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21. 发明授权

US08344000B2 Compounds which have activity at M1 receptor and their uses in medicine 失效
标题翻译：具有M1受体活性的化合物及其在药物中的用途
公开(公告)号：US08344000B2
公开(公告)日：2013-01-01
申请号：US12678360
申请日：2008-09-18
申请人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Paul Adrian Wyman
发明人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Paul Adrian Wyman
IPC分类号： C07D401/14 , A61K31/454 , A61P25/18 , A61P25/28
CPC分类号： C07D413/14
摘要： Compounds of formula (I) and salts thereof are provided: wherein R4, R5, R6, Q, A, and Y are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物及其盐：其中R4，R5，R6，Q，A和Y如说明书中所定义。公开了化合物作为药物的用途和用于治疗精神病，认知障碍和阿尔茨海默氏病的药物的制备。本发明还公开了包含该化合物的药物组合物。

22. 发明申请

US20120316196A1 Compounds Which Have Activity at M1 Receptor and Their Uses in Medicine 失效
标题翻译：在M1受体中具有活性的化合物及其在医学中的应用
公开(公告)号：US20120316196A1
公开(公告)日：2012-12-13
申请号：US13592785
申请日：2012-08-23
申请人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Graeme Irvine Stevenson , Paul Adrian Wyman
发明人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Graeme Irvine Stevenson , Paul Adrian Wyman
IPC分类号： A61K31/454 , A61P25/28 , A61P25/18 , A61K31/4545
CPC分类号： C07D498/04 , C07D209/34 , C07D215/227
摘要： Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐：其中R 4，R 5，R 6，Q，A，Y和R如说明书中所定义。公开了化合物作为药物的用途和用于治疗精神病，认知障碍和阿尔茨海默氏病的药物的制备。本发明还公开了包含该化合物的药物组合物。

23. 发明申请

US20120316202A1 Compounds which have activity at M1 receptor and their uses in medicine 审中-公开
标题翻译：具有M1受体活性的化合物及其在药物中的用途
公开(公告)号：US20120316202A1
公开(公告)日：2012-12-13
申请号：US13584956
申请日：2012-08-14
申请人： David Gwyn COOPER , Ian Thomson Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
发明人： David Gwyn COOPER , Ian Thomson Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
IPC分类号： A61K31/454 , A61P25/00 , A61P25/28 , C07D401/04
CPC分类号： C07D235/26
摘要： Compounds of the general formula And their use in the treatment of psychotic disorders and cognitive impairment are disclosed.
摘要翻译：公开了通式的化合物及其在治疗精神病和认知障碍中的用途。

24. 发明授权

US08299257B2 Compounds which have activity at M1receptor and their uses in medicine 失效
标题翻译：在M1受体上具有活性的化合物及其在医学中的应用
公开(公告)号：US08299257B2
公开(公告)日：2012-10-30
申请号：US12678353
申请日：2008-09-18
申请人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Graeme Irvine Stevenson , Paul Adrian Wyman
发明人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Graeme Irvine Stevenson , Paul Adrian Wyman
IPC分类号： C07D261/20 , A61K31/445
CPC分类号： C07D413/04
摘要： Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐：其中R 4，R 5，R 6，Q，A，Y和R如说明书中所定义。公开了化合物作为药物的用途和用于治疗精神病，认知障碍和阿尔茨海默氏病的药物的制备。本发明还公开了包含该化合物的药物组合物。

25. 发明申请

US20100204272A1 Compounds which have activity at M1 receptor and their uses in medicine 失效
标题翻译：具有M1受体活性的化合物及其在药物中的用途
公开(公告)号：US20100204272A1
公开(公告)日：2010-08-12
申请号：US12678347
申请日：2008-09-18
申请人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Graeme Irvine Stevenson , Paul Adrian Wyman
发明人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Graeme Irvine Stevenson , Paul Adrian Wyman
IPC分类号： A61K31/47 , C07D401/04 , A61K31/454 , A61P25/18 , A61P25/28
CPC分类号： C07D498/04 , C07D209/34 , C07D215/227
摘要： Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐：其中R 4，R 5，R 6，Q，A，Y和R如说明书中所定义。公开了化合物作为药物的用途和用于治疗精神病，认知障碍和阿尔茨海默氏病的药物的制备。本发明还公开了包含该化合物的药物组合物。

