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    Method of treatment of visceral pain
    2.
    发明授权
    Method of treatment of visceral pain 失效
    治疗粘膜疼痛的方法

    公开(公告)号：US5063231A

    公开(公告)日：1991-11-05

    申请号：US520108

    申请日：1990-05-07

    申请人： Gareth J. Sanger ,  Helen E. Marr

    发明人： Gareth J. Sanger ,  Helen E. Marr

    IPC分类号： C07D209/52 ,  A61K31/40 ,  A61K31/403 ,  A61K31/435 ,  A61K31/445 ,  A61K31/46 ,  A61K31/55 ,  A61P1/00 ,  A61P25/04 ,  C07D451/06 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  A61K31/44

    CPC分类号： A61K31/46 ,  A61K31/435 ,  A61K31/445 ,  A61K31/55

    摘要： A method of treatment of visceral pain in mammals, including humans, which method comprises the administration to the mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X--CO--Y--Z (I)whereinX is a group of formula (a), (b), (c), (d) or (e): ##STR1## wherein R.sub.a to R.sub.d are selected from hydrogen, halogen or hydroxy;R.sub.1 is hydrogen and R.sub.2 is hydrogen or C.sub.1-4 alkyl; orR.sub.1 and R.sub.2 together are a bond;R.sub.3 to R.sub.7 are independently hydrogen or C.sub.1-6 alkyl; andR.sub.4 together with R.sub.2 may be C.sub.2-7 polymethylene when R.sub.1 is hydrogen; either R.sub.8 is C.sub.1-6 alkoxy;R.sub.9 is hydrogen;R.sub.10 is amino or C.sub.1-7 alkanoylamino; andR.sub.11 is halo or C.sub.1-6 alkylthio; orR.sub.8 is hydrogen;R.sub.9 is halo, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.10 is hydrogen or C.sub.1-6 alkoxy; andR.sub.11 is halo, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;L is CH or N;Y is NH or O, with the proviso that Y is NH when X is (e) and R.sub.8 is C.sub.1-6 alkoxy;Z is a group of formula (f), (g) or (h): ##STR2## wherein n is 2 or 3;p and q are independently 1 to 3; andR.sub.12 or R.sub.13 is methyl or ethyl.

    Novel treatment
    3.
    发明授权
    Novel treatment 失效

    公开(公告)号：US4942160A

    公开(公告)日：1990-07-17

    申请号：US348051

    申请日：1989-05-05

    申请人： Gareth J. Sanger ,  Helen E. Marr

    发明人： Gareth J. Sanger ,  Helen E. Marr

    IPC分类号： C07D209/52 ,  A61K31/40 ,  A61K31/403 ,  A61K31/435 ,  A61K31/445 ,  A61K31/46 ,  A61K31/55 ,  A61P1/00 ,  A61P25/04 ,  C07D451/06 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06

    CPC分类号： A61K31/46 ,  A61K31/435 ,  A61K31/445 ,  A61K31/55

    摘要： A method of treatment of visceral pain in mammals, including humans, which method comprises the administration to the mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X--CO--Y--Z (I)whereinX is a group of formula (a), (b), (c), (d) or (e): ##STR1## wherein R.sub.a to R.sub.d are selected from hydrogen, halogen or hydroxy;R.sub.1 is hydrogen and R.sub.2 is a hydrogen or C.sub.1-4 alkyl; orR.sub.1 and R.sub.2 together are a bond;R.sub.3 to R.sub.7 are independently hydrogen or C.sub.1-6 alkyl; andR.sub.4 together with R.sub.2 may be C.sub.2-7 polymethylene when R.sub.1 is hydrogen;either R.sub.8 is C.sub.1-6 alkoxy;R.sub.9 is hydrogen;R.sub.10 is amino or C.sub.1-7 alkanoylamino; andR.sub.11 is halo or C.sub.1-6 alkylthio; orR.sub.8 is hydrogen;R.sub.9 is halo, or C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.10 is hydrogen or C.sub.1-6 alkoxy; andR.sub.11 is halo, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;L is CH or N;Y is NH or O, with the proviso that Y is NH when X is (e) and R.sub.8 is C.sub.1-6 alkoxy;Z is a group of formula (f), (g) or (h): ##STR2## wherein n is 2 or 3;p and q are independently 1 to 3; andR.sub.12 or R.sub.13 is methyl or ethyl.

