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1. 发明申请

US20050176772A1 Pharmaceutically active compounds 有权
标题翻译：药物活性化合物
公开(公告)号：US20050176772A1
公开(公告)日：2005-08-11
申请号：US11051144
申请日：2005-02-03
申请人： Andrew Calabrese , David Fradet , David Hepworth , Mark Lansdell
发明人： Andrew Calabrese , David Fradet , David Hepworth , Mark Lansdell
IPC分类号： A61K31/454 , C07D401/06 , C07D401/14 , C07D405/14 , C07D43/02
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
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R 1，R 2，R 3，R 3， SUP> 4和R 5如本文所定义，特别是选择性MCR4激动剂化合物，其在医学上的用途，含有它们的组合物，其制备方法和用于这样的过程。

2. 发明申请

US20050014789A1 Amide derivatives as selective serotonin re-uptake inhibitors 审中-公开
标题翻译：酰胺衍生物作为选择性5-羟色胺再摄取抑制剂
公开(公告)号：US20050014789A1
公开(公告)日：2005-01-20
申请号：US10865408
申请日：2004-06-10
申请人： Mark Andrews , Alan Brown , David Fradet , David Gordon , Mark Lansdell , Malcolm MacKenny
发明人： Mark Andrews , Alan Brown , David Fradet , David Gordon , Mark Lansdell , Malcolm MacKenny
IPC分类号： A61P25/24 , A61P25/30 , C07D207/14 , C07D211/58 , C07D401/12 , A61K31/445 , A61K31/40 , C07D207/10 , C07D211/56
CPC分类号： C07D401/12 , C07D207/14 , C07D211/58
摘要： The present invention relates to compounds of formula (I), wherein R1 is selected from: (a) (C1-C6)alkyl, optionally substituted by 1-3 substituents, each independently selected from: (i) CF3, OH, (C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C6)alkoxy and halo. (ii) Phenyl, optionally fused with phenyl or cyclohexyl, said phenyl or fused phenyl optionally substituted with 1-3 groups selected from (C1-C6)alkyl, (C1-C6)alkyl ester, OH and halo; and (b) (C3-C6)cycloalkyl, optionally fused with (C5-C7)cycloalkyl, said cycloalkyl or fused cycloalkyl optionally substituted by OH, (C1-C6)alkyl, (C1-C6)alkoxy and halo. R2 is Phenyl, optionally fused to (C4-C6)cycloalkyl, phenyl or pyridyl, said phenyl or fused phenyl moiety optionally substituted with 1-3 groups each independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, halo and OH; n is 1 to 2; and pharmaceutically acceptable salts, solvates or polymorphs thereof; With the proviso that when n is 2 and R1 is 2-(3,4-dimethoxylphenyl)-1-ethyl, 3,3-diphenyl-1-propyl or 2,4-difluorophenyl, then R2 cannot be 4-trifluoromethoxyphenyl, 2,4,6-trimethoxyphenyl, 4-acetoxyphenyl or 2,4-difluorophenyl; which are a class of selective serotonin re-uptake inhibitors (SSRIs).
摘要翻译：本发明涉及式（I）化合物，其中R 1选自：（a）任选被1-3个取代基取代的（C 1 -C 6）烷基，各自独立地选自：（i）CF 3，OH ，（C 1 -C 6）烷基，（C 3 -C 6）环烷基，（C 1 -C 6）烷氧基和卤素。（ii）苯基，任选地与苯基或环己基稠合，所述苯基或稠合苯基任选被1-3个选自（C 1 -C 6）烷基，（C 1 -C 6）烷基酯，OH和卤素的基团取代; 任选地与（C 5 -C 7）环烷基稠合的所述环烷基或任选被OH，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基和卤素取代的稠合环烷基。 R 2是苯基，任选地与（C 1 -C 6）环烷基，苯基或吡啶基稠合，所述苯基或稠合苯基部分任选被1-3个基团独立地选自（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，卤素和OH; n为1〜2; 及其药学上可接受的盐，溶剂化物或多晶型物; 条件是当n为2且R 1为2-（3,4-二甲氧基苯基）-1-乙基，3,3-二苯基-1-丙基或2,4-二氟苯基时，则R 2不能 4-三氟甲氧基苯基，2,4,6-三甲氧基苯基，4-乙酰氧基苯基或2,4-二氟苯基; 其是一类选择性5-羟色胺再摄取抑制剂（SSRI）。

