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11. 发明授权

US06730681B2 Triazolo-pyrimidine derivatives as ligands for gaba receptors 失效
标题翻译：三唑并嘧啶衍生物作为gaba受体的配体
公开(公告)号：US06730681B2
公开(公告)日：2004-05-04
申请号：US10149851
申请日：2002-06-14
申请人： Mark Stuart Chambers , Ian James Collins , Simon Charles Goodacre , David James Hallett , Philip Jones , Linda Elizabeth Keown , Robert James Maxey , Leslie Joseph Street
发明人： Mark Stuart Chambers , Ian James Collins , Simon Charles Goodacre , David James Hallett , Philip Jones , Linda Elizabeth Keown , Robert James Maxey , Leslie Joseph Street
IPC分类号： A61K31519
CPC分类号： C07D487/04
摘要： A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
摘要翻译：一类取代或6,7环稠合的[1,2,3]三唑并[1,5-a]嘧啶衍生物，其在3-位上具有任选取代的环烷基，苯基或杂芳基取代基，氨基部分 5位是GABA A受体的选择性配体，特别是对其α2和/或α3亚基具有高亲和力，因此有益于治疗和/或预防中枢神经系统疾病，包括焦虑和抽搐

12. 发明授权

US07485640B2 Imidazopyrazinones as GABA-A receptor anxiolytics 失效
标题翻译：咪唑并吡嗪酮作为GABA-A受体抗焦虑药
公开(公告)号：US07485640B2
公开(公告)日：2009-02-03
申请号：US10533152
申请日：2003-10-29
申请人： William Robert Carling , Jose Luis Castro Pineiro , Simon Charles Goodacre , David James Hallett , Leslie Joseph Street
发明人： William Robert Carling , Jose Luis Castro Pineiro , Simon Charles Goodacre , David James Hallett , Leslie Joseph Street
IPC分类号： A01N43/64 , A01N43/90 , A61K31/53 , A61K31/519 , C07D253/08 , C07D487/00
CPC分类号： C07D487/04
摘要： The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein —U—V— represents —CH═CH—, or —CH2—CH2—, —N═CH— or —CH═N—; X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— or —OCH2— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, —SO2Ra, —SO2NRaRb, —CORa, —CO2Ra or —CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.
摘要翻译：本发明公开了式I化合物或其药学上可接受的盐：（I）其中-U-V-表示-CH-CH-或-CH 2 -CH 2 - ， - N-CH-或-CH-N-; X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6烷氧基; X2表示氢或卤素; Y代表化学键，氧原子或-NH-或-OCH2-键; Z表示任选取代的芳基或杂芳基; R1表示烃，杂环基，三氟甲基，-SO2Ra，-SO2NRaRb，-CORa，-CO2Ra或-CONRaRb; 并且R a和R b独立地表示氢，烃或杂环基; 包含它的药物组合物; 其用于治疗方法; 在制备用于治疗和/或预防焦虑的药物中的用途; 惊厥或认知障碍; 和使用它的治疗方法。

13. 发明授权

US06914063B2 Imidazo-pyrazine derivatives as ligands for GABA receptors 失效
标题翻译：咪唑并吡嗪衍生物作为GABA受体的配体
公开(公告)号：US06914063B2
公开(公告)日：2005-07-05
申请号：US10333964
申请日：2001-07-18
申请人： Simon Charles Goodacre , David James Hallett , Leslie Joseph Street
发明人： Simon Charles Goodacre , David James Hallett , Leslie Joseph Street
IPC分类号： A61K31/4985 , A61P25/08 , A61P25/22 , A61P25/28 , C07B61/00 , C07D487/04 , A61P25/06
CPC分类号： C07D487/04
摘要： A class of imidazo[1,2-α]pyrazine analogues substituted in the 3-position by a substituted phenyl ring, being selective ligands for GABAA receptors which interact more favourably with the α2 and/or α3 subunit than with the α1 subunit, are accordingly of benefit in the treatment and/or prevention of a variety of disorders of the central nervous system, including anxiety and convulsions, with a reduced propensity to cause sedation.
摘要翻译：通过取代的苯环在3-位上被取代的一类咪唑并[1,2-α]吡嗪类似物，是与α2和/或α3相互作用更好的GABA A A受体的选择性配体亚单位与α1亚基相比，因此在治疗和/或预防中枢神经系统的各种障碍（包括焦虑和惊厥）中具有降低的引起镇静倾向的益处。

