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    COMPOUNDS WITH A COMBINATION OF CANNABINOID-CB1 ANTAGONISM AND ACETYLCHOLINESTERASE INHIBITION
    1.
    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。

    COMPOUNDS WITH A COMBINATION OF CANNABINOID CB1 ANTAGONISM AND SEROTONIN REUPTAKE INHIBITION
    2.
    发明申请
    COMPOUNDS WITH A COMBINATION OF CANNABINOID CB1 ANTAGONISM AND SEROTONIN REUPTAKE INHIBITION 有权
    具有CANNABINOID CB1拮抗剂和丝氨酸蛋白酶重排抑制组合的化合物

    公开(公告)号：US20080214559A1

    公开(公告)日：2008-09-04

    申请号：US11970229

    申请日：2008-01-07

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

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

    IPC分类号： A61K31/497 ,  C07D231/38 ,  C07D233/54 ,  C07D403/02 ,  A61P3/04 ,  A61K31/415 ,  A61K31/4164

    CPC分类号： C07D403/12 ,  C07D231/06 ,  C07D233/90

    摘要： Compounds with a combination of cannabinoid CB1 antagonism and serotonin re-uptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed.In at least one embodiment, the invention relates to compounds of the general formula (1); wherein the substitutents have the definitions given in the specification.

    摘要翻译： 具有大麻素CB 1拮抗剂和5-羟色胺再吸收抑制的组合的化合物，含有这些化合物的药物组合物，制备这些化合物的方法，制备用于其合成的新中间体的方法及其制备方法 公开了组合物。 这些化合物和组合物的用途，特别是它们在给予患者以在精神病，焦虑症，抑郁症，注意力缺陷，认知障碍，肥胖症，药物依赖，帕金森病，阿尔茨海默病，疼痛障碍，神经性疼痛障碍中治疗效果方面的用途 并且公开了性障碍。 在至少一个实施方案中，本发明涉及通式（1）的化合物; 其中取代基具有说明书中给出的定义。

    SULPHUR CONTAINING PYRAZOLE DERIVATIVES AS SELECTIVE CANNABINOID CB1 RECEPTOR ANTAGONISTS
    3.
    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。

    Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition
    5.
    发明授权
    Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition 有权
    具有大麻素 - CB1拮抗作用和乙酰胆碱酯酶抑制作用的化合物

    公开(公告)号：US08063062B2

    公开(公告)日：2011-11-22

    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： A61K31/473 ,  C07D401/12

    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-CB1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，制备用于合成这些化合物的新型中间体的方法和制备方法 包含这些化合物的组合物。 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-CB1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。

    Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition
    6.
    发明授权
    Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition 有权
    具有部分烟碱乙酰胆碱受体激动和多巴胺再吸收抑制的组合的阿维醇衍生物

    公开(公告)号：US08252930B2

    公开(公告)日：2012-08-28

    申请号：US12940271

    申请日：2010-11-05

    申请人： Axel Stoit ,  Hein K. A. C. Coolen ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

    发明人： Axel Stoit ,  Hein K. A. C. Coolen ,  Martina A. W. Van Der Neut ,  Cornelis G. Kruse

    IPC分类号： C07D471/02

    CPC分类号： C07D471/04 ,  C07D519/00

    摘要： Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.

    摘要翻译： 描述了式（I）的Azaindole衍生物：其中符号具有说明书中给出的含义。 这些化合物具有部分烟碱乙酰胆碱受体激动和多巴胺再摄取抑制的组合。 本发明还涉及含有这些化合物的药物组合物，其制备方法，制备用于其合成的新型中间体的方法，制备组合物的方法，以及这些化合物和组合物的用途，例如其用于给予患者的用途 以在涉及烟碱受体和/或多巴胺转运蛋白的病症中获得治疗效果，或者可以通过这些受体的操纵来治疗。

    Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition
    7.
    发明授权
    Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition 有权
    具有大麻素CB1拮抗作用和5-羟色胺再摄取抑制作用的化合物

    公开(公告)号：US08138174B2

    公开(公告)日：2012-03-20

    申请号：US11970229

    申请日：2008-01-07

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

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

    IPC分类号： A61K31/55

    CPC分类号： C07D403/12 ,  C07D231/06 ,  C07D233/90

    摘要： Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed.In at least one embodiment, the invention relates to compounds of the general formula (1): wherein the substitutents have the definitions given in the specification.

