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    Spiroazabicyclic heterocyclic compounds
    4.
    发明授权
    Spiroazabicyclic heterocyclic compounds 有权
    螺环双环杂环化合物

    公开(公告)号：US6110914A

    公开(公告)日：2000-08-29

    申请号：US171983

    申请日：1998-10-29

    申请人： Eifion Phillips ,  Robert Mack ,  John Macor ,  Simon Semus

    发明人： Eifion Phillips ,  Robert Mack ,  John Macor ,  Simon Semus

    IPC分类号： C07D491/22 ,  A61K20060101 ,  A61K31/395 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/4365 ,  A61K31/438 ,  A61K31/439 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4738 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/695 ,  A61P20060101 ,  A61P1/00 ,  A61P1/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P43/00 ,  C07D20060101 ,  C07D491/12 ,  C07D491/20 ,  C07D495/12 ,  C07D499/21 ,  C07F5/02 ,  C07F7/18 ,  C07P499/21

    CPC分类号： C07D491/22

    摘要： A compound of formula ##STR1## wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H.sub.2 or F.sub.2 ;A is N or C(R.sup.2); G is N or C(R.sup.3); D is N or C(R.sup.4);with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO;R.sup.1 is hydrogen or C.sub.1 to C.sub.4 alkyl;R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, aryl, heteroaryl, OH, OC.sub.1 -C.sub.4 alkyl, CO.sub.2 R.sup.1, --CN, --NO.sub.2, --NR.sup.5 R.sup.6, --CF.sub.3, --OSO.sub.2 CF.sub.3 or R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, aryl, heteroaryl, OH, OC.sub.1 -C.sub.4 alkyl, CO.sub.2 R.sup.1, --CN, --NO.sub.2, --NR.sup.5 R.sup.6, --CF.sub.3, --OSO.sub.2 CF.sub.3 ; R.sup.5 and R.sup.6 are independently hydrogen, C.sub.1 -C.sub.4 alkyl, C(O)R.sup.7, C(O)NHR.sup.8, C(O)OR.sup.9, SO.sub.2 R.sup.10 or may together be (CH.sub.2).sub.j Q(CH.sub.2).sub.k where Q is O, S, NR.sup.11, or a bond; j is 2 to 7, k is 0 to 2; R.sup.7, R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are independently C.sub.1 -C.sub.4 alkyl, aryl, or heteroaryl, or an enantiomer thereof,and the pharmaceutically acceptable salts thereof, processes for preparing them, composition containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.

    摘要翻译： PCT No.PCT / SE98 / 01364 Sec。 371日期：1998年10月29日第 102（e）1998年10月29日PCT PCT 1998年7月10日PCT公布。 公开号WO99 /​​ 03859 日期1999年1月28日其中n为0或1的下式化合物： m为0或1; p为0或1; X是氧或硫; Y是CH，N或NO; W是氧，H2或F2; A为N或C（R2）; G为N或C（R3）; D是N或C（R4）; 条件是A，G和D中不超过一个为氮，但Y，A，G和D中的至少一个为氮或NO; R1是氢或C1-C4烷基; R2，R3和R4独立地是氢，卤素，C1-C4烷基，C2-C4烯基，C2-C4炔基，芳基，杂芳基，OH，OC1-C4烷基，CO2R1，-CN，-NO2，-NR5R6， CF 3，-OSO 2 CF 3或R 2，R 3或R 3和R 4分别可以一起形成分别含有0和2个氮原子之间的分别为A和G或G和D的六元芳族或杂芳族环，并被一个 C 1 -C 4烷基，C 2 -C 4烯基，C 2 -C 4炔基，芳基，杂芳基，OH，OC 1 -C 4烷基，CO 2 R 1，-CN，-NO 2，-NR 5 R 6 - CF 3，-OSO 2 CF 3; R 5和R 6独立地是氢，C 1 -C 4烷基，C（O）R 7，C（O）NHR 8，C（O）OR 9，SO 2 R 10或可以一起为（CH 2）j Q（CH 2） NR11，或债券; j为2〜7，k为0〜2; R 7，R 8，R 9，R 10和R 11独立地为C 1 -C 4烷基，芳基或杂芳基，或其对映异构体及其药学上可接受的盐，其制备方法，含有它们的组合物及其在治疗中的用途， 在治疗或预防精神病和智力障碍。

