Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same
    1.
    发明授权
    Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same 有权
    哌嗪基 - 丙基 - 吡唑衍生物作为多巴胺D4受体拮抗剂,以及含有它们的药物组合物

    公开(公告)号:US08372844B2

    公开(公告)日:2013-02-12

    申请号:US13454817

    申请日:2012-04-24

    CPC分类号: C07D403/06

    摘要: The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.

    摘要翻译: 本发明涉及一种新的哌嗪基 - 丙基 - 吡唑衍生物,其制备方法和包含其的药学上可接受的组合物。 本发明的新型哌嗪基 - 丙基 - 吡唑衍生物对多巴胺D4受体具有优异的选择性亲和力,可有效抑制阿扑吗啡诱导的精神病性行为(笼养),并在小鼠旋转试验中具有较低的不良反应。 因此,它可以被开发为用于治疗和预防中枢神经系统(CNS)障碍,特别是精神分裂症,注意缺陷多动障碍,抑郁症,压力疾病,恐慌症,恐惧症,强迫症,创伤后疼痛的治疗剂 压力障碍,认知障碍,阿尔茨海默病,帕金森病,焦虑症,过敏性反应,躁狂症,癫痫发作,人格障碍,偏头痛,药物成瘾,酒精成瘾,肥胖,进食障碍和睡眠障碍。

    PIPERAZINYL-PROPYL-PYRAZOLE DERIVATIVES AS DOPAMINE D4 RECEPTOR ANTAGONISTS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    2.
    发明申请
    PIPERAZINYL-PROPYL-PYRAZOLE DERIVATIVES AS DOPAMINE D4 RECEPTOR ANTAGONISTS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 有权
    作为DOPAMINE D4受体拮抗剂的哌嗪衍生物 - 吡咯并吡啶衍生物,以及含有它们的药物组合物

    公开(公告)号:US20100063286A1

    公开(公告)日:2010-03-11

    申请号:US12530312

    申请日:2007-07-13

    IPC分类号: C07D403/06

    CPC分类号: C07D403/06

    摘要: The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.

    摘要翻译: 本发明涉及一种新的哌嗪基 - 丙基 - 吡唑衍生物,其制备方法和包含其的药学上可接受的组合物。 本发明的新型哌嗪基 - 丙基 - 吡唑衍生物对多巴胺D4受体具有优异的选择性亲和力,可有效抑制阿扑吗啡诱导的精神病性行为(笼养),并在小鼠旋转试验中具有较低的不良反应。 因此,它可以被开发为用于治疗和预防中枢神经系统(CNS)障碍,特别是精神分裂症,注意缺陷多动障碍,抑郁症,压力疾病,恐慌症,恐惧症,强迫症,创伤后疼痛的治疗剂 压力障碍,认知障碍,阿尔茨海默病,帕金森病,焦虑症,过敏性反应,躁狂症,癫痫发作,人格障碍,偏头痛,药物成瘾,酒精成瘾,肥胖,进食障碍和睡眠障碍。

    Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same
    3.
    发明授权
    Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same 有权
    哌嗪基 - 丙基 - 吡唑衍生物作为多巴胺D4受体拮抗剂,以及含有它们的药物组合物

    公开(公告)号:US08236806B2

    公开(公告)日:2012-08-07

    申请号:US12530312

    申请日:2007-07-13

    CPC分类号: C07D403/06

    摘要: The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.

    摘要翻译: 本发明涉及一种新的哌嗪基 - 丙基 - 吡唑衍生物,其制备方法和包含其的药学上可接受的组合物。 本发明的新型哌嗪基 - 丙基 - 吡唑衍生物对多巴胺D4受体具有优异的选择性亲和力,可有效抑制阿扑吗啡诱导的精神病性行为(笼养),并在小鼠旋转试验中具有较低的不良反应。 因此,它可以被开发为用于治疗和预防中枢神经系统(CNS)障碍,特别是精神分裂症,注意缺陷多动障碍,抑郁症,压力疾病,恐慌症,恐惧症,强迫症,创伤后疼痛的治疗剂 压力障碍,认知障碍,阿尔茨海默病,帕金森病,焦虑症,过敏性反应,躁狂症,癫痫发作,人格障碍,偏头痛,药物成瘾,酒精成瘾,肥胖,进食障碍和睡眠障碍。

