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1. 发明授权

US07169921B2 Process for the preparation of oxabispidines 失效
标题翻译：氧杂二苯胺的制备方法
公开(公告)号：US07169921B2
公开(公告)日：2007-01-30
申请号：US10474593
申请日：2002-04-12
申请人： Lal Cheema , David Cladingboel , Rhona Sinclair
发明人： Lal Cheema , David Cladingboel , Rhona Sinclair
IPC分类号： C07D498/08
CPC分类号： C07D498/08 , Y02P20/55
摘要： There is provided a process for the preparation of a compound of formula (I): which process comprises reaction of a compound of formula (II): with either a compound of formula (III): or acrylamide, followed, in the latter case, by reaction of the resulting intermediate of formula (IV): with an alcohol of formula R2—OH and an agent that promotes, or agents that in combination promote, rearrangement and oxidation of the compound of formula IV to an intermediate isocyanate, which may then react with the alcohol of formula R2—OH, and wherein R1, R2 and R16 have meanings given in the description
摘要翻译：提供了制备式（I）化合物的方法：该方法包括式（II）化合物与式（III）化合物或丙烯酰胺反应，然后在后一种情况下，通过所得到的式（IV）中间体与式R 2 -OH的醇反应，以及促进式IV化合物或其组合促进重排和氧化的试剂与中间体异氰酸酯反应，然后其可以与式R 2 -OH的醇反应，并且其中R 1，R 2和R 2， SUP> 16 具有在说明书中给出的含义

2. 发明申请

US20070197519A1 New Process For The Preparation Of Oxabispidines 审中-公开
标题翻译：新二氧化二氮的制备方法
公开(公告)号：US20070197519A1
公开(公告)日：2007-08-23
申请号：US11612826
申请日：2006-12-19
申请人： Lal Cheema , David Cladingboel , Rhona Sinclair
发明人： Lal Cheema , David Cladingboel , Rhona Sinclair
IPC分类号： C07D498/04 , A61K31/5383
CPC分类号： C07D498/08 , Y02P20/55
摘要： There is provided a process for the preparation of a compound of formula (I): which process comprises reaction of a compound of formula (TI): with either a compound of formula (ITT): or acrylamide, followed, in the latter case, by reaction of the resulting intermediate of formula (IV): with an alcohol of formula R2═OH and an agent that promotes, or agents that in combination promote, rearrangement and oxidation of the compound of formula IV to an intermediate isocyanate, which may then react with the alcohol of formula R2═OH, and wherein R1, R2 and R16 have meanings given in the description.
摘要翻译：提供了制备式（I）化合物的方法：该方法包括式（TI）化合物与式（ITT）化合物或丙烯酰胺反应，然后在后一种情况下，通过所得到的式（IV）中间体与式R 2 -OH的醇反应，以及促进式IV化合物或其组合促进重排和氧化的试剂与中间体异氰酸酯反应，然后其可以与式R 2 -OH的醇反应，并且其中R 1，R 2和R 2， SUP> 16 具有在说明书中给出的含义。

3. 发明申请

US20080200673A1 Process for The Preparation of Sulfonic Acid Salts of Oxabispidines 审中-公开
标题翻译：制备Oxabispidines磺酸盐的方法
公开(公告)号：US20080200673A1
公开(公告)日：2008-08-21
申请号：US11993026
申请日：2006-06-12
申请人： Lal Cheema , David Cladingboel
发明人： Lal Cheema , David Cladingboel
IPC分类号： C07D498/08
CPC分类号： C07D498/08
摘要： There is provided a process for the isolation of a sulfonic acid salt of formula I, or a solvate thereof, from a mixture comprising: (i) the corresponding free base; and (ii) a compound of formula III. or a salt and/or solvate thereof, which process comprises providing an aqueous dispersion of the compounds of formulae II and III and a source of R3SO3− anions and then, if necessary, adjusting the pH of the aqueous dispersion to any value from 3 to 8. There are further provided processes wherein the mixture of compounds of formulae II and III is provided by incomplete reaction, for example in the presence of base and an aqueous phase, between a compound of formula III and a compound of formula IV In such processes, the RSO3− anions of the resulting salt of formula I may be derived from the compound of formula IV. Also for all of these processes, D, R1, R2 and R3 have meanings given in the description.
摘要翻译：提供了从包含以下物质的混合物中分离式I的磺酸盐或其溶剂合物的方法：（i）相应的游离碱; 和（ii）式III化合物。或其盐和/或溶剂化物，该方法包括提供式II和III化合物的水分散体和R 3 SO 3 SO 3的源，阴离子，然后如果需要，将水分散体的pH调节至3至8的任何值。还提供了其中提供式II和III化合物的混合物的方法通过不完全反应，例如在碱和水相存在下，在式III化合物与式IV化合物之间。在这些方法中，RSO 3 - 得到的式I的盐的阴离子可以衍生自式IV化合物。同样对于所有这些方法，D，R 1，R 2和R 3都具有说明书中给出的含义。

