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公开(公告)号:US6008240A
公开(公告)日:1999-12-28
申请号:US991030
申请日:1997-12-15
IPC分类号: C07D233/54 , C07D233/56 , C07D233/64 , C07D403/12 , A61K31/415
CPC分类号: C07D233/56 , C07D233/64 , C07D403/12
摘要: The present invention provides compounds having H.sub.3 histamine receptor antagonist activity of the general formula: ##STR1## 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 1, 2, 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) phenyl or substituted phenyl; (c) alkyl; (d) heterocyclic; (e) decahydronapthalene; and (f) octahydroindene;with the provisos thatwhen X is H, A can be --CH.sub.2 CH.sub.2 --,--COCH.sub.2 --,--CONH--,--CON(CH.sub.3), CH.dbd.CH, --c.ident.c--,--CH.sub.2 --NH--, --CH.sub.2 --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, NH(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.CH--; --COCH.sub.2, --CH.sub.2 CH.sub.2 --,--CH(OH)CH.sub.2, or --C.ident.C--; andwhen R.sub.1 and X taken together denote a 5,6 or 6,6 saturated bicyclic ring structure X NH, O, or S and the pharmaceutically acceptable salts, and individual stereoisomers of compounds of structural formula (1.0) above. This invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of the above 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: 本发明提供了具有以下通式的H3组胺受体拮抗剂活性的化合物:R2是氢或甲基或乙基; R3是氢或甲基或乙基; n为1,2,3,4,5或6; 并且R 1选自(a)C 3至C 8环烷基; (b)苯基或取代的苯基; (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 - , - CONH - , - CON(CH 3),CH = CH,-c = c - , - CH 2 -NH-, - CH 2 -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,NH(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 = CH-; -COCH 2,-CH 2 CH 2 - , - CH(OH)CH 2或-C = C-; 当R1和X一起表示5,6或6,6饱和双环结构X NH,O或S时,以及上述结构式(1.0)化合物的药学上可接受的盐和单独的立体异构体。 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上述化合物的组合以及治疗其中组胺H3受体的拮抗作用具有治疗意义的病症的方法。
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公开(公告)号:US6166060A
公开(公告)日:2000-12-26
申请号:US948801
申请日:1997-10-10
IPC分类号: C07D233/58 , A61K31/415 , A61K31/417 , A61K31/4178 , A61K31/47 , A61P1/00 , A61P9/00 , A61P25/00 , A61P25/18 , A61P25/28 , A61P29/00 , A61P37/08 , C07D233/54 , C07D233/60 , C07D233/64 , C07D401/12 , C07D403/12 , C07D405/12 , A61K31/4174
CPC分类号: C07D233/56 , A61K31/417 , A61K31/4174 , A61K31/4178 , C07D233/64 , C07D403/12 , C07D405/12
摘要: The present invention provides, in its principal aspect, compounds of the general formula: ##STR1## when A is --NHCO--, --N(CH.sub.3)--CO--, --NHCH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --CH.dbd.CH--, --COCH.sub.2 --, CH.sub.2 CH.sub.2 --, --CH(OH)CH.sub.2 -- or --C.tbd.C--;X can be H, CH.sub.3, NH.sub.2, NH(CH.sub.3),N(CH.sub.3).sub.2, OH, OCH.sub.3, SH,R.sub.2 is hydrogen or a methyl or ethyl group;R.sub.3 is 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) alkyl; (b) C.sub.3 to C.sub.8 cycloalkyl; (c) phenyl or substituted phenyl; (d) heteroocyclic; and (f) decahydronaphthalene or octahydroindane; andWhen R.sub.1 and X taken together denote a 5, 6 or 6, 6 saturated bicyclic ring structure, X can be NH, O, S, SO.sub.2,When X is constrained in a 5, 6 or 6, 6, saturated bicyclic ring structure, then for example, when X.dbd.NH, R.sub.1 and X taken together mean an octahydroindole ring structure directly attached to A.
