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    • 4. 发明申请
    • ALPHA,BETA-UNSATURATED SULFONES FOR TREATING PROLIFERATIVE DISORDERS
    • 用于治疗增生性疾病的ALPHA,硫酸不饱和磺酸
    • WO01078733A1
    • 2001-10-25
    • PCT/US2001/012133
    • 2001-04-13
    • C07D295/04A61K31/10A61K31/381A61K31/40A61K31/426A61K31/4402A61K31/4406A61K31/4409A61K31/495A61P7/00A61P9/10A61P17/02A61P19/08A61P25/00A61P35/00A61P35/02C07C317/10C07D207/32C07D207/333C07D213/32C07D213/34C07D277/26C07D277/36C07D307/10C07D307/38C07D333/18C07D333/28C07D333/42C07D333/48A61K31/275A61K31/385A61K31/435C07D207/08C07D211/70C07D241/04C07D307/02C07D355/02
    • C07D207/333C07C317/10C07D213/34C07D277/36C07D307/10C07D333/18C07D333/42C07D333/48
    • 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), wherein R1, 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), wherein n1 is 1 or 2, Y1 and Y2 are independently selected from the group consisting of hydrogen, halogen, and nitro, and X1 is selected from the group consisting of oxygen, nitrogen, sulfur; and (F2); and Q2 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) wherein n1 is 1 or 2, Y3 and Y4 are independently selected from the group consisting of hydrogen, halogen, and nitro, and X2, X3 and X4 are independently selected from the group consisting of carbon, oxygen, nitrogen, sulfur and (F2) 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.
    • 式(I)的砜可用作抗增殖剂,包括例如抗癌剂,其中Q 1'选自:(a)根据式(II)的苯基,其中R 1,R 2,R 3 R 4和R 5独立地选自氢,卤素,C 1 -C 6烷基,C 1 -C 6烷氧基,硝基,氰基,羧基,羟基,氨基,C 1 -C 6三氟烷氧基和三氟甲基; (b)选自1-萘基,2-萘基和9-蒽基的芳族基团; 和(c)根据式(III)的芳族基团,其中n1是1或2,Y1和Y2独立地选自氢,卤素和硝基,X1选自氧, 氮,硫; 和(F2); 和Q2选自:(d)如上定义的根据式(II)的苯基; (e)选自1-萘基,2-萘基和9-蒽基的芳族基团; (f)根据式(IV)的芳基,其中n1是1或2,Y3和Y4独立地选自氢,卤素和硝基,X2,X3和X4独立地选自 的碳,氧,氮,硫和(F2),条件是不是全部的X 2,X 3和X 4可以是碳; 和(g)1-哌嗪基; 条件是Q1或Q2中的至少一个不是根据式(II)的苯基; 或其药学上可接受的盐。 式(V)的砜也可用作抗增殖剂,包括例如抗癌剂,其中X是硫或氧; Ya和Yb独立地选自氢,卤素和硝基; 和R 1 -R 5如上定义; 或其药学上可接受的盐。