Dopamine receptor modulators as antipsychotic agents

    公开(公告)号:US20070043026A1

    公开(公告)日:2007-02-22

    申请号:US10513919

    申请日:2003-05-09

    CPC分类号: C07D223/16 C07D217/04

    摘要: The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m—and —(CH2)n-respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8—(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl; R3 represents hydrogen or C1-6alkyl; R4 represents optionally substituted aryl or optionally substituted heteroaryl; R5 and R6each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8, —(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl; R7 and R8 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; and either: Z represents —CR9R10X— or —XCR9R10— and X represents oxygen, sulfur, —SO— or —SO2, or Z represents —CONR11— or —NR9CO— and X represents —CH2—, oxygen, sulfur, —SO— or —SO2; R9 and R10 each independently represent hydrogen, C1-6alkyl or fluoro; R11 represents hydrogen or C1-6alkyl; or a pharmaceutically acceptable salt or solvate thereof. The compounds of the invention are useful in therapy, in particular as antipsychotic agents.

    7-Heteroarylsulfonyl-tetrahydro-3-benzazepine derivatives as antipsychotic agents

    公开(公告)号:US20070093473A1

    公开(公告)日:2007-04-26

    申请号:US10571220

    申请日:2004-09-09

    摘要: The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m— and —(CH2)n— respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR3R4, —SO2NR3R4, —(CH2)pNR3R4, —(CH2)pNR3COR4, optionally substituted aryl ring, optionally substituted heteroaryl ring, a fused bicyclic heteroaromatic ring system or optionally substituted heterocyclyl ring; Ar1 represents optionally substituted heteroaryl ring; Ar2 represents optionally substituted aryl ring or optionally substituted heteroaryl ring; Z represents —(CH2)qX— wherein the —(CH2)q— group is attached to Ar2, or —X(CH2)q— wherein X is attached to Ar2, and wherein any of the —CH2— groups may be optionally substituted by one or more C1-6alkyl groups; X represents oxygen, —CH(OR5)—, —NR5— or —CH2— wherein the —CH2— group may be optionally substituted by one or more C1-6alkyl groups; R3 and R4 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; R5 represents hydrogen or C1-6alkyl; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; q independently represents an integer selected from 0, 1, 2 and 3; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that when Ar1 is a pyridyl group, and Z is —CH2X— where X is attached to the Ar1 group, X is selected from —CH(OR5)—, —NR5— and —CH2— wherein the —CH2— group may be optionally substituted by one or more C1-6alkyl groups. The compounds of formula (I) are useful in therapy, in particular as antipsychotic agents.

    Benzenesulfonamide derivatives
    4.
    发明申请

    公开(公告)号:US20050085461A1

    公开(公告)日:2005-04-21

    申请号:US10504110

    申请日:2003-02-13

    CPC分类号: C07D223/16 C07D217/02

    摘要: The invention provides compounds of formula (I) wherein A and B represent the groups CH2)m— and CH2)n— respectively; R1 represents hydrogen or C1-4alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pC3-6cycloalkyloxy, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S-C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8, —(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; R3 represents hydrogen or C1-6alkyl; R4 represents halogen, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl or —(CH2)pC3-6cycloalkyloxy; R5 and R6 each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pC3-6cycloalkyloxy, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8, —(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; R7 and R8 each independently represent hydrogen or C1-6alkyl; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that the compounds 4-methyl-N-(1,2,3,4-tetrahydroisoquinolin-6-yl)-benzenesulfonamide, 7-(4-chlorophenyl)sulfonamido-1,2,3,4-tetrahydroisoquinoline hydrochloride and N-(2-ethyl-5-isoindolinyl)-p-toluenesulfonamide are excluded. The compounds are useful in therapy, in particular as antipsychotic agents.