    Spiroazabicyclic heterocyclic compounds
    5.
    发明授权
    Spiroazabicyclic heterocyclic compounds 失效
    螺环双环杂环化合物

    公开(公告)号：US07507744B2

    公开(公告)日：2009-03-24

    申请号：US10801085

    申请日：2004-03-15

    申请人： Eifion Phillips ,  Robert Mack ,  John Macor ,  Simon Semus

    发明人： Eifion Phillips ,  Robert Mack ,  John Macor ,  Simon Semus

    IPC分类号： A61K31/4747 ,  C07D221/20

    CPC分类号： C07D491/22

    摘要： A pharmaceutical composition comprising a compound of formula wherein n, m, p, X, Y, W, A, G and D are as defined in the specification, enantiomers thereof, or pharmaceutically acceptable salts thereof, its use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.

    摘要翻译： 一种药物组合物，其包含下式化合物其中n，m，p，X，Y，W，A，G和D如说明书中所定义，其对映体或其药学上可接受的盐，其用于治疗， 治疗或预防精神病和智力障碍。

    Spiroazabicyclic heterocyclic compounds
    7.
    发明授权
    Spiroazabicyclic heterocyclic compounds 失效
    螺环双环杂环化合物

    公开(公告)号：US06706878B2

    公开(公告)日：2004-03-16

    申请号：US10396215

    申请日：2003-03-24

    申请人： Eifion Phillips ,  Robert Mack ,  John Macor ,  Simon Semus

    发明人： Eifion Phillips ,  Robert Mack ,  John Macor ,  Simon Semus

    IPC分类号： C07D49921

    CPC分类号： C07D491/22

    摘要： A compound of formula wherein n, m, p, X, Y, W, A, G and D are as defined in the specification, enantiomers thereof, pharmaceutically acceptable salts thereof, processes for preparing them, composition containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.

    摘要翻译： 制备方法n，m，p，X，Y，W，A，G和D的化合物如说明书中所定义，其对映体，其药学上可接受的盐，制备方法，含有它们的组合物及其在治疗中的用途 特别是治疗或预防精神病和智力障碍。

    Compounds
    8.
    发明授权
    Compounds 有权
    化合物

    公开(公告)号：US06369224B1

    公开(公告)日：2002-04-09

    申请号：US09594703

    申请日：2000-06-16

    申请人： Eifion Phillips ,  Robert Mack ,  John Macor ,  Simon Semus

    发明人： Eifion Phillips ,  Robert Mack ,  John Macor ,  Simon Semus

    IPC分类号： C07F502

    CPC分类号： C07D491/22

    摘要： A compound of formula wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H2 or F2; A is N or C(R2); G is N or C(R3); D is N or C(R4); with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO; R1 is hydrogen or C1 to C4 alkyl; R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3 or R2 and R3, or R3 and R4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3; R5 and R6 are independently hydrogen, C1-C4 alkyl, C(O)R7, C(O)NHR8, C(O)OR9, SO2R10 or may together be (CH2)jQ(CH2)k where Q is O, S, NR11, or a bond; j is 2 to 7, k is 0 to 2; R7, R8, R9, R10, and R11 are independently C1-C4 alkyl, aryl, or heteroaryl, or an enantiomer thereof, and the pharmaceutically acceptable salts thereof, processes for preparing them, composition containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.

