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11. 发明申请

US20070161638A1 Compounds which potentiate glutamate receptor and uses thereof in medicine 失效
公开(公告)号：US20070161638A1
公开(公告)日：2007-07-12
申请号：US11573370
申请日：2005-08-05
申请人： Daniel Bradley , Kevin Thewlis , Simon Ward
发明人： Daniel Bradley , Kevin Thewlis , Simon Ward
IPC分类号： A61K31/505 , A61K31/50 , A61K31/44 , A61K31/415 , A61K31/4164 , A61K31/381
CPC分类号： C07D213/64 , C07D213/42 , C07D213/50 , C07D213/61 , C07D213/84 , C07D213/85 , C07D231/12 , C07D233/64 , C07D237/08 , C07D239/26 , C07D333/20
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting of C1-6alkyl, C1-6alkoxy, acetyl, halogen, haloC1-6alkyl, cyano, nitro, amino, monoC1-4alkylamino and diC1-4alkylamino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.

12. 发明申请

US20050176724A1 Piperidine and piperazine derivatives possessing affinity at 5ht-1 type receptors 审中-公开
公开(公告)号：US20050176724A1
公开(公告)日：2005-08-11
申请号：US10504114
申请日：2003-02-17
申请人： Sean Flynn , Paul Smith , Kevin Thewlis , Simon Ward
发明人： Sean Flynn , Paul Smith , Kevin Thewlis , Simon Ward
IPC分类号： A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/5377 , A61P25/00 , A61P25/22 , A61P25/24 , A61P43/00 , C07D215/20 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D43/02
CPC分类号： C07D401/12 , C07D215/20 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein A is optionally substituted phenyl, indolyl, quinolinyl, quinazolinyl, indazolyl or isoquinolinyl; X is carbon, Y is CH and ═ is a double bond; or X is CH, Y is CH2 or oxygen and ═ is a single bond; or X is nitrogen, Y is CH2 and ═ is a single bond; R1 is halogen, cyano, nitro, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy, C3-7heterocyclylC1-6alkyl, C3-7heterocyclyl C1-6alkoxy; a is 0, 1, 2, 3 or 4; R2 is either: halogen, —CN, an optionally substituted C3-7cycloalkyl, an optionally substituted aryl or an optionally substituted C-linked 3-7 membered heterocyclic group; or a group -(Z)b-B wherein: (i) Z is oxygen, CH2, C═O, SO2 or C═N—OR3 wherein R3 is hydrogen or C1-6alkyl; b is 1, 2, or 3; and B is hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or NR4R5 wherein R4 and R5 are independently hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl or C1-6alkylcarbamoyl, or R4 and R5, together with the nitrogen atom to which they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group; or (ii) Z is oxygen, CH or CH2, b is 1, and B forms the rest of an aryl or a C3-7heterocyclic group fused to the phenyl ring; excluding 1-[2-[2-(phenylmethyl)phenoxy]ethyl]-4-[(2,3,4-trimethoxyphenyl)methyl]-piperazine and pharmaceutically acceptable salts thereof, and N-[4-[2-[4-[(3,4-dimethoxyphenyl)methyl]-1-piperazinyl]ethoxy]phenyl]-ethanesulfonamide and pharmaceutically acceptable salts thereof. Methods of preparing the compounds and uses of the compounds in therapy, in particular for CNS disorders such as depression and anxiety, are also disclosed.

