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281 条记录 (耗时 0.032 秒)

    Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives; new classes of dopamine receptor subtype specific ligands
    6.
    发明授权
    Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives; new classes of dopamine receptor subtype specific ligands 失效
    某些4-氨基甲基-2-取代的咪唑衍生物和2-氨基甲基-4-取代的咪唑衍生物; 新类型的多巴胺受体亚型特异性配体

    公开(公告)号：US06797824B2

    公开(公告)日：2004-09-28

    申请号：US10100691

    申请日：2002-03-18

    申请人： Andrew Thurkauf ,  Raymond F. Horvath ,  Jun Yuan ,  John M. Peterson

    发明人： Andrew Thurkauf ,  Raymond F. Horvath ,  Jun Yuan ,  John M. Peterson

    IPC分类号： C07D40304

    CPC分类号： C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

    摘要： Disclosed are compounds of the formula: wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substitutents which may together form ring structutes; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and 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R 1表示任选取代的芳基，杂芳基，芳基烷基或环烷基; X，Z和Y任选被取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基;及其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，可用于诊断和治疗情感障碍如精神分裂症 抑郁症以及某些运动障碍如帕金森综合征。

    Substituted imidazoles as subtype specific dopamine receptor ligands and pharmaceutical compositions containing such substituted imidazole
    7.
    发明授权
    Substituted imidazoles as subtype specific dopamine receptor ligands and pharmaceutical compositions containing such substituted imidazole 失效
    取代的咪唑作为亚型特异性多巴胺受体配体和含有这种取代的咪唑的药物组合物

    公开(公告)号：US06358955B1

    公开(公告)日：2002-03-19

    申请号：US09497988

    申请日：2000-02-04

    申请人： Andrew Thurkauf ,  Raymond F. Horvath ,  Jun Yuan ,  John M. Peterson

    发明人： Andrew Thurkauf ,  Raymond F. Horvath ,  Jun Yuan ,  John M. Peterson

    IPC分类号： A61K31454

    CPC分类号： C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

    摘要： Disclosed are compounds of the formula: wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substituents which may together form ring structures; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and 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R 1表示任选取代的芳基，杂芳基，芳烷基或环烷基; X，Z和Y任选被取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基;及其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，可用于诊断和治疗情感障碍如精神分裂症 抑郁症以及某些运动障碍如帕金森综合征。

    Certain tricyclic substituted diazabicylo�3.2.1! octane derivatives
    8.
    发明授权
    Certain tricyclic substituted diazabicylo�3.2.1! octane derivatives 失效
    某些三环取代二氮杂双环[3.2.1]辛烷衍生物

    公开(公告)号：US5952501A

    公开(公告)日：1999-09-14

    申请号：US429060

    申请日：1995-04-26

    申请人： Alan Hutchison ,  Jun Yuan ,  Raymond F. Horvath

    发明人： Alan Hutchison ,  Jun Yuan ,  Raymond F. Horvath

    IPC分类号： C07D487/08 ,  C07D247/00 ,  A61K31/495

    CPC分类号： C07D487/08

    摘要： This invention encompasses compounds of the formula: where either R.sub.1 or R.sub.2 represents ##STR1## and the other represents hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; andX is oxygen, methylene, or NH;Y is represents various inorganic and organinc substituents;Z is hydrogen, amino or NHR.sub.6 where R.sub.6 is lower alkyl having 1-6 carbon atoms;T is hydrogen, halogen, hydroxy, or lower alkoxy having 1-6 carbon atoms; andA is methylene, carbonyl or CHOH.These compounds are selective partial agonists or antagonists at brain monoamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents. These compounds show unexpectedly atypical antipsychotic profiles (clozapine-like) in the animal models described in this patent.

    摘要翻译： 本发明包括下式的化合物：其中R 1或R 2表示，另一个表示氢或具有1-6个碳原子的直链或支链低级烷基; X为氧，亚甲基或NH; Y代表各种无机和有机取代基; Z是氢，氨基或NHR6，其中R6是具有1-6个碳原子的低级烷基; T是氢，卤素，羟基或具有1-6个碳原子的低级烷氧基; A是亚甲基，羰基或CHOH。 这些化合物是脑单胺受体亚型或其前药的选择性部分激动剂或拮抗剂，并且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。 此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。 这些化合物在本专利描述的动物模型中显示出意想不到的非典型抗精神病药谱（氯氮平样）。

    Certain tricyclic substituted diazabicyclo (3.2.1) octane derivatives
    9.
    发明授权
    Certain tricyclic substituted diazabicyclo (3.2.1) octane derivatives 失效
    某些三环取代的二氮杂双环（3.2.1）辛烷衍生物

    公开(公告)号：US6156751A

    公开(公告)日：2000-12-05

    申请号：US393789

    申请日：1999-09-10

    申请人： Alan Hutchison ,  Jun Yuan ,  Raymond F. Horvath

    发明人： Alan Hutchison ,  Jun Yuan ,  Raymond F. Horvath

    IPC分类号： C07D487/08 ,  A61K31/495 ,  C07D247/00

    CPC分类号： C07D487/08

    摘要： This invention encompasses compounds of the formula: ##STR1## where either R.sub.1 or R.sub.2 represents ##STR2## and the other represents hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; andX is oxygen, methylene, or NH;Y is represents various inorganic and organic substituents;Z is hydrogen, amino or NHR.sub.6 where R.sub.6 is lowere alkyl having 1-6 carbon atoms;T is hydrogen, halogen, hydroxy, or lower alkoxy having 1-6 carbon atoms; andA is methylene, carbonyl or CHOH.These compounds are selective partial agonists or antagonists at brain monoamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neurolepticagents. These compounds show unexpectedly atypical antipsychotic profiles (clozapine-like) in the animal models described in this patent.

    摘要翻译： 本发明包括下式的化合物：其中R 1或R 2表示，另一个表示氢或具有1-6个碳原子的直链或支链低级烷基; X为氧，亚甲基或NH; Y代表各种无机和有机取代基; Z是氢，氨基或NHR 6，其中R6是具有1-6个碳原子的低级烷基; T是氢，卤素，羟基或具有1-6个碳原子的低级烷氧基; A是亚甲基，羰基或CHOH。 这些化合物是脑单胺受体亚型或其前药的选择性部分激动剂或拮抗剂，并且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。 此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。 这些化合物在本专利描述的动物模型中显示出意想不到的非典型抗精神病药谱（氯氮平样）。

    Certain methylpiperazinyl and methylpiperidinyl substituted biphenyl derivatives; novel dopamine receptor subtype selective ligands
    10.
    发明授权
    Certain methylpiperazinyl and methylpiperidinyl substituted biphenyl derivatives; novel dopamine receptor subtype selective ligands 失效
    某些甲基哌嗪基和甲基哌啶基取代的联苯衍生物; 新型多巴胺受体亚型选择性配体

    公开(公告)号：US5677454A

    公开(公告)日：1997-10-14

    申请号：US457633

    申请日：1995-06-01

    申请人： Jun Yuan ,  Andrew Thurkauf

    发明人： Jun Yuan ,  Andrew Thurkauf

    IPC分类号： C07C211/27 ,  C07D211/14 ,  C07D211/70 ,  C07D239/42 ,  C07D295/096 ,  C07D401/06 ,  C07D239/24 ,  C07D401/04 ,  C07D403/04

    CPC分类号： C07D239/42 ,  C07C211/27 ,  C07D211/14 ,  C07D211/70 ,  C07D295/096 ,  C07D401/06

    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; and R.sub.2 and R.sub.3 represent hydrogen or organic substituents; or NR.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。