Calcium Ion Channel Modulators & Uses Thereof

    公开(公告)号:US20110166136A1

    公开(公告)日:2011-07-07

    申请号:US13002374

    申请日:2009-07-03

    摘要: Compounds of formula (1), salts and pro-drugs wherein: R1, R2, R3 and R4 are hydrogen, alkyl, hydroxyalkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, nitro, amino, monalkylamino, dialkylamino, acylamino, alkoxycarbonylamino, alkylsulphonyl, arylsulphonyl, alkylsulphonylamino, arylsulphonylamino, aminosulphonyl or cyano, or any two of R1 to R4 that are adjacent on the ring may together represent the moiety —O—(CH2)n—O— wherein n is 1 to 3; R5 is hydrogen or alkyl; R6 is hydrogen or alkyl; and X is selected from the group consisting of: (a) groups of formula OR7 wherein R7 is hydrogen or alkyl which is optionally substituted with a substituent selected from alkylsulfonylalkyl, saturated or partially unsaturated heterocyclic, alkoxy, carboxyl, nitro, amino, monalkylamino, dialkylamino, halogen, and alkoxycarbonyl, provided that when R7 is hydrogen or ethyl, then R1, R2, R3 and R4 cannot be selected from hydrogen, halogen and alkyl; and (b) groups of formula NR8R9 wherein R8 and R9 together with the nitrogen atom to which they are attached form a saturated or partially unsaturated heterocyclic group which optionally contains at least one more heteroatom selected from nitrogen, oxygen and sulphur atoms, said saturated or partially unsaturated heterocyclic group optionally further being substituted by one or more substituents selected from alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, nitro, amino, monalkylamino, dialkylamino and hydroxyl, provided that: (i) when R8+R9+N=piperazine, and ≧1 of R1 to R4 are hydrogen, hydroxyl, nitro, amino, alkylamino, dialkylamino, alkoxycarbonylamino, halogen, alkoxy or alkyl, the nitrogen atom at the 4-position of the piperazine is not alkyl substituted, (ii) when each of R1, R2, R3, R4, R5 and R6 is hydrogen, X is not unsubstituted piperazinyl or unsubstituted morpholino, (iii) when each of R1, R2, R4, R5 and R6 is hydrogen and R3 hydrogen, bromine or hydroxyl, X is not methoxy, (iv) when each of R2 and R3 is methoxy or they together represent —O—CH2—O— and each of R1, R4, R5 and R6 is hydrogen, X is not unsubstituted piperidine, are Cavx channel blockers and are of use in the treatment of various conditions including pain.

    Realtime coaching system
    23.
    发明申请
    Realtime coaching system 有权
    实习辅导系统

    公开(公告)号:US20090256688A1

    公开(公告)日:2009-10-15

    申请号:US12082793

    申请日:2008-04-14

    IPC分类号: G07C1/22 A63B71/06

    摘要: A method and system for improving the effectiveness of coaches and video game designers for games like soccer, American football, basketball, lacrosse or ice hockey by using RF technology and software. A base station is equipped with a computer programmed with algorithms to track the players and game equipment and thereby produce data of interest to a coach or game designer.

    摘要翻译: 通过使用射频技术和软件,提高足球,美式橄榄球,篮球,曲棍球或冰球等游戏的教练和视频游戏设计师的有效性的方法和系统。 基站配备有用算法编程的计算机来跟踪玩家和游戏设备,从而产生教练或游戏设计者感兴趣的数据。

    System and method for providing statistics gathering within a packet network
    24.
    发明授权
    System and method for providing statistics gathering within a packet network 有权
    用于在分组网络内提供统计信息收集的系统和方法

    公开(公告)号:US07376731B2

    公开(公告)日:2008-05-20

    申请号:US10059919

    申请日:2002-01-29

    IPC分类号: G06F15/173

    摘要: A system and method for providing statistics gathering within a packet network is disclosed. The system comprises a network processor, a traffic manager, a host processor, and a field programmable gate array. The network processor adds a header to received multimedia packets and the traffic manager measures and enforces multimedia flow rates. The host processor performs multimedia flow quality measurement services on a per flow basis, wherein the multimedia flow quality measurement services comprise maintaining current statistics for multimedia flows within the network processor including aggregate and minimum/maximum statistics for the multimedia flow. The field programmable gate array (FPGA) copies a received multimedia packet or a portion of the received multimedia packet, wherein the copy is utilized by the FPGA to perform statistics gathering via use of a latency engine, a lost packet calculation engine, a real-time transport control protocol packet jitter engine and a real-time transport protocol packet jitter engine.

