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2(1H)-quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities. 1998
Y Koga, and
Y Kihara, and
M Okada, and
Y Inoue, and
S Tochizawa, and
K Toga, and
K Tachibana, and
Y Kimura, and
T Nishi, and
H Hidaka
3rd Tokushima Institute of New Drug Research, Otsuka Pharmaceutical Co., Ltd., Japan.
In order to search for anti-arteriostenotic agents, a series of 2(1H)-quinolinone derivatives was synthesized and evaluated for anti-thrombotic activity and for anti-hyperplastic activity. From this series, (-)-6-[3-[3-cyclopropyl-3-[(1R,2R)-2-hydroxycyclohexyl]ureido]propoxy]-2 (1H)-quinolinone (1p, OPC-33509) was selected as the best candidate by balancing the efficacy on anti-thrombosis and anti-hyperplasia.
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