摘要翻译: 本发明在其主要方面提供了以下通式的化合物:当A是-NHCO-,-N(CH 3)-CO-,-NHCH 2 - , - N(CH 3)-CH 2 - , - CH = CH- ,-COCH 2 - ,CH 2 CH 2 - , - CH(OH)CH 2 - 或-C X可以是H,CH 3,NH 2,NH(CH 3),N(CH 3)2,OH,OCH 3,SH,R 2是氢或甲基或乙基; R3是氢或甲基或乙基; n为0,1,2,3,4,5或6; R1选自(a)烷基; (b)C3至C8环烷基; (c)苯基或取代的苯基; (d)杂环; 和(f)十氢萘或八氢化茚; 当R 1和X一起表示5,6或6,6个饱和双环结构时,X可以是NH,O,S,SO 2,当X被约束在5,6或6,6饱和双环结构中时 ,那么例如当X = NH时,R 1和X一起表示直接连接到A的八氢吲哚环结构。
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公开(公告)号:US06448282B1
公开(公告)日:2002-09-10
申请号:US09631189
申请日:2000-08-02
IPC分类号: A61K31417
CPC分类号: C07D233/56 , A61K31/417 , A61K31/4174 , A61K31/4178 , C07D233/64
摘要: The present invention provides, in its principal aspect, compounds of the general formula: where A is —NHCO—, —N(CH3)—CO—, —NHCH2—, —N(CH3)—CH2—, —COCH2—, —CH2CH2—, or —CH(OH)CH2—, X is H, CH3, NH2, NH(CH3), N(CH3)2, OCH3, or SH; R2 is hydrogen or a methyl or ethyl group; R3 is hydrogen or a methyl or ehtyl group; n is 0, 1, 2, 3, 4, 5 or 6; R1 is selected from the group consisting of (a) alkyl; (b) C3 to C8 cycloalkyl; (c) phenyl or substituted phenyl; (d) heterocyclic; (e) decahydronaphthalene and (f) octahydroindane; or R1 and X may be taken together to denote a 5,6 or 6,6 saturated bicycle ring structure. The compounds of the present invention have H3 histamine receptor antagonist activity. This invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of formula 1.0. The present invention also provides a method of treating conditions in which antagonism of histamine H3 receptors may of therapeutic importance.
摘要翻译: 本发明主要由下列通式表示:其中A是-NHCO - , - N(CH 3)-CO - , - NHCH 2 - , - N(CH 3)-CH 2 - , - COCH 2 - , - CH 2 CH 2 - 或-CH(OH)CH 2 - ,X是H,CH 3,NH 2,NH(CH 3),N(CH 3)2,OCH 3或SH; R 2是氢或甲基或乙基; R 3是氢或 甲基或庚基; n为0,1,2,3,4,5或6; R 1选自(a)烷基; (b)C3至C8环烷基; (c)苯基或取代的苯基; (d)杂环; (e)十氢萘和(f)八氢化茚; 或R 1和X可以一起表示5,6或6,6饱和自由基环结构。本发明化合物具有H3组胺受体拮抗剂活性。 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式1.0化合物的组合。 本发明还提供了治疗组胺H 3受体的拮抗作用具有治疗意义的病症的方法。
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公开(公告)号:US20090136499A1
公开(公告)日:2009-05-28
申请号:US12356097
申请日:2009-01-20
申请人: Jean-Marc Lapierre , Nivedita D. Namdev , Mark A. Ashwell , Dennis S. France , Hui Wu , Patrick M. Hutchins , Manish Tandon , Yanbin Liu , Jeff S. Link , Syed M. Ali , Chris J. Brassard , Robb B. Nicewonger , Anton Filikov , Rebecca J. Carazza
发明人: Jean-Marc Lapierre , Nivedita D. Namdev , Mark A. Ashwell , Dennis S. France , Hui Wu , Patrick M. Hutchins , Manish Tandon , Yanbin Liu , Jeff S. Link , Syed M. Ali , Chris J. Brassard , Robb B. Nicewonger , Anton Filikov , Rebecca J. Carazza
IPC分类号: A61K39/395 , C07D513/04 , A61K31/506 , A61K31/5377 , C07D498/04 , A61P35/00
CPC分类号: C07D513/04
摘要: The present invention provides imidazooxazole and imidazothiazole compounds and their synthesis. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAFV600E. The compounds are useful for the treatment of cell proliferative disorders such as cancer.
