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1. 发明申请

WO2006077025A3 MORPHOLINES AS 5HT2C AGONISTS 审中-公开
标题翻译：吗啡啉作为5HT2C激动剂
公开(公告)号：WO2006077025A3
公开(公告)日：2006-09-08
申请号：PCT/EP2006000126
申请日：2006-01-10
申请人： HOFFMANN LA ROCHE , VERNALIS RES LTD , BENTLEY JONATHAN MARK , DAWSON CLAIRE ELIZABETH , GUBA WOLFGANG , HEBEISEN PAUL , MONCK NATHANIEL , PRATT ROBERT MARK , RICHTER HANS , ROEVER STEPHAN , RUSTON VICKI
发明人： BENTLEY JONATHAN MARK , DAWSON CLAIRE ELIZABETH , GUBA WOLFGANG , HEBEISEN PAUL , MONCK NATHANIEL , PRATT ROBERT MARK , RICHTER HANS , ROEVER STEPHAN , RUSTON VICKI
IPC分类号： C07D265/30 , A61K31/5375 , A61P3/04 , A61P3/10
CPC分类号： C07D265/30
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.
摘要翻译：本发明涉及式（I）的化学化合物及其药学上可接受的盐和酯，其中R 1至R 5具有权利要求1中给出的含义。这些化合物可以用于制备药物。

2. 发明申请

WO2006024517A1 FUSED TRICYCLIC DERIVATIVES FOR THE TREATMENT OF PSYCHOTIC DISORDERS 审中-公开
标题翻译：用于治疗心理障碍的融合三聚体衍生物
公开(公告)号：WO2006024517A1
公开(公告)日：2006-03-09
申请号：PCT/EP2005/009379
申请日：2005-08-29
申请人： GLAXO GROUP LIMITED , BENTLEY, Jonathan , BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BORRIELLO, Manuela , BROMIDGE, Steven, Mark , GIANOTTI, Massimo , GRANCI, Enrica , LESLIE, Colin, Philip , PASQUARELLO, Alessandra , ZUCCHELLI, Valeria
发明人： BENTLEY, Jonathan , BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BORRIELLO, Manuela , BROMIDGE, Steven, Mark , GIANOTTI, Massimo , GRANCI, Enrica , LESLIE, Colin, Philip , PASQUARELLO, Alessandra , ZUCCHELLI, Valeria
IPC分类号： C07D498/04
CPC分类号： C07D471/04
摘要： Compounds of formula (I) wherein R 1 , R 2 , X, A, Y, B, Z 1 , Q, p, r and s are defined in the specification for treating inter alia psychotic disorders, depressive disorders, anxiety disorders and sexual dysfunctions.
摘要翻译：式（I）化合物，其中R

3. 发明申请

WO2011138266A1 INDOLIZINE AND IMIDAZOPYRIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吲哚美辛和咪唑吡啶衍生物作为OREXIN受体拮抗剂
公开(公告)号：WO2011138266A1
公开(公告)日：2011-11-10
申请号：PCT/EP2011/056939
申请日：2011-05-02
申请人： EVOTEC AG , BENTLEY, Jonathan, Mark , DAVENPORT, Tara , HALLETT, David, James
发明人： BENTLEY, Jonathan, Mark , DAVENPORT, Tara , HALLETT, David, James
IPC分类号： C07D471/04 , A61K31/437 , A61P3/08 , A61P25/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) wherein A, R 1 to R 8 have the meaning as cited in the description and the claims. Said compounds are useful as Orexin 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）的化合物，其中A，R 1至R 8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Orexin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。

4. 发明申请

WO2006077025A2 MORPHOLINES AS 5HT2C AGONISTS 审中-公开
标题翻译：吗啡作为5HT2C激动剂
公开(公告)号：WO2006077025A2
公开(公告)日：2006-07-27
申请号：PCT/EP2006/000126
申请日：2006-01-10
申请人： F. HOFFMANN-LA ROCHE AG , VERNALIS RESEARCH LIMITED , BENTLEY, Jonathan, Mark , DAWSON, Claire, Elizabeth , GUBA, Wolfgang , HEBEISEN, Paul , MONCK, Nathaniel , PRATT, Robert, Mark , RICHTER, Hans , ROEVER, Stephan , RUSTON, Vicki
发明人： BENTLEY, Jonathan, Mark , DAWSON, Claire, Elizabeth , GUBA, Wolfgang , HEBEISEN, Paul , MONCK, Nathaniel , PRATT, Robert, Mark , RICHTER, Hans , ROEVER, Stephan , RUSTON, Vicki
IPC分类号： C07D265/30 , A61K31/5375 , A61P3/04 , A61P3/10
CPC分类号： C07D265/30
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐和酯，其中R 1至R 5具有权利要求1中给出的含义。这些化合物可用于制备药物。

