876147-69-2Relevant academic research and scientific papers
Discovery of cyclic amine-substituted benzoic acids as PPARα agonists
Nomura, Masahiro,Yumoto, Kazuhiro,Shinozaki, Takehiro,Isogai, Shigeki,Takano, Yasuo,Murakami, Koji
experimental part, p. 334 - 338 (2012/02/15)
A series of novel cyclic amine-substituted benzoic acid derivatives were synthesized and evaluated for their PPARα agonist activity. Strucure-activity relationship studies led to the identification of (S)-3-[3-[2-(4-chlorophenyl)-4-methylthyazole-5-carboxamido]piperidin-1-yl] benzoic acid (S)-4f (KRP-105) as a potent and high subtype-selective human PPARα agonist. (S)-4f showed excellent PK profile and oral administration of (S)-4f to high-fat diet dogs effectively lowered triglycerides.
NOVEL CYCLIC AMINOBENZOIC ACID DERIVATIVE
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Page/Page column 72-73, (2010/11/27)
The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds. A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or - (CH2)n- (n represents 0,1 or 2) ; X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and -COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.
NOVEL CYCLIC AMINOPHENYLALKANOIC ACID DERIVATIVE
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Page/Page column 51, (2008/06/13)
The present invention provides cyclic aminophenylalkanoic acid derivatives that act as agonists for human peroxisome proliferator-activated receptors (PPARs), in particular human PPARα isoform, and are effective in the treatment of abnormal lipid metabolism, diabetes and other disorders. The present invention also provides addition salts of such cyclic aminophenylalkanoic acid derivatives and pharmaceutical compositions containing these compounds. Specifically, the present invention provides cyclic aminophenylalkanoic acid derivatives represented by the following general formula (1) : or pharmaceutically acceptable salts thereof.
