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公开(公告)号:US20070015799A1
公开(公告)日:2007-01-18
申请号:US10556901
申请日:2004-05-14
申请人: Mark Ashton , Alan Davidson , Russell Thomas , Mark Whittaker
发明人: Mark Ashton , Alan Davidson , Russell Thomas , Mark Whittaker
IPC分类号: A61K31/4436 , A61K31/44 , A61K31/381
CPC分类号: C07D405/04 , A61K31/10 , A61K31/381 , A61K31/44 , A61K31/4436 , C07C323/62 , C07D213/85 , C07D217/26 , C07D409/04 , C07D409/14
摘要: This invention relates to compounds of formula (I) which are glyoxalase I inhibitors, pharmaceutical salts or compositions comprising such compounds, and the use of such compositions and compounds to treat various conditions alleviated by the inhibition of glyoxalase 1. Wherein X is N or CH. R2 is H, CF3; or optionally substituted C5-6 aryl, C3-7 cycloalkyl, C5-7 heterocyclyl. R3 is H; or optionally substituted C5-6 aryl, C3-7 cycloalkyl, C5-7 heterocyclyl. Alternatively R2 and R3 together form an optionally substituted C3-4alkylene group wherein L3 and L4 are single bonds thus forming a C5-6 ring fused with the aromatic ring to which L3 and L4 are attached. L3 and L4 are independently selected from a single bond, optionally substituted C1-4 alkylene, -L9YN(OH)C(═O)L10- and -L9C(═O)N(OH)YL10-, wherein L9 and L10 are independently selected from optionally substituted C1-4 alkylene, C5-6 arylene, C1-4 alkylene-C5-6arylene and a single bond, wherein Y is NH or a single bond.
摘要翻译: 本发明涉及作为乙二醛酶I抑制剂的式(I)化合物,包含这些化合物的药物盐或组合物,以及这些组合物和化合物用于治疗通过抑制乙二醛酶1减轻的各种病症的用途。其中X是N或CH 。 R 2是H,CF 3 N; 或任选取代的C 5-6芳基,C 3-7环烷基,C 5-7杂环基。 R 3是H; 或任选取代的C 5-6芳基,C 3-7环烷基,C 5-7杂环基。 或者R 2和R 3一起形成任选取代的C 3-4亚烷基,其中L 3和L 3 因此形成与L 3和L 4的芳环稠合的C 5〜6环, SUP>连接。 L 3和L 4独立地选自单键,任选取代的C 1-4亚烷基,-L 9, SUP-YN(OH)C(-O)L 10 - 和-L 9 C( - )N(OH)Y L 10 - ,其中L 9和L 10独立地选自任选取代的C 1-4 - 亚烷基,C 5-6 - 亚芳基,C 1-4亚烷基-C 5-6亚芳基和单键,其中Y是NH或单键。
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2.
公开(公告)号:US20060205697A1
公开(公告)日:2006-09-14
申请号:US11272019
申请日:2005-11-14
申请人: Gary Robinson , Carl Wild , Mark Ashton , Russell Thomas , Christian Montalbetti , Thomas Coulter , Filippo Magaraci , Robert Townsend , Theodore Nitz
发明人: Gary Robinson , Carl Wild , Mark Ashton , Russell Thomas , Christian Montalbetti , Thomas Coulter , Filippo Magaraci , Robert Townsend , Theodore Nitz
摘要: The present invention relates to novel synthetic derivatives of betulin and the use of such derivatives as pharmaceuticals. The present invention is directed to novel compounds of Formula I: or a pharmaceutically acceptable salt or prodrug thereof.
摘要翻译: 本发明涉及新颖的桦木素合成衍生物和药物衍生物的用途。 本发明涉及新的式I化合物:或其药学上可接受的盐或前药。
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3.
