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15 条记录 (耗时 0.014 秒)

    Phenylpiperazines
    2.
    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。

    Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites
    5.
    发明授权
    Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 有权
    具有对多巴胺-D2受体和5-羟色胺再摄取位点的亲和力的组合的四氢吡啶-4-基吲哚

    公开(公告)号：US07371769B2

    公开(公告)日：2008-05-13

    申请号：US11294657

    申请日：2005-12-06

    申请人： Roelof van Hes ,  Pieter Smid ,  Cornelis G. Kruse ,  Martinus Th. M. Tulp

    发明人： Roelof van Hes ,  Pieter Smid ,  Cornelis G. Kruse ,  Martinus Th. M. Tulp

    IPC分类号： A01N43/64 ,  A61K31/41 ,  C07D209/04

    CPC分类号： C07D401/14

    摘要： The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect.The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof, wherein: R1 is hydrogen, halogen, alkyl(C1-3) or alkoxy(C1-3), CN or CF3, R2 is hydrogen or alkyl(C1-3), R3 is hydrogen or alkyl(C1-3), Z is hydrogen or alkyl(C1-3), alkoxy(C1-3) or alkylthio(C1-3), A is hydrogen or alkyl(C1-3), or A and Z together form a saturated or (partly) unsaturated 5- or 6-membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.

    摘要翻译： 本发明涉及一组具有双重作用方式的新的四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D 2受体的亲和性，制备这些化合物的方法和 涉及可用于合成所述四氢吡啶-4-基吲哚的新型中间体。 本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。 本发明涉及下式的新的四氢吡啶-4-基吲哚。 和其互变异构体，立体异构体，前药，N-氧化物，其药理学上可接受的盐，水合物和溶剂化物，其中：R 1是氢，卤素，烷基（C 1-3 - 或烷氧基（C 1-3 - ），CN或CF 3 R 2，R 2是氢或烷基（C 1-3 - R 3是氢或烷基（C 1-3），Z是氢或烷基（C 1-3） ，烷氧基（C 1-3-3）或烷硫基（C 1-3-3），A是氢或烷基（C 1-3-3）， 或A和Z一起形成饱和或（部分）不饱和的5或6元环，其可被卤素，烷基（C 1-3-3）或苯基取代，其中环Z表示碳 ，硫氮。

    Phenylpiperazines
    6.
    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。

    Benzoylurea compounds, and insecticidal and acaricidal compositions comprising same
    7.
    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：US4656193A

    公开(公告)日：1987-04-07

    申请号：US778433

    申请日：1985-09-20

    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 ,  A01P7/04 ,  C07C273/18 ,  C07C275/54 ,  C07C127/22

    CPC分类号： A01N47/34

    摘要： The invention relates to new benzoylurea compounds of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of halogen and alkyl and haloalkyl having 1-4 carbon atoms,R.sub.2 is a hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of chlorine, methyl and trifluoromethyl, andR.sub.3 is a hydrogen atom or represents 1-3 alkyl and/or alkenyl groups each having 1-6 and/or 2-6 carbon atoms respectively,or wherein R.sub.3 together with the cyclohexyl ring to which it is attached forms a bi- or polycyclic hydrocarbyl group having 8-14 carbon atoms and, if desired, substituted with 1-3 alkyl groups each having 1-4 carbon atoms.The compounds have an insecticidal and acaricidal activity. After having been processed to compositions, the compounds may be used for the control of insects and/or mites in a dosage from 1 to 5000 g of active substance per hectare.

    摘要翻译： 本发明涉及通式为“IMAGE”的新的苯甲酰脲化合物，其中R 1是氢原子或代表1或2个选自卤素和具有1-4个碳原子的烷基和卤代烷基的取代基，R 2是氢 原子或表示1或2个选自氯，甲基和三氟甲基的取代基，R3为氢原子或表示1-3个分别具有1-6个碳原子和/或2-6个碳原子的烷基和/或烯基基团 或其中R 3与其所连接的环己基环一起形成具有8-14个碳原子的双或多环烃基，如果需要，由1-3个分别具有1-4个碳原子的烷基取代。 这些化合物具有杀虫和杀螨活性。 经处理成组合物后，化合物可用于以每公顷1至5000克活性物质的剂量控制昆虫和/或螨虫。

    New Phenylpiperazine
    8.
    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。

    1-Alkoxycarbonylphenylcarbamoyl-3-phenyl-4-cyanoalkyl-2-pyrazolines and use as insecticides
    10.
    发明授权
    1-Alkoxycarbonylphenylcarbamoyl-3-phenyl-4-cyanoalkyl-2-pyrazolines and use as insecticides 失效
    1-烷氧基羰基苯基氨基甲酰基-3-苯基-4-氰基烷基-2-吡唑啉并用作杀虫剂

    公开(公告)号：US4439440A

    公开(公告)日：1984-03-27

    申请号：US375869

    申请日：1982-05-07

    申请人： Roelof van Hes ,  Arnoldus C. Grosscurt

    发明人： Roelof van Hes ,  Arnoldus C. Grosscurt

    IPC分类号： A01N47/36 ,  A01N43/56 ,  A01N47/38 ,  A01P7/04 ,  C07D231/06

    CPC分类号： C07D231/06 ,  A01N47/38 ,  C07C265/12

    摘要： The invention relates to new pyrazoline derivatives having insecticidal activity; the new compounds can be represented by the general formula ##STR1## wherein R is an alkoxycarbonyl group having 2 to 6 carbon atoms,X and Y are equal or different and represent hydrogen atoms or halogen atoms,and n is 2, 3 or 4.After having been processed to compositions, the compounds may be used for the control of insects in a dosage from 0.01 to 1 kg of active substance per hectare.

    摘要翻译： 本发明涉及具有杀虫活性的新的吡唑啉衍生物; 新化合物可以由通式“IMAGE”表示，其中R是具有2至6个碳原子的烷氧羰基，X和Y相同或不同，表示氢原子或卤原子，n为2,3或4。 在被加工成组合物之后，化合物可以用于以0.01至1kg活性物质/公顷的剂量控制昆虫。