4. 发明授权

US07217708B2 3,7-Diazabicyclo [3.3.1] formulations as anti-arrhythmic compounds 失效
标题翻译： 3,7-二氮杂双环[3.3.1]制剂作为抗心律失常化合物
公开(公告)号：US07217708B2
公开(公告)日：2007-05-15
申请号：US10474592
申请日：2002-04-12
申请人： Neil Barnwell , Annika Björe , Lal Cheema , David Cladingboel , Adam Herring , Karin Lövqvist
发明人： Neil Barnwell , Annika Björe , Lal Cheema , David Cladingboel , Adam Herring , Karin Lövqvist
IPC分类号： C07D498/08 , A61K31/5386
CPC分类号： C07D498/08
摘要： There is provided substantially crystalline forms of 4-({3-[7-(3,3-dimethyl-2-oxobutyl) -9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]propyl}amino)benzo-nitrile; tert-butyl 2 -{7-[3-(4-cyanoanilino)propyl]-9-oxa-3,7-diazabicyclo-[3.3.1]non-3-yl}ethylcarbamate; tert-butyl 2-{7-[4-(4-cyanophenyl)butyl]-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl}ethylcarbamate; or tert-butyl 2-{7-[2S)-3-(4-cyanophenoxy)-2-hydroxypropyl]-9-oxa-3,7-diazabicyclo-[3.3.1]non-3-yl}ethylcarbamate and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of cardiac arhythmias.
摘要翻译：提供4 - （{3- [7-（3,3-二甲基-2-氧代丁基）-9-氧杂-3,7-二氮杂双环[3.3.1]壬-3-基]丙基} 氨基）苯并 - 腈; 2- {7- [3-（4-氰基苯胺基）丙基] -9-氧杂-3,7-二氮杂双环[3.3.1]壬-3-基}乙基氨基甲酸叔丁酯; 2- {7- [4-（4-氰基苯基）丁基] -9-氧杂-3,7-二氮杂双环[3.3.1]壬-3-基}乙基氨基甲酸叔丁酯; 或2- {7- [2S）-3-（4-氰基苯氧基）-2-羟丙基] -9-氧杂-3,7-二氮杂双环[3.3.1]壬-3-基}乙基氨基甲酸叔丁酯和药学上其可接受的盐，其可用于治疗心律失常。

5. 发明申请

US20100041911A1 Process For The Production Of (Alkoxycarbonylamino)alkyl Sulfonates 审中-公开
标题翻译：（烷氧基羰基氨基）烷基磺酸盐的制备方法
公开(公告)号：US20100041911A1
公开(公告)日：2010-02-18
申请号：US11993029
申请日：2006-06-12
申请人： David Cladingboel , Adam Herring , Rhona Sinclair
发明人： David Cladingboel , Adam Herring , Rhona Sinclair
IPC分类号： C07C303/02
CPC分类号： C07C303/28 , C07C309/73
摘要： There is provided a process for the preparation of a compound of formula I, which process comprises: (a) reaction of a compound of formula II, HO-D-NH2 II with a compound of formula III, followed by (b) reaction of the intermediate of formula IV thereby formed, IV with base and a compound of formula V, R2S(O)2L2 V, wherein the intermediate of formula IV is not isolated, and wherein D, R1, R2, L1 and L2 have meanings given in the description.
摘要翻译：提供了制备式I化合物的方法，该方法包括：（a）将式II化合物，HO-D-NH 2 II与式III化合物反应，然后（b）由此形成式IV的中间体，IV与碱和式V化合物R 2 S（O）2 L 2 V，其中式IV的中间体不分离，并且其中D，R 1，R 2，L 1和L 2具有以下含义：说明。