公开(公告)号:US20050148561A1
公开(公告)日:2005-07-07
申请号:US10949875
申请日:2004-09-27
申请人: Carl Wild , Gary Robinson , Mark Ashton , Russell Thomas
发明人: Carl Wild , Gary Robinson , Mark Ashton , Russell Thomas
IPC分类号: A61K31/513 , A61K31/522 , A61K31/551 , A61K31/57 , A61K31/7072 , A61K31/7076 , A61K38/20 , A61K38/21 , C07C69/00 , C07C69/40 , C07C69/42 , C07C69/608 , C07C69/708 , C07J1/00 , C07J53/00
CPC分类号: C07C69/708 , C07C69/40 , C07C69/42 , C07C69/608 , C07C2603/52 , C07J1/00 , C07J53/00 , C07J63/008
摘要: The present invention relates to novel synthetic derivatives of triterpenes and the use of such derivatives as pharmaceuticals. The present invention is directed to novel compounds of Formula I: or pharmaceutically acceptable salt or ester thereof, wherein R1 is a carboxyalkanoyl, where the alkanoyl chain can be interrupted by a nitrogen, sulfur or oxygen atom, or combinations thereof.
摘要翻译: 本发明涉及三萜烯的新型合成衍生物和药物衍生物的用途。 本发明涉及新的式I化合物或其药学上可接受的盐或酯,其中R 1是羧烷基,其中烷酰基链可被氮,硫或氧原子间隔, 或其组合。
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公开(公告)号:US09124648B2
公开(公告)日:2015-09-01
申请号:US12404385
申请日:2009-03-16
申请人: Pablo Castro , Andrew Conrad , Michael Flasko , Pratik Patel , Mark Ashton
发明人: Pablo Castro , Andrew Conrad , Michael Flasko , Pratik Patel , Mark Ashton
CPC分类号: H04L67/2823 , H04L67/02 , H04L67/2876
摘要: Data communications are enabled to be performed between first and second computer systems without having to match data types at the first and second computer systems. A first data type is associated with a request for a resource. The request for the resource is transmitted from a first agent at the first computer system to a second agent at the second computer system. The resource is instantiated at the second computer system according to a second data type that is different from the first data type. The resource is received by the first agent from the second agent. The received resource is materialized into an instance of the first data type using the first agent.
摘要翻译: 能够在第一和第二计算机系统之间执行数据通信,而不必在第一和第二计算机系统处匹配数据类型。 第一种数据类型与资源请求相关联。 资源的请求从第一计算机系统的第一代理发送到第二计算机系统处的第二代理。 该资源根据与第一数据类型不同的第二数据类型在第二计算机系统中实例化。 该资源由第二代理程序接收第一代理程序。 接收的资源使用第一代理实现为第一数据类型的实例。
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公开(公告)号:US20070232681A1
公开(公告)日:2007-10-04
申请号:US10573670
申请日:2004-10-13
申请人: David Middlemiss , Mark Ashton , Edward Boyd , Frederick Brookfield , Richard Armer , Eric Pettipher
发明人: David Middlemiss , Mark Ashton , Edward Boyd , Frederick Brookfield , Richard Armer , Eric Pettipher
IPC分类号: A61K31/40 , A61K31/405 , C07D209/04 , C07D209/34
CPC分类号: C04B35/632 , C07D209/30 , C07D401/12 , C07D403/12 , C07D417/12
摘要: Compounds of general formula (I): wherein R1, R2, R3 and R4 are independently hydrogen, halo, C1-C6 alkyl, —O(C1-C6 alkyl), —CON(R9)2, —SOR9, —SO2R9, —SO2N(R9)2, —N(R9)2, —NR9COR9, —CO2R9, —COR9, —SR9, —OH, —NO2 or —CN; each R9 is independently hydrogen or C1-C6 alkyl; R5 and R6 are each independently hydrogen, or C1-C6 alkyl or together with the carbon atom to which they are attached form a C3-C7 cycloalkyl group; R7 is hydrogen or C1-C6 alkyl n is 1 or 2; X is a bond or, when n is 2, X may also be a NR9 group; wherein R9 is as defined above; when X is a bond R8 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, biphenyl or a 9-14 membered bicyclic or tricyclic