    Compounds which have activity at M1 receptor and their uses in medicine.
    5.
    发明申请
    Compounds which have activity at M1 receptor and their uses in medicine. 失效
    具有M1受体活性的化合物及其在药物中的用途。

    公开(公告)号:US20080058378A1

    公开(公告)日:2008-03-06

    申请号:US11852455

    申请日:2007-09-10

    IPC分类号: A61K31/445 A61P43/00

    CPC分类号: C07D405/12 C07D235/26

    摘要: Compounds of formula (I) and salts and solvates are provided: wherein R4 is fluoro, R5 is selected from hydrogen, halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6alkoxy, and C1-6alkoxy substituted with one or more fluorine atoms; and R6 is selected from halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6alkoxy and C1-6alkoxy substituted with one or more fluorine atoms, and Q is hydrogen or C1-6alkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.

    摘要翻译: 提供式(I)化合物和盐和溶剂化物:其中R 4是氟,R 5选自氢,卤素,氰基,C 1〜 C 1-6烷基,被一个或多个氟原子取代的C 1-6烷基,C 1-6烷氧基和C 1-6 - 被一个或多个氟原子取代的烷氧基; 和R 6选自卤素,氰基,C 1-6烷基,被一个或多个氟原子取代的C 1-6烷基, C 3-6环烷基,被一个或多个氟原子取代的C 3-6环烷基,C 1-6烷氧基和C 1-6烷基, 1-6个被一个或多个氟原子取代的烷氧基,Q是氢或C 1-6烷基。 预期化合物可用于治疗,例如治疗精神病和认知障碍。

    HANDOVER BETWEEN MOBILE COMMUNICATION NETWORKS
    6.
    发明申请
    HANDOVER BETWEEN MOBILE COMMUNICATION NETWORKS 有权
    移动通信网络之间的切换

    公开(公告)号:US20110003594A1

    公开(公告)日:2011-01-06

    申请号:US12846466

    申请日:2010-07-29

    申请人: David Cooper

    发明人: David Cooper

    IPC分类号: H04W36/00

    摘要: The invention provides a method of handover from an active network to a selected one of a plurality of potential other networks. In addition to the overall solution, the solution proposed has several individual aspects. All subsidiary aspects are related to the common problem mentioned above and sharing the underlying common solution concept of implementing a system in which selective handover is possible and in which a list of available other networks provided by an active network can be handled and selection made by a terminal, so that neighbor cell information can be transmitted based on expressed terminal preferences.

    摘要翻译: 本发明提供了一种从活动网络切换到多个潜在的其他网络中选定的一个的方法。 除了整体解决方案,提出的解决方案有几个方面。 所有附属方面与上述常见问题相关,并且共享实现可选择切换的系统的基本共同解决方案概念,其中由主动网络提供的可用的其他网络的列表可以被处理,并且由 终端,使得可以基于表达的终端偏好来发送相邻小区信息。

    Vehicle accessory rack
    7.
    发明申请
    Vehicle accessory rack 审中-公开
    车载附件架

    公开(公告)号:US20070034658A1

    公开(公告)日:2007-02-15

    申请号:US11200814

    申请日:2005-08-10

    IPC分类号: B60R11/00 B60R9/00

    CPC分类号: B60R9/06

    摘要: An accessory rack for mounting on a vehicle is described. In an embodiment, the accessory rack includes an anchor that mounts to the frame and a stand that is supported by the anchor so as to provide a strong yet compact accessory rack. The small size provides potential benefits in the reduction of fuel consumption and/or reductions in wind noise in the event the user does not remove the accessory rack from the vehicle during periods of disuse. The accessory rack may include a stand configured to support standard sized carriers while providing improved ergonomics during installation of objects onto the carrier.

    摘要翻译: 描述了用于安装在车辆上的附件架。 在一个实施例中,附件架包括安装到框架的锚固件和由锚固件支撑的支架,以便提供坚固而紧凑的附件架。 在用户在不使用期间不从车辆移除附件架的情况下,小尺寸在减少燃料消耗和/或降低风噪声方面提供潜在的益处。 附件机架可以包括支架,其被配置为支撑标准尺寸的载体,同时在将物体安装到载体上的同时提供改进的人机工程学。

    Oil composition for lubricating an EGR equipped diesel engine and an EGR equipped diesel engine comprising same
    9.
    发明申请
    Oil composition for lubricating an EGR equipped diesel engine and an EGR equipped diesel engine comprising same 有权
    用于润滑配备有EGR的柴油发动机和包括EGR的柴油发动机的EGR组合物

