公开(公告)号：US20100286151A1

公开(公告)日：2010-11-11

申请号：US12524080

申请日：2008-01-30

申请人： Jonathan Bentley ,  Matteo Biagetti ,  Romano Di Fabio ,  Thorsten Genski ,  Sebastien Guery ,  Silvia Rosalia Kopf ,  Colin philip Leslie ,  Angelica Mazzali ,  Sergio Melotto ,  Domenica Antonia Pizzi ,  Fabio Maria Sabbatini ,  Catia Seri

发明人： Jonathan Bentley ,  Matteo Biagetti ,  Romano Di Fabio ,  Thorsten Genski ,  Sebastien Guery ,  Silvia Rosalia Kopf ,  Colin philip Leslie ,  Angelica Mazzali ,  Sergio Melotto ,  Domenica Antonia Pizzi ,  Fabio Maria Sabbatini ,  Catia Seri

IPC分类号： A61K31/423 ,  C07D417/14 ,  A61K31/4439 ,  A61K31/505 ,  C07D413/14 ,  A61K31/501 ,  A61K31/444 ,  A61K31/497 ,  A61K31/433 ,  C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  A61K31/4985 ,  C07D413/12 ,  A61P3/04 ,  A61P3/00

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; Z1 is H, C1-C4 alkyl or F; Z is CH2, 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, Cl 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合物，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/或预防进食障碍如狂饮病症的药剂。

公开(公告)号：US20090042897A1

公开(公告)日：2009-02-12

申请号：US12022327

申请日：2008-01-30

申请人： Jonathan Bentley ,  Matteo Biagetti ,  Thorsten Genski ,  Silvia Rosalia Kopf ,  Colin Philip Leslie ,  Sergio Melotto

发明人： Jonathan Bentley ,  Matteo Biagetti ,  Thorsten Genski ,  Silvia Rosalia Kopf ,  Colin Philip Leslie ,  Sergio Melotto

IPC分类号： C07D413/02 ,  A61K31/501 ,  A61K31/4439 ,  A61K31/423 ,  A61P3/00 ,  A61P25/00 ,  A61P25/24

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-one; （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。

公开(公告)号：US20100197699A1

公开(公告)日：2010-08-05

申请号：US12524038

申请日：2008-01-30

申请人： Jonathan Bentley ,  Matteo Biagetti ,  Francesca Cardullo ,  Thorsten Genski ,  Silvia Rosalia Kopf ,  Colin Philip Leslie ,  Sergio Melotto ,  Mirco Meniconi ,  Giancarlo Merlo ,  Domenica Antonia Pizzi ,  Catia Seri

发明人： Jonathan Bentley ,  Matteo Biagetti ,  Francesca Cardullo ,  Thorsten Genski ,  Silvia Rosalia Kopf ,  Colin Philip Leslie ,  Sergio Melotto ,  Mirco Meniconi ,  Giancarlo Merlo ,  Domenica Antonia Pizzi ,  Catia Seri

IPC分类号： A61K31/423 ,  C07D498/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  A61K31/444 ,  A61K31/501 ,  A61K31/497 ,  A61K31/506 ,  A61P3/04 ,  A61P25/24

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, 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 —CZ1 or nitrogen; Z1 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-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is —CZ1, 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，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-CZ1或氮; Z1是氢，C1-C4烷基; A是可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卤素取代的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-CZ1时，式（I）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。