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1. 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.

2. 发明申请

US20050107410A1 Compound possessing affinity at 5ht1-type receptors and use thereof in therapy of cns disorders 审中-公开
标题翻译：在5ht1型受体具有亲和力的化合物及其在治疗cns病症中的用途
公开(公告)号：US20050107410A1
公开(公告)日：2005-05-19
申请号：US10503833
申请日：2003-02-17
申请人： Paul Smith , Kevin Thewlis , Antonio Vong , Simon Ward
发明人： Paul Smith , Kevin Thewlis , Antonio Vong , Simon Ward
IPC分类号： A61K31/4709 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/551 , A61P1/04 , A61P3/04 , A61P3/10 , A61P9/10 , A61P11/00 , A61P15/00 , A61P15/06 , A61P15/10 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/36 , A61P29/00 , A61P43/00 , C07D215/20 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D41/02 , C07D43/02
CPC分类号： C07D401/12 , C07D215/20 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
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; is halogen, hydroxy, cyano, C1-6alkyl, haloC1-6alkyl or C1-6alkoxy; a is 0, 1, 2, 3 or 4; R2 and R3, together with the nitrogen atom to which they are attached, form a nitro group or an optionally substituted 3 to 7 membered heterocyclic group, or R2 and R3 are independently hydrogen, aroyl, C1-6alkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl, C1-6alkylcarbamoyl, arylC1-6alkyl or a group CO(CH2)bNR4R5 wherein b is 1, 2, 3 or 4; and R4 and R5 are independently hydrogen or C1-6alkyl, or R4 and R5, together with the nitrogen atom to they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group. 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.
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; 是卤素，羟基，氰基，C 1-6烷基，卤代C 1-6烷基或C 1-6烷氧基; a是0，1，2，3或4; R2和R3与它们所连接的氮原子一起形成硝基或任选取代的3至7元杂环基，或R 2和R 3独立地是氢，芳酰基，C 1-6 烷基，C 1-6烷酰基，氟代C 1-6烷酰基，C 1-6烷基磺酰基，氟代C 1-6烷基，烷基磺酰基，氨基甲酰基，C 1-6烷基氨基甲酰基，芳基C 1-6 - 烷基或基团CO（CH 2）2 bRR 4 R 5，其中b 是1，2，3或4; 并且R 4和R 5独立地为氢或C 1-6烷基，或者R 4和R 5与它们连接的氮原子一起形成任选取代的3至7元杂环基的一部分。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CNS障碍如抑郁和焦虑。

3. 发明申请

US20070270471A1 Compounds Which Potentiate Glutamate Receptor and Uses Thereof in Medicine 审中-公开
公开(公告)号：US20070270471A1
公开(公告)日：2007-11-22
申请号：US11573366
申请日：2005-08-05
申请人： Kevin Thewlis , Simon Ward
发明人： Kevin Thewlis , Simon Ward
IPC分类号： A61K31/40 , A61K31/4439 , A61P25/18 , C07D207/14 , C07D401/10
CPC分类号： C07D207/14 , C07D403/10 , C07D409/10
摘要： This case discloses compounds of formula (I) wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; B is —N(R4)— or —O—; A and D, which may be the same or different, are —C(R5)2—; each R2, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; n is 0, 1 or 2; R3 is C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, —(CH2)pNR3aSO2R3b, —(CH2)pNR3a(C═O)R3b, —(CH2)pNR3a(C═O)N(R3c)2, —(CH2)p(C═O)R3d, —(CH2)pSO2R3e, phenyl or heterocyclyl, wherein when R3 is phenyl or heterocyclyl, it is optionally substituted by one or more groups independently selected from: C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, —(CH2)pNR3aSO2R3b, —(CH2)pNR3a(C═O)R3b, —(CH2)pNR3a(C═O)N(R3c)2, —(CH2)p(C═O)R3d and —(CH2)pSO2R3e; where R3a and each R3c, which may be the same or different, is hydrogen or C1-6alkyl; R3b and R3e are C1-6alkyl or haloC1-6alkyl; R3d is C1-6alkyl, C1-4alkoxy or haloC1-6alkyl; or R3a and R3b, or R3a and R3c, together with the interconnecting atoms, may form a 5- or 6-membered ring; and p is 0, 1, or 2; R4 is carbocyclyl or carbocyclylC1-4alkyl, wherein the carbocyclyl group of either is optionally substituted by one or more groups independently selected from C1-6alkyl and halogen; or R4 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-6alkylcarbonyl, C1-6alkylsulfonyl or C1-6alkylaminocarbonyl; each R5, which may be the same or different, is hydrogen, C1-6alkyl or halogen; and R6 is hydrogen or fluorine.

