IP Library Granted Patent US 9,102,630
Granted Patent B2
US 9,102,630 · App. 14/206,540 · Granted Aug 11, 2015

Crystals of salts of phenylalanine derivatives

Inventors: Noriyasu Kataoka (Ota-ku, JP); Riho Kodama (Kawasaki, JP); Akinori Tatara (Yokohama, JP)
Assignee: AJINOMOTO CO., INC.
C07D239/96
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Quick Facts
Patent No.
US 9,102,630
App. No.
14/206,540
Granted
Aug 11, 2015
Kind
B2
Abstract

Provided is a crystal of a salt of the compound represented by formula (I), which is excellent in its solubility in water. In particular, also provided is a crystal of hydrochloride, hydrobromate, sulfate, nitrate, p-toluenesulfonate or methanesulfonate of the compound represented by formula (I).

Claims (12)

1. A method of treating rheumatoid arthritis, inflammatory, intestinal diseases, systemic lupus erythematosus, disseminated or multiple sclerosis, Sjogren's syndromes, asthma, psoriasis, allergy, diabetes (mellitus), cardiovascular diseases, arterial sclerosis, restenosis, tumor hyperplasia, tumor metastasis, or graft rejection, comprising administering to a subject in need thereof an effective amount of a the compound represented by formula (I):

or a pharmaceutically-acceptable acid addition salt thereof, and

at least one additional pharmaceutical agent selected from the group consisting of 5-ASA pharmaceutical preparations, adrenocortical hormone-containing pharmaceutical preparations, antibacterial agents, immunosuppressive agents and anti-cytokine agents.

2. The method of claim 1 , which is a method of treating an inflammatory intestinal disease.

3. The method of claim 1 , which is a method of treating Crohn's disease.

4. The method of claim 1 , which is a method of treating ulcerative colitis.

5. The method of claim 1 , wherein the compound represented by formula (I) is in the form of a pharmaceutically-acceptable acid addition salt.

6. The method of claim 1 , wherein the compound represented by formula (I) is in the form of a crystal of a pharmaceutically-acceptable acid addition salt.

7. The method of claim 1 , wherein the compound represented by formula (I) is a hydrochloric acid addition salt.

8. The method of claim 1 , wherein the compound represented by formula (I) is in the form of a crystal of a hydrochloric acid addition salt.

9. The method of claim 1 , wherein the additional pharmaceutical agent is a 5-ASA pharmaceutical preparation which is mesalazine or salzosulfapyrizine.

10. The method of claim 1 , wherein the additional pharmaceutical agent is a anti-cytokine agent selected from the group consisting of anti-TNF antibodies, anti-IL6-receptor antibodies, anti-IL-12/23 antibodies and anti-IL-17 receptor antibodies.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 21, 2016
From: AJINOMOTO CO., INC.
To: EA PHARMA CO., LTD.
Reel/Frame 039094/0087 →
Priority Claims (1)
JP 2010-074617 · Mar 29, 2010 · national
Continuity (3)
Continuation 13632474 · Oct 1, 2012
Continuation PCTJP2011057798 · Mar 29, 2011
Related Publication 20140206705A1 · Jul 24, 2014