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1. 发明申请

WO2006067423A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：WO2006067423A1
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004951
申请日：2005-12-21
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , JAXA-CHAMIEC, Albert, Andrzej , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , JAXA-CHAMIEC, Albert, Andrzej , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07C233/78 , A61K31/166 , C07C211/36
CPC分类号： C07C233/78 , C07C235/50 , C07C235/60 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/20 , C07D209/02 , C07D295/13 , C07D307/22
摘要： The present invention relates to compounds of formula (I), or to salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂化物，其用于制备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。本发明还包括制备这些化合物及其药物制剂的方法。

2. 发明申请

WO2006094840A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2006094840A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/002480
申请日：2006-03-09
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
IPC分类号： C07D295/18 , A61P25/00 , A61K31/495
CPC分类号： C07D295/192
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 1 , n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译：本发明提供式（I）化合物或其盐或溶剂化物：其中R 1，n，X，Y和Z如说明书中所定义，以及这些化合物的用途。该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍，包括精神分裂症。

3. 发明申请

WO2004041791A1 N-ARYL ACETYL CYCLIC AMINE DERIVATIVES AS OREXIN ANTAGONISTS 审中-公开
标题翻译： N-ARYL ACETYL循环胺衍生物作为OREXIN ANTAGONISTS
公开(公告)号：WO2004041791A1
公开(公告)日：2004-05-21
申请号：PCT/EP2003/012407
申请日：2003-11-04
申请人： GLAXO GROUP LIMITED , CHAN, Wai, Ngor , NASH, David, John , PORTER, Roderick, Alan , STEAD, Rachel, Elizabeth, Anne
发明人： CHAN, Wai, Ngor , NASH, David, John , PORTER, Roderick, Alan , STEAD, Rachel, Elizabeth, Anne
IPC分类号： C07D241/44
CPC分类号： C07D401/12 , C07D405/14
摘要： The present invention provides N -aryl acetyl cyclic amine derivatives which are non-peptide antagonists of human orexin receptors, in particular orexin-1 receptors. In particular, theses compounds are of potential use in the treatment of obesity, including obesity observed in Type 2 (non-insulin-dependent) diabetes patients, and/or sleep disorders. Additionally these compounds are useful in the treatment of stroke, particularly ischemic or haemorrhagic stroke, and/or blocking the emetic response, i.e. useful in the treatment of nausea and vomiting. (I) wherein: Y represents a bond, oxygen, NQ or a group (CH 2 ) n , wherein n represents 1, 2 or 3 m is 0 or 1; X is NR, wherein R is H or (C 1-4 )alkyl; Q is H or (C 1-4 )alkyl; Ar 1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar 2 represents optionally substituted phenyl, an optionally substituted 5- or 6- membered heterocyclyl group containing up to 4 heteroatoms selected from N, O and S, or an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 4 heteroatoms selected from N, O and S; R 1 and R 2 independently represent hydrogen, optionally substituted amino, optionally substituted (C 1-6 )alkyl or optionally substituted phenyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供作为人食欲素受体的非肽拮抗剂的N-芳基乙酰基环胺衍生物，特别是食欲素-1受体。特别地，这些化合物可用于治疗肥胖症，包括在2型（非胰岛素依赖性）糖尿病患者中观察到的肥胖症和/或睡眠障碍。另外，这些化合物可用于治疗中风，特别是缺血性或出血性中风，和/或阻断催吐反应，即可用于治疗恶心和呕吐。（I）其中：Y表示键，氧，NQ或基团（CH 2）n，其中n表示1,2或3m为0或1; X是NR，其中R是H或（C 1-4）烷基; Q是H或（C 1-4）烷基; Ar 1是芳基或含有至多4个选自N，O和S的杂原子的单或双环杂芳基; 任何一个可以任选地被取代; Ar 2表示任选取代的苯基，任选取代的含有至多4个选自N，O和S的杂原子的5-或6-元杂环基，或含有至多4个选自以下的杂原子的任选取代的双环芳族或双环杂芳族基团： N，O和S; R 1和R 2独立地表示氢，任选取代的氨基，任选取代的（C 1-6）烷基或任选取代的苯基; 或其药学上可接受的盐。

4. 发明申请

WO2009053449A1 THIAZOLES WHICH POTENTIATE AMPA RECEPTOR AND MEDICINAL USES THEREOF 审中-公开
标题翻译：潜在的AMPA受体的THIAZOLES及其药物用途
公开(公告)号：WO2009053449A1
公开(公告)日：2009-04-30
申请号：PCT/EP2008/064408
申请日：2008-10-24
申请人： GLAXO GROUP LIMITED , CHAN, Wai, Ngor , THEWLIS, Kevin, Michael , WARD, Simon, E.
发明人： CHAN, Wai, Ngor , THEWLIS, Kevin, Michael , WARD, Simon, E.
IPC分类号： C07D277/42 , C07D417/12 , A61K31/426 , A61K31/44 , A61P25/18
CPC分类号： C07D277/42 , C07D417/12
摘要： The invention provides compounds of formula (I) and salts thereof: wherein R1, R2, R3, R4 and X are as defined in the description. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：本发明提供式（I）化合物及其盐：其中R1，R2，R3，R4和X如说明书中所定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