13. 发明申请

US20050153974A1 Heterocyclymethylpiperidines and -piperazines possessing affinity at 5ht-1 type receptors 失效
标题翻译：在5ht-1型受体具有亲和力的杂环甲基哌啶和哌嗪
公开(公告)号：US20050153974A1
公开(公告)日：2005-07-14
申请号：US10503969
申请日：2003-02-17
申请人： Simon Ward
发明人： Simon Ward
IPC分类号： A61K31/496 , A61K31/498 , A61K31/538 , A61P1/04 , A61P15/10 , A61P25/00 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P43/00 , C07D215/20 , C07D401/12 , C07D413/14 , A61K31/517 , C07D43/02
CPC分类号： C07D401/12 , C07D215/20 , C07D413/14
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH2 or oxygen and is a single bond; or X is nitrogen, Y is CH2 and is a single bond; R1 is halogen, cyano, or C1-6alkoxy; a is 0, 1, 2 or 3; b is 0 or 1; R2 is hydrogen, C1-6alkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl, C1-6alkylcarbamoyl or arylC1-6alkyl; and R3, together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐：其中：A为任选取代的苯基，萘基，吲哚基，喹啉基，喹唑啉基，吲唑基，异喹啉基或苯并呋喃基; X是碳，Y是CH并且是双键; 或X是CH，Y是CH 2或氧并且是单键; 或X是氮，Y是CH 2，并且是单键; R 1是卤素，氰基或C 1-6烷氧基; a是0,1,2或3; b为0或1; R 2是氢，C 1-6烷基，C 1-6烷酰基，氟C 1-6烷酰基，C 1-6 烷基磺酰基，氟代C 1-6烷基磺酰基，氨基甲酰基，C 1-6烷基氨基甲酰基或芳基C 1-6烷基; 并且R 3与连接的氮原子一起形成与苯环稠合的任选取代的5至7元杂环基。还公开了制备化合物的方法和化合物在治疗中的用途，特别是用于CNS疾病如抑郁或焦虑症的用途。

14. 发明申请

US20080292615A1 DIAGNOSIS AND TREATMENT OF DISEASE 审中-公开
标题翻译：诊断和治疗疾病
公开(公告)号：US20080292615A1
公开(公告)日：2008-11-27
申请号：US12016012
申请日：2008-01-17
申请人： Rachid Tazi-Ahnini , Claes Bavik , Simon Ward , Gordon Duff , Michael Cork
发明人： Rachid Tazi-Ahnini , Claes Bavik , Simon Ward , Gordon Duff , Michael Cork
IPC分类号： A61K39/395 , A61K31/711 , A61K38/08 , A61P11/06 , A61P17/00 , A61K38/02
CPC分类号： G01N33/564 , G01N33/6881 , G01N2500/00 , G01N2800/20 , G01N2800/205
摘要： We disclose a method of diagnosis of a disease, or susceptibility to a disease associated with abnormal cell-cell adhesion between epithelial cells, the method comprising detection of a mutation in a nucleic acid encoding an adhesion protein, a protease, or a protease inhibitor of an individual. Methods of making medicaments and methods of treatment and/or prophylaxis are also disclosed.
摘要翻译：我们公开了诊断疾病的方法或与上皮细胞之间异常细胞粘附相关的疾病的易感性，所述方法包括检测编码粘附蛋白的核酸中的突变，蛋白酶或蛋白酶抑制剂个人。还公开了制备药物的方法和治疗和/或预防方法。

15. 发明申请

US20080045532A1 Compounds which potentiate AMPA receptor and uses thereof in medicine 失效
标题翻译：增强AMPA受体的化合物及其在药物中的用途
公开(公告)号：US20080045532A1
公开(公告)日：2008-02-21
申请号：US11687729
申请日：2007-03-19
申请人： Stephen Harrison , Kevin Thewlis , Simon Ward
发明人： Stephen Harrison , Kevin Thewlis , Simon Ward
IPC分类号： A61K31/535 , A61K31/415 , A61P25/00 , A61K31/4164
CPC分类号： C07D403/12 , C07D231/56 , C07D401/10 , C07D403/10 , C07D405/12 , C07D409/12 , C07D413/10 , C07D417/10
摘要： Compounds of formula (I) and salts are provided: along with pharmaceutical compositions, uses in medicine, e.g., treating disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment.
摘要翻译：提供式（I）和盐的化合物：与药物组合物一起在药物中的用途，例如治疗由谷氨酸受体功能如精神分裂症或认知障碍的减少或不平衡介导的疾病或病症。