6. 发明申请

US20060166980A1 New oxabispidine compounds useful in the treatment of cardiac arrhythmias 审中-公开
公开(公告)号：US20060166980A1
公开(公告)日：2006-07-27
申请号：US11385861
申请日：2006-03-22
申请人： Annika Bjore , Magnus Bjorsne , David Cladingboel , Kurt-Jurgen Hoffmann , John Pavey , Fritiof Ponten , Gert Strandlund , Peder Svensson , Colin Thomson , Michael Wilsterman
发明人： Annika Bjore , Magnus Bjorsne , David Cladingboel , Kurt-Jurgen Hoffmann , John Pavey , Fritiof Ponten , Gert Strandlund , Peder Svensson , Colin Thomson , Michael Wilsterman
IPC分类号： C07D487/04 , A61K31/538
CPC分类号： C07D498/08
摘要： There is provided compounds of formula I, wherein R1, R2, R3, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.

7. 发明授权

US06265409B1 Pyridine derivatives and pharmaceutical compositions containing them 失效
标题翻译：吡啶衍生物和含有它们的药物组合物
公开(公告)号：US06265409B1
公开(公告)日：2001-07-24
申请号：US09068520
申请日：1998-05-11
申请人： David Cheshire , David Cladingboel , Simon Hirst , Carol Manners , Michael Stocks
发明人： David Cheshire , David Cladingboel , Simon Hirst , Carol Manners , Michael Stocks
IPC分类号： C07D40112
CPC分类号： C07D213/30
摘要： The invention relates to novel pyridyl derivatives, their use as medicaments, pharmaceutical formulations including them and methods for their preparation.
摘要翻译：本发明涉及新颖的吡啶基衍生物，它们作为药物的用途，包括它们的药物制剂及其制备方法。

8. 发明申请

US20070037830A1 2-Adamantyl derivatives as p2X7 receptor antagonists. 审中-公开
标题翻译： 2-金刚烷基衍生物作为p2X7受体拮抗剂。
公开(公告)号：US20070037830A1
公开(公告)日：2007-02-15
申请号：US10567711
申请日：2004-07-28
申请人： David Cladingboel , Rhonan Ford , Paul Willis
发明人： David Cladingboel , Rhonan Ford , Paul Willis
IPC分类号： A61K31/52 , A61K31/505 , A61K31/44 , A61K31/47 , A61K31/4162 , A61K31/381 , A61K31/165 , C07D333/22 , C07D277/62 , C07D215/12
CPC分类号： C07C233/26 , C07C2603/74 , C07D209/08 , C07D215/38
摘要： The invention provides compounds of formula (I) or a pharmaceutically acceptable salt or solvate or pro-drug thereof, wherein A, B, X, n and m have the meanings as defined in the specification. Processes for their preparation; pharmaceutical compositions containing them; and their use in therapy are also described.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐或溶剂化物或前体药物，其中A，B，X，n和m具有如说明书中所定义的含义。其准备过程; 含有它们的药物组合物; 还描述了它们在治疗中的用途。

9. 发明申请

US20060199814A1 Chemical Intermediate 失效
标题翻译：化学中间体
公开(公告)号：US20060199814A1
公开(公告)日：2006-09-07
申请号：US10532223
申请日：2003-10-13
申请人： David Cladingboel
发明人： David Cladingboel
IPC分类号： A61K31/538 , C07D491/04
CPC分类号： C07D498/08
摘要： Compounds of Formula I, wherein R2 represents C1-6 alkyl (optionally substituted by one or more substituents selected from —OH, halo, cyano, nitro and aryl) or aryl, wherein each aryl and aryloxy group, unless otherwise specified, is optionally substituted, and methods of preparation thereof are disclosed.
摘要翻译：式I的化合物，其中R 2表示C 1-6烷基（任选被一个或多个选自-OH，卤素，氰基，硝基和芳基的取代基取代）或芳基，其中除非另有说明，每个芳基和芳氧基任选被取代，并且其制备方法被公开。

10. 发明授权

US06303659B2 Compounds 失效
公开(公告)号：US06303659B2
公开(公告)日：2001-10-16
申请号：US09745740
申请日：2000-12-26
申请人： Andrew Baxter , Thomas McInally , Michael Mortimore , David Cladingboel
发明人： Andrew Baxter , Thomas McInally , Michael Mortimore , David Cladingboel
IPC分类号： A61K31166
CPC分类号： C07D203/14 , C07C233/65 , C07C235/46 , C07C235/60 , C07C237/30 , C07C323/62 , C07C2603/74 , C07D209/08 , C07D213/82 , C07D233/64 , C07D295/13
摘要： The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

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