摘要翻译: 本发明提供咪唑并恶唑和咪唑并噻唑化合物及其合成。 本发明的化合物能够抑制RAF激酶如B-RAFV600E的活性。 该化合物可用于治疗细胞增殖性疾病如癌症。
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公开(公告)号:US20090130117A1
公开(公告)日:2009-05-21
申请号:US12251093
申请日:2008-10-14
申请人: Rui-Yang Yang , Syed M. Ali , Mark A. Ashwell , Eugene Kelleher , Rocio Palma , Neil Westlund
发明人: Rui-Yang Yang , Syed M. Ali , Mark A. Ashwell , Eugene Kelleher , Rocio Palma , Neil Westlund
IPC分类号: A61K31/41 , C07D257/04 , C07D403/04 , C07D401/04 , C07D401/14 , C07D403/10 , A61P35/00 , A61K31/4196 , A61K31/675 , A61K39/395 , A61K31/519 , A61K31/505 , A61K31/7068 , A61K33/24 , A61K31/4535 , C07D413/14 , C07D413/12 , A61K31/5377 , A61K31/496 , A61K31/454
CPC分类号: C07D257/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D403/12
摘要: The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.
摘要翻译: 本发明提供了四唑化合物,以及这些化合物的制备方法。 本发明还涉及包含四唑化合物的药物组合物。 本发明提供了通过向有需要的受试者施用治疗有效量的本发明化合物来治疗细胞增殖性疾病如癌症的方法。
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公开(公告)号:US07062756B2
公开(公告)日:2006-06-13
申请号:US09998035
申请日:2001-11-30
IPC分类号: G06F9/44
CPC分类号: H04L67/2819 , G06F17/30902 , H04L29/06 , H04L67/10 , H04L67/2847 , H04L67/2852 , H04L67/289 , H04L69/329
摘要: A method for transparently optimizing data access. The method includes gathering information related to data usage when a system is processing and determining a usage pattern of the system using gathered information.
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公开(公告)号:US08273754B2
公开(公告)日:2012-09-25
申请号:US12649721
申请日:2009-12-30
申请人: Syed M. Ali , Mark A. Ashwell , Jason Hill , Jean-Marc Lapierre , Magdi Moussa , Nivedita Namdev , Robert Nicewonger , Manish Tandon , Rui-Yang Yang
发明人: Syed M. Ali , Mark A. Ashwell , Jason Hill , Jean-Marc Lapierre , Magdi Moussa , Nivedita Namdev , Robert Nicewonger , Manish Tandon , Rui-Yang Yang
IPC分类号: A01N43/90 , A61K31/519 , C07D487/00
CPC分类号: C07D487/04
摘要: The present invention relates to substituted 1H-pyrazolo-[3,4-d]pyrimidine-6-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 1H-pyrazolo-[3,4-d]pyrimidine-6-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
摘要翻译: 本发明涉及取代的1H-吡唑并[3,4-d]嘧啶-6-胺化合物及其合成方法。 本发明还涉及含有取代的1H-吡唑并[3,4-d]嘧啶-6-胺化合物的药物组合物和通过将这些化合物和药物组合物给予需要的受试者来治疗细胞增殖性疾病如癌症的方法 其中。
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8.