5. 发明申请

WO0017170A3 N1-SUBSTITUTED BENZOPYRAZOLES AS INHIBITORS OF 5-HT2 RECEPTORS 审中-公开
标题翻译：作为5-HT2受体的抑制剂的N-取代的苯并噻唑
公开(公告)号：WO0017170A3
公开(公告)日：2000-08-03
申请号：PCT/GB9903187
申请日：1999-09-23
申请人： CEREBRUS PHARM LTD , ADAMS DAVID REGINALD , BENTLEY JONATHAN MARK , ROFFEY JONATHAN RICHARD ANTHON , DUNCTON MATTHEW ALEXANDER JAME
发明人： ADAMS DAVID REGINALD , BENTLEY JONATHAN MARK , ROFFEY JONATHAN RICHARD ANTHON , DUNCTON MATTHEW ALEXANDER JAME
IPC分类号： C07D231/56 , A61K31/415
CPC分类号： C07D231/56
摘要： A chemical compound of formula (I): wherein R1 to R3 are independently selected from hydrogen and alkyl; R5 is selected from alkylthio, arylthio, alkylsulfoxyl, arylsulfoxyl, alkylsulfonyl and arylsulfonyl; R4, R6, and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, arylsulfoxyl, alkylsulfoxyl, alkylsulfonyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus; and sleep apnea, and particularly for the treatment of obesity.
摘要翻译：式（I）的化合物：其中R 1至R 3独立地选自氢和烷基; R5选自烷硫基，芳硫基，烷基亚磺酰基，芳基亚砜基，烷基磺酰基和芳基磺酰基; R4，R6和R7独立地选自氢，卤素，羟基，烷基，芳基，烷氧基，芳氧基，烷硫基，芳硫基，芳基亚砜基，烷基磺酰基，烷基磺酰基，芳基磺酰基，氨基，单烷基氨基，二烷基氨基，硝基，氰基，芳基羰基，氨基羰基，单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基及其药学上可接受的盐和前药，以及其在治疗中的用途，特别是用于治疗中枢神经系统疾病。损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症并且睡眠呼吸暂停，特别是用于治疗肥胖。

6. 发明申请

WO0012481A3 INDAZOLE DERIVATIVES WITH 5-HT2 RECEPTOR ACTIVITY________________ 审中-公开
标题翻译：具有5-HT2受体活性的吲哚衍生物
公开(公告)号：WO0012481A3
公开(公告)日：2000-06-08
申请号：PCT/GB9902875
申请日：1999-09-01
申请人： CEREBRUS PHARM LTD , ADAMS DAVID REGINALD , BENTLEY JONATHAN MARK , ROFFEY JONATHAN RICHARD ANTHON , HAMLYN RICHARD JOHN , GEORGE ASHLEY ROGER
发明人： ADAMS DAVID REGINALD , BENTLEY JONATHAN MARK , ROFFEY JONATHAN RICHARD ANTHON , HAMLYN RICHARD JOHN , GEORGE ASHLEY ROGER
IPC分类号： A61K31/416 , A61P1/00 , A61P3/04 , A61P7/02 , A61P9/00 , A61P13/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P43/00 , C07D231/56
CPC分类号： C07D231/56
摘要： A chemical compound of formula (I) wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, monoalkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, arylthio, arylsulfoxyl, arylsulfonyl, alkylsulfoxyl, alkylsulfonyl, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino; and R8 is selected from alkyl and alkoxy, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.
摘要翻译：式（I）的化合物，其中R 1至R 3独立地选自氢和烷基; R4至R7独立地选自氢，卤素，羟基，烷基，芳基，氨基，单烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，芳硫基，芳基亚砜基，芳基磺酰基，烷基亚砜基，烷基磺酰基，硝基，氰基，甲醛，烷基羰基，芳基羰基，氨基羰基单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基; 并且R 8选自烷基和烷氧基及其药学上可接受的盐和前药，及其在治疗中的用途，特别是用于治疗中枢神经系统疾病的用途; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖症。