14. 发明申请

US20110201589A1 NEW BRADYKININ B1 ANTAGONISTS 失效
标题翻译：新BRADYKININ B1拮抗剂
公开(公告)号：US20110201589A1
公开(公告)日：2011-08-18
申请号：US13059659
申请日：2009-08-10
申请人： James Madden , David James Hallett , Alastair Parkes , Ali Raoof , Xialou Wang
发明人： James Madden , David James Hallett , Alastair Parkes , Ali Raoof , Xialou Wang
IPC分类号： A61K31/422 , C07D405/14 , A61K31/496 , C07D405/12 , A61K31/4178 , A61K31/4525 , A61K31/4025 , A61K31/506 , A61K31/443 , A61K31/551 , C07D413/14 , A61K31/5377 , A61K31/397 , A61K31/55 , C07D413/12 , A61P3/04 , A61P3/10 , A61P29/00 , A61P1/00 , A61P17/00 , A61P17/02 , A61P19/00 , A61P11/06 , A61P11/00 , A61P37/08
CPC分类号： A61K31/551 , A61K31/397 , A61K31/4025 , A61K31/4178 , A61K31/443 , A61K31/4525 , A61K31/496 , A61K31/506 , C07D295/155 , C07D295/192 , C07D307/68 , C07D405/12 , C07D407/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
摘要翻译：本发明涉及式（I）化合物，其中R1，R1a，R1b，R2，R3和X，X1，X2，X3具有在说明书和权利要求书中引用的含义。所述化合物可用作缓激肽B1拮抗剂。本发明还涉及药物组合物，这种化合物的制备以及作为药物的生产和使用。

15. 发明授权

US08623859B2 Bradykinin B1 antagonists 失效
标题翻译：缓激肽B1拮抗剂
公开(公告)号：US08623859B2
公开(公告)日：2014-01-07
申请号：US13059659
申请日：2009-08-10
申请人： James Madden , David James Hallett , Alastair Parkes , Ali Raoof , Xiaolu Wang
发明人： James Madden , David James Hallett , Alastair Parkes , Ali Raoof , Xiaolu Wang
IPC分类号： A61K31/341 , A61K31/4523 , A61K31/4525 , A61K31/18 , C07C311/13 , C07D307/38
CPC分类号： A61K31/551 , A61K31/397 , A61K31/4025 , A61K31/4178 , A61K31/443 , A61K31/4525 , A61K31/496 , A61K31/506 , C07D295/155 , C07D295/192 , C07D307/68 , C07D405/12 , C07D407/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
摘要翻译：本发明涉及式（I）化合物，其中R1，R1a，R1b，R2，R3和X，X1，X2，X3具有在说明书和权利要求书中引用的含义。所述化合物可用作缓激肽B1拮抗剂。本发明还涉及药物组合物，这种化合物的制备以及作为药物的生产和使用。

16. 发明授权

US07226922B2 Imidazo[1,2-b]pyridazine analogues as anxiolytics and cognition enhancers 失效
标题翻译：咪唑并[1,2-b]哒嗪类似物作为抗焦虑药和认知增强剂
公开(公告)号：US07226922B2
公开(公告)日：2007-06-05
申请号：US10680855
申请日：2003-10-07
申请人： David James Hallett
发明人： David James Hallett
IPC分类号： A61K31/5025 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula I: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, —CO2Ra, —CONRaRb or —CRa═NORb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions comprising this compound and methods of treating and/or preventing anxiety and convulsions using it.
摘要翻译：本发明提供式I化合物：其中X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6 烷氧基 X 2表示氢或卤素; Y表示化学键，氧原子或-NH-键; Z表示任选取代的芳基或杂芳基; R 1表示氢，烃，杂环基，卤素，氰基，三氟甲基，硝基，-OR a，-SR a，-SOR 一个或两个以上的一个或多个，其中，R 1，R 2，R 2，其中，R a，R b，R b，R b，R b， CO 2，CO 2 R 2，...，CO 2，一个或多个，一个或多个，一个或多个，一个或多个。 R a和R b各自独立地表示氢，烃或杂环基; 包含该化合物的药物组合物和使用它的治疗和/或预防焦虑和抽搐的方法。