公开(公告)号:US08114873B2
公开(公告)日:2012-02-14
申请号:US12854687
申请日:2010-08-11
申请人: Mark A. Ashwell , Yanbin Liu , Syed M. Ali , Jason Hill , Woj Wrona
发明人: Mark A. Ashwell , Yanbin Liu , Syed M. Ali , Jason Hill , Woj Wrona
IPC分类号: A61K31/5355 , A61K31/5375 , C07D265/30 , A61P29/00
CPC分类号: C07D295/185 , C07D207/27 , C07D207/327 , C07D207/404 , C07D209/12 , C07D209/42 , C07D209/44 , C07D209/48 , C07D211/22 , C07D211/46 , C07D211/58 , C07D211/60 , C07D213/30 , C07D213/56 , C07D213/61 , C07D213/81 , C07D213/82 , C07D215/38 , C07D217/04 , C07D217/26 , C07D231/12 , C07D231/14 , C07D239/38 , C07D239/42 , C07D239/47 , C07D239/48 , C07D239/56 , C07D241/08 , C07D249/12 , C07D257/04 , C07D261/08 , C07D263/14 , C07D277/24 , C07D285/14 , C07D295/088 , C07D295/155 , C07D307/42 , C07D317/60 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D491/10
摘要: Naphthalene-based compounds having linked heterocyclic and aromatic rings capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating conditions associated with P38 activity or cytokine activity; more particularly naphthalene-based compounds of Formula (I) having a morpholine heterocyclic ring, and methods of use thereof
摘要翻译: 具有能够抑制P38的连接的杂环和芳环的萘基化合物,体内或体外抑制P38的方法,用于确定治疗P38和/或细胞因子相关病症的活性的诊断和用于治疗与P38活性相关的病症的方法 或细胞因子活性; 更具体地,具有吗啉杂环的式(I)的萘系化合物及其使用方法
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公开(公告)号:US20100327858A1
公开(公告)日:2010-12-30
申请号:US12642031
申请日:2009-12-18
申请人: James Simek , Jed Ludlow , John H. Flora , Syed M. Ali , Huidong Gao
发明人: James Simek , Jed Ludlow , John H. Flora , Syed M. Ali , Huidong Gao
IPC分类号: G01N27/82
CPC分类号: G01N27/87
摘要: A pipeline inspection tool includes two pole magnets oriented at an oblique angle relative to the central longitudinal axis of the tool body. An array of sensor coil sets is located between opposing edges of the two pole magnets and oriented perpendicular to the central longitudinal axis. Each sensor coil set includes a transmitter coil and two opposing pairs of receiver coils that are gated to receive reflections from the wall of a tubular member. Because the line of sensor coils is rotated relative to the magnetic bias field, the receiver coils are in-line with, and have the same angular orientation as, the transmitter coil. The tool provides improved sensitivity to small defects, substantial decrease in RF pulser power requirements, full circumferential coverage, self-calibration of the transmitted signals, and less interference between transmitter coils caused by acoustic ring around.
摘要翻译: 管道检查工具包括相对于工具主体的中心纵向轴线倾斜定向的两个磁极。 传感器线圈组的阵列位于两个极磁体的相对边缘之间并且垂直于中心纵向轴线定向。 每个传感器线圈组包括发射器线圈和两个相对的接收器线圈对,其被门控以从管状构件的壁接收反射。 因为传感器线圈的线相对于磁偏置场旋转,所以接收器线圈与发射器线圈成一直线并具有相同的角度定向。 该工具提供对小缺陷的改进的灵敏度,RF脉冲发生器功率要求的显着降低,全周期覆盖,发射信号的自校准以及由环形周围引起的发射器线圈之间的较小干扰。
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公开(公告)号:US07703074B2
公开(公告)日:2010-04-20
申请号:US11133831
申请日:2005-05-20
申请人: Yury Kamen , Syed M. Ali , Deepak Alur , John P. Crupi , Daniel B. Malks
发明人: Yury Kamen , Syed M. Ali , Deepak Alur , John P. Crupi , Daniel B. Malks
CPC分类号: G06F8/60
摘要: A method for analyzing a target system that includes obtaining a plurality of characteristics from the target system using a characteristics extractor, wherein the plurality of characteristics is associated with a characteristics model, storing each of the plurality of characteristics in a characteristics store using a tracking mechanism, and analyzing the target system by issuing a query to the characteristics store to obtain an analysis result, wherein the query uses tracking information associated with the tracking mechanism.
摘要翻译: 一种用于分析目标系统的方法,所述目标系统包括使用特征提取器从所述目标系统获得多个特征,其中所述多个特征与特征模型相关联,使用跟踪机制将所述多个特征中的每一个存储在特征存储器中 并且通过向所述特征商店发出查询以获得分析结果来分析所述目标系统,其中所述查询使用跟踪机制相关联的跟踪信息。
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