公开(公告)号：US07626056B2

公开(公告)日：2009-12-01

申请号：US11446735

申请日：2006-06-05

申请人： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Richard Thomas Lewis ,  Elizabeth Mary Naylor ,  Leslie Joseph Street

发明人： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Richard Thomas Lewis ,  Elizabeth Mary Naylor ,  Leslie Joseph Street

IPC分类号： C07C233/65 ,  A61K31/16

CPC分类号： C07D213/82 ,  C07C233/70 ,  C07C233/76 ,  C07C317/30 ,  C07C2601/02 ,  C07C2601/14 ,  C07D231/12 ,  C07D231/18 ,  C07D239/28 ,  C07D249/04 ,  C07D285/125 ,  C07D295/108 ,  C07D295/135 ,  C07D307/68 ,  C07D333/38 ,  C07D471/04 ,  C07D495/04

摘要： The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.

摘要翻译： 本发明提供式I化合物：其中R 1是烷基，苯基，杂环基，环烷基，烷氧基，酯，氨基或酰胺基; R2是苯基，杂环基，烷基，环烷基或环烷基烷基; R3是烷基，环烷基，环烷基烷基，氨基或杂环基; R4和R5是氢或烷基或形成环烷基环; A是O或N; m为零或一; 作为GlyT1的抑制剂，因此可用于治疗或预防精神分裂症等疾病; 提供药物组合物，第一和第二医疗用途和治疗方法。

公开(公告)号：US07030128B2

公开(公告)日：2006-04-18

申请号：US10472680

申请日：2002-03-19

申请人： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Simon Charles Goodacre ,  David James Hallett ,  Philip Jones ,  Richard Thomas Lewis ,  Angus Murray MacLeod ,  Robert James Maxey ,  Kevin William Moore ,  Leslie Joseph Street

发明人： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Simon Charles Goodacre ,  David James Hallett ,  Philip Jones ,  Richard Thomas Lewis ,  Angus Murray MacLeod ,  Robert James Maxey ,  Kevin William Moore ,  Leslie Joseph Street

IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P25/22

CPC分类号： C07D487/04 ,  A61K31/519

摘要： A class of imidazo[1,2-α]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, and 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-位上被取代的咪唑并[1,2-α]嘧啶衍生物，是GABA A A受体的选择性配体， 特别是对α2和/或α3和/或α5亚基具有良好的亲和力，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。

公开(公告)号：US07851638B2

公开(公告)日：2010-12-14

申请号：US12571904

申请日：2009-10-01

申请人： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Richard Thomas Lewis ,  Elizabeth Mary Naylor ,  Leslie Joseph Street

发明人： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Richard Thomas Lewis ,  Elizabeth Mary Naylor ,  Leslie Joseph Street

IPC分类号： C07D249/02 ,  A61K31/4192

CPC分类号： C07D213/82 ,  C07C233/70 ,  C07C233/76 ,  C07C317/30 ,  C07C2601/02 ,  C07C2601/14 ,  C07D231/12 ,  C07D231/18 ,  C07D239/28 ,  C07D249/04 ,  C07D285/125 ,  C07D295/108 ,  C07D295/135 ,  C07D307/68 ,  C07D333/38 ,  C07D471/04 ,  C07D495/04

摘要： The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.

摘要翻译： 本发明提供式I化合物：其中R 1是烷基，苯基，杂环基，环烷基，烷氧基，酯，氨基或酰胺基; R2是苯基，杂环基，烷基，环烷基或环烷基烷基; R3是烷基，环烷基，环烷基烷基，氨基或杂环基; R4和R5是氢或烷基或形成环烷基环; A是O或N; m为零或一; 作为GlyT1的抑制剂，因此可用于治疗或预防精神分裂症等疾病; 提供药物组合物，第一和第二医疗用途和治疗方法。

公开(公告)号：US06969716B2

公开(公告)日：2005-11-29

申请号：US10769070

申请日：2004-01-30

申请人： Wesley Peter Blackaby ,  Simon Charles Goodacre ,  David James Hallett ,  Andrew Jennings ,  Richard Thomas Lewis ,  Leslie Joseph Street ,  Kevin Wilson