16. 发明申请

US20070167423A1 QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS 失效
标题翻译：具有5HT1型受体亲和力的喹啉和喹唑啉衍生物
公开(公告)号：US20070167423A1
公开(公告)日：2007-07-19
申请号：US11687098
申请日：2007-03-16
申请人： Markus Bergauer , Barbara Bertani , Matteo Biagetti , Steven Bromidge , Alessandro Falchi , Colin Leslie , Giancarlo Merlo , Domenica Pizzi , Marilisa Rinaldi , Luigi Stasi , Jessica Tibasco , Antonio Vong , Simon Ward
发明人： Markus Bergauer , Barbara Bertani , Matteo Biagetti , Steven Bromidge , Alessandro Falchi , Colin Leslie , Giancarlo Merlo , Domenica Pizzi , Marilisa Rinaldi , Luigi Stasi , Jessica Tibasco , Antonio Vong , Simon Ward
IPC分类号： A61K31/517 , A61K31/496 , C07D403/02 , A61K31/5377 , C07D413/14 , C07D403/14
CPC分类号： C07D401/12 , C04B35/632
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression or anxiety, are also disclosed.
摘要翻译：提供式（I）化合物及其药学上可接受的盐：其中R 1，m，X，R 2，n，W，p，Y，Z，R R 3，R 4，R 5和q具有如说明书中定义的含义。还公开了其治疗方法及其在治疗中的用途，特别是CNS疾病如抑郁或焦虑症。

17. 发明申请

US20060229312A1 Quinoline and quinazoline derivatives having affinity for 5ht1-type receptors 失效
标题翻译：对5ht1型受体具有亲和力的喹啉和喹唑啉衍生物
公开(公告)号：US20060229312A1
公开(公告)日：2006-10-12
申请号：US10565066
申请日：2004-07-15
申请人： Markus Bergauer , Barbara Bertani , Matteo Biagetti , Steven Bromidge , Alessandro Falchi , Colin Leslie , Giancarlo Merlo , Domenica Pizzi , Marilisa Rinaldi , Luigi Stasi , Jessica Tibasco , Antonio Vong , Simon Ward
发明人： Markus Bergauer , Barbara Bertani , Matteo Biagetti , Steven Bromidge , Alessandro Falchi , Colin Leslie , Giancarlo Merlo , Domenica Pizzi , Marilisa Rinaldi , Luigi Stasi , Jessica Tibasco , Antonio Vong , Simon Ward
IPC分类号： A61K31/517 , A61K31/496 , C07D403/02
CPC分类号： C07D401/12 , C04B35/632
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression or anxiety, are also disclosed.
摘要翻译：提供式（I）化合物及其药学上可接受的盐：其中R 1，m，X，R 2，n，W，p，Y，Z，R R 3，R 4，R 5和q具有如说明书中所定义的含义。还公开了其治疗方法及其在治疗中的用途，特别是CNS疾病如抑郁或焦虑症。

18. 发明申请

US20060108462A1 Cutting or crushing implement 有权
标题翻译：切割或破碎工具
公开(公告)号：US20060108462A1
公开(公告)日：2006-05-25
申请号：US10523898
申请日：2003-08-06
申请人： Simon Ward
发明人： Simon Ward
IPC分类号： B02C1/06
CPC分类号： E04G23/08 , B23D17/00 , B23D31/008 , E02F3/965 , E04G23/082
摘要： A cutting or crushing implement (1) as disclosed which includes a plurality of sets of jaws (3) which when operated are adapted to cut and/or crush a single length of material at a plurality of separate positions along the length of the material wherein a single actuation of the implement (1) causes each of the jaws (3) to at least partially and consecutively close. The consecutive closing of adjacent jaws (3) places a first jaw in a cutting or crushing configuration and a second, immediately adjacent jaw in a clamping configuration. The cutting or crushing implement (1) disclosed is configured to connect to and be actuated by the actuator arm of an excavator (9).
摘要翻译：所公开的切割或破碎工具（1）包括多组钳口（3），其在操作时适于在沿着材料的长度的多个分开的位置处切割和/或挤压单个长度的材料，其中工具（1）的单个致动使得每个钳口（3）至少部分地并且连续地关闭。相邻夹爪（3）的连续关闭将第一钳口放置在切割或破碎构型中，并且以夹紧构型将第二钳口紧紧相邻。所公开的切割或破碎装置（1）构造成连接到挖掘机（9）的致动器臂并由其致动。