5. 发明申请

WO2007107539A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：WO2007107539A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/052568
申请日：2007-03-19
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , HARRISON, Stephen , THATCHER, Robert , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , HARRISON, Stephen , THATCHER, Robert , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07D231/56 , C07D401/10 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D417/10 , A61K31/416 , A61P25/00
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 and solvates are provided: formula (I). Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物和盐和溶剂化物：式（I）。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

6. 发明申请

WO2009080637A1 COMPOUNDS WHICH POTENTIATE THE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：可能拮抗AMPA受体的化合物及其在医药中的应用
公开(公告)号：WO2009080637A1
公开(公告)日：2009-07-02
申请号：PCT/EP2008/067681
申请日：2008-12-17
申请人： GLAXO GROUP LIMITED , BERTHELEME, Nicolas , CHAN, Wai, Ngor , SCOTT, Jaqueline, Sandra , WARD, Simon, E.
发明人： BERTHELEME, Nicolas , CHAN, Wai, Ngor , SCOTT, Jaqueline, Sandra , WARD, Simon, E.
IPC分类号： C07C311/08 , C07D213/30 , C07D213/65 , C07D213/643 , A61K31/18 , A61K31/44 , A61P25/18
CPC分类号： C07C311/08 , C07C2602/08 , C07D213/30 , C07D213/643 , C07D213/65
摘要： Compounds of formula (I) and salts thereof are provided: wherein n is 0, 1, 2 or 3; R 1 is selected from phenyl and pyridyl, each of which is optionally substituted by one or two groups independently selected from C 1-4 alkyl and halogen; and R 2 is selected from H and CH 3 when n is 1 and R 2 is H when n is 2 or 3. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物及其盐：其中n为0,1,2或3; R 1选自苯基和吡啶基，其各自任选被一个或两个独立地选自C 1-4烷基和卤素的基团取代; 当n为1时，R 2选自H和CH 3，当n为2或3时，R 2为H。制备方法，药物组合物及其作为药物的用途，例如用于治疗由还公开了谷氨酸受体功能的降低或不平衡，例如精神分裂症或认知障碍。

7. 发明申请

WO2008110566A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：WO2008110566A1
公开(公告)日：2008-09-18
申请号：PCT/EP2008/052906
申请日：2008-03-12
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , HARRISON, Stephen, Anthony , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , HARRISON, Stephen, Anthony , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07D231/56 , C07D401/04 , C07D401/14 , C07D403/10 , C07D417/10 , A61K31/416 , A61P25/00
CPC分类号： C07D231/56 , C07D401/04 , C07D401/14 , C07D403/10 , C07D417/10
摘要： A compound of formula (I) and salts thereof are provided: wherein A is defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物及其盐：其中A在说明书中定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

8. 发明申请

WO2006067417A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：WO2006067417A1
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004943
申请日：2005-12-21
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07C233/78 , A61K31/166 , C07C211/27
CPC分类号： C07C235/60 , C07C211/27 , C07C233/78 , C07C235/50 , C07C323/62
摘要： The present invention relates to compounds of Formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂合物，它们在制备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中的用途。本发明还包括制备这些化合物及其药物制剂的方法。

9. 发明申请

WO2009053448A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：WO2009053448A1
公开(公告)日：2009-04-30
申请号：PCT/EP2008/064407
申请日：2008-10-24
申请人： GLAXO GROUP LIMITED , CHAN, Wai, Ngor , HARRISON, Stephen , HUGHES, Owen, Rhys , NEESOM, James, Kenneth , THEWLIS, Kevin, Michael , WARD, Simon, E
发明人： CHAN, Wai, Ngor , HARRISON, Stephen , HUGHES, Owen, Rhys , NEESOM, James, Kenneth , THEWLIS, Kevin, Michael , WARD, Simon, E
IPC分类号： C07D263/48 , C07D417/12 , A61K31/427 , A61P25/00
CPC分类号： C07D277/42 , C07D417/12 , C07D491/052
摘要： The invention provides compounds of formula (I) and salts thereof wherein R1, R2, R3, R4 and X are as defined in the description. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：本发明提供式（I）化合物及其盐，其中R 1，R 2，R 3，R 4和X如说明书中所定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

10. 发明申请

WO2008148836A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：WO2008148836A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/056971
申请日：2008-06-05
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , WARD, Simon, E.
发明人： BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , WARD, Simon, E.
IPC分类号： C07D403/10 , A61K31/416 , A61P25/00 , C07D231/12
CPC分类号： C07D403/10 , C07D231/12
摘要： Compound of formula (I) and salts thereof are provided: Wherein R 1 , R 2 , R 4 and R 5 are as defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物及其盐：其中R1，R2，R4和R5如说明书中所定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

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