    摘要翻译: 公开了一种用于在分组网络内提供统计收集的系统和方法。 该系统包括网络处理器,业务管理器,主机处理器和现场可编程门阵列。 网络处理器向接收的多媒体分组添加报头,流量管理器测量和实施多媒体流量。 主处理器在每个流的基础上执行多媒体流质量测量服务,其中多媒体流质量测量服务包括维持网络处理器内的多媒体流的当前统计信息,包括多媒体流的聚合和最小/最大统计。 现场可编程门阵列(FPGA)复制接收到的多媒体分组或接收到的多媒体分组的一部分,其中该复制由FPGA利用以通过使用延迟引擎,丢包分组计算引擎, 时间传输控制协议包抖动引擎和实时传输协议包抖动引擎。

    2-(1H-4(5)-imidazoyl) cyclopropyl compounds
    26.
    发明授权
    2-(1H-4(5)-imidazoyl) cyclopropyl compounds 失效
    2-(1H-4(5) - 咪唑基)环丙基化合物

    公开(公告)号:US5990317A

    公开(公告)日:1999-11-23

    申请号:US945915

    申请日:1998-02-06

    CPC分类号: C07D233/64

    摘要: The present invention provides compounds having H.sub.3 histamine receptor antagonist activity of formula (1.0) wherein R.sub.2 is a hydrogen or a methyl or ethyl group; R.sub.3 is a hydrogen or a methyl or ethyl group; n is 0, 1, 2, 3, 4, 5, or 6; and R.sub.1 is selected from the group consisting of (a) C.sub.3 to C.sub.8 cycloalkyl; (b) phenyl or substituted pneyly; (c) alkyl; (d) heterocyclic; (e) decahydronaphthalene; and (f) octahydroindene; with the proviso that when X is H, A can be --CH.sub.2 CH.sub.2, --COCH.sub.2 --CON(CH.sub.3)--, --CH.dbd.CH--, .alpha., --CH.sub.2 --NH--, --CH.sub.3 --N(CH.sub.3)--, --CH(OH)CH.sub.2 --, --NH--CH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --CH.sub.2 O--, --CH.sub.2 S--, and --NHCOO--; when X is NH.sub.2, HN(CH.sub.3), N(CH.sub.3).sub.2, OH, OCH.sub.3, CH.sub.3, SH and SCH.sub.3 ; A can be --NHCO--, --N(CH.sub.3)--CO--, --NHCH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --CH.dbd.XH--, --COCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH( )H)CH.sub.2 --, or .beta.; and when R.sub.1 and X taken together denote a 5,6 or 6,6 saturated bicyclic ring structure, X can be NH, O, or S. The pharmaceutically acceptable salts, hydrates, and individual stereoisomers of compounds of structural formula (1.0), as well as mixtures thereof, are also contemplated as falling within the scope of the present invention. The invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of said formula and a method of treating conditions in which antagonism of histamine H.sub.3 receptors may be of therapeutic importance.

    摘要翻译: PCT No.PCT / US96 / 07833 Sec。 371日期1998年2月6日 102(e)1998年2月6日PCT PCT 1996年5月29日PCT公布。 公开号WO96 / 38141 日期:1996年12月5日本发明提供具有式(1.0)的H3组胺受体拮抗剂活性的化合物,其中R 2为氢或甲基或乙基; R3是氢或甲基或乙基; n是0,1,2,3,4,5或6; 并且R 1选自(a)C 3至C 8环烷基; (b)苯基或取代的吡啶基; (c)烷基; (d)杂环; (e)十氢萘; 和(f)八氢茚; 条件是当X是H时,A可以是-CH 2 CH 2,-COCH 2 -CON(CH 3) - , - CH = CH-,α,-CH 2 -NH-, - CH 3 -N(CH 3) - , - CH OH)CH 2 - , - NH-CH 2 - , - N(CH 3)-CH 2 - , - CH 2 O - , - CH 2 S-和-NHCOO-; 当X是NH 2时,HN(CH 3),N(CH 3)2,OH,OCH 3,CH 3,SH和SCH 3; A可以是-NHCO - , - N(CH 3)-CO - , - NHCH 2 - , - N(CH 3)-CH 2 - , - CH = XH-,-COCH 2 - , - CH 2 CH 2 - , - CH - 或beta 当R1和X一起表示5,6或6,6饱和双环结构时,X可以是NH,O或S.结构式(1.0)化合物的药学上可接受的盐,水合物和单个立体异构体, 以及它们的混合物也被认为落入本发明的范围内。 本发明还提供药物组合物,其包含药学上可接受的载体与有效量的所述式的化合物和治疗其中组胺H3受体拮抗作用具有治疗意义的病症的方法。

    2-(4-imidazoyl) cyclopropyl derivatives
    28.
    发明授权
    2-(4-imidazoyl) cyclopropyl derivatives 失效
    2-(4-咪唑基)环丙基衍生物

