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1. 发明申请

WO2008092888A1 1-OXA-3-AZASPIRO[4,5]DECAN--2-ONE DERIVATIVES FOR THE TREATMENT OF EATING DISORDERS 审中-公开
标题翻译： 1-OXA-3-AZASPIRO [4,5] DECAN - 用于治疗排卵障碍的2-ONE衍生物
公开(公告)号：WO2008092888A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/051111
申请日：2008-01-30
申请人： GLAXO GROUP LIMITED , BENTLEY, Jonathan , BIAGETTI, Matteo , DI FABIO, Romano , GENSKI, Thorsten , GUERY, Sebastien , KOPF, Silvia, Rosalia , LESLIE, Colin, Philip , MAZZALI, Angelica , MELOTTO, Sergio , PIZZI, Domenica, Antonia , SABBATINI, Fabio, Maria , SERI, Catia
发明人： BENTLEY, Jonathan , BIAGETTI, Matteo , DI FABIO, Romano , GENSKI, Thorsten , GUERY, Sebastien , KOPF, Silvia, Rosalia , LESLIE, Colin, Philip , MAZZALI, Angelica , MELOTTO, Sergio , PIZZI, Domenica, Antonia , SABBATINI, Fabio, Maria , SERI, Catia
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , A61K31/423 , A61P3/00 , A61P25/00
CPC分类号： C07D413/14
摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; Z 1 is H, C1-C4 alkyl or F; Z is CH 2 , CH(C1-C4 alkyl), C(C1-C4 alkyl) 2 or a bond; A is a 5 membered heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; B is hydrogen or is a 5-6 membered heteroaryl, or phenyl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; being A and B linked via any atom; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
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R是芳基或杂芳基; 其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; Z 1是H，C 1 -C 4烷基或F; Z是CH 2，CH（C 1 -C 4烷基），C（C 1 -C 4烷基）2或键; A是5元杂芳基，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; B是氢或是5-6元杂芳基，或苯基，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 是通过任何原子连接的A和B; 它们的制备方法，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，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如暴饮暴食症的药剂。

2. 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。

3. 发明申请

WO2008129007A1 BENZIMIDAZOLES WITH A HETERO SPIRO-DECANE RESIDUE AS NPY-Y5 ANTAGONISTS 审中-公开
标题翻译：具有异戊二烯残基的苯并咪唑作为NPY-Y5拮抗剂
公开(公告)号：WO2008129007A1
公开(公告)日：2008-10-30
申请号：PCT/EP2008/054757
申请日：2008-04-18
申请人： GLAXO GROUP LIMITED , BARTON, Nick , BELLENIE, Ben , BENTLEY, Jonathan , BIAGETTI, Matteo , GENSKI, Thorsten , LESLIE, Colin, Philip , MAZZALI, Angelica , PIZZI, Domenica, Antonia , SABBATINI, Fabio, Maria , SERI, Catia
发明人： BARTON, Nick , BELLENIE, Ben , BENTLEY, Jonathan , BIAGETTI, Matteo , GENSKI, Thorsten , LESLIE, Colin, Philip , MAZZALI, Angelica , PIZZI, Domenica, Antonia , SABBATINI, Fabio, Maria , SERI, Catia
IPC分类号： C07D221/20 , C07D471/10 , C07D471/20
CPC分类号： C07D498/10 , C07D221/20 , C07D403/04 , C07D413/04 , C07D413/14 , C07D471/04
摘要： The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts, solvates, stereoisomers thereof, formula (I), R 1 may be C 1 -C 4 alkyl, aryl or heteroaryl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; R 2 may be halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano, nitro; or aryl, heteroaryl or heterocycle, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; or R 2 may correspond to -0-R 3 ; R 3 is a 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen X is carbon or oxygen; Z is carbon or nitrogen; G is a fused 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen; m may be 0 or an integer ranging from 1 to 4; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY- Y5 receptor antagonists.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物，其立体异构体，式（I），R 1可以是C 1 -C 可以被一个或多个取代基取代的烷基，芳基或杂芳基：卤素，C 1 -C 4烷基，C 1 -C 4烷基， C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 3烷基，C 1 -C 4烷基，C 1 -C 4烷基，卤代烷氧基，氰基; R 2可以是卤素，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基， C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基，硝基 ; 或芳基，杂芳基或杂环，其可被一个或多个取代基取代：卤素，C 1 -C 4烷基，C 1 -C C 1-4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4烷基，C 1 -C 4烷基，卤代烷氧基，氰基; 或R 2可以对应于-O-R 3; R 3是6元芳族碳环，其可以含有1或2个氮，X是碳或氧; Z是碳或氮; G是稠合的6元芳族碳环，其可以含有1或2个氮; m可以是0或1至4的整数; 作为其制备方法，在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，作为NPY-Y5受体拮抗剂。