7. 发明申请

WO2011138265A3 INDOLE AND INDAZOLE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吲哚和吲哚衍生物作为OREXIN受体拮抗剂
公开(公告)号：WO2011138265A3
公开(公告)日：2015-06-25
申请号：PCT/EP2011056938
申请日：2011-05-02
申请人： EVOTEC AG , BENTLEY JONATHAN MARK , DAVENPORT TARA , SLACK MARK
发明人： BENTLEY JONATHAN MARK , DAVENPORT TARA , SLACK MARK
IPC分类号： C07D209/30 , A61K31/404 , A61K31/416 , A61P25/28 , A61P25/30 , C07D231/56
CPC分类号： C07D209/30 , C07D231/56
摘要： The invention relates to compounds of formula (I) wherein A, R1 to R8 have the meaning as cited in the description and the claims. Said compounds are useful as Orexin 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）的化合物，其中A，R 1至R 8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Orexin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。

8. 发明申请

WO2008092891A1 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）用于治疗排毒障碍的DECAN-2-ONE衍生物
公开(公告)号：WO2008092891A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/051116
申请日：2008-01-30
申请人： GLAXO GROUP LIMITED , BENTLEY, Jonathan , BIAGETTI, Matteo , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio
发明人： BENTLEY, Jonathan , BIAGETTI, Matteo , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio
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 or a pharmaceutically acceptable salt or solvate thereof, selected from a group consisting of: (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)3-(2-fluoro-3-pyridinyl)-1-oxa-3-azaspiro[4.5]decan-2-one; (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(3-pyridazinyl)-1-oxa-3- azaspiro[4.5]decan-2-one; (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(1-methyl-1H-pyrazol-3-yl)- 1-oxa-3-azaspiro[4.5]decan-2-one; 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：本发明涉及选自以下的新的化合物或其药学上可接受的盐或溶剂化物：（反）-8 - （{[1-（2-氟苯基）-1H-吡唑-3-基]氨基} 甲基）-3-（2-氟-3-吡啶基）-1-氧杂-3-氮杂螺[4.5]癸-2-酮; （反式）-8 - （{[1-（2-氟苯基）-1H-吡唑-3-基]氨基}甲基）-3-（3-哒嗪基）-1-氧杂-3-氮杂螺[4.5] -2-酮; （反式）-8 - （{[1-（2-氟苯基）-1H-吡唑-3-基]氨基}甲基）-3-（1-甲基-1H-吡唑-3-基）-1-氧杂 - 3-氮杂螺[4.5]癸-2-酮; 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。

9. 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。

10. 发明申请

WO2008092887A1 I-OXA-3-AZASPIRO (4.5) DECAN-2-ONE AND 1-OXA-3, 8-DIAZASPIRO (4.5) DECAN-2-ONE DERIVATIVES FOR THE TREATMENT OF EATING DISORDERS 审中-公开
标题翻译： I-OXA-3-AZASPIRO（4.5）Decan-2-ONE和1-OXA-3,8-DIAZASPIRO（4.5）Decan-2-ONE衍生物用于治疗排卵病
公开(公告)号：WO2008092887A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/051110
申请日：2008-01-30
申请人： GLAXO GROUP LIMITED , BENTLEY, Jonathan , BIAGETTI, Matteo , CARDULLO, Francesca , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio , MENICONI, Mirco , MERLO, Giancarlo , PIZZI, Domenica Antonia , SERI, Catia
发明人： BENTLEY, Jonathan , BIAGETTI, Matteo , CARDULLO, Francesca , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio , MENICONI, Mirco , MERLO, Giancarlo , PIZZI, Domenica Antonia , SERI, Catia
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , C07D498/10 , A61K31/423 , A61P3/00 , A61P25/00
CPC分类号： C07D498/10 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, formula (I) 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; W is -CZ 1 or nitrogen; Z 1 is hydrogen, C1 -C4 alkyl; A is a 5 membered heteroaryl, pyrazine, pyrimidine, or quinoline or quinazoline 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 a 5-10 membered aryl or heteroaryl which may be substituted by one or more: halogen, C1-C 4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is -CZ 1 , compounds of formula (I) have a trans stereochemistry; 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合物，式（I）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; W是-CZ 1 N或氮; Z 1是氢，C 1 -C 4烷基; A是可以被一个或多个卤素取代的5元杂芳基，吡嗪，嘧啶或喹啉或喹唑啉：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是氢或可被一个或多个取代基取代的5-10元芳基或杂芳基：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; 是通过任何原子连接的A和B; 条件是当W是-CZ 1时，式（I）的化合物具有反式立体化学; 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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