| US 7,402,605 B2 | ||
| 8-azaprostaglandin derivative compounds and drugs containing the compounds as the active ingredient | ||
| Kousuke Tani, Mishima-gun (Japan); Kaoru Kobayashi, Mishima-gun (Japan); Toru Maruyama, Mishima-gun (Japan); Tohru Kambe, Mishima-gun (Japan); Mikio Ogawa, Mishima-gun (Japan); and Tsutomu Shiroya, Mishima-gun (Japan) | ||
| Assigned to Ono Pharmaceutical Co., Ltd., Osaka (Japan) | ||
| Appl. No. 10/506,536 PCT Filed Mar. 04, 2003, PCT No. PCT/JP03/02478 § 371(c)(1), (2), (4) Date Sep. 03, 2004, PCT Pub. No. WO03/074483, PCT Pub. Date Sep. 12, 2003. |
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| Claims priority of application No. 2002-058487 (JP), filed on Mar. 05, 2002; application No. 2002-216567 (JP), filed on Jul. 25, 2002; and application No. 2003-013447 (JP), filed on Jan. 22, 2003. | ||
| Prior Publication US 2005/0124577 A1, Jun. 09, 2005 | ||
| Int. Cl. A61K 31/40 (2006.01); C07D 207/00 (2006.01) | ||
| U.S. Cl. 514—424 [548/551] | 4 Claims |
1. An 8-azaprostaglandin derivative compound represented by formula (I-a1-1)
 Ya is —S— or —SO2—;
ring6 is 5 or 6 membered mono-heterocyclic aryl consisting of hetero atoms selected from 1 to 4 nitrogen, 1 to 2 oxygen, and/or
1 to 2 sulfur atoms which may be partially or fully saturated;
R100 is a hydrogen atom or C1-4 alkyl;
U3a-1 is ring4;
ring 4 is C3-15 mono-, bi- or tri-carbocyclic aryl which may be partially or fully saturated;
ring4 may be substituted by 1 to 5 R;
R is (1) C1-10 alkyl, (2) C2-10 alkenyl, (3) C2-10 alkynyl, (4) C1-10 alkoxy, (5) C1-10 alkylthio, (6) halogen, (7) hydroxy,
(8) nitro, (9) —NR15R16, (10) C1-10 alkyl substituted by C1-10 alkoxy, (11) C1-10 alkyl substituted by 1 to 3 halogen atom(s), (12) C1-C10 alkyl
substituted by C1-10 alkoxy substituted by 1 to 3 halogen atom(s), (13) C1-10 alkyl substituted by —NR15R16, (14) ring5, (15) —O-ring5, (16) C1-10 alkyl substituted by ring5, (17) C2-10 alkenyl substituted by ring5, (18) C2-10 alkynyl
substituted by ring5, (19) C1-10 alkoxy substituted by ring5, (20) C1-10 alkyl substituted by —O-ring5, (21) COOR17, (22) C1-10 alkoxy substituted by 1 to 4 halogen atom(s), (23) formyl, (24) C1-10 alkyl substituted by hydroxy or (25) C2-10
acyl;
R15, R16 and R17 are, each independently, (1) a hydrogen atom or (2) C1-10 alkyl;
ring5 is
(1) C3-15 mono-, bi- or tri-carbocyclic aryl which may be partially or fully saturated or (2) 3- to 15-membered mono-, bi-
or tri-heterocyclic aryl which may be partially or fully saturated and contains a hetero atom(s) selected from 1 to 4 nitrogen,
1 to 2 oxygen and/or 1 to 2 sulfur atom(s);
ring5 may be substituted by 1 to 3 sustituent(s) selected from following (1)-(9):
(1) C1-10 alkyl, (2) C2-10 alkenyl, (3) C2-10 alkynyl, (4) C1-10 alkoxy, (5) C1-10 alkyl substituted by C1-10 alkoxy, (6)
halogen atom, (7) hydroxy, (8) C1-10 alkyl substituted by 1 to 3 halogen atom(s), (9) C1-10 alkyl substituted by C1-10 alkoxy
substituted by 1 to 3 halogen atom(s);
a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof.
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