发明人： Wesley Peter Blackaby ,  Simon Charles Goodacre ,  David James Hallett ,  Andrew Jennings ,  Richard Thomas Lewis ,  Leslie Joseph Street ,  Kevin Wilson

IPC分类号： A61K31/53 ,  C07D253/065 ,  A61P25/22

CPC分类号： A61K31/53

摘要： The present invention provides a compound of formula I, or an N-oxide thereof or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy;X2 represents hydrogen or halogen;Z represents hydrogen, halogen, cyano, cyanomethyl, trifluoromethyl, nitro, hydroxy, hydroxy(C1-6)alkyl, C1-6 alkoxy, C1-6 alkoxy(C1-6)alkyl, trifluoromethoxy, trifluoromethylthio, trifluoromethanesulfinyl, formyl, C2-6 alkoxycarbonyl, oxopyrrolidinyl, or an optionally substituted aryl, heteroaryl or heteroaryl(C1-6)alkoxy group; andR1 represents aryl or heteroaryl, either of which groups may be optionally substituted;pharmaceutical compositions comprising it, its use in therapy and methods of treatment of anxiety and/or depression using it.

摘要翻译： 本发明提供式I化合物或其N-氧化物或其药学上可接受的盐：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; Z表示氢，卤素，氰基，氰基甲基，三氟甲基，硝基，羟基，羟基（C 1-6 - ）烷基，C 1-6烷氧基，C 1 C 1-6烷氧基（C 1-6）烷基，三氟甲氧基，三氟甲硫基，三氟甲磺酰基，甲酰基，C 2-6烷氧基羰基，氧代吡咯烷基或任选取代的芳基 ，杂芳基或杂芳基（C 1-6 - ）烷氧基; 且R 1表示芳基或杂芳基，其中任一个可以任选被取代; 包含它的药物组合物，其在治疗中的用途以及使用其治疗焦虑和/或抑郁症的方法。

公开(公告)号：US20100029726A1

公开(公告)日：2010-02-04

申请号：US12571904

申请日：2009-10-01

申请人： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Richard Thomas Lewis ,  Elizabeth Mary Naylor ,  Leslie Joseph Street

发明人： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Richard Thomas Lewis ,  Elizabeth Mary Naylor ,  Leslie Joseph Street

IPC分类号： A61K31/4192 ,  C07D249/04 ,  A61K31/16 ,  C07C233/00

CPC分类号： C07D213/82 ,  C07C233/70 ,  C07C233/76 ,  C07C317/30 ,  C07C2601/02 ,  C07C2601/14 ,  C07D231/12 ,  C07D231/18 ,  C07D239/28 ,  C07D249/04 ,  C07D285/125 ,  C07D295/108 ,  C07D295/135 ,  C07D307/68 ,  C07D333/38 ,  C07D471/04 ,  C07D495/04

摘要： The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.

摘要翻译： 本发明提供式I化合物：其中R 1是烷基，苯基，杂环基，环烷基，烷氧基，酯，氨基或酰胺基; R2是苯基，杂环基，烷基，环烷基或环烷基烷基; R3是烷基，环烷基，环烷基烷基，氨基或杂环基; R4和R5是氢或烷基或形成环烷基环; A是O或N; m为零或一; 作为GlyT1的抑制剂，因此可用于治疗或预防精神分裂症等疾病; 提供药物组合物，第一和第二医疗用途和治疗方法。

公开(公告)号：US06730676B2

公开(公告)日：2004-05-04

申请号：US10168234

申请日：2002-06-18

申请人： Wesley Peter Blackaby ,  Richard Thomas Lewis ,  Leslie Joseph Street

发明人： Wesley Peter Blackaby ,  Richard Thomas Lewis ,  Leslie Joseph Street

IPC分类号： C07D48704

CPC分类号： C07D487/04

摘要： A class of pyrazino[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 5-position, a substituted alkoxy moiety at the 3-position, and a range of substituents at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and 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： 一类吡嗪并[2,3-d]哒嗪衍生物，其在5-位上具有任选取代的环烷基，苯基或杂芳基取代基，3-位上的取代烷氧基部分和2-位上的取代基范围 是用于GABA 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良状况，包括焦虑 抽搐和认知障碍。