    Method of treating emesis, anxiety and/or IBS
    4.
    发明授权
    Method of treating emesis, anxiety and/or IBS 失效
    治疗呕吐，焦虑和/或IBS的方法

    公开(公告)号：US4721720A

    公开(公告)日：1988-01-26

    申请号：US838904

    申请日：1986-03-12

    申请人： Gordon Wootton ,  Gareth J. Sanger

    发明人： Gordon Wootton ,  Gareth J. Sanger

    IPC分类号： C07D403/06 ,  A61K31/40 ,  A61K31/403 ,  A61K31/405 ,  A61K31/415 ,  A61K31/435 ,  A61K31/46 ,  A61K31/55 ,  A61P1/00 ,  A61P1/08 ,  A61P11/00 ,  A61P25/20 ,  A61P35/00 ,  C07D209/52 ,  C07D451/04 ,  C07D451/12 ,  C07D453/02 ,  C07D453/06 ,  A61K31/44

    CPC分类号： A61K31/435 ,  A61K31/40 ,  A61K31/405 ,  A61K31/415 ,  A61K31/46

    摘要： A method of treatment of emesis, anxiety and/or IBS in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or (II) or a pharmaceutically acceptable salt thereof:Ar--Co--Y--Z (I)wherein Ar is a group of formula (a): ##STR1## wherein: R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl groups, thiol, C.sub.1-4 alkylthio; X is CH.sub.2, NR.sub.3, --O-- or --S-- wherein R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.3-5 alkenyl, phenyl or phenyl C.sub.1-4 alkyl; or Ar is a group of formula (b): ##STR2## wherein R.sub.4 to R.sub.7 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl, by C.sub.1-4 alkanoylamino or pyrrolyl, one of R.sub.4 to R.sub.7 being other than hydrogen;Y is --O-- or --NH--; andZ is a group of formula (c), (d) or (e): ##STR3## wherein n is 2, 3 or 4;R.sub.8 is hydrogen, C.sub.1-7 alkyl, C.sub.3-5 alkenyl or phenyl C.sub.1-4 alkyl optionally substituted by one or two halogen, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; ##STR4## wherein: p is 1, 2 or 3; andR.sub.9 is as defined above for R.sub.8 ;and with the proviso that, when Ar is of formula (b) and Y is --NH--, Z is a group of formula (d) or (e); ##STR5## wherein R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl-C.sub.1-3 alkyl; andone of the groups represented by R.sub.11, R.sub.12 and R.sub.13 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-C.sub.1-3 alkyl and each of the other groups, which may be the same or different, is hydrogen or C.sub.1-6 alkyl.

    Novel treatment
    5.
    发明授权
    Novel treatment 失效
    小说治疗

    公开(公告)号：US4851407A

    公开(公告)日：1989-07-25

    申请号：US245892

    申请日：1988-09-16

    申请人： Gordon Wootton ,  Gareth J. Sanger

    发明人： Gordon Wootton ,  Gareth J. Sanger

    IPC分类号： C07D403/06 ,  A61K31/40 ,  A61K31/403 ,  A61K31/405 ,  A61K31/415 ,  A61K31/435 ,  A61K31/46 ,  A61K31/55 ,  A61P1/00 ,  A61P1/08 ,  A61P11/00 ,  A61P25/20 ,  A61P35/00 ,  C07D209/52 ,  C07D451/04 ,  C07D451/12 ,  C07D453/02 ,  C07D453/06

    CPC分类号： A61K31/435 ,  A61K31/40 ,  A61K31/405 ,  A61K31/415 ,  A61K31/46

    摘要： A method of treatment of emesis, anxiety and/or IBS in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or (II) or a pharmaceutically acceptable salt thereof:Ar--CO--Y--Z (I)wherein Ar is a group of formula (a): ##STR1## wherein: R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl groups, thiol, C.sub.1-4 alkylthio; X is CH.sub.2, NR.sub.3, --O-- or --S-- wherein R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.3-5 alkenyl, phenyl or phenyl C.sub.1-4 alkyl; or Ar is a group of formula (b): ##STR2## wherein R.sub.4 to R.sub.7 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl, by C.sub.1-4 alkanoylamino or pyrrolyl, one of R.sub.4 to R.sub.7 being other than hydrogen;Y is --O-- or --NH--; andZ is a group of formula (c), (d) or (e): ##STR3## wherein n is 2, 3 or 4;R.sub.8 is hydrogen, C.sub.1-7 alkyl, C.sub.3-5 alkenyl or phenyl C.sub.1-4 alkyl optionally substituted by one or two halogen, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; ##STR4## wherein: p is 1, 2 or 3; andR.sub.9 is as defined above for R.sub.8 ; and with the proviso that, when Ar is of formula (b) and Y is --NH--, Z is a group of formula (d) or (e); ##STR5## wherein R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl-C.sub.1-3 alkyl; andone of the groups represented by R.sub.11, R.sub.12 and R.sub.13 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-C.sub.1-3 alkyl and each of the other groups, which may be the same or different, is hydrogen or C.sub.1-6 alkyl.