26. 发明申请

US20080261945A1 Compounds Having Activity at Nk3 Receptor and Uses Thereof in Medicine 审中-公开
标题翻译：在Nk3受体中具有活性的化合物及其在医学中的应用
公开(公告)号：US20080261945A1
公开(公告)日：2008-10-23
申请号：US11718908
申请日：2005-11-10
申请人： Paul William Smith , Paul Adrian Wyman
发明人： Paul William Smith , Paul Adrian Wyman
IPC分类号： A61K31/397 , C07D215/38 , A61K31/4709 , A61P25/00 , A61K31/47
CPC分类号： C07D401/12 , C07D215/52 , C07D409/14
摘要： The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1 is phenyl optionally substituted by 1, 2 or 3 halogen atoms which halogen atoms may be the same or different; R2 is C1-6alkyl, C3-6cycloalkyl or acetyl; X is oxygen or sulphur; a is 1, 2 or 3; b is 0 or 1; c is 0, 1 or 2; R3 is hydrogen or C1-6alkyl; R4 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxyC1-6alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-6alkyl; R5 is hydrogen; or R5 and R3, together with the interconnecting atoms, form a 4, 5 or 6 membered ring; R6 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; and z is 0, 1 or 2; wherein when z is 1 or 2, Z is a halogen atom, and wherein when z is 2 the halogen atoms may be the same or different. Also disclosed are processes for their preparation, pharmaceutical compositions containing them and their use as medicaments particularly in treating disorders of the Central Nervous System (CNS).
摘要翻译：本发明涉及式（I）化合物，其药学上可接受的盐，溶剂化物或前药：其中R 1是任选被1,2或3个卤素原子取代的苯基，该卤素原子可以是相同或不同; R 2是C 1-6烷基，C 3-6环烷基或乙酰基; X是氧或硫; a是1,2或3; b为0或1; c为0,1或2; R 3是氢或C 1-6烷基; R 4是氢，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基C C 1-6烷基，C 3-6环烷基或C 3-6环烷基C 1-6烷基; R 5是氢; 或R 5和R 3与连接的原子一起形成4,5或6元环; R 6是苯基或噻吩基，其任一个任选被1,2或3个卤素原子取代，该原子可以相同或不同; 且z为0,1或2; 其中当z为1或2时，Z为卤素原子，并且其中当z为2时，卤素原子可以相同或不同。还公开了其制备方法，含有它们的药物组合物及其作为药物的用途，特别是用于治疗中枢神经系统（CNS）的疾病。

27. 发明授权

US07109201B2 Piperazine derivatives, their preparation and uses in therapy 失效
公开(公告)号：US07109201B2
公开(公告)日：2006-09-19
申请号：US10471433
申请日：2002-03-11
申请人： Mervyn Thompson , Paul Adrian Wyman
发明人： Mervyn Thompson , Paul Adrian Wyman
IPC分类号： A61K31/496 , C07D403/04 , C07D401/14
CPC分类号： C07D401/10 , C07D209/08
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: in which Ra is a group of formula (i) wherein P2 is phenyl, naphthyl, heteroaryl or a 5 to 7 membered heterocyclic ring; P3 is phenyl, naphthyl or heteroaryl; R1 is NR4COR5, NR4SO2R5, CH2NR4SO2R5, CH2NR4COR5 or CH2NR4CO2R5 where R4 and R5 are independently hydrogen or C1-6alkyl; R2 and R3 are independently halogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkoxy, COC1-6alkyl, haloC1-6alkyl, cyano or NR6R7 where R6 and R7 are independently hydrogen or C1-6alkyl; b and c are independently 0, 1, 2 or 3; Y is a single bond, CH2 or NH; W is —(CR9R10)t—where t is 2, 3 or 4 and R9 and R10 are independently hydrogen or C1-6alkyl or W is a group CH═CH; Rb is hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, COC1-6alkyl, cyano or C1-6alkoxy; and Rc is hydrogen or C1-6alkyl. Processes for preparation of the compounds and their uses in therapy, particularly depression, are also disclosed.

28. 发明申请

US20120041028A1 BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的BENZIMIDAZOLES及其在医学中的用途
公开(公告)号：US20120041028A1
公开(公告)日：2012-02-16
申请号：US13282610
申请日：2011-10-27
申请人： David Gwyn COOPER , Ian Thomas Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
发明人： David Gwyn COOPER , Ian Thomas Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
IPC分类号： A61K31/454 , A61P25/18 , A61P25/28 , C07D401/04
CPC分类号： C07D235/26
摘要： Compounds of formula (I), salts and solvates are provided: Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.
摘要翻译：提供式（I）化合物，盐和溶剂合物：还公开了用于治疗的化合物的用途，例如治疗精神病和认知障碍。

29. 发明申请

US20100317704A1 SPIRO-CONDENSED IMIDAZOLONE DERIVATIVES INHIBITING THE GLYCINE TRANSPORTER 审中-公开
标题翻译：螺旋状咪唑啉酮衍生物抑制糖蛋白转运蛋白
公开(公告)号：US20100317704A1
公开(公告)日：2010-12-16
申请号：US12676625
申请日：2008-09-09
申请人： Richard Blunt , David Gwyn Cooper , Roderick Alan Porter , Paul Adrian Wyman
发明人： Richard Blunt , David Gwyn Cooper , Roderick Alan Porter , Paul Adrian Wyman
IPC分类号： A61K31/4188 , C07D487/10 , A61K31/4184 , A61P25/28 , A61P25/18
CPC分类号： C07D235/02 , C07D401/10 , C07D403/10 , C07D491/04
摘要： Compounds of formula (I) and salts thereof are provided: wherein the groups are as defined in the specification. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：提供式（I）化合物及其盐：其中基团如说明书中所定义。还公开了化合物作为药物的用途，以及用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物的制备。本发明还包括制备这些化合物及其药物制剂的方法。

30. 发明申请

US20100190825A1 BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的BENZIMIDAZOLES及其在医学中的用途
公开(公告)号：US20100190825A1
公开(公告)日：2010-07-29
申请号：US12293572
申请日：2007-03-20
申请人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
发明人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
IPC分类号： A61K31/454 , C07D401/04 , A61P25/18 , A61P25/00
CPC分类号： C07D235/26
摘要： Compounds of formula (I) and salts and solvates are provided: whereinUses of the compounds for the treatment of psychotic disorders and cognitive mpairment, are also disclosed.
摘要翻译：提供式（I）化合物和盐和溶剂合物：其中还公开了用于治疗精神病和认知功能的化合物的用途。

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