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    New Phenylpiperazine
    1.
    发明申请
    New Phenylpiperazine 失效
    新苯基哌嗪

    公开(公告)号：US20090143406A1

    公开(公告)日：2009-06-04

    申请号：US12258591

    申请日：2008-10-27

    申请人： Roelof Van Hes ,  Johannes A. M. Van der Heijden ,  Cornelis G. Kruse ,  Jacobus Tipker ,  Martinus T.M Tulp ,  Gerben M. Visser ,  Bernard J. Van Vliet

    发明人： Roelof Van Hes ,  Johannes A. M. Van der Heijden ,  Cornelis G. Kruse ,  Jacobus Tipker ,  Martinus T.M Tulp ,  Gerben M. Visser ,  Bernard J. Van Vliet

    IPC分类号： A61K31/496 ,  C07D403/04

    CPC分类号： C07D401/12 ,  C07D209/34 ,  C07D209/40 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia.The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.

    摘要翻译： 本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D2受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与多巴胺能和/或血清素能系统中的干扰相关的病症的能力，例如 作为焦虑障碍，抑郁症，帕金森病和精神分裂症。 本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R5和R6独立地是氢或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）p - 其中p具有3-5，R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或R6 + R7（吲哚基的第7位的R7）表示基团 - （CH 2）q，其中q具有2-4，及其盐。

    Phenylpiperazines
    3.
    发明授权
    Phenylpiperazines 有权
    苯基哌嗪

    公开(公告)号：US07456182B2

    公开(公告)日：2008-11-25

    申请号：US11450323

    申请日：2006-06-12

    申请人： Roelof Van Hes ,  Johannes A. M. Van der Heijden ,  Cornelis G. Kruse ,  Jacobus Tipker ,  Martinus T. M. Tulp ,  Gerben M. Visser ,  Bernard J. Van Vliet

    发明人： Roelof Van Hes ,  Johannes A. M. Van der Heijden ,  Cornelis G. Kruse ,  Jacobus Tipker ,  Martinus T. M. Tulp ,  Gerben M. Visser ,  Bernard J. Van Vliet

    IPC分类号： A61K31/496 ,  C07D403/12 ,  C07D413/12

    CPC分类号： C07D401/12 ,  C07D209/34 ,  C07D209/40 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia.The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.

    摘要翻译： 本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D 2 O受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与 多巴胺能和/或血清素能系统如焦虑障碍，抑郁症，帕金森病和精神分裂症。 本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R 5和R 6独立地是H或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）2 - ，其中p的值为3 -5和R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或吲哚基的第7位上的R 6（R 7）表示 - （CH 2）2 - 其中q具有2-4，及其盐。

    Phenylpiperazine
    4.
    发明授权
    Phenylpiperazine 失效
    苯基哌嗪

    公开(公告)号：US07605162B2

    公开(公告)日：2009-10-20

    申请号：US12258591

    申请日：2008-10-27

    申请人： Roelof Van Hes ,  Johannes A. M. Van der Heijden ,  Cornelis G. Kruse ,  Jacobus Tipker ,  Martinus T. M. Tulp ,  Gerben M. Visser ,  Bernard J. Van Vliet

    发明人： Roelof Van Hes ,  Johannes A. M. Van der Heijden ,  Cornelis G. Kruse ,  Jacobus Tipker ,  Martinus T. M. Tulp ,  Gerben M. Visser ,  Bernard J. Van Vliet

    IPC分类号： A61K31/496 ,  C07D403/12

    CPC分类号： C07D401/12 ,  C07D209/34 ,  C07D209/40 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia.The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.

    摘要翻译： 本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D2受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与多巴胺能和/或血清素能系统中的干扰相关的病症的能力，例如 作为焦虑障碍，抑郁症，帕金森病和精神分裂症。 本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R5和R6独立地是氢或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）p - 其中p具有3-5，R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或R6 + R7（吲哚基的第7位的R7）表示基团 - （CH 2）q，其中q具有2-4，及其盐。

    Phenylpiperazines
    5.
    发明授权
    Phenylpiperazines 失效
    苯基哌嗪

    公开(公告)号：US07067513B1

    公开(公告)日：2006-06-27

    申请号：US10069256

    申请日：2000-08-22

    申请人： Roelof Van Hes ,  Johannes A. M. Van der Heijden ,  Cornelis G Kruse ,  Jacobus Tipker ,  Martinus T. M Tulp ,  Gerben M Visser ,  Bernard J Van Vliet

    发明人： Roelof Van Hes ,  Johannes A. M. Van der Heijden ,  Cornelis G Kruse ,  Jacobus Tipker ,  Martinus T. M Tulp ,  Gerben M Visser ,  Bernard J Van Vliet

    IPC分类号： A61K31/536 ,  A61K31/5415 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

    CPC分类号： C07D401/12 ,  C07D209/34 ,  C07D209/40 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders.The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.