    Novel treatment
    6.
    发明授权
    Novel treatment 失效

    公开(公告)号：US4845092A

    公开(公告)日：1989-07-04

    申请号：US145537

    申请日：1988-01-19

    申请人： Gareth J. Sanger ,  Helen E. Marr

    发明人： Gareth J. Sanger ,  Helen E. Marr

    IPC分类号： C07D209/52 ,  A61K31/40 ,  A61K31/403 ,  A61K31/435 ,  A61K31/445 ,  A61K31/46 ,  A61K31/55 ,  A61P1/00 ,  A61P25/04 ,  C07D451/06 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06

    CPC分类号： A61K31/46 ,  A61K31/435 ,  A61K31/445 ,  A61K31/55

    摘要： A method of treatment of visceral pain in mammals, including humans, which method comprises the administration to the mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X-CO-Y-Z (I)whereinX is a group of formula (a), (b), (c), (d) or (e): ##STR1## wherein R.sub.a to R.sub.d are selected from hydrogen, halogen or hydroxy;R.sub.1 is hydrogen and R.sub.2 is hydrogen or C.sub.1-4 alkyl; orR.sub.1 and R.sub.2 together are a bond;R.sub.3 and R.sub.7 are independently hydrogen or C.sub.1-6 alkyl; andR.sub.4 together with R.sub.2 may be C.sub.2-7 polymethylene when R.sub.1 is hydrogen;either R.sub.8 is C.sub.1-6 alkoxy;R.sub.9 is hydrogen;R.sub.10 is amino or C.sub.1-7 alkanoylamino; andR.sub.11 is halo or C.sub.1-6 alkylthio; orR.sub.8 is hydrogen;R.sub.9 is halo, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.10 is hydrogen or C.sub.1-6 alkoxy; andR.sub.11 is halo, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;L is CH or N;Y is NH or O, with the proviso that Y is NH when X is (e) and R.sub.8 is C.sub.1-6 alkoxy;Z is a group of formula (f), (g) or (h): ##STR2## wherein n is 2 or 3;p and q are independently 1 to 3; andR.sub.12 and R.sub.13 is methyl or ethyl.

    Treatment of migraine, cluster headaches and trigeminal neuralgia
    7.
    发明授权
    Treatment of migraine, cluster headaches and trigeminal neuralgia 失效
    治疗偏头痛，丛集性头痛和三叉神经痛

    公开(公告)号：US4786643A

    公开(公告)日：1988-11-22

    申请号：US122920

    申请日：1987-11-19

    申请人： Gareth J. Sanger ,  Wesley D. Miner

    发明人： Gareth J. Sanger ,  Wesley D. Miner

    IPC分类号： C07D451/14 ,  A61K31/435 ,  A61K31/445 ,  A61K31/46 ,  A61K31/55 ,  A61P1/08 ,  A61P9/06 ,  A61P25/04

    CPC分类号： A61K31/55 ,  A61K31/445 ,  A61K31/46

    摘要： A method of treatment of migraine, cluster headaches and trigeminal neuralgia, radiation or cytotoxic agent induced nausea and vomiting and/or cardiac arrhythmia in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkyl;R.sub.2 is amino or C.sub.1-7 acylamino;R.sub.3 is halo;one of R.sub.4 and R.sub.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-3 alkyl, which phenyl moieties may be substituted by one or more substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen;the other of R.sub.4 and R.sub.5 is hydrogen or C.sub.1-6 alkyl;p is 0 to 2; andq is 0 to 3.