    公开(公告)号:US5652258A

    公开(公告)日:1997-07-29

    申请号:US453359

    申请日:1995-05-30

    CPC分类号: C07D233/64

    摘要: The present invention provides compounds having H.sub.3 histamine receptor antagonist activity of the general formula: ##STR1## where X is H, A is --CH.sub.2 CH.sub.2 --, --COCH.sub.2 --, --CONH--, --CON(CH.sub.3)--, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 --NH--, --CH.sub.2 --NCH.sub.3 --, --CH(OH)CH.sub.2 --, --NH--CH.sub.2 --, --N(CH.sub.3) --CH.sub.2 --, --NHSO.sub.2 --, --CH.sub.2 O--, --CH.sub.2 S--, CH.sub.2 SO.sub.2 --, or --CH.sub.2 S(O)--;R.sub.2 is a hydrogen or a methyl or ethyl group;R.sub.3 is a hydrogen or a methyl or ethyl group;n is 0, 1, 2, 3, 4, 5, or 6; andR.sub.1 is selected from the group consisting of (a) C.sub.3 to C.sub.8 cycloalkyl; (b) H; (c) phenyl or substituted phenyl; (d) alkyl; (e) heterocyclic; and (f) bicyclic alkyl; andwhenX is NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, OH, OCH.sub.3, NHR.sub.4, OR.sub.4, SH, SR.sub.4, or SO.sub.2 R.sub.4 ; A is --NHCO--, --N(CH.sub.3)--CO--, --NHCH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --NHSO.sub.2 --, --CH.dbd.CH--, --CH.dbd.CHF--, --COCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH(OH)CH.sub.2 --, or --C.tbd.C--;R.sub.2 is a hydrogen or a methyl or ethyl group;R.sub.3 is a hydrogen or a methyl or ethyl group;n is 0, 1, 2, 3, 4, 5, or 6;R.sub.1 is selected from the group consisting of (a) C.sub.3 to C.sub.8 cycloalkyl; (b) H; (c) phenyl or substituted phenyl; (d) alkyl; (e) heterocyclic; and (f) bicyclic alkyl andR.sub.4 is designated to mean that X is contained within a ring such as octahydroindole.

    摘要翻译: 本发明提供具有以下通式的H3组胺受体拮抗剂活性的化合物:其中X是H,A是-CH 2 CH 2 - , - COCH 2 - , - CONH - , - CON(CH 3) - , - CH = CH - , - C 3-6(C 1 -C 3) - , - CH 2 -NH-,-CH 2 -NCH 3 - , - CH(OH)CH 2 - , - NH-CH 2 - CH 2 O - , - CH 2 S - ,CH 2 SO 2 - 或-CH 2 S(O) - ; R2是氢或甲基或乙基; R3是氢或甲基或乙基; n是0,1,2,3,4,5或6; 并且R 1选自(a)C 3至C 8环烷基; (b)H; (c)苯基或取代的苯基; (d)烷基; (e)杂环; 和(f)双环烷基; 并且当X是NH 2,NHCH 3,N(CH 3)2,OH,OCH 3,NHR 4,OR 4,SH,SR 4或SO 2 R 4时; A是-NHCO-,-N(CH 3)-CO - , - NHCH 2 - , - N(CH 3)-CH 2 - , - NHSO 2 - , - CH = CH-, - CH = CHF-,-COCH 2 - , - CH 2 CH 2 - , - CH(OH)CH 2 - 或-C 3位C; R2是氢或甲基或乙基; R3是氢或甲基或乙基; n是0,1,2,3,4,5或6; R 1选自(a)C 3至C 8环烷基; (b)H; (c)苯基或取代的苯基; (d)烷基; (e)杂环; 和(f)双环烷基和R4表示X包含在环如八氢吲哚中。

    COORDINATING REAL-WORLD GATHERINGS TO PROMOTE ONLINE COMMUNITY
    30.
    发明申请
    COORDINATING REAL-WORLD GATHERINGS TO PROMOTE ONLINE COMMUNITY 有权
    协调真正的世界文化促进在线社区

    公开(公告)号:US20120094763A1

    公开(公告)日:2012-04-19

    申请号:US12904077

    申请日:2010-10-13

    申请人: Mohammed Khan

    发明人: Mohammed Khan

    IPC分类号: A63F9/24

    CPC分类号: H04L67/38 G07F17/3272

    摘要: Coordinating real-world gatherings to promote an online community, the method including: encouraging participants of the online community to participate in a real-world gathering by providing incentives for the participants; promoting familiarity among the participants by providing and introducing online community titles of the participants at the real-world gathering; and providing online benefits or rewards to the participants for participating in the real-world gathering. Keywords include socializing in the real world, community building and bridging the gap between the game world and the real world.

    摘要翻译: 协调现实世界的聚会,以促进在线社区,其方法包括:通过为参与者提供奖励来鼓励在线社区的参与者参加现实世界的聚会; 通过在现实世界聚会中提供和介绍参与者的在线社区标题,促进参与者之间的熟悉程度; 并向与会者提供参与现场聚会的在线福利或奖励。 关键词包括社会化现实世界,社区建设,弥合游戏世界与现实世界的差距。