    1,3-DIOXOISOINDOLE DERIVATIVES HAVING SELECTIVE ANTAGONISM OF T-TYPE CALCIUM CHANNEL
    4.
    发明申请
    1,3-DIOXOISOINDOLE DERIVATIVES HAVING SELECTIVE ANTAGONISM OF T-TYPE CALCIUM CHANNEL 失效
    具有T型钙通道选择性拮抗剂的1,3-二氧化物衍生物

    公开(公告)号:US20070259867A1

    公开(公告)日:2007-11-08

    申请号:US11600391

    申请日:2006-11-16

    CPC分类号: C07D209/48

    摘要: The present invention relates to 1,3-dioxoisoindole derivatives of Formula (1) or pharmaceutically acceptable salts thereof, a preparation method thereof and use thereof as a T-type calcium channel antagonist, based on the fact that 1,3-dioxoisoindole derivatives of Formula (1) show selective antagonistic activity against T-type calcium channel, thus being effective in treating brain diseases, cardiac diseases and neurogenic pains: wherein R1 is a phenyl or a benzyl group, optionally substituted with a moiety selected from the group consisting of a halogen atom, a C1-C6 alkoxy, a C1-C6 alkyl, and a cyano group; R2 is a heterocyclic group selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, and piperazinyl groups, wherein the heterocyclic group is optionally substituted with a C1-C6 alkyl group; and n is 1 or 2.

    摘要翻译: 本发明涉及式(1)的1,3-二氧代异吲哚衍生物或其药学上可接受的盐,其制备方法及其作为T型钙通道拮抗剂的用途,基于以下事实: 式(1)表示对T型钙通道的选择性拮抗活性,因此有效治疗脑疾病,心脏病和神经源性疼痛:其中R 1是苯基或苄基,任选被 选自卤素原子,C 1 -C 6 - 烷氧基,C 1 -C 6烷氧基,C 1 -C 6 - 烷基和氰基; R 2是选自哌啶基,吡咯烷基,吗啉基和哌嗪基的杂环基,其中杂环基任选被C 1 -C 6烷基取代, C 1-6烷基; n为1或2。

    1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel
    5.
    发明授权
    1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel 失效
    具有T型钙通道选择性拮抗作用的1,3-二氧代异吲哚衍生物

    公开(公告)号:US07319098B2

    公开(公告)日:2008-01-15

    申请号:US11600391

    申请日:2006-11-16

    CPC分类号: C07D209/48

    摘要: The present invention relates to 1,3-dioxoisoindole derivatives of Formula (1) or pharmaceutically acceptable salts thereof, a preparation method thereof and use thereof as a T-type calcium channel antagonist, based on the fact that 1,3-dioxoisoindole derivatives of Formula (1) show selective antagonistic activity against T-type calcium channel, thus being effective in treating brain diseases, cardiac diseases and neurogenic pains: wherein R1 is a phenyl or a benzyl group, optionally substituted with a moiety selected from the group consisting of a halogen atom, a C1-C6 alkoxy, a C1-C6 alkyl, and a cyano group; R2 is a heterocyclic group selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, and piperazinyl groups, wherein the heterocyclic group is optionally substituted with a C1-C6 alkyl group; and n is 1 or 2.