    Treatment of emesis, nausea and vomiting
    9.
    发明授权
    Treatment of emesis, nausea and vomiting 失效
    治疗呕吐，恶心和呕吐

    公开(公告)号：US4783478A

    公开(公告)日：1988-11-08

    申请号：US71424

    申请日：1987-07-09

    申请人： Gordon Wootton ,  Gareth J. Sanger

    发明人： Gordon Wootton ,  Gareth J. Sanger

    IPC分类号： C07D403/06 ,  A61K31/40 ,  A61K31/403 ,  A61K31/405 ,  A61K31/415 ,  A61K31/435 ,  A61K31/46 ,  A61K31/55 ,  A61P1/00 ,  A61P1/08 ,  A61P11/00 ,  A61P25/20 ,  A61P35/00 ,  C07D209/52 ,  C07D451/04 ,  C07D451/12 ,  C07D453/02 ,  C07D453/06

    CPC分类号： A61K31/435 ,  A61K31/40 ,  A61K31/405 ,  A61K31/415 ,  A61K31/46

    摘要： A method of treatment of emesis, anxiety and/or IBS in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or (II) or a pharmaceutically acceptable salt thereof:Ar--CO--Y--Z (I)wherein Ar is a group of formula (a): ##STR1## wherein: R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl groups, thiol, C.sub.1-4 alkylthio; X is CH.sub.2, NR.sub.3, --O-- or --S-- wherein R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.3-5 alkenyl, phenyl or phenyl C.sub.1-4 alkyl;or Ar is a group of formula (b): ##STR2## wherein R.sub.4 to R.sub.7 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl, by C.sub.1-4 alkanoylamino or pyrrolyl, one of R.sub.4 to R.sub.7 being other than hydrogen;Y is --O-- or --NH--; andZ is a group of formula (c), (d) or (e): ##STR3## wherein n is 2, 3 or 4;R.sub.8 is hydrogen, C.sub.1-7 alkyl, C.sub.3-5 alkenyl or phenyl C.sub.1-4 alkyl optionally substituted by one or two halogen, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; ##STR4## wherein: p is 1, 2 or 3; andR.sub.9 is as defined above for R.sub.8 ;and with the proviso that, when Ar is of formula (b) and Y is --NH--, Z is a group of formula (d) or (e); ##STR5## wherein R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl-C.sub.1-3 alkyl; andone of the group represented by R.sub.11, R.sub.12 and R.sub.13 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-C.sub.1-3 alkyl and each of the other groups, which may be the same or different, is hydrogen or C.sub.1-6 alkyl.

    Novel treatment
    10.
    发明授权
    Novel treatment 失效
    小说治疗

    公开(公告)号：US4725603A

    公开(公告)日：1988-02-16

    申请号：US876724

    申请日：1986-06-20

    申请人： Gareth J. Sanger ,  Wesley D. Miner

    发明人： Gareth J. Sanger ,  Wesley D. Miner

    IPC分类号： C07D451/14 ,  A61K31/435 ,  A61K31/445 ,  A61K31/46 ,  A61K31/55 ,  A61P1/08 ,  A61P9/06 ,  A61P25/04 ,  A61K31/44

    CPC分类号： A61K31/55 ,  A61K31/445 ,  A61K31/46

    摘要： A method of treatment of migraine, cluster headaches and trigeminal neuralgia, radiation or cytotoxic agent induced nausea and vomiting and/or cardiac arrhythmia in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkyl;R.sub.2 is amino or C.sub.1-7 acylamino;R.sub.3 is halo;one of R.sub.4 and R.sub.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-3 alkyl, which phenyl moieties may be substituted by one or more substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen;the other of R.sub.4 and R.sub.5 is hydrogen or C.sub.1-6 alkyl;p is 0 to 2; andq is 0 to 3.

    摘要翻译： 一种治疗偏头痛，丛集性头痛和三叉神经痛，辐射或细胞毒剂的哺乳动物包括人的恶心和呕吐和/或心律失常的方法，包括给予有效量的式（I）化合物或其药学上可接受的盐 （I）其中：R 1是C 1-6烷基; R2是氨基或C1-7酰氨基; R3是卤素; R4和R5之一是氢，C1-6烷基，苯基或苯基C1-3烷基，该苯基部分可以被一个或多个选自C 1-6烷基，C 1-6烷氧基，CF 3或卤素的取代基取代; R4和R5中的另一个是氢或C 1-6烷基; p为0〜2; q为0〜3。