heteroaryl group; when X is a NR9 group R8 may additionally be phenyl, naphthyl or a 5-7 membered heteroaromatic ring; and the R8 group is optionally substituted with one or more substituents selected from halo, C1-C6 alkyl, —O(C1-C6)alkyl, aryl, —O-aryl, heteroaryl, —O-heteroaryl, —CON(R9)2, —SOR9, —SO2R9, SO2N(9)2, —N(9)2, —NR9COR9, —CO2R9, —COR9, —SR9, —OH, —NO2 or —CN; wherein R9 is as defined above; and their pharmaceutically acceptable salts, hydrates, solvates, complexes and prodrugs are useful in the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
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公开(公告)号:US20060106045A1
公开(公告)日:2006-05-18
申请号:US10517957
申请日:2003-06-04
申请人: David John Hughes , Paul Worthington , Charles Russell , Eric Clarke , James Peace , Mark Ashton , Thomas Coulter , Richard Roberts , Louis-Pierre Molleyres , Fredrik Cederbaum , Jerome Cassayre , Peter Maienfisch
发明人: David John Hughes , Paul Worthington , Charles Russell , Eric Clarke , James Peace , Mark Ashton , Thomas Coulter , Richard Roberts , Louis-Pierre Molleyres , Fredrik Cederbaum , Jerome Cassayre , Peter Maienfisch
IPC分类号: A01N43/42
CPC分类号: A01N43/90 , A01N47/34 , A01N47/38 , C07B2200/11 , C07D211/70 , C07D211/76 , C07D471/10 , C07D491/10
摘要: Insecticidal, acaricidal, nematicidal or molluscicidal compounds of formula (I) wherein Y is a single bond, C═O, C═S or C═(O)q where q is 0, 1 or 2; and R1, R2, R3, R4, R8, R9 and R10 are as defined in the claims or salts or N-oxides thereof, processes for preparing them and compositions containing them.
摘要翻译: 其中Y是单键,C-O,C-S或C(O)q q,其中q是0,1或2的式(I)的杀虫,杀螨,杀螨,杀线虫或杀软体动物化合物; 和R 1,R 2,R 3,R 4,R 8, R 9和R 10如权利要求中所定义,或其盐或N-氧化物,制备方法和含有它们的组合物。
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公开(公告)号:US20050119268A1
公开(公告)日:2005-06-02
申请号:US10972060
申请日:2004-10-22
IPC分类号: A61K31/404 , A61K31/426 , A61K31/428 , A61K31/4709 , A61K31/498 , C07D209/08 , C07D209/10 , C07D209/12 , C07D401/06 , C07D403/06 , C07D417/06 , A61K31/405 , A61K31/427 , C07D417/02 , C07D43/02
CPC分类号: C07D209/12 , A61K31/404 , A61K31/426 , A61K31/428 , A61K31/4709 , A61K31/498 , C07D209/08 , C07D209/10 , C07D401/06 , C07D403/06 , C07D417/06
摘要: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.
摘要翻译: 本发明提供了拮抗前列腺素D 2 N的吲哚衍生物,其可用于治疗由前列腺素D 2 2介导的炎性疾病。
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公开(公告)号:US20100146036A1
公开(公告)日:2010-06-10
申请号:US12404385
申请日:2009-03-16
申请人: Pablo Castro , Andrew Conrad , Michael Flasko , Pratik Patel , Mark Ashton
发明人: Pablo Castro , Andrew Conrad , Michael Flasko , Pratik Patel , Mark Ashton
IPC分类号: G06F15/16
CPC分类号: H04L67/2823 , H04L67/02 , H04L67/2876
摘要: Data communications are enabled to be performed between first and second computer systems without having to match data types at the first and second computer systems. A first data type is associated with a request for a resource. The request for the resource is transmitted from a first agent at the first computer system to a second agent at the second computer system. The resource is instantiated at the second computer system according to a second data type that is different from the first data type. The resource is received by the first agent from the second agent. The received resource is materialized into an instance of the first data type using the first agent.
