| US 7,498,323 B2 | ||
| Spiro-piperidine compounds and medicinal use thereof | ||
| Rena Nishizawa, Mishima-gun (Japan); Yoshikazu Takaoka, Mishima-gun (Japan); Hiromu Habashita, Mishima-gun (Japan); Shiro Shibayama, Tsukuba (Japan); and Masaya Kokubo, Mishima-gun (Japan) | ||
| Assigned to Ono Pharmaceuticals Co., Ltd., Osaka (Japan) | ||
| Appl. No. 10/553,596 PCT Filed Apr. 16, 2004, PCT No. PCT/JP2004/005493 § 371(c)(1), (2), (4) Date Oct. 18, 2005, PCT Pub. No. WO2004/092169, PCT Pub. Date Oct. 28, 2004. |
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| Claims priority of application No. 2003-114188 (JP), filed on Apr. 18, 2003. | ||
| Prior Publication US 2006/0229301 A1, Oct. 12, 2006 | ||
| Int. Cl. A01N 43/62 (2006.01); A01N 43/58 (2006.01); A01N 43/60 (2006.01); A01N 43/42 (2006.01); A61K 31/55 (2006.01); A61K 31/50 (2006.01); A61K 31/495 (2006.01); A61K 31/44 (2006.01); C07D 471/04 (2006.01); C07D 471/22 (2006.01); C07D 487/00 (2006.01); C07D 491/00 (2006.01); C07D 495/00 (2006.01); C07D 215/00 (2006.01); C07D 217/00 (2006.01); C07D 219/00 (2006.01); C07D 221/00 (2006.01); C07D 237/00 (2006.01); C07D 239/00 (2006.01); C07D 241/00 (2006.01) | ||
| U.S. Cl. 514—221 [514/249; 514/257; 514/278; 540/502; 546/16; 544/231] | 6 Claims |
1. A spiro-piperidine compound represented by formula (I):
 wherein R1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s);
and
ring A represents a tetrahydropyrimidin-2-(1H)-one group represented by the following formula which may have a substituent(s),
in which 2,5-diketopiperazine having a spiro bond at the 3-position is excluded,
 wherein R2 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) in which the aliphatic hydrocarbon group
is selected from the group consisting of ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, hexyl,
heptyl, octyl, C2-8 alkenyl and C2-8 alkynyl, a hydroxyl group which may be protected, carboxy which may be protected, carbamoyl
which may be protected, or a cyclic group which may have a substituent(s) and,
R5 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s), hydroxyl which may be protected, carboxy
which may be protected, or a cyclic group which may have a substituent(s),
a salt thereof or a quaternary ammonium salt thereof,
wherein the cyclic group of R1, R2 and R5 is selected from the group consisting of cyclopropane, benzene, cyclohexane, cyclohexene, thiophene, pyrazole, isothiazole,
thiazole, imidazole, furan, dihydropyrazole, quinoline, benzodioxane, dioxaindane, benzofuran, pyridine, tetrahydropyran,
triazole, pyrrole, oxazole, isoxazole, and oxadiazole.
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