19. 发明申请

US20050267686A1 Wellbore evaluation system and method 有权
标题翻译：井眼评估体系和方法
公开(公告)号：US20050267686A1
公开(公告)日：2005-12-01
申请号：US10853592
申请日：2004-05-25
申请人： Simon Ward
发明人： Simon Ward
IPC分类号： E21B47/02 , E21B43/12 , E21B47/002 , E21B47/08 , G06F19/00
CPC分类号： E21B47/022 , E21B43/127 , E21B47/0007 , E21B47/0008 , E21B47/082
摘要： A wellbore evaluation system evaluates mechanical wear and corrosion to components of a well system including a production tubing string positionable in a well and a sucker rod string movable within the production tubing string. A deviation sensor determines a deviation profile of the well, a rod sensor senses and measures wear and corrosion to the sucker rod string as it is removed from the well to determine a rod profile, and a tubing sensor senses and measures wear and corrosion to the production tubing string as it is removed from the well to determine a tubing profile. A data acquisition computer is in communication with the sensors for computing and comparing two or more of the respective deviation profile, rod profile, and tubing profile as a function of depth in the well. A 3-dimensional image of wellbores, with isogram mapping, may be generated and examined over the internet.
摘要翻译：井眼评估系统评估对井系统的部件的机械磨损和腐蚀，包括可定位在井中的生产油管柱和可在生产油管柱内移动的抽油杆串。偏差传感器确定井的偏差轮廓，杆传感器感测并测量抽油杆柱从井中移除时的磨损和腐蚀，以确定杆轮廓，并且油管传感器感测并测量对油管的磨损和腐蚀生产油管柱从井中取出以确定油管剖面。数据采集计算机与传感器通信，用于计算和比较作为井中深度的函数的相应偏差轮廓，杆轮廓和油管剖面中的两个或更多个。可以通过互联网生成和检查具有等位线映射的井筒的三维图像。

20. 发明申请

US20050085458A1 Heterocyclic compounds possessing affinity at 5ht1-type receptors and use thereof in therapy 失效
公开(公告)号：US20050085458A1
公开(公告)日：2005-04-21
申请号：US10504109
申请日：2003-02-17
申请人： Frank Harrington , Paul Smith , Simon Ward
发明人： Frank Harrington , Paul Smith , Simon Ward
IPC分类号： A61K31/4709 , A61K31/496 , A61K31/498 , A61K31/538 , A61P25/00 , A61P25/22 , A61P25/24 , A61P43/00 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D498/02 , A61K31/58
CPC分类号： C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; b is 1, 2 or 3 and c is 1, 2 or 3, wherein b+c is 2, 3, 4 or 5; X is carbon, Y is CH, is a double bond and e is 0; or X is carbon, Y is CH2 or oxygen, is a single bond and e is 1; or X is nitrogen, Y is CH2, is a single bond and e is 0; R1 is hydrogen, cyano, halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, NHCOCH3 or OCONR5R6, wherein R5 and R6 are independently hydrogen or C1-6alkyl; R2 is halogen, cyano or C1-6alkoxy; d is 0, 1, 2 or 3; R3 is hydrogen, C1-6alkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl, C1-6alkylcarbamoyl or arylC1-6alkyl; and R4, together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring, provided that when a compound of formula (I) has the following structure: wherein A, b, c, R1, e, X, Y, R2 and d are as defined above and R3 is hydrogen, C1-6alkyl or arylC1-6alkyl, then (i) X is carbon, Y is CH and is a double bond; or (ii) b and c are both 1; or (iii) the carbon atom adjacent to the oxo-substituted carbon atom in the morpholinyl ring, marked “*”, is substituted. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.

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