IP Library Granted Patent US 9,238,634
Granted Patent B2
US 9,238,634 · App. 13/817,079 · Granted Jan 19, 2016

Anti-inflammatory metabolite derived from omega-3-type fatty acid

Inventors: Makoto Arita (Tokyo, JP); Hiroyuki Arai (Tokyo, JP); Yosuke Isobe (Tokyo, JP); Tadafumi Kubota (Tokyo, JP)
Assignee: THE UNIVERSITY OF TOKYO
C07D303/14C07D303/38C12P7/6427C12P17/02C12Y113/11G01N30/34G01N30/7233G01N2030/884
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Quick Facts
Patent No.
US 9,238,634
App. No.
13/817,079
Granted
Jan 19, 2016
Kind
B2
Abstract

The purpose is to provide a compound which can overcomes the disadvantages of conventional steroid drugs and NSAID. It is found that specific epoxy monohydroxy forms of eicosapentaenoic acid, docosahexaenoic acid and docosapentaenoic acid which are independently represented by formulae [chemical formula 1], [chemical formula 5] and the like have an inhibitory activity on neutrophils. This compound can inhibit the invasion of neutrophils into tissues and the activation of neutrophils which are observed in acute inflammations.

Claims (27)

1. A compound selected from the group consisting of:

hydrates of the compound, pharmaceutically acceptable salts of the compound, and hydrates of the salts; wherein,

when

is a single bond,

P 1 is hydrogen, alkyl, or hydroxy and

R 1 is hydrogen, or substituted or unsubstituted, branched or unbranched alkyl;

when

is a double bond, P 1 and R 1 are not present;

X is —C(O)OR 2 ;

R 2 is a hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl; and

double bonds of the compound may each be independently in either a cis or trans configuration.

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

or hydrates of the compound, pharmaceutically acceptable salts of the compound, and hydrates of the salts.

3. A neutrophil suppressant composition comprising a compound according to claim 1 , a hydrate of the compound, a pharmaceutically acceptable salt of the compound, or a hydrate of the salt.

4. A pharmaceutical composition comprising a compound according to claim 1 , a hydrate of the compound, a pharmaceutically acceptable salt of the compound, or a hydrate of the salt.

5. The compound according to claim 1 , which is:

or hydrates of the compound, pharmaceutically acceptable salts of the compound, and hydrates of the salts.

6. The compound according to claim 1 , which is:

or hydrates of the compound, pharmaceutically acceptable salts of the compound, and hydrates of the salts.

7. The compound according to claim 1 , which is:

or hydrates of the compound, pharmaceutically acceptable salts of the compound, and hydrates of the salts.

8. The compound according to claim 1 , which is:

or hydrates of the compound, pharmaceutically acceptable salts of the compound, and hydrates of the salts.

9. The compound according to claim 1 , which is:

or hydrates of the compound, pharmaceutically acceptable salts of the compound, and hydrates of the salts.

10. A neutrophil suppressant composition comprising a compound according to claim 2 , a hydrate of the compound, a pharmaceutically acceptable salt of the compound, or a hydrate of the salt.

11. A pharmaceutical composition comprising a compound according to claim 2 , a hydrate of the compound, a pharmaceutically acceptable salt of the compound, or a hydrate of the salt.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2013
From: ARITA, MAKOTO; ARAI, HIROYUKI; ISOBE, YOSUKE; KUBOTA, TADAFUMI
To: THE UNIVERSITY OF TOKYO
Reel/Frame 030088/0580 →
Priority Claims (1)
JP 2010-184473 · Aug 19, 2010 · national
Continuity (1)
Related Publication 20130274327A1 · Oct 17, 2013