    摘要翻译： 化学式为0或1; m为0或1; p为0或1; X是氧或硫; Y是CH，N或NO; W是氧，H 2或F 2; A是N或C（R 2）; G为N或C（R3）; D是N或C（R4）;条件是A，G和D中不超过一个是氮，但Y，A，G和D中的至少一个是氮或NO; R 1是氢或C 1 至C 4烷基; R 2，R 3和R 4独立地是氢，卤素，C 1 -C 4烷基，C 2 -C 4烯基，C 2 -C 4炔基，芳基，杂芳基，OH，OC 1 -C 4烷基，CO 2 R 1，-CN，-NO 2， -NR5R6，-CF3，-OSO2CF3或R2和R3或R3和R4分别可以共同形成分别含有0和2个氮原子之间的分别为A和G或G和D的六元芳族或杂芳族环， 并被一至两个以下取代基取代：独立地是氢，卤素，C 1 -C 4烷基，C 2 -C 4烯基，C 2 -C 4炔基，芳基，杂芳基，OH，OC 1 -C 4烷基，CO 2 R 1，-CN，-NO 2， -NR5R6，-CF3，-OSO2CF3; R 5和R 6独立地是氢，C 1 -C 4烷基，C（O）R 7，C（O）NHR 8，C（O）OR 9，SO 2 R 10或可以一起为（CH 2）j Q（CH 2） NR11，或债券; j为2〜7，k为0〜2; R 7，R 8，R 9，R 10和R 11独立地为C 1 -C 4烷基，芳基或杂芳基，或其对映体及其药学上可接受的盐，其制备方法，含有它们的组合物及其在治疗中的用途， 在治疗或预防精神病和智力障碍。

    Spiroazo bicyclic heterocyclic
    10.
    发明授权
    Spiroazo bicyclic heterocyclic 失效
    螺环双环杂环

    公开(公告)号：US06703502B2

    公开(公告)日：2004-03-09

    申请号：US10093939

    申请日：2002-03-08

    申请人： Eifion Phillips ,  Robert Mack ,  John Macor ,  Simon Semus

    发明人： Eifion Phillips ,  Robert Mack ,  John Macor ,  Simon Semus

    IPC分类号： C07D49122

    CPC分类号： C07D491/22

    摘要： A compound of formula wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H2 or F2; A is N or C(R2); G is N or C(R3); D is N or C(R4); with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO; R1 is hydrogen or C1 to C4 alkyl; R2, R3, and R4 are independently hydrogen, halogen, C1, C4 alkyl, C2, C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1, C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3 or R2 and R3, or R3 and R4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3; R5 and R6 are independently hydrogen, C1-C4 alkyl, C(O)R7, C(O)NHR8, C(O)OR9, SO2R10 or may together be (CH2)jQ(CH2)k where Q is O, S, NR11, or a bond; j is 2 to 7, k is 0 to 2; R7, R8, R9, R10, and R11 are independently C1-C4 alkyl, aryl, or heteroaryl, or an enantiomer thereof, and the pharmaceutically acceptable salts thereof, processes for preparing them, composition containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.

    摘要翻译： 化合物n为0或1; m为0或1; p为0或1; X是氧或硫; Y是CH，N或NO; W是氧，H 2或F 2; A是N或C（R 2）; G是N或C（R 3）; D是N或C（R 4）;条件是A，G和D中不超过一个是氮，但Y，A，G和D中的至少一个是氮或NO; 1>是氢或C1-C4烷基; R 2，R 3和R 4独立地是氢，卤素，C 1，C 4烷基，C 2，C 4烯基，C 2 -C 4炔基，芳基，杂芳基， OH，OC 1，C 4烷基，CO 2 R 1，-CN，-NO 2，-NR 5 R 6，-CF 3，-OSO 2 CF 3或R 2和R 3或R 3和 R 4分别可以一起形成分别含有0和2个氮原子之间并且被一至两个以下取代基取代的分别为A和G或G和D的六元芳族或杂芳族环：独立地为氢 卤素，C 1 -C 4烷基，C 2 -C 4烯基，C 2 -C 4炔基，芳基，杂芳基，OH，OC 1 -C 4烷基，CO 2 R 1，-CN，-NO 2，-NR 5 R 6， -CF 3，-OSO 2 CF 3; R 5和R 6独立地是氢，C 1 -C 4烷基，C（O）R 7，C（O）NHR 8，C（O）OR 9，SO 2 R 10或 可以一起为（CH 2）j Q（CH 2）k，其中Q为O，S，NR 11或键; j为2〜7，k为0〜2; R 7，R 8，R 9，R 10和R 11独立地为C 1 -C 4烷基，芳基，杂芳基或其对映异构体及其药学上可接受的盐， 制备它们，含有它们的组合物及其在治疗中的用途，特别是在治疗或预防精神病和智力障碍障碍中的用途。