    摘要翻译: 本发明涉及式(1)的1,3-二氧代异吲哚衍生物或其药学上可接受的盐,其制备方法及其作为T型钙通道拮抗剂的用途,基于以下事实: 式(1)表示对T型钙通道的选择性拮抗活性,因此有效治疗脑疾病,心脏病和神经源性疼痛:其中R 1是苯基或苄基,任选被 选自卤素原子,C 1 -C 6烷氧基,C 1 -C 6烷基的部分 烷基和氰基; R 2是选自哌啶基,吡咯烷基,吗啉基和哌嗪基的杂环基,其中杂环基任选被C 1 -C 6烷基取代, C 1-6烷基; n为1或2。

    Bycyclic tetrahydrofuran derivatives and process for the preparation thereof
    7.
    发明授权
    Bycyclic tetrahydrofuran derivatives and process for the preparation thereof 失效
    环四氢呋喃衍生物及其制备方法

    公开(公告)号:US07241906B2

    公开(公告)日:2007-07-10

    申请号:US11300966

    申请日:2005-12-15

    IPC分类号: C07D493/02

    CPC分类号: C07D493/04

    摘要: The present invention relates to bicyclic tetrahydrofuran derivatives of Formula (1) and a preparation method thereof, and particularly it relates to a process of preparing compounds of Formula (1) by performing an intramolecular cyclization of tetrahydrofuran-allenol derivatives in the presence of alcohol compound, transitional metal catalyst and carbon monoxide: wherein n is 1 or 2; R is phenyl optionally substituted with C1-C6 alkyl, C1-C6 alkoxy, hydroxyl or C1-C6 hydroxyalkyl group; and R1 is C1-C6 alkyl group.

    摘要翻译: 本发明涉及式(1)的二环四氢呋喃衍生物及其制备方法,特别涉及通过在醇化合物存在下进行四氢呋喃 - 联苯酚衍生物的分子内环化制备式(1)化合物的方法 过渡金属催化剂和一氧化碳,其中n为1或2; R是任选被C 1 -C 6烷基,C 1 -C 6烷基,羟基或C 1 -C 6烷基取代的苯基 C 1 -C 6羟烷基; 且R 1是C 1 -C 6烷基。

    Tetrahydrofuran derivatives having cis substituent, their intermediates, and their preparation method
    9.
    发明授权
    Tetrahydrofuran derivatives having cis substituent, their intermediates, and their preparation method 失效
    具有顺式取代基的四氢​​呋喃衍生物及其制备方法

    公开(公告)号:US07388101B1

    公开(公告)日:2008-06-17

    申请号:US11732602

    申请日:2007-04-04

    IPC分类号: C07D307/02

    CPC分类号: C07D307/12

    摘要: The present invention relates to a tetrahydrofuran compound having cis substituents, the derivatives thereof and a process for preparing the same, and in particular relates to a dihydrofuran-3-ylidene triflate compound having cis substituents at C2 and C5 positions prepared through Prins-type cyclization using a homopropargylic alcohol derivative as a starting material in the presence of Lewis acid catalyst, a tetrahydrofuran compound having cis substituents at C2, C3 and C5 positions prepared through the hydrolysis of triflate group in the derivatives of the dihydrofuran-3-ylidene triflate compound, and a preparation method thereof.The derivatives and the target tetrahydrofuran compound prepared according to the present invention are hydrofuran compounds with novel structures having cis substituents at C2, C3 and/or C5 positions, which are useful as a derivative for synthesizing drugs such as an antagonist for neurokinin receptor.

    摘要翻译: 本发明涉及具有顺式取代基的四氢​​呋喃化合物及其衍生物及其制备方法,特别涉及在C 2上具有顺式取代基的二氢呋喃-3-亚基三氟甲磺酸酯化合物和 在路易斯酸催化剂存在下,使用均二炔醇衍生物作为起始原料,在C 2 N 2上具有顺式取代基的四氢​​呋喃化合物,通过Prins-型环化制备的C 5 H 3位, 通过在二氢呋喃-3-亚基三氟甲磺酸酯化合物的衍生物中水解三氟甲磺酸酯基制备的C 3和C 5 H 3位及其制备方法。 根据本发明制备的衍生物和目标四氢呋喃化合物是具有在C 2,C 3和/或C 5上具有顺式取代基的新结构的氢呋喃化合物 其可用作合成药物的衍生物,例如用于神经激肽受体的拮抗剂。