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    Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists
    3.
    发明授权
    Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists 有权
    含硫吡唑衍生物作为选择性大麻素CB1受体拮抗剂

    公开(公告)号：US07786144B2

    公开(公告)日：2010-08-31

    申请号：US11754544

    申请日：2007-05-29

    申请人： Josephus H. M. Lange ,  Cornelis G. Kruse ,  Bernard J. Van Vliet

    发明人： Josephus H. M. Lange ,  Cornelis G. Kruse ,  Bernard J. Van Vliet

    IPC分类号： A61K31/4155 ,  A61K31/4453 ,  C07D231/10 ,  C07D403/12

    CPC分类号： C07D401/12 ,  C07D403/12

    摘要： The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

    摘要翻译： 本发明涉及含硫吡唑衍生物及其S-氧化的活性代谢物，作为具有高CB1 / CB2受体亚型选择性的选择性大麻素CB1受体拮抗剂，用于制备这些化合物的方法，可用于合成的新中间体 这些吡唑衍生物，包含一种或多种这些吡唑衍生物作为活性成分的药物组合物，以及这些药物组合物用于治疗精神和神经障碍的用途。 化合物具有通式（I），其中符号具有说明书中给出的含义。

    New Phenylpiperazine
    5.
    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。

    COMPOUNDS WITH A COMBINATION OF CANNABINOID-CB1 ANTAGONISM AND ACETYLCHOLINESTERASE INHIBITION
    6.
    发明申请
    COMPOUNDS WITH A COMBINATION OF CANNABINOID-CB1 ANTAGONISM AND ACETYLCHOLINESTERASE INHIBITION 有权
    具有CANNABINOID-CB1拮抗剂和乙酰胆碱酯酶抑制剂的组合的化合物

    公开(公告)号：US20080153867A1

    公开(公告)日：2008-06-26

    申请号：US11957948

    申请日：2007-12-17

    申请人： Josephus H.M. Lange ,  Cornelis G. Kruse ,  Belal Shadid

    发明人： Josephus H.M. Lange ,  Cornelis G. Kruse ,  Belal Shadid

    IPC分类号： A61K31/4439 ,  C07D219/12 ,  A61P35/00 ,  A61P25/00 ,  A61P25/28

    CPC分类号： C07D401/12

    摘要： Embodiments of this invention relate to compounds having a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition is a compound of formula (1) wherein the symbols have the meanings given in the specification.

    摘要翻译： 本发明的实施方案涉及具有大麻素-CB 1拮抗作用和胆碱酯酶抑制的组合的化合物，包含这些化合物的药物组合物，制备这些化合物的方法，制备用于合成的新中间体的方法 的这些化合物，以及制备包含这些化合物的组合物的方法。 本发明还涉及通过向有需要的患者施用包含这些化合物的药物组合物来治疗阿尔茨海默病，认知障碍，记忆障碍，痴呆，注意力缺陷障碍，创伤性脑损伤，药物依赖，成瘾或药物滥用的方法。 具有大麻素-CB 1拮抗剂和胆碱酯酶抑制剂的组合的化合物是式（1）的化合物，其中符号具有说明书中给出的含义。

    SULPHUR CONTAINING PYRAZOLE DERIVATIVES AS SELECTIVE CANNABINOID CB1 RECEPTOR ANTAGONISTS
    7.
    发明申请
    SULPHUR CONTAINING PYRAZOLE DERIVATIVES AS SELECTIVE CANNABINOID CB1 RECEPTOR ANTAGONISTS 有权
    含硫胺衍生物作为选择性CANNABINOID CB1受体拮抗剂

    公开(公告)号：US20070281973A1

    公开(公告)日：2007-12-06

    申请号：US11754544

    申请日：2007-05-29

    申请人： Josephus H.M. Lange ,  Cornelis G. Kruse ,  Bernard J. Van Vliet

    发明人： Josephus H.M. Lange ,  Cornelis G. Kruse ,  Bernard J. Van Vliet

    IPC分类号： A61K31/454 ,  A61K31/416 ,  C07D403/02

    CPC分类号： C07D401/12 ,  C07D403/12

    摘要： The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

    摘要翻译： 本发明涉及含硫吡唑衍生物及其S-氧化的活性代谢物，作为具有高CB 1 / CB 2的选择性大麻素CB 1受体拮抗剂 受体亚型选择性，制备这些化合物的方法，可用于合成这些吡唑衍生物的新中间体，包含一种或多种这些吡唑衍生物作为活性成分的药物组合物，以及使用 的这些用于治疗精神和神经障碍的药物组合物。 化合物具有通式（I），其中符号具有说明书中给出的含义。

    2-aminoquinoline derivatives having d4-agonistic activity
    9.
    发明授权
    2-aminoquinoline derivatives having d4-agonistic activity 有权
    具有d4-激动活性的2-氨基喹啉衍生物

    公开(公告)号：US06281216B1

    公开(公告)日：2001-08-28

    申请号：US09601765

    申请日：2000-10-23

    申请人： Jacobus A. J. Den Hartog ,  Gerben M. Visser ,  Bartholomeus J. Van Steen ,  Martinus T. M. Tulp ,  Eric Ronken ,  Cornelis G. Kruse

    发明人： Jacobus A. J. Den Hartog ,  Gerben M. Visser ,  Bartholomeus J. Van Steen ,  Martinus T. M. Tulp ,  Eric Ronken ,  Cornelis G. Kruse

    IPC分类号： A61K31496

    CPC分类号： C07D215/38 ,  C07D401/12 ,  C07D405/12

    摘要： The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 1 or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)amino, or two groups R1 at adjacent carbon atoms together with the benzene ring may form the benzdioxane group or benzofuran group, X represents nitrogen or carbon, and the dotted line may represent a double bond, (R2)p represents 0, 1 or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)p is a methylene bridge or ethylene bridge, R3 is hydrogen or methyl, and (R)m represents 0, 1, or 2 substituents, which can be the same or different and can be located at all available positions of the quinolyl group, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)amino, on the understanding that R1 cannot represent o-OCH3 when X is nitrogen, (R2)p and R3 are hydrogen, m is 0 and n is 1

    摘要翻译： 本发明涉及一组新的2-氨基喹啉衍生物，其是多巴胺D4-受体的有效和选择性激动剂。 化合物具有通式（I），其中（R1）n表示1或2个可以相同或不同的取代基，可以是C1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基和单 - 或 二烷基（C1-2）氨基或相邻碳原子上的两个基团R 1与苯环可以形成苯并二恶烷基或苯并呋喃基，X代表氮或碳，虚线可以表示双键，（R2）p 代表0,1或2个与甲基和乙基基团相同或不同的取代基，或（R2）p是亚甲基桥或乙烯桥，R3是氢或甲基，（R）m表示0， 1或2个取代基，其可以相同或不同，并且可以位于喹啉基的所有可用位置，C 1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基和单 - 或二烷基 （C1-2）氨基，可以理解，当X是氮时，R1不能表示o-OCH3，（R2）p和R3是氢，m是0，而ni s 1