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1. 发明申请

US20090036459A1 Melanocortin Type 4 Receptor Agonist Piperidinoylpyrrolidines 有权
标题翻译：黑皮质素4型受体激动剂哌啶子基吡咯烷酮
公开(公告)号：US20090036459A1
公开(公告)日：2009-02-05
申请号：US12280444
申请日：2007-02-19
申请人： Mark David Andrews , Alan Daniel Brown , Mark Ian Lansdell , Nicholas William Summerhill
发明人： Mark David Andrews , Alan Daniel Brown , Mark Ian Lansdell , Nicholas William Summerhill
IPC分类号： A61K31/501 , C07D401/14 , A61P3/00 , A61K31/4545
CPC分类号： C07D401/14
摘要： The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
摘要翻译：本发明涉及一类通式（I）的黑皮质素MCR4激动剂，其中变量和取代基如本文所定义，特别是选择性MCR4激动剂化合物在医学中的用途，特别是用于治疗性功能障碍和肥胖症，可用于其合成的中间体和含有它们的组合物。

2. 发明授权

US08138188B2 Melanocortin type 4 receptor agonist piperidinoylpyrrolidines 有权
标题翻译：黑皮质素4型受体激动剂哌啶子基吡咯烷酮
公开(公告)号：US08138188B2
公开(公告)日：2012-03-20
申请号：US12280444
申请日：2007-02-19
申请人： Mark David Andrews , Alan Daniel Brown , Mark Ian Lansdell , Nicholas William Summerhill
发明人： Mark David Andrews , Alan Daniel Brown , Mark Ian Lansdell , Nicholas William Summerhill
IPC分类号： C07D401/14 , A61K31/4402 , A61P15/00 , A61P3/00
CPC分类号： C07D401/14
摘要： The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
摘要翻译：本发明涉及一类通式（I）的黑皮质素MCR4激动剂，其中变量和取代基如本文所定义，特别是选择性MCR4激动剂化合物在医学中的用途，特别是用于治疗性功能障碍和肥胖症，可用于其合成的中间体和含有它们的组合物。

3. 发明授权

US07378436B2 Compounds 失效
公开(公告)号：US07378436B2
公开(公告)日：2008-05-27
申请号：US10872160
申请日：2004-06-17
申请人： Paul Vincent Fish , Michael Jonathan Fray , Alan Stobie , Florian Wakenhut , Gavin Alistair Whitlock , Mark David Andrews , Alan Daniel Brown , Mark Ian Lansdell
发明人： Paul Vincent Fish , Michael Jonathan Fray , Alan Stobie , Florian Wakenhut , Gavin Alistair Whitlock , Mark David Andrews , Alan Daniel Brown , Mark Ian Lansdell
IPC分类号： A61K31/40 , C07D295/10
CPC分类号： C07D207/14
摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy —C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S or O; Y is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

4. 发明申请

US20080306123A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：US20080306123A1
公开(公告)日：2008-12-11
申请号：US12124755
申请日：2008-05-21
申请人： Paul Vincent Fish , Michael Jonathan Fray , Deborah Jane Lovering , Alan Stobie , Florian Wakenhut , Gavin Alistair Whitlock , Mark David Andrews , Alan Daniel Brown , Mark Ian Lansdell
发明人： Paul Vincent Fish , Michael Jonathan Fray , Deborah Jane Lovering , Alan Stobie , Florian Wakenhut , Gavin Alistair Whitlock , Mark David Andrews , Alan Daniel Brown , Mark Ian Lansdell
IPC分类号： A61K31/4468 , A61P13/00 , A61P29/00 , A61P15/00 , A61P25/24
CPC分类号： C07D207/14
摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S or O; Y is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.
摘要翻译：式（I）化合物及其药学上和/或兽医学上可接受的衍生物，其中R 1是H，C 1-6烷基，-C（X）Y，C 3-8环烷基，芳基，het，芳基-C 1-4烷基或叔丁基其中环烷基，芳基或苯基基团任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基 - C 1-6烷基和C 1-4烷基-S-C 1-4烷基; R 2是芳基或杂芳基，各自任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1 -4-烷基-S-C 1-4烷基; R 3为C 1-6烷基，C 3-8环烷基，C 3-8环烷基-C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔-C 1-4烷基，其中环烷基，芳基或苯基基团任选被至少一个取代基取代独立地选自C 1-6烷基，C 1-6烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S-C 1-4烷基; X是S或O; Y是H，C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基C 1-4烷基; n为1或2，条件是当n为1时，m为0或1，当n为2时，m为0，其中如果m为0，则*表示手性中心。本发明的化合物表现出5-羟色胺和去甲肾上腺素再摄取抑制剂的活性，因此可用于各种治疗领域，例如尿失禁。

5. 发明申请

US20080269233A1 Piperidinoyl-Pyrrolidine and Piperidinoyl-Piperidine Compounds 审中-公开
标题翻译：哌啶子基 - 吡咯烷和哌啶子基 - 哌啶化合物
公开(公告)号：US20080269233A1
公开(公告)日：2008-10-30
申请号：US11997824
申请日：2006-07-26
申请人： Mark David Andrews , Alan Daniel Brown , David Sebastien , Mark Ian Lansdell
发明人： Mark David Andrews , Alan Daniel Brown , David Sebastien , Mark Ian Lansdell
IPC分类号： A61K31/501 , C07D401/06 , A61K31/435 , A61P3/04 , A61P15/10 , C07D403/14
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention relates to a class of compounds of general formula (I) and the salts, hydrates, solvates, polymorphs and prodrugs wherein n, R6, R7 and R10 are as defined herein and especially to MCR4 agonist compounds of formula (I), to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
摘要翻译：本发明涉及一类通式（I）的化合物及其盐，水合物，溶剂合物，多晶型物和前药，其中n，R 6，R 7和R 7 特别是式（I）的MCR4激动剂化合物在药物中的用途，特别是用于治疗性功能障碍和肥胖症的中间体在其合成中的用途以及含有他们。

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