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1. 发明申请

WO2008148853A1 N-PHENYL HYDRAZIDES AS MODULATORS OF THE GHRELIN RECEPTOR 审中-公开
标题翻译：作为GHRELIN受体的调节剂的N-苯基水杨酸
公开(公告)号：WO2008148853A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057018
申请日：2008-06-05
申请人： GLAXO GROUP LIMITED , BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
发明人： BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
IPC分类号： C07D213/54 , C07D239/26 , C07D307/79 , C07D307/85 , C07D307/91 , C07D317/46 , C07D317/60 , C07D319/18 , C07D333/72 , C07D333/76 , C07D405/06 , C07D471/04 , C07D487/04 , C07D295/15 , A61K31/498
CPC分类号： C07D333/76 , C07D211/34 , C07D213/56 , C07D213/61 , C07D239/26 , C07D295/15 , C07D307/81 , C07D307/85 , C07D307/91 , C07D317/46 , C07D317/60 , C07D319/18 , C07D333/60 , C07D405/06 , C07D471/04 , C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: each R 1 is independently selected from the group consisting of Cl, Br, CH 3 and CF 3 ; X is carbon or nitrogen; R 1a is H or a straight C 1-3 alkyl group; R 2a is H or a methyl group R 2 is selected from the group consisting of C 1-3 alkyl, H and -(CH 2 ) n -, wherein n is 3 or 4 and the terminal carbon of the chain is bonded to the carbon atom adjacent to the nitrogen bearing the R 2 group, such that a fused 6,5 or 6,6-bicyclic ring is formed. Y is selected from the group consisting of: phenyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of C 1-3 alkyl, C 1-3 alkoxy, halogen, C 1-3 alkyl substituted by 1 to 7 fluoro atoms and C 1-3 alkoxy substituted by 1 to 7 fluoro atoms; pyridyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of C 1-3 alkyl, OCH 3 , CF 3 , CN, and halogen; naphthyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of F and OCH 3 ; pyrimidinyl; imidazo[1,2-a]pyridine-6-yl; benzothiophen-2-yl; benzothiophen-5-yl; benzofuran-2-yl; dibenzo[b,d]furan-3-yl; dibenzo[b,d]thiophen-2-yl; dibenzo[b,d]thiophen-4-yl; 1,3- benzodioxol-5-yl; 2,3-dihydro-1,4-benzodioxin-5-yl; 2,3-dihydro-1,4-benzodioxin-6-yl; 2,3- dihydro-1-benzofuran-4-yl; 2,2-difluoro-1,3-benzodiox-4-yl; pyridazinyl; imidazolyl; oxazolyl; pyrazolyl; thiazolyl; and triazolyl; with the proviso that when Y is 2,3-dihydro-1,4-benzodioxin-6-yl, R 1 is not Cl; processes for their preparation, intermediates useble in these processes, pharmaceutical compositions containing them and their use in therapy, for example as modulators of of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂化物，其中：每个R 1独立地选自Cl，Br，CH 3和CF 3; X是碳或氮; R 1a是H或直链C 1-3烷基; R2a是H或甲基R2选自C1-3烷基，H和 - （CH2）n-，其中n是3或4，并且该链的末端碳键合到邻近的碳原子上含有R2基团的氮，使得形成稠合的6,5或6,6-双环。 Y选自：可以是未取代的或被一个或多个独立地选自C 1-3烷基，C 1-3烷氧基，卤素，被1至7个氟原子取代的C 1-3烷基和C 1 由1-7个氟原子取代的3-烷氧基; 吡啶基，其可以是未取代的或被一个或多个独立地选自C 1-3烷基，OCH 3，CF 3，CN和卤素的取代基取代; 萘基，其可以是未取代的或被一个或多个独立地选自F和OCH 3的取代基取代; 嘧啶; 咪唑并[1,2-a]吡啶-6-基; 苯并噻吩-2-基; 苯并噻吩-5-基; 苯并呋喃-2-基; 二苯并[b，d]呋喃-3-基; 二苯并[b，D]噻吩-2-基; 二苯并[b，D]噻吩-4-基; 1,3-苯并间二氧杂环戊烯-5-基; 2,3-二氢-1,4-苯并二恶英-5-基; 2,3-二氢-1,4-苯并二恶英-6-基; 2,3-二氢-1-苯并呋喃-4-基; 2,2-二氟-1,3- benzodiox -4-基; 哒嗪; 咪唑; 恶唑; 吡唑; 噻唑基; 和三唑基; 条件是当Y是2,3-二氢-1,4-苯并二恶英-6-基时，R 1不是Cl; 其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，例如作为生长激素促分泌素受体（也称为生长素释放肽受体或GHSR1a受体）的调节剂和/或用于治疗和/或预防由生长素释放肽受体介导的病症。