    摘要翻译： 具有大麻素CB1拮抗作用和5-羟色胺再摄取抑制作用的化合物，含有这些化合物的药物组合物，制备这些化合物的方法，制备用于它们合成的新中间体的方法和制备这些组合物的方法。 这些化合物和组合物的用途，特别是它们在给予患者以在精神病，焦虑症，抑郁症，注意力缺陷，认知障碍，肥胖症，药物依赖，帕金森病，阿尔茨海默病，疼痛障碍，神经性疼痛障碍中治疗效果方面的用途 并且公开了性障碍。 在至少一个实施方案中，本发明涉及通式（1）的化合物：其中取代基具有说明书中给出的定义。

    Piperazine and piperidine compounds
    9.
    再颁专利
    Piperazine and piperidine compounds 有权
    哌嗪和哌啶化合物

    公开(公告)号：USRE41425E1

    公开(公告)日：2010-07-06

    申请号：US12081710

    申请日：2008-04-18

    申请人： Roelof Willem Feenstra ,  Jacobus A. J. Den Hartog ,  Cornelis G. Kruse ,  Martinus T. M. Tulp ,  Stephen K. Long

    发明人： Roelof Willem Feenstra ,  Jacobus A. J. Den Hartog ,  Cornelis G. Kruse ,  Martinus T. M. Tulp ,  Stephen K. Long

    IPC分类号： C07D295/12 ,  A61K31/496

    CPC分类号： C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12

    摘要： A group of new piperazine and piperidine compounds having interesting advantageous pharmacological properties and have the formula (a) wherein A represents a heterocyclic group having 5-7 ring atoms wherein 1-3 heteroatoms selected from the group O, N and S are present, R1 is hydrogen or fluoro, R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2, Z represents carbon or nitrogen, and the dotted line represents a single bond when Z is nitrogen, and represents a single or double bond when Z is carbon, R3 and R4 independently are hydrogen or C1-4-alkyl, n has the value 1 or 2, R5 is 2-pyridyl, 3-pyridyl or 4-pyridyl substituted at the meta-position with respect to the methylene bridge with a group Y, and optionally substituted with (R6)q, Y is a phenyl, furanyl or thienyl group, which groups may be substituted with 1-3 substituents from the group hydroxy, halogen, CF3, C1-4-alkoxy, C1-4-alkyl, cyano aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl, R6 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3 and salts thereof, are disclosed.

    摘要翻译： 一组具有有趣的药理学性质的新的哌嗪和哌啶化合物，其具有式（a）其中A表示具有5-7个环原子的杂环基，其中存在1-3个选自O，N和S的杂原子，R 1 是氢或氟，R 2是C 1-4 - 烷基，C 1-4 - 烷氧基或氧代基，p是0,1或2，Z表示碳或氮，当Z是氮时，虚线表示单键 并且当Z是碳时表示单键或双键，R 3和R 4独立地是氢或C 1-4 - 烷基，n具有1或2，R 5是2-吡啶基，3-吡啶基或4-吡啶基 相对于具有基团Y的亚甲基桥的间位，并且任选地被（R 6）q取代，Y是苯基，呋喃基或噻吩基，该基团可以被1-3个取代基取代，羟基，卤素， CF 3，C 1-4 - 烷氧基，C 1-4 - 烷基，氰基氨基羰基，单 - 或二-C 1-4 - 烷基氨基羰基，R 6是卤素，羟基， C 1-4 - 烷氧基或C 1-4 - 烷基，q为0,1,2或3及其盐。

    SILDENAFIL N-OXIDE AS PRODRUG
    10.
    发明申请
    SILDENAFIL N-OXIDE AS PRODRUG 审中-公开
    SILDENAFIL N-OXIDE作为PRODRUG

    公开(公告)号：US20090005395A1

    公开(公告)日：2009-01-01

    申请号：US12143915

    申请日：2008-06-23

    申请人： Lechoslaw A. Turski ,  Axel Stoit ,  Cornelis G. Kruse ,  Sander Vader ,  Martinus Th.M. Tulp

    发明人： Lechoslaw A. Turski ,  Axel Stoit ,  Cornelis G. Kruse ,  Sander Vader ,  Martinus Th.M. Tulp

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P15/10 ,  A61P9/12

    CPC分类号： C07D487/04

    摘要： Embodiments of the present invention relate to a compound of formula (1A) or a pharmacologically acceptable salt, hydrate, or solvate thereof. Other embodiments of the present invention relate to a pharmaceutical composition containing this compound, to methods for preparing this compound, and to methods for preparing compositions containing this compound. Yet other embodiments of the invention relate to uses of this compound, and compositions containing it, for the manufacture of medicaments and pharmaceutical compositions for treating erectile dysfunction or pulmonary arterial hypertension.

    摘要翻译： 本发明的实施方案涉及式（1A）化合物或其药理学上可接受的盐，水合物或溶剂化物。 本发明的其它实施方案涉及含有该化合物的药物组合物，该化合物的制备方法以及含有该化合物的组合物的制备方法。 本发明的其它实施方案涉及该化合物及其含有组合物用于制备用于治疗勃起功能障碍或肺动脉高压的药物和药物组合物的用途。