4. 发明申请

WO1998007704A1 TETRAHYDROQUINOLINE DERIVATIVES AS EAA ANTAGONISTS 审中-公开
标题翻译：四氢喹啉衍生物作为EAA拮抗剂
公开(公告)号：WO1998007704A1
公开(公告)日：1998-02-26
申请号：PCT/EP1997004440
申请日：1997-08-14
申请人： GLAXO WELLCOME S.P.A. , DI-FABIO, Romano , PASQUARELLO, Alessandra , SABBATINI, Fabio, Maria
发明人： GLAXO WELLCOME S.P.A.
IPC分类号： C07D215/48
CPC分类号： C07D215/48
摘要： Compounds of formula (I) or a salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO2R2 or COR2 wherein R2 represents hydroxy, methoxy, amino, alkylamino or dialkylamino; m is zero or an integer 1 or 2; R1 represents a group (CH2)nCN, -CH=CHR3, (CH2)nNHCOCH2R4 or O(CH2)pNR5R6; R3 represents cyano or the group COR7; R4 represents alkoxy or a group NHCOR8; R5 and R6 each represent independently hydrogen or alkyl, or R5 and R6 together with the nitrogen atom to which they are attached represent a heterocyclic group, or R5 is hydrogen and R6 is the group COR9; R7 represents an alkoxy, amino or hydroxyl group; R8 represents a hydrogen atom or optionally substituted alkyl, alkoxy, aryl or heterocyclic group; R9 is the group R8 or the group NR10R11 wherein R10 represents hydrogen or alkyl group; R11 represents optionally substituted alkyl, aryl, heterocyclic or cycloalkyl group; n is zero or an integer from 1 to 4; p is an integer from 2 to 4, processes for their preparation and to their use in medicine.
摘要翻译：式（I）化合物或其盐或其代谢不稳定的酯，其中R表示选自卤素，烷基，烷氧基，氨基，烷基氨基，二烷基氨基，羟基，三氟甲基，三氟甲氧基，硝基，氰基，SO2R2或COR2的基团，其中R2表示羟基，甲氧基，氨基，烷基氨基或二烷基氨基; m为零或整数1或2; R1表示基团（CH2）nCN，-CH = CHR3，（CH2）nNHCOCH2R4或O（CH2）pNR5R6; R3代表氰基或基团COR7; R4表示烷氧基或NHCOR8基团; R 5和R 6各自独立地表示氢或烷基，或者R 5和R 6与它们所连接的氮原子一起代表杂环基，或R5是氢，R6是基团COR9; R7表示烷氧基，氨基或羟基; R8表示氢原子或任选取代的烷基，烷氧基，芳基或杂环基团; R9为基团R8或基团NR10R11，其中R10表示氢或烷基; R11表示任选取代的烷基，芳基，杂环或环烷基; n为0或1至4的整数; p是2至4的整数，其制备方法及其在医学中的应用。