4. 发明申请

US20070203218A1 Compounds Which Potentiate Glutamate Receptor And Uses Thereof In Medicine 失效
公开(公告)号：US20070203218A1
公开(公告)日：2007-08-30
申请号：US11573368
申请日：2005-08-05
申请人： Kevin Thewlis , Simon Ward
发明人： Kevin Thewlis , Simon Ward
IPC分类号： A61K31/4015 , A61K31/277 , A61K31/18
CPC分类号： C07D207/27 , C07C311/07 , C07C311/08 , C07C311/37 , C07C317/28 , C07C2602/08 , C07D275/02
摘要： This case discloses compounds of formula (I) 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 or amino; each R4, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; p is 0, 1 or 2; each R5, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; q is 0,1 or 2; R6 is −NR6aSO2R6b, —NR6aC(═O)R6b, —NR6a(C═O)N(R6c)2, —(C═O)R6d, —CH2NR6aSO2R6b, —CH2NR6aC(═O)R6b, CH2NR6a(C═O)N(R6c)2 or —CH2(C═O)R6d; where R6a and each R6c, which may be the same or different, is hydrogen or C1-6alkyl; R6b and R6d are C1-6alkyl or haloC1-6alkyl; or R6a and R6b, or R6a and R6c, together with the interconnecting atoms, may form a 5- or 6-membered ring; n is 1 or 2; and R7 and R8, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano or amino. It also discloses methods for preparing the compounds and their use in therapy such as treating schizophrenia.

5. 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.

6. 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。

7. 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.

8. 发明申请

US20130028986A1 Pharmaceutical Compositions 审中-公开
公开(公告)号：US20130028986A1
公开(公告)日：2013-01-31
申请号：US13568234
申请日：2012-08-07
申请人： Simon Ward , Alice MacGowan , Michael J. Cork , Jonathan Hadgraft , Majella Lane , Adrian Davis , Richard Guy
发明人： Simon Ward , Alice MacGowan , Michael J. Cork , Jonathan Hadgraft , Majella Lane , Adrian Davis , Richard Guy
IPC分类号： A61K33/30 , A61K31/315 , A61P17/00
CPC分类号： A61K33/30 , A61K31/315 , A61K33/00
摘要： A composition comprising a pharmaceutically acceptable group (2, 4, 12, 13 or 14) metal compound for the treatment of a dermatological condition involving an abnormal decrease in the cell-to-cell adhesion between epithelial cells in the epidermal barrier.

9. 发明申请

US20090076032A1 Derivatives of 18Beta-Glycyrrhetinic Acid 审中-公开
标题翻译： 18β-甘草次酸的衍生物
公开(公告)号：US20090076032A1
公开(公告)日：2009-03-19
申请号：US12207899
申请日：2008-09-10
申请人： Simon Ward , Alice Macgowan , Stanley Roberts , Jenny Littlechild , Kirsty Line , Ed Irving , Sam Donnelly
发明人： Simon Ward , Alice Macgowan , Stanley Roberts , Jenny Littlechild , Kirsty Line , Ed Irving , Sam Donnelly
IPC分类号： A61K31/4965 , C07C69/757 , A61K31/215 , C07C69/76 , C07D241/24 , C07C69/73
CPC分类号： C07J63/008
摘要： The present invention relates to novel derivatives of 18β-glycyrrhetinic acid and methods of synthesising the derivatives. Also included within the scope of the present invention are pharmaceutical compositions comprising the derivatives of the present invention and medical uses of the derivatives, including their use in inhibiting enzymes such as retinol dehydrogenases. The present invention also relates to methods of treating diseases, such as hyperproliferative diseases, neoplasms, cancers and photoageing.
摘要翻译：本发明涉及18beta-glycyrryrinic acid的新衍生物和合成衍生物的方法。还包括在本发明范围内的药物组合物是包含本发明衍生物和衍生物的医学用途的药物组合物，包括它们在抑制酶如视黄醇脱氢酶中的用途。本发明还涉及治疗疾病如过度增殖性疾病，肿瘤，癌症和光老化的方法。

10. 发明申请

US20070262772A1 Method and apparatus for correcting magnetic flux sensor signals 审中-公开
标题翻译：用于校正磁通量传感器信号的方法和装置
公开(公告)号：US20070262772A1
公开(公告)日：2007-11-15
申请号：US11430572
申请日：2006-05-09
申请人： John Rogers , Simon Ward
发明人： John Rogers , Simon Ward
IPC分类号： G01N27/82
CPC分类号： E21B17/006 , E21B47/0007 , E21B47/0008 , E21B47/08
摘要： Apparatus for detecting defects in an oilfield string at a well site as the string is pulled from the well include a plurality of magnetic flux sensors 12 circumferentially spaced about the string, and a plurality of stand-off sensors 14 circumferentially spaced about the string for determining changes in stand-off distance between one or more stand-off sensors and an external surface of the string. Computer 18 corrects signals from the plurality of magnetic flux sensors as a function of the detected stand-off distance.
摘要翻译：用于检测井的井场中的缺陷的设备，当从井中拉出绳索时，包括围绕绳索周向间隔开的多个磁通量传感器12和围绕该串的圆周间隔的多个支座传感器14，用于确定在一个或多个支架传感器和弦的外表面之间的间隔距离的变化。计算机18根据检测到的间隔距离校正来自多个磁通量传感器的信号。

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