17. 发明授权

US06872731B2 Imidazo-pyridine derivatives as ligands for GABA receptors 失效
标题翻译：咪唑并吡啶衍生物作为GABA受体的配体
公开(公告)号：US06872731B2
公开(公告)日：2005-03-29
申请号：US10155691
申请日：2002-05-23
申请人： James Michael Crawforth , Simon Charles Goodacre , Timothy Harrison , David James Hallett , Andrew Pate Owens , Michael Rowley , Martin Richard Teall
发明人： James Michael Crawforth , Simon Charles Goodacre , Timothy Harrison , David James Hallett , Andrew Pate Owens , Michael Rowley , Martin Richard Teall
IPC分类号： A61K31/437 , A61K31/444 , A61P1/08 , A61P3/04 , A61P15/00 , A61P21/00 , A61P23/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P27/16 , A61P43/00 , C07B61/00 , C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： A class of 3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH-linkage, are selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
摘要翻译：一类3-苯基咪唑并[1,2-a]吡啶衍生物，其在苯环的间位被被氧原子或-NH-键直接连接或桥连的任选取代的芳基或杂芳基取代，是GABA A受体的选择性配体，特别是对其α2和/或α3亚基具有高亲和力，因此有益于治疗和/或预防中枢神经系统疾病，包括焦虑和抽搐。

18. 发明申请

US20110105459A1 AZETIDINES AND CYCLOBUTANES AS HISTAMINE H3 RECEPTOR ANTAGONISTS 有权
标题翻译：作为组胺H3受体拮抗剂的AZETIDINES和CYCLOBUTANES
公开(公告)号：US20110105459A1
公开(公告)日：2011-05-05
申请号：US12991225
申请日：2009-05-05
申请人： Adam James Davenport , David James Hallett , Massimo Corsi
发明人： Adam James Davenport , David James Hallett , Massimo Corsi
IPC分类号： A61K31/551 , C07D403/06 , C07D401/14 , C07D403/14 , C07D413/14 , A61P29/00 , A61P3/00 , A61P9/00 , A61P1/00 , A61P11/02 , A61P11/06 , A61P25/00
CPC分类号： C07D401/14 , C07D401/12 , C07D403/06 , C07D403/14 , C07D471/04
摘要： The invention relates to compounds of formula (I) wherein R, R0, R1, m, n and X1 to X4 have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
摘要翻译：本发明涉及其中R，R 0，R 1，m，n和X 1至X 4具有如在说明书和权利要求书中引用的含义的式（I）化合物。所述化合物可用作组胺H3受体拮抗剂。本发明还涉及药物组合物，这种化合物的制备以及作为药物的生产和使用。

19. 发明授权

US07226926B2 8-fluoroimidazo 1,2-a pyridine derivatives as ligands for GABA receptors 失效
标题翻译： 8-氟咪唑并[1,2-a]吡啶衍生物作为GABA受体的配体
公开(公告)号：US07226926B2
公开(公告)日：2007-06-05
申请号：US10515165
申请日：2003-05-23
申请人： Wesley Peter Blackaby , Jose Luis Castro Pineiro , Simon Charles Goodacre , David James Hallett , Alexander Charles Humphries , Philip Jones , Kevin John Merchant , Michael Reader
发明人： Wesley Peter Blackaby , Jose Luis Castro Pineiro , Simon Charles Goodacre , David James Hallett , Alexander Charles Humphries , Philip Jones , Kevin John Merchant , Michael Reader
IPC分类号： A61K31/437 , A61K31/506 , C07D544/294 , C07D546/121
CPC分类号： C07D471/04
摘要： A class of 8-fluoroimidazo[1,2-α]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类由任选取代的五元或六元杂芳环在3-位被取代的8-氟咪唑并[1,2-α]吡啶衍生物，是GABA A A受体的选择性配体特别是对α2和/或α3和/或α5亚基具有高亲和力，因此有益于治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

20. 发明授权

US08912176B2 Azetidines as histamine H3 receptor antagonists 有权
标题翻译：氮杂环丁烷作为组胺H3受体拮抗剂
公开(公告)号：US08912176B2
公开(公告)日：2014-12-16
申请号：US13147337
申请日：2010-01-29
申请人： Adam James Davenport , David James Hallett , Christopher Charles Stimson
发明人： Adam James Davenport , David James Hallett , Christopher Charles Stimson
IPC分类号： A61K31/551 , C07D243/08 , C07D413/14 , C07D403/14 , C07D405/14
CPC分类号： C07D403/14 , C07D405/14 , C07D413/14
摘要： The invention relates to compounds of formula (I), wherein R, R1, m, n and X1 to X3 have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
摘要翻译：本发明涉及式（I）化合物，其中R，R 1，m，n和X 1至X 3具有在说明书和权利要求书中引用的含义。所述化合物可用作组胺H3受体拮抗剂。本发明还涉及药物组合物，这种化合物的制备以及作为药物的生产和使用。

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