy group,
4) an optionally substituted C7-22 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 C1-22 alkyl group,
c) an optionally substituted unsaturated C2-22 alkyl group,
d) an optionally substituted C6-14 aryl group,
e) an optionally substituted 5 to 14-membered heteroaryl group,
f) an optionally substituted C7-22 aralkyl group,
g) an optionally substituted 5 to 14-membered heteroaralkyl group,
h) an optionally substituted C1-22 alkoxy group,
i) an optionally substituted unsaturated C2-22 alkoxy group,
j) an optionally substituted C6-14 aryloxy group or
k) an optionally substituted 5 to 14-membered heteroaryloxy group),
7) RS1RS2RS3SiO— (wherein RS1, RS2 and RS3 are the same as or different from one another and each represents
a) a C1-6 alkyl group or
b) a C6-14 aryl group),
8) a halogen atom,
9) RN1RN2N—RM— (wherein RM represents
a) a single bond,
b) —CO—O—,
c) —S2—O—,
d) —CS—O— or
e) —CO—NRN3— (wherein RN3 represents a hydrogen atom or an optionally substituted C1-6 alkyl group), provided that each of the leftmost bond in b) to e) is bound to the nitrogen atom; and
RN1 and RN2 are the same as or different from each other and each represents
a) a hydrogen atom,
b) an optionally substituted C1-22 alkyl group,
c) an optionally substituted unsaturated C2-22 alkyl group,
d) an optionally substituted aliphatic C2-22 acyl group,
e) an optionally substituted aromatic C7-15 acyl group,
f) an optionally substituted C6-14 aryl group,
g) an optionally substituted 5 to 14-membered heteroaryl group,
h) an optionally substituted C7-22 aralkyl group,
i) an optionally substituted C1-22 alkylsulfonyl group,
j) an optionally substituted C6-14 arylsulfonyl group,
k) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group formed by
RN1 and RN2 together with the nitrogen atom to which RN1 and RN2 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 C3-14 cycloalkyl group or
n) an optionally substituted 3 to 14-membered non-aromatic heterocyclic group),
10) RN4SO2—O— (wherein RN4 represents
a) an optionally substituted C1-22 alkyl group,
b) an optionally substituted C6-14 aryl group,
c) an optionally substituted C1-22 alkoxy group,
d) an optionally substituted unsaturated C2-22 alkoxy group,
e) an optionally substituted C6-14 aryloxy group,
f) an optionally substituted 5 to 14-membered heteroaryloxy group,
g) an optionally substituted C7-22 aralkyloxy group or
h) an optionally substituted 5 to 14-membered heteroaralkyloxy group),
11) (RN5O)2PO—O— (wherein RN5 represents
a) an optionally substituted C1-22 alkyl group,
b) an optionally substituted unsaturated C2-22 alkyl group,
c) an optionally substituted C6-14 aryl group,
d) an optionally substituted 5 to 14-membered heteroaryl group,
e) an optionally substituted C7-22 aralkyl group or
f) an optionally substituted 5 to 14-membered heteroaralkyl group),
12) (RN1RN2N)2PO—O— (wherein RN1 and RN2 have the same meanings as defined above) or
13) (RN1RN2N)(RN5O)PO—O— (wherein RN1, RN2 and R have the same meanings as defined above), provided that a compound in which R3, R6, R7 and R21 are all hydroxyl groups, and a compound in which R3, R6 and R21 are all hydroxyl groups and R7 is an acetoxy group and a compound in which R3 and R6 are hydroxyl groups, R7 is an acetoxy group and R21 is an oxo group formed together with the carbon atom to which R21 is bound are excluded), or a pharmacologically acceptable salt thereof.
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