摘要翻译: 能够在第一和第二计算机系统之间执行数据通信,而不必在第一和第二计算机系统处匹配数据类型。 第一种数据类型与资源请求相关联。 资源的请求从第一计算机系统的第一代理发送到第二计算机系统处的第二代理。 该资源根据与第一数据类型不同的第二数据类型在第二计算机系统中实例化。 该资源由第二代理程序接收第一代理程序。 接收的资源使用第一代理实现为第一数据类型的实例。
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公开(公告)号:US20050256170A1
公开(公告)日:2005-11-17
申请号:US11055724
申请日:2005-02-11
申请人: Alexander Oxford , Richard Davis , Robert Coleman , Kenneth Clark , David Clark , Neil Harris , Garry Fenton , George Hynd , Keith Stuttle , Jonathan Sutton , Mark Ashton , Edward Boyd , Shirley Brunton
发明人: Alexander Oxford , Richard Davis , Robert Coleman , Kenneth Clark , David Clark , Neil Harris , Garry Fenton , George Hynd , Keith Stuttle , Jonathan Sutton , Mark Ashton , Edward Boyd , Shirley Brunton
IPC分类号: A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/4439 , C07C233/75 , C07C233/81 , C07C235/84 , C07D213/81 , C07D233/90 , C07D257/04 , C07D277/24 , C07D277/26 , C07D277/56 , C07D307/46 , C07D307/68 , C07D307/91 , C07D333/38 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号: C07D213/81 , C07C233/75 , C07C233/81 , C07C235/84 , C07D233/90 , C07D257/04 , C07D277/24 , C07D277/26 , C07D277/56 , C07D307/46 , C07D307/68 , C07D307/91 , C07D333/38 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12
摘要: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein: R5is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of: wherein X and Y are selected from the group consisiting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O., and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: where RN′ is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm alkylene-R2 and the other of RP3 and RP4 is H, m and n can be 0 or 1, and m+n=1 or 2; and additionally when RP3 is —Cm alkylene-R2, m can also be 2 or 3, and m+n=1, 2, 3 or 4, and when R2 is tetrazol-5-yl, m+n may be 0; or where one of RP3 and RP4 is —O—CH2—R2, and the other of RP3 and RP4 is H, n is 0; RN is H or optionally substituted C1-4 alkyl; R2 is either: —CO2H (carboxy); —CONH2; —CH2-OH; or tetrazol-5-yl.
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公开(公告)号:US4687979A
公开(公告)日:1987-08-18
申请号:US817582
申请日:1986-01-10
申请人: Mark Ashton , Godfrey N. Hounsfield
发明人: Mark Ashton , Godfrey N. Hounsfield
IPC分类号: B25J9/16 , B25J13/08 , G01B7/00 , G05B19/4063 , G05B19/4155 , G05B19/42 , G05B1/06
CPC分类号: G01B7/002 , G05B19/42 , G05B2219/36357 , Y02P90/265
摘要: In a control system for a robotic gripper a processing circuit (10) controls movement of the gripper (20) on a prearranged path. An article (A) held by gripper (20) comes into contact with the probe member (32) of a "known-down" sensor (30). A support assembly (33), on which the probe member (32) is mounted, is displaced with respect to a base member (31) allowing a continuous, uninhibited movement of the gripper along the path, even after contact has been established. In an alternative arrangement the sensor is mounted on the gripper and establishes contact with an article located at a fixed work station.
摘要翻译: 在用于机器人夹具的控制系统中,处理电路(10)控制夹具(20)在预先布置的路径上的运动。 由夹具(20)保持的物品(A)与“已知的”传感器(30)的探针部件(32)接触。 安装有探针构件(32)的支撑组件(33)相对于基部构件(31)移位,允许夹持器沿着路径的连续的,不受阻碍的移动,即使在接触已经建立之后。 在替代布置中,传感器安装在夹持器上并且与位于固定工作站处的物品建立接触。
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