Title:
2-FLUOROPHENYLPROPIONIC ACID DERIVATIVE
Document Type and Number:
WIPO Patent Application WO/2013/099553
Kind Code:
A1
Abstract:
Provided is a novel 2-fluorophenylpropionic acid derivative which has excellent anti-inflammatory/analgesic effects, while avoiding side effects such as gastrointestinal disorders, namely a 2-fluorophenylpropionic acid derivative represented by formula (I) or a pharmacologically acceptable salt thereof. (In the formula, R1 represents a hydrogen atom, a halogen atom or a substituted or unsubstituted phenyl group; X represents -CH2-, -NH-, -O- or -S-; and Y specifically represents a group represented by formula (II) (wherein Z1 represents -CO-, -CH(OH)- or -CH2-; and n represents an integer of 1 or 2).)
Inventors:
MIZUSHIMA TORU (JP)
OTSUKA MASAMI (JP)
OKAMOTO YOSHINARI (JP)
YAMAKAWA NAOKI (JP)
OTSUKA MASAMI (JP)
OKAMOTO YOSHINARI (JP)
YAMAKAWA NAOKI (JP)
Application Number:
PCT/JP2012/081646
Publication Date:
July 04, 2013
Filing Date:
December 06, 2012
Export Citation:
Assignee:
LTT BIO PHARMA CO LTD (JP)
MIZUSHIMA TORU (JP)
OTSUKA MASAMI (JP)
OKAMOTO YOSHINARI (JP)
YAMAKAWA NAOKI (JP)
MIZUSHIMA TORU (JP)
OTSUKA MASAMI (JP)
OKAMOTO YOSHINARI (JP)
YAMAKAWA NAOKI (JP)
International Classes:
C07C59/135; A61K31/192; A61K31/195; A61K31/341; A61K31/381; A61P29/00; C07C59/21; C07C229/40; C07C323/56; C07D307/54; C07D333/24
Domestic Patent References:
| WO2010098251A1 | 2010-09-02 | |||
| WO1993002999A1 | 1993-02-18 | |||
| WO2011016376A1 | 2011-02-10 |
Foreign References:
| JP2010195727A | 2010-09-09 |
Other References:
NAOKI YAMAKAWA, ET AL.: "Properties and Synthesis of 2-{2-Fluoro (or Bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic Acid: Nonsteroidal Anti-inflammatory Drugs with Low Membrane Permeabilizing and Gastric Lesion-Producing Activities", JOURNAL OF MEDICINAL CHEMISTRY, vol. 53, no. 21, 18 October 2010 (2010-10-18), pages 7879 - 7882, XP055073416
NAOKI YAMAKAWA, ET AL: "Synthesis and biological evaluation of loxoprofen derivatives", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 19, no. 11, 1 May 2011 (2011-05-01), pages 3299 - 3311, XP028091622
NAOKI YAMAKAWA, ET AL: "Synthesis and Biological Evaluation of Derivatives of 2-{2-Fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic Acid: Nonsteroidal Anti-Inflammatory Drugs with Low Gastric Ulcerogenic Activity", JOURNAL OF MEDICINAL CHEMISTRY, vol. 55, no. 11, 12 March 2012 (2012-03-12), pages 5143 - 5150, XP055073418
N. ENGL. J. MED., vol. 345, 2001, pages 433 - 442
JAMA, vol. 286, 2001, pages 954 - 959
BIOCHEM. PHARMACOL., vol. 63, 2001, pages 817 - 821
BIOCHEM. PHARMACOL., vol. 67, 2004, pages 575 - 585
BIOCHEM. BIOPHYS. RES. COMMUN., vol. 323, 2004, pages 1032 - 1039
J. MED. CHEM., vol. 53, 2010, pages 7879
BIOORG. MED. CHEM., vol. 19, 2011, pages 3299
INFLAMM. RES., vol. 45, 1996, pages 68 - 74
BIOCHEM. PHARMACOL., vol. 67, 2004, pages 575 - 85
BR. J. PHARMACOL., vol. 151, 2007, pages 285 - 91
NAOKI YAMAKAWA, ET AL: "Synthesis and biological evaluation of loxoprofen derivatives", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 19, no. 11, 1 May 2011 (2011-05-01), pages 3299 - 3311, XP028091622
NAOKI YAMAKAWA, ET AL: "Synthesis and Biological Evaluation of Derivatives of 2-{2-Fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic Acid: Nonsteroidal Anti-Inflammatory Drugs with Low Gastric Ulcerogenic Activity", JOURNAL OF MEDICINAL CHEMISTRY, vol. 55, no. 11, 12 March 2012 (2012-03-12), pages 5143 - 5150, XP055073418
N. ENGL. J. MED., vol. 345, 2001, pages 433 - 442
JAMA, vol. 286, 2001, pages 954 - 959
BIOCHEM. PHARMACOL., vol. 63, 2001, pages 817 - 821
BIOCHEM. PHARMACOL., vol. 67, 2004, pages 575 - 585
BIOCHEM. BIOPHYS. RES. COMMUN., vol. 323, 2004, pages 1032 - 1039
J. MED. CHEM., vol. 53, 2010, pages 7879
BIOORG. MED. CHEM., vol. 19, 2011, pages 3299
INFLAMM. RES., vol. 45, 1996, pages 68 - 74
BIOCHEM. PHARMACOL., vol. 67, 2004, pages 575 - 85
BR. J. PHARMACOL., vol. 151, 2007, pages 285 - 91
Attorney, Agent or Firm:
KUSAMA, OSAMU (JP)
Osamu Kusama (JP)
Osamu Kusama (JP)
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