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1. 发明申请

US20100179127A1 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：US20100179127A1
公开(公告)日：2010-07-15
申请号：US11993630
申请日：2006-06-23
申请人： Philipp Floersheim , Wolfgang Froestl , Sebastien Guery , Kiemens Kaupmann , Manuel Koller
发明人： Philipp Floersheim , Wolfgang Froestl , Sebastien Guery , Kiemens Kaupmann , Manuel Koller
IPC分类号： A61K31/505 , C07D239/56 , A61K31/513 , C07D239/47 , C07D239/553 , C07D239/30 , C07D239/42 , C07D239/48 , C07D405/10 , A61K31/506 , C07D401/04 , C07D487/04 , A61K31/519 , C07D413/10 , C07D403/12 , A61K31/55 , A61P25/24 , A61P25/18 , A61P25/30 , A61P25/00 , A61P25/08 , A61P25/22
CPC分类号： C07F7/0812 , C07D239/42 , C07D239/48 , C07D403/12 , C07D405/04 , C07D413/04 , C07D471/04 , C07D487/04 , C07F9/6512
摘要： The invention relates to novel heterocyclic compounds of the formula in free base form or in acid addition salt form, in which R1, R2, R3, R4 and A are as defined in the specification, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及游离碱形式或酸加成盐形式的新颖杂环化合物，其中R 1，R 2，R 3，R 4和A如本说明书中所定义，其制备，用作药物，以及包括它们的药物。

2. 发明申请

US20100286152A1 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：US20100286152A1
公开(公告)日：2010-11-11
申请号：US12602829
申请日：2008-06-05
申请人： Giovanni Bernasconi , Steven Mark Bromidge , Andrew James Carpenter , Lucilla D'Adamo , Romano Di Fabio , Sebastien Guery , Francesca Pavone , Alfonso Pozzan , Marilisa Rinaldi , Fabio Maria Sabbatini , Yves St-Denis
发明人： Giovanni Bernasconi , Steven Mark Bromidge , Andrew James Carpenter , Lucilla D'Adamo , Romano Di Fabio , Sebastien Guery , Francesca Pavone , Alfonso Pozzan , Marilisa Rinaldi , Fabio Maria Sabbatini , Yves St-Denis
IPC分类号： A61K31/495 , C07D409/06 , C07D405/06 , C07D295/13 , C07D401/06 , C07D403/06 , C07D211/28 , A61K31/496 , A61K31/4525 , A61K31/445 , A61K31/506 , A61P3/00
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,
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，

3. 发明申请

US20090203705A1 Spiro Compounds As NPY Y5 Receptor Antagonists 审中-公开
标题翻译：螺环化合物作为NPY Y5受体拮抗剂
公开(公告)号：US20090203705A1
公开(公告)日：2009-08-13
申请号：US12360166
申请日：2009-01-27
申请人： Matteo Biagetti , Stefania Anna Contini , Thorsten Genski , Sebastien Guery , Colin Philip Leslie , Angelica Mazzali , Domenica Antonia Pizzi , Fabio Maria Sabbatini , Catia Seri
发明人： Matteo Biagetti , Stefania Anna Contini , Thorsten Genski , Sebastien Guery , Colin Philip Leslie , Angelica Mazzali , Domenica Antonia Pizzi , Fabio Maria Sabbatini , Catia Seri
IPC分类号： A61K31/501 , C07D413/14 , A61P3/04
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, 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 6-10 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; or —C(═O)—X; or —O(CH2)0-1R1; 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, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, hydroxyl, cyano; A and B being linked via any atom; R1 is —(C1-C4)alkyl(C1-C4)alkoxy; or C3-C8 cycloalkyl; or R1 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; or R1 is a 4-6 membered heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; X is OR2 or NR3R4; R2 is C1-C4 alkyl; R3 is hydrogen or together with R4 and the nitrogen form a 5-6 saturated membered ring; R4 is C3-C8 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是可被一个或多个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 -C4卤代烷基，C1-C4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。

4. 发明申请

US20100286151A1 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-2-One衍生物治疗饮食失调
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。

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