    公开(公告)号:US20060142168A1

    公开(公告)日:2006-06-29

    申请号:US11019256

    申请日:2004-12-23

    IPC分类号: C10M149/02

    摘要: The present invention is directed to a lubricating oil composition, a diesel engine comprising a lubricating oil composition, and a method of lubricating a diesel engine provided with an exhaust gas recirculation system, comprising lubricating said engine with a lubricating oil composition comprising an oil of lubricating viscosity, and a polymeric N-dispersant booster comprising monomer units of: a) 0 to 40 wt. % of one or more ethylenically unsaturated ester compounds of formula (I) wherein R is equal to H or CH3, R1 represents a linear or branched alkyl group with 1 to 5 carbon atoms, R2 and R3 independently represent H or a group of the formula —COOR′, wherein R′ is H or an alkyl group with 1 to 5 carbon atoms, b) 10 to 98 wt. % of one or more ethylenically unsaturated ester compounds of formula (II) wherein R is equal to H or CH3, R4 represents a linear or branched alkyl group with 6 to 15 carbon atoms, R5 and R6 independently represent H or a group of the formula —COOR″, wherein R″ is H or an alkyl group with 6 to 15 carbon atoms, c) 0 to 30 wt. % of one or more ethylenically unsaturated ester compounds of formula (III) wherein R is equal to H or CH3, R7 represents a linear or branched alkyl group with 16 to 30 carbon atoms, R8 and R9 independently represent H or a group of the formula —COOR′″, wherein R′″ is H or an alkyl group with 16 to 30 carbon atoms, d) 0 to 30 wt. % vinyl monomers, e) 7 to 25 wt. % of at least one N— dispersant monomer, wherein a)-e) add up to 100 wt. %.

    摘要翻译: 本发明涉及润滑油组合物,包含润滑油组合物的柴油发动机,以及润滑具有废气再循环系统的柴油发动机的方法,包括用润滑油组合物润滑所述发动机,所述润滑油组合物包含润滑油 粘度和聚合N-分散剂增强剂,其包含以下单体单元:a)0至40wt。 %的一种或多种式(I)的烯键式不饱和酯化合物,其中R等于H或CH 3,R 1表示直链或支链烷基,其中1至 5个碳原子,R 2和R 3独立地表示H或式-COOR'的基团,其中R'是H或具有1至5个碳原子的烷基 原子,b)10〜98重量% %的一种或多种式(II)的烯属不饱和酯化合物,其中R等于H或CH 3,R 4表示直链或支链烷基,其中6至 15个碳原子,R 5和R 6独立地表示H或式-COOR“的基团,其中R”是H或具有6至 15个碳原子,c)0-30重量% %的一种或多种式(III)的烯属不饱和酯化合物,其中R等于H或CH 3,R 7表示直链或支链烷基,其中16至 30个碳原子,R 8和R 9独立地表示H或式-COOR“'的基团,其中R”'是H或具有 16〜30个碳原子,d)0〜30重量% %乙烯基单体,e)7〜25wt。 %的至少一种N-分散剂单体,其中a)-e)加到100wt。 %。

    Dynamic resource allocation in packet data transfer
    10.
    发明申请
    Dynamic resource allocation in packet data transfer 审中-公开
    分组数据传输中的动态资源分配

    公开(公告)号:US20050135327A1

    公开(公告)日:2005-06-23

    申请号:US10814784

    申请日:2004-04-01

    申请人: David Cooper

    发明人: David Cooper

    CPC分类号: H04W24/10 H04W72/044

    摘要: A method for control of packet data transmissions in a TDMA wireless network to provide for additional choices in the allocation of communication channels. Measurement and recovery periods are re-assigned to avoid conflicts in operating conditions. The re-assignments for the GPRS system may be reduced to a simple formula.

    摘要翻译: 一种用于控制TDMA无线网络中的分组数据传输以提供通信信道分配中的附加选择的方法。 测量和恢复时间被重新分配,以避免操作条件的冲突。 GPRS系统的重新分配可以简化为简单的公式。