    摘要翻译： 本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D 2 O受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与 多巴胺能和/或血清素能系统如侵略，焦虑障碍，孤独症，眩晕，抑郁，认知障碍，记忆障碍，帕金森病，精神分裂症和精神病性疾病。 本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R 5和R 6独立地是H或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）2 - ，其中p的值为3 -5和R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或吲哚基的第7位上的R 6（R 7）表示 - （CH 2）2 - 其中q具有2-4，及其盐。

    3,4-dehydropiperidine derivatives having psychotropic activity
    7.
    发明授权
    3,4-dehydropiperidine derivatives having psychotropic activity 失效
    具有精神活性的3,4-脱水哌啶衍生物

    公开(公告)号：US5296497A

    公开(公告)日：1994-03-22

    申请号：US968267

    申请日：1992-10-30

    申请人： Jan Hartog ,  Roelof Van Hes ,  Berend Olivier ,  Ineke Van Wijngaarden

    发明人： Jan Hartog ,  Roelof Van Hes ,  Berend Olivier ,  Ineke Van Wijngaarden

    IPC分类号： C07D211/70 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D411/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  A61K31/44

    CPC分类号： C07D405/04 ,  C07D211/70 ,  C07D405/14 ,  C07D409/04 ,  C07D411/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    摘要： The invention relates to 3,4-dehydropiperidine derivatives having psychotropic activity, which compounds are represented by the general formula 1 ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.3 alkyl;R.sub.2 is hydrogen, an unsubstituted or substituted C.sub.1 -C.sub.10 hydrocarbon group, or a group of the general formula ##STR2## wherein A is C.sub.2 -C.sub.10 alkylene,R.sub.5 is hydrogen or C.sub.1 -C.sub.3 alkyl, andR.sub.6 is unsubstituted or substituted aryl or heteroaryl, hydrocarbon, substituted or unsubstituted (hetero)aralkyl, or substituted or unsubstituted heterocyclic; or wherein R.sub.5 and R.sub.6 together with the carbamoyl group to which they are bound constitute a heterocyclic ring system;n has the value 1 or 2; andZ is a heterocyclic group.

    摘要翻译： 本发明涉及具有精神活性的3,4-脱水哌啶衍生物，该化合物由通式1（*化学结构*）（1）表示，其中R是氢或C 1 -C 3烷基; R2是氢，未取代或取代的C1-C10烃基或通式（*化学结构*）的基团，其中A是C2-C10亚烷基，R5是氢或C1-C3烷基，R6是未取代或取代的 芳基或杂芳基，烃，取代或未取代的（杂）芳烷基或取代或未取代的杂环; 或其中R 5和R 6与它们所连接的氨基甲酰基一起构成杂环体系; n的值为1或2; Z为杂环基。

    Benzoylurea compounds, and insecticidal and acaricidal compositions comprising same
    8.
    发明授权
    Benzoylurea compounds, and insecticidal and acaricidal compositions comprising same 失效
    苯甲酰脲化合物和包含它们的杀虫和杀螨组合物

    公开(公告)号：US4783485A

    公开(公告)日：1988-11-08

    申请号：US912169

    申请日：1986-09-26

    申请人： Marius S. Brouwer ,  Arnoldus C. Grosscurt ,  Roelof Van Hes

    发明人： Marius S. Brouwer ,  Arnoldus C. Grosscurt ,  Roelof Van Hes

    IPC分类号： A01N47/34 ,  A01N47/36 ,  C07D213/75 ,  C07C127/22

    CPC分类号： C07D213/75 ,  A01N47/34 ,  A01N47/36

    摘要： The invention relates to new benzoylurea compounds having insecticidal and acaricidal activity, of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom or represents 1 or 2 halogen atoms;Ar is a para-phenylene group or a para-pyridylene group, which groups may be substituted with 1 or 2 substituents selected from the group consisting of chlorine, methyl and trifluoromethyl;B is an oxygen atom or represents a group having the formula ##STR2## wherein R.sub.2 is a hydrogen atom or an alkyl group having 1-4 carbon atoms; andR is a cycloalkyl group or a cycloalkenyl group having 6-12 carbon atoms, which groups may be substituted with 1-3 substituents selected from the group consisting of alkyl and alkenyl having 1-6 carbon atoms, or whereinR is a bi- or polycyclic, saturated or unsaturated, hydrocarbyl group, having 8-14 carbon atoms and, if desired, substituted with 1-3 substituents selected from the group consisting of alkyl and alkenyl having 1-6 carbon atoms;with the proviso, that,if Ar is a whether or not substituted para-phenylene group, andR is a whether or not substituted cyclohexyl-group, or a saturated bi- or polycyclic hydrocarbyl group having 8-14 carbon atoms, then B does not represent an oxygen atom.

    摘要翻译： 本发明涉及具有杀虫和杀螨活性的新的苯甲酰脲化合物，通式为其中R 1为氢原子或表示1或2个卤原子的通式（Ⅰ） Ar是对亚苯基或对 - 亚吡啶基，该基团可以被1或2个选自氯，甲基和三氟甲基的取代基取代; B是氧原子，或表示具有式“IMAGE”的基团，其中R2是氢原子或具有1-4个碳原子的烷基; 并且R是具有6-12个碳原子的环烷基或环烯基，该基团可以被选自具有1-6个碳原子的烷基和烯基的1-3个取代基取代，或其中R是双 - 或具有8-14个碳原子的多环，饱和或不饱和的烃基，如果需要，被1-3个选自具有1-6个碳原子的烷基和烯基的取代基取代; 条件是，如果Ar是否为取代的对亚苯基，R为无取代的环己基，还是具有8-14个碳原子的饱和双环或多环烃基，则B为 不代表氧原子。