185200-33-3Relevant articles and documents
Synthesis and biological evaluation of benzoic acid derivatives as potent, orally active VLA-4 antagonists
Chiba, Jun,Iimura, Shin,Yoneda, Yoshiyuki,Watanabe, Toshiyuki,Muro, Fumito,Tsubokawa, Masao,Iigou, Yutaka,Satoh, Atsushi,Takayama, Gensuke,Yokoyama, Mika,Takashi, Tohru,Nakayama, Atsushi,Machinaga, Nobuo
, p. 1679 - 1693 (2008/02/03)
A series of benzoic acid derivatives was synthesized as VLA-4 antagonists. Introduction of chlorine or bromine into the 3-position on the central benzene of the diphenylurea portion as in lead compound 2 led to improvement in the pharmacokinetic properties. In particular, 12l demonstrated an acceptable plasma clearance and bioavailability in mice and rats as well as dogs (mice, CL = 18.5 ml/min/kg, F = 28 %; rats, CL = 5.2 ml/min/kg, F = 36 %; dogs, CL = 3.6 ml/min/kg, F = 55 %). Additionally, 12l exhibited potent activity with an IC50 value of 0.51 nM and efficacy by oral administration at a dosage of 10 mg/kg in a rat pleurisy model.
ESTER COMPOUND AND MEDICINAL USE THEREOF
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Page 157, (2008/06/13)
A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1") (wherein ???R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; ???X is -COO- or -CON(R10)-; ???R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; ???R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; ???R8 and R9 are each independently hydrogen atom, C1-C6 alkyl, -CON(R18)(R19) or -COO(R20), etc.; ???ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; ???Alk1 and Alk2 are each independently alkanediyl, etc.; ???l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.
Synthesis of Tiliacora alkaloids. III: Synthesis of biaryls by the Ullmann reaction
Radau, Gregor,Buellesbach, Ralf,Pachaly, Peter
, p. 14735 - 14744 (2007/10/03)
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