3. 发明授权

US07649002B2 (3,5-dimethylpiperidin-1yl)(4-phenylpyrrolidin-3-yl)methanone derivatives as MCR4 agonists 有权
标题翻译：（3,5-二甲基哌啶-1-基）（4-苯基吡咯烷-3-基）甲酮衍生物作为MCR4激动剂
公开(公告)号：US07649002B2
公开(公告)日：2010-01-19
申请号：US11051144
申请日：2005-02-03
申请人： Andrew Antony Calabrese , David Sebastien Fradet , David Hepworth , Mark Lansdell
发明人： Andrew Antony Calabrese , David Sebastien Fradet , David Hepworth , Mark Lansdell
IPC分类号： A61K31/454 , C07D403/02
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
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R1，R2，R3，R4和R5如本文所定义，特别是涉及选择性MCR4激动剂化合物在医药中的用途，含有它们的组合物，其制备方法和在这些方法中使用的中间体。

4. 发明申请

US20080085884A1 Melanin Concentrating Hormone Receptor-1 Antagonist Pyridinones 审中-公开
标题翻译：黑色素浓度激素受体-1拮抗剂吡啶酮
公开(公告)号：US20080085884A1
公开(公告)日：2008-04-10
申请号：US11862284
申请日：2007-09-27
申请人： Duncan Armour , Sebastian Galan , Charlotte Lane , Mark Lansdell , Paul Stupple
发明人： Duncan Armour , Sebastian Galan , Charlotte Lane , Mark Lansdell , Paul Stupple
IPC分类号： A61K31/397 , A61K31/4427 , A61K31/4523 , A61K31/496 , A61K31/501 , A61K31/55 , A61P1/00 , A61P15/00 , A61P25/00 , A61P29/00 , A61P3/04 , A61P9/00 , C07D205/02 , C07D213/02 , C07D221/00 , C07D223/02 , C07D237/02 , C07D295/00
CPC分类号： C07D213/74 , C07D487/04
摘要： The present invention provides for MCHR1 antagonist compounds of formula (I) and the pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein the substituents are as defined herein, and the pharmaceutically acceptable salts, solvates and prodrugs thereof, which are useful in treating diseases or conditions wherein antagonism of the MCHR1 receptor is beneficial.
摘要翻译：本发明提供式（I）的MCHR1拮抗剂化合物及其药学上可接受的盐，溶剂合物和前药，其中取代基如本文所定义，及其药学上可接受的盐，溶剂合物和前药，其可用于治疗疾病或其中MCHR1受体的拮抗作用是有益的。

5. 发明授权

US5228996A Method for treating waste water 失效
标题翻译：废水处理方法
公开(公告)号：US5228996A
公开(公告)日：1993-07-20
申请号：US655913
申请日：1991-02-15
申请人： Mark Lansdell
发明人： Mark Lansdell
IPC分类号： C02F3/12 , C02F3/30
CPC分类号： C02F3/1263 , C02F3/301 , C02F3/308 , Y02W10/15
摘要： Conventional biological processes for treating wastewater include the so-called activated sludge process which is continuous and the sequencing batch reactor (SBR) activated sludge process. The first process requires the use of dedicated, relatively expensive external clarifiers, and the second process is inefficient in terms of treatment volume. A modified sequencing batch reactor process and system enable the efficient, continuous treatment of wastewater, combining the advantages of the SBR and activated sludge processes. Wastewater is treated in three contiguous treatment sections, each of which includes a plurality of contiguous cells. In a first series of operations, the flow direction is from the first to the third sections, and in a second series of operations the flow is reversed. In each series of operations, the first step is to aerobically treat the wastewater, and then allow the sludge to settle before discharging the treated wastewater from the system. The settling steps of the process include pre-settling while wastewater is flowing through a section, and quiescent settling while aerobic treatment and flowing or pre-settling are occurring in other sections of the system.
摘要翻译：用于处理废水的常规生物过程包括所谓的连续的活性污泥法和顺序间歇反应器（SBR）活性污泥法。第一个过程需要使用专门的，相对昂贵的外部澄清池，第二个过程在处理量方面是低效的。改进的顺序间歇反应器工艺和系统能够有效，持续地处理废水，结合SBR和活性污泥工艺的优点。在三个连续处理区域中处理废水，其中每个处理段包括多个连续的细胞。在第一系列操作中，流动方向是从第一部分到第三部分，并且在第二系列操作中，流动相反。在每一系列操作中，第一步是对废水进行有氧处理，然后在排出经处理的废水之前使污泥沉淀。该过程的沉降步骤包括在废水流过一段时进行预沉降，并在系统的其他部分发生好氧处理和流动或预沉降时进行静态沉降。

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