5. 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。

6. 发明申请

WO2011151361A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2011151361A1
公开(公告)日：2011-12-08
申请号：PCT/EP2011/059011
申请日：2011-06-01
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , CREMONESI, Susanna , GARZYA, Vincenzo , MICHELI, Fabrizio , RUPCIC, Renata , SABBATINI, Fabio Maria
发明人： BERTANI, Barbara , CREMONESI, Susanna , GARZYA, Vincenzo , MICHELI, Fabrizio , RUPCIC, Renata , SABBATINI, Fabio Maria
IPC分类号： C07D513/04 , A61K31/542 , A61P25/00
CPC分类号： C07D513/04
摘要： The invention relates to tricyclic derivatives, and their use in treating diseases and conditions mediated by antagonism of the mGluR 5 receptor, in particular substance related disorders. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及三环衍生物及其在治疗由mGluR5受体的拮抗作用介导的疾病和病症中的用途，特别是与物质有关的疾病。此外，本发明涉及含有衍生物的组合物及其制备方法。

7. 发明申请

WO2009095377A1 SPIRO COMPOUNDS AS NPY Y5 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： SPIRO化合物作为NPY Y5受体拮抗剂
公开(公告)号：WO2009095377A1
公开(公告)日：2009-08-06
申请号：PCT/EP2009/050867
申请日：2009-01-27
申请人： GLAXO GROUP LIMITED , BIAGETTI, Matteo , CONTINI, Stefania Anne , GENSKI, Thorsten , GUERY, Sebastien , LESLIE, Colin Philip , MAZZALI, Angelica , PIZZI, Domenica Antonia , SABBATINI, Fabio Maria , SERI, Catia
发明人： BIAGETTI, Matteo , CONTINI, Stefania Anne , GENSKI, Thorsten , GUERY, Sebastien , LESLIE, Colin Philip , MAZZALI, Angelica , PIZZI, Domenica Antonia , SABBATINI, Fabio Maria , SERI, Catia
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , A61K31/423 , A61P3/00
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, (I) wherein R is an aryl or heteroaryl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; Z 1 is H, C 1 -C 4 alkyl or F; Z is CH 2 , CH(C 1 -C 4 alkyl), C(C 1 -C 4 alkyl)2 or a bond; A is a 6-10 membered aryl or heteroaryl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; or -C(=O)-X; or O(CH 2 ) 0-1 R 1 ; B is hydrogen or is a 5-6 membered heteroaryl, or a 4-6 membered heterocycle, or phenyl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, hydroxyl, cyano; A and B being linked via any atom; R 1 is -(C 1 -C 4 )alkyl(C 1 -C 4 )alkoxy; or C 3 -C 8 cycloalkyl; or R 1 is an aryl or heteroaryl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; or R 1 is a 4-6 membered heterocycle, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; X is OR 2 or NR 3 R 4 ; R 2 is C 1 -C 4 alkyl; R 3 is hydrogen or together with R 4 and the nitrogen form a 5-6 saturated membered ring; R 4 is C 3 -C 8 cycloalkyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
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，其中R是芳基或杂芳基，其可被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4 烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; Z 1是H，C 1 -C 4烷基或F; Z是CH 2，CH（C 1 -C 4烷基），C（C 1 -C 4烷基）2或键; A是6-10元芳基或杂芳基，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 或-C（= O）-X; 或O（CH 2）0-1R1; B是氢或是5-6元杂芳基或4-6元杂环，或苯基，其可被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C4卤代烷氧基，羟基，氰基; A和B通过任何原子相连; R1是 - （C1-C4）烷基（C1-C4）烷氧基; 或C 3 -C 8环烷基; 或者R 1是可被一个或多个卤素取代的芳基或杂芳基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 或R 1是4-6元杂环，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; X为OR2或NR3R4; R2是C1-C4烷基; R3是氢或与R4一起形成5-6饱和的元环; R4是C3-C8环烷基; 它们的制备方法，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，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。

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