IP Library › Granted Patent US 8,575,134
Granted Patent B2
US 8,575,134 · App. 12/986,760 · Granted Nov 5, 2013

Aminocarboxylic acid derivative and medicinal use thereof

Inventors: Hiromu Habashita (Osaka, JP); Haruto Kurata (Osaka, JP); Shinji Nakade (Tsukuba, JP)
Assignee: Ono Pharmaceutical Co., Ltd.
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Quick Facts
Patent No.
US 8,575,134
App. No.
12/986,760
Granted
Nov 5, 2013
Kind
B2
Abstract

The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.

Claims (10)

1. 1-[(6-{[2,4-bis(trifluoromethyl)benzyl]oxy}-1-methyl-3,4-dihydro-2-naphthalenyl)methyl]-3-azetidinecarboxylic acid, a salt thereof, an N-oxide form thereof, a solvate thereof or a prodrug thereof.

2. The compound according to claim 1 , which is selected from the group consisting of

(1) 1-[(6-{[2,4-bis (trifluoromethyl)benzyl] oxy } -1-methyl-3,4-dihydro-2-naphthalenyl)methyl]-3-azetidinecarboxylic acid,

(2) ethyl 1-[(6-{[2,4-bis(trifluoromethyl)benzyl]oxy}-1-methyl-3,4-dihydro-2-naphthalenyl)methyl]-3-azetidinecarboxylate,

(3) 1-[(6-{[2,4-bis (trifluoromethyl)benzyl] oxy } -1-methyl-3,4-dihydro-2-naphthalenyl)methyl]-3-azetidinecarboxylic acid monohydrate,

(4) 1-[(6-{[2,4-bis (trifluoromethyl)benzyl] oxy } -1-methyl-3,4-dihydro-2-naphthalenyl)methyl]-3-azetidinecarboxylic acid hydrochloride,

(5) sodium 1-[(6-{[2,4-bis (trifluoromethyl)benzyl] oxy } -1-methyl-3,4-dihydro-2-naphthalenyl)methyl]-3-azetidinecarboxylate, and

(6) potassium 1-[(6-{[2,4-bis(trifluoromethyl)benzyl] oxy}-1-methyl-3,4-dihydro-2-naphthalenyl)methyl] -3-azetidinecarboxylate.

3. A compound which is 1-[(6-{[2,4-bis(trifluoromethyl)benzyl] oxy}-1-methyl-3,4-dihydro-2-naphthalenyl)methyl]-3-azetidinecarboxylic acid.

4. A pharmaceutical composition which comprises the compound according to claim 1 , a salt thereof, an N-oxide form thereof, a solvate thereof or a prodrug thereof.

Priority Claims (3)
JP 2004-360539 · Dec 13, 2004 · national
JP 2005-125740 · Apr 22, 2005 · national
JP 2005-233790 · Aug 11, 2005 · national
Continuity (2)
Continuation 11721601
Related Publication 20110105432A1 · May 5, 2011