1-phenyl-4-benzlpiperazines: dopamine receptor subtype specific ligands
    82.
    发明授权
    1-phenyl-4-benzlpiperazines: dopamine receptor subtype specific ligands 失效
    1-苯基-4-苯并哌嗪:多巴胺受体亚型特异性配体

    公开(公告)号:US06656943B2

    公开(公告)日:2003-12-02

    申请号:US10186235

    申请日:2002-06-28

    IPC分类号: A61K31495

    摘要: Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein: R1 is halogen or C1-C4 alkyl; and R2 and R3 are the same or different and represent hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, alkylthio, hydroxy, amino, mono(C1-C4)alkylamino, di(C1-C4)alkylamino, or R2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety, which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.

    摘要翻译: 公开了下式的化合物或其药学上可接受的加成盐,其中:R 1是卤素或C 1 -C 4烷基; 并且R 2和R 3相同或不同,表示氢,卤素,C 1 -C 4烷基,C 1 -C 4烷氧基,烷硫基,羟基,氨基,单(C 1 -C 4)烷基氨基,二(C 1 -C 4)烷基氨基或R 2和R 3一起 代表与其所连接的苯环一起形成萘基部分的4碳亚烯基部分,该化合物可用于治疗神经疾病疾病如精神分裂症,精神抑郁症和躁狂症。

    5,6-dihydro-napth[1,2-d]-imidazole, napth[1,2-d]imidazole, and chromane[3,4-d]imidazole derivatives

    公开(公告)号:US06436941B1

    公开(公告)日:2002-08-20

    申请号:US09783476

    申请日:2001-02-14

    IPC分类号: A61K31495

    摘要: Disclosed are 5,6-Dihydro-napth[1,2-d]-imidazoles, Naphth[1,2-d]imidazoles, and Chromane[3,4-d]imidazoles compounds having the formula: and the pharmaceutically acceptable salts thereof, wherein, A represents ethenylene, or A represents —X—CH2—; where X is CH2 or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring; R1, R2, R3 and R4 are inorganic or organic substituents; and R5 and R6 is are optionally substituted organic substituents; or NR5R6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various organic or inorganic groups. Such compounds are useful in the treatment of neuropsychological disorders.

    1-phenyl-4-benzylpiperazines dopamine receptor subtype specific ligands
    84.
    发明授权
    1-phenyl-4-benzylpiperazines dopamine receptor subtype specific ligands 失效
    1-苯基-4-苄基哌嗪多巴胺受体亚型特异性配体

    公开(公告)号:US06426347B2

    公开(公告)日:2002-07-30

    申请号:US09736566

    申请日:2000-12-13

    IPC分类号: C07D295073

    摘要: Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein: R1 is halogen or C1-C4 alkyl; and R2 and R3 are the same or different and represent hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, alkylthio, hydroxy, amino, mono(C1-C4)alkylamino, di(C1-C4)alkylamino, or R2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety, which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.

    摘要翻译: 公开了下式的化合物或其药学上可接受的加成盐,其中:R 1是卤素或C 1 -C 4烷基; 并且R 2和R 3相同或不同,表示氢,卤素,C 1 -C 4烷基,C 1 -C 4烷氧基,烷硫基,羟基,氨基,单(C 1 -C 4)烷基氨基,二(C 1 -C 4)烷基氨基或R 2和R 3一起 代表与其所连接的苯环一起形成萘基部分的4碳亚烯基部分,该化合物可用于治疗神经疾病疾病如精神分裂症,精神抑郁症和躁狂症。

    Benzylpiperazinyl and piperidinyl ethanone derivatives: dopamine
receptor subtype specific ligands
    85.
    发明授权
    Benzylpiperazinyl and piperidinyl ethanone derivatives: dopamine receptor subtype specific ligands 失效
    苄基哌嗪基和哌啶基乙酮衍生物:多巴胺受体亚型特异性配体

    公开(公告)号:US6084098A

    公开(公告)日:2000-07-04

    申请号:US259239

    申请日:1999-02-26

    摘要: Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH;R.sub.1, R.sub.2 and R.sub.3 independently represent organic or inorganic substituents;R.sub.4 and R.sub.4 ' independently represent hydrogen, alkyl or form a ring with the atom to which they are attached;R.sub.5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R.sub.6 represents hydrogen or alkyl; or R.sub.5 and R.sub.6 form a ring together with the atoms to which they are attached; andR.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 independently represent hydrogen or alkyl,which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

    摘要翻译: 公开了下式的化合物或其药学上可接受的加成盐,其中:Y表示氧或硫; Z是氮或CH; R1,R2和R3独立地表示有机或无机取代基; R4和R4'独立地表示氢,烷基或与它们所连接的原子形成环; R5代表氢,烷基,烷氧基或烷硫基,R6代表氢或烷基; 或R 5和R 6与它们所连接的原子一起形成环; 并且R 7,R 8,R 9,R 10和R 11独立地表示氢或烷基,该化合物可用于治疗和/或预防神经心理障碍,包括但不限于精神分裂症,躁狂症,痴呆,抑郁,焦虑,强迫行为, 药物滥用,帕金森样运动障碍和与使用精神安定药有关的运动障碍。

    Certain aminomethyl biphenyl, aminomethyl phenyl pyridine and
aminomethyl phenyl pyrimidine derivatives; novel dopamine receptor
subtype selective ligands
    88.
    发明授权
    Certain aminomethyl biphenyl, aminomethyl phenyl pyridine and aminomethyl phenyl pyrimidine derivatives; novel dopamine receptor subtype selective ligands 失效
    某些氨基甲基联苯,氨基甲基苯基吡啶和氨基甲基苯基嘧啶衍生物; 新型多巴胺受体亚型选择性配体

    公开(公告)号:US5594141A

    公开(公告)日:1997-01-14

    申请号:US344497

    申请日:1994-11-23

    摘要: Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents;G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent;R is hydrogen or an alkyl group;R.sub.1, X, Y, Z and T are organic or inorganic substituents; andR.sub.2 and R.sub.3 represent hydrogen or organic substituents; orNR.sub.2 R.sub.3 together represents a heterocyclic ring system;and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.

    摘要翻译: 公开了下式的化合物:其中S和V是各种有机或无机取代基; G和K相同或不同,表示N或CR',其中R'是有机或无机取代基; R是氢或烷基; R1,X,Y,Z和T​​是有机或无机取代基; R2和R3代表氢或有机取代基; 或NR2R3一起表示杂环体系; 及其药学上可接受的盐; 其是脑多巴胺受体亚型的高度选择性部分激动剂或拮抗剂,因此可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。