1241405-27-5Relevant academic research and scientific papers
Loxoprofen derivative
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Paragraph 0035-0036; 0042, (2019/01/23)
The invention provides a Loxoprofen derivative. Gastrointestinal tract side effects are low, and the bioavailability can be improved.
2-FLUOROPHENYL PROPIONIC ACID DERIVATIVES
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, (2014/11/13)
Provided are novel 2-fluorophenyl propionic acid derivatives which have excellent anti-inflammatory/analgesic effects while avoiding side effects such as gastrointestinal disorders, namely 2-fluorophenyl propionic acid derivatives represented by the formula (I) below or pharmaceutically acceptable salts thereof, [wherein, 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 group (II) (wherein, Z1 represents —CO—, —CH(OH)—, or —CH2—, and n represents an integer of 1 or 2.)]
LOXOPROFEN DERIVATIVE AND PHARMACEUTICAL PREPARATION CONTAINING THE SAME
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Page/Page column 3-4, (2012/02/01)
There is provided a novel loxoprofen derivative that has no side effect such as a gastrointestinal disorder and also has excellent anti-inflammatory and analgesic effects and is represented by the following formula (I) or (II): (wherein R1 and
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
Yamakawa, Naoki,Suemasu, Shintaro,Okamoto, Yoshinari,Tanaka, Ken-Ichiro,Ishihara, Tomoaki,Asano, Teita,Miyata, Keishi,Otsuka, Masami,Mizushima, Tohru
, p. 5143 - 5150 (2012/09/07)
We previously reported that 2-fluoroloxoprofen has lower gastric ulcerogenic activity than loxoprofen, a nonsteroidal anti-inflammatory drug (NSAID) without selectivity for COX-2. We synthesized derivatives of 2-fluoroloxoprofen and studied their properti
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
Yamakawa, Naoki,Suemasu, Shintaro,Matoyama, Masaaki,Kimoto, Ayumi,Takeda, Miho,Tanaka, Ken-Ichiro,Ishihara, Tomoaki,Katsu, Takashi,Okamoto, Yoshinari,Otsuka, Masami,Mizushima, Tohru
supporting information; experimental part, p. 7879 - 7882 (2011/02/22)
We previously proposed that membrane permeabilization activity of NSAIDs is involved in NSAID-induced gastric lesions. We here synthesized derivatives of loxoprofen that have lower membrane permeabilization activity than other NSAIDs. Compared to loxoprofen, the derivatives 10a and 10b have lower membrane permeabilization activity and their oral administration produced fewer gastric lesions but showed an equivalent anti-inflammatory effect. These results suggest that 10a and 10b are likely to be therapeutically beneficial as safer NSAIDs.
