发明名称 Alpha, beta-unsaturated sulfones for treating proliferative disorders
摘要 Sulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents:wherein:Q1 is selected from the group consisting of(a) a phenyl radical according to formula II whereinR1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, amino, C1-C6 trifluoroalkoxy and trifluoromethyl;(b) an aromatic radical selected from the group consisting of 1-naphthyl, 2-naphthyl and 9-anthryl; and(c) an aromatic radical according to formula III whereinn1 is 1 or 2,Y1 and Y2 are independently selected from the group consisting of hydrogen, halogen, and nitro, andX1 is selected from the group consisting of oxygen, nitrogen, sulfur andandQ2 is selected from the group consisting of(d) a phenyl radical according to formula II, as defined above;(e) an aromatic radical selected from the group consisting of 1-naphthyl, 2-naphthyl and 9-anthryl;(f) an aromatic radical according to formula IV whereinn1 is 1 or 2,Y3 and Y4 are independently selected from the group consisting of hydrogen, halogen, and nitro, andX2, X3 and X4 are independently selected from the group consisting of carbon, oxygen, nitrogen, sulfur and provided that not all of X2, X3 and X4 may be carbon; and(g) 1-piperazinyl;provided that at least one of Q1 or Q2 is other than a phenyl radical according to formula II;or a pharmaceutically acceptable salt thereof.Sulfones of formula V are also useful as antiproliferative agents, including, for example, anticancer agents:wherein:X is sulfur or oxygen; Ya and Yb are independently selected from the group consisting of hydrogen, halogen, and nitro; and R1-R5 are defined as above;or a pharmaceutically acceptable salt thereof.
申请公布号 US6599932(B1) 申请公布日期 2003.07.29
申请号 US20020301332 申请日期 2002.11.21
申请人 TEMPLE UNIVERSITY-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION 发明人 REDDY E. PREMKUMAR;REDDY M. V. RAMANA
分类号 C07D295/04;A61K31/10;A61K31/381;A61K31/40;A61K31/426;A61K31/4402;A61K31/4406;A61K31/4409;A61K31/495;A61P7/00;A61P9/10;A61P17/02;A61P19/08;A61P25/00;A61P35/00;A61P35/02;C07C317/10;C07D207/32;C07D207/333;C07D213/32;C07D213/34;C07D277/26;C07D277/36;C07D307/10;C07D307/38;C07D333/18;C07D333/28;C07D333/42;C07D333/48;(IPC1-7):A61K31/38;A61K31/34 主分类号 C07D295/04
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