2. 发明申请

WO2008022994A1 USE OF AZABICYCLO HEXANE DERIVATIVES 审中-公开
标题翻译：使用异丁醇衍生物衍生物
公开(公告)号：WO2008022994A1
公开(公告)日：2008-02-28
申请号：PCT/EP2007/058636
申请日：2007-08-20
申请人： GLAXO GROUP LIMITED , ANDERTON, Clare Louise , BACCHI, Sergio , BEATO, Stefania , SARTOR, Franco
发明人： ANDERTON, Clare Louise , BACCHI, Sergio , BEATO, Stefania , SARTOR, Franco
IPC分类号： A61K31/403
CPC分类号： C07D413/14
摘要： The present invention relates to the tartrate salt of 1-[2-fluoro-4-(trifluoromethyl)phenyl]-3-(3-{[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4 H -1,2,4-triazol-3-yl]thio}propyl)-3-azabicyclo[3.1.0]-hexane and solvates thereof, pharmaceutical formulations, processes for their preparation, and their use in medicine.
摘要翻译：本发明涉及1- [2-氟-4-（三氟甲基）苯基] -3-（3 - {[4-甲基-5-（4-甲基-1,3-恶唑-5-基）吡啶-2-基）-4H-1,2,4-三唑-3-基]硫基}丙基）-3-氮杂双环[3.1.0] - 己烷及其溶剂合物，药物制剂，其制备方法及其在医药中的应用。

3. 发明申请

WO2008148854A1 GHRELIN MODULATORS 审中-公开
标题翻译： GHRELIN调制器
公开(公告)号：WO2008148854A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057019
申请日：2008-06-05
申请人： GLAXO GROUP LIMITED , BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
发明人： BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
IPC分类号： C07D401/06
CPC分类号： C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes for their preparation, intermediates useble in these processes, pharmaceutical compositions containing them and their use in therapy, for example as modulators of of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂化物，其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，例如作为生长调节剂激素促分泌素受体（也称为生长素释放肽受体或GHSR1a受体）和/或用于治疗和/或预防由生长素释放肽受体介导的病症。

4. 发明申请

WO2008031771A3 3-AZABICYCLO [4. 1. 0] HEPTANE DERIVATIVES FOR THE TREATMENT OF DEPRESSION 审中-公开
公开(公告)号：WO2008031771A3
公开(公告)日：2008-03-20
申请号：PCT/EP2007/059380
申请日：2007-09-07
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： A61K31/435 , A61P25/24 , C07D221/04
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof: formula (I), wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; such G may be substituted by (R 2 ) p , which can be the same or different; R 1 is hydrogen or C 1-4 alkyl; R 2 is halogen, hydroxy, cyano,C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to R 8 ; R 5 is hydrogen or C 1-4 alkyl; R 6 is hydrogen or C 1-4 alkyl; R 7 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to X, X 1 , X 2 or X 3 ; wherein X corresponds to: formula (a) X 1 corresponds to: formula (b) X 2 corresponds to: formula (c) X 3 corresponds to: formula (d) R 3 is hydrogen or C 1-4 alkyl; or corresponds to X or X 1 ; R 4 is hydrogen or C 1-4 alkyl; or corresponds to X or X 1 ; R 8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents selected from a group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy and C 1-4 alkanoyl; R 9 is C 1-4 alkyl; R 10 is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl or C 3-6 cycloalkylC 1-3 alkyl; R 11 is haloC 1-2 alkyl; p is an integer from 0 to 5; n is 1 or 2. processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

5. 发明申请

WO2008148856A1 N- ( (3, 5-DICHLOROPHENYL) METHYL) -2- U-METHYL-1-PIPERAZINYL) -2- ( 1-NAPHTALENYL) ETHAN AMIDE AS GHRELIN RECEPTOR MODULATOR 审中-公开
标题翻译：作为GHRELIN受体调节剂的N-（（3,5-二氯苯基）甲基）-2-（N-甲基-1-哌啶子基）-2-（1-硝基苯基）乙酰胺
公开(公告)号：WO2008148856A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057021
申请日：2008-06-05
申请人： GLAXO GROUP LIMITED , HEIGHTMAN, Thomas Daniel
发明人： HEIGHTMAN, Thomas Daniel
IPC分类号： C07D295/104
CPC分类号： C07D295/15
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes for their preparation, intermediates useble in these processes, pharmaceutical compositions containing them and their use in therapy, for example as modulators of of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂化物，其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，例如作为生长调节剂激素促分泌素受体（也称为生长素释放肽受体或GHSR1a受体）和/或用于治疗和/或预防由生长素释放肽受体介导的病症。

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