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1. 发明申请

US20130331369A1 3-Spirocyclic Piperidine Derivatives as Ghrelin Receptor Agonists 审中-公开
公开(公告)号：US20130331369A1
公开(公告)日：2013-12-12
申请号：US13962689
申请日：2013-08-08
申请人： Ameet Vijay Ambarkhane , Gurdip Bhalay , Martin Beckett , James Dale , Ahmed Hamadi , Alessandro Mazzacani , Jeffrey McKenna , Christopher Thomson
发明人： Ameet Vijay Ambarkhane , Gurdip Bhalay , Martin Beckett , James Dale , Ahmed Hamadi , Alessandro Mazzacani , Jeffrey McKenna , Christopher Thomson
IPC分类号： C07D471/10 , A61K31/55 , C07D487/10 , A61K31/407 , A61K31/435 , A61K45/06
CPC分类号： C07D471/10 , A61K31/407 , A61K31/435 , A61K31/55 , A61K45/06 , C07D487/10
摘要： The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
摘要翻译：本发明涉及式（I）的衍生物，其中取代基如说明书中所定义; 制备此类衍生物的方法; 包含这些衍生物的药物组合物; 这种衍生物作为药物; 用于治疗疾病或由生长素释放肽受体介导的疾病的衍生物。

2. 发明申请

US20070060563A1 Quinuclidine derivatives binding to mucarinic m3 receptors 审中-公开
标题翻译：奎宁环衍生物与粘蛋白m3受体结合
公开(公告)号：US20070060563A1
公开(公告)日：2007-03-15
申请号：US10554558
申请日：2004-04-30
申请人： Stephen Collingwood , Brian Cox , Gurdip Bhalay , Nicholas Devereux
发明人： Stephen Collingwood , Brian Cox , Gurdip Bhalay , Nicholas Devereux
IPC分类号： C07D471/02 , C07D453/02 , A61K31/506 , A61K31/497 , A61K31/4745
CPC分类号： C07D453/02
摘要： Compounds of formula I in salt or zwitterionic form wherein, wherein R1, R2, R3, and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：盐或两性离子形式的式I化合物，其中R 1，R 2，R 3和R 4， SUP>具有说明书中所示的含义，可用于治疗由毒蕈碱M3受体介导的病症。还描述了含有化合物的药物组合物和制备该化合物的方法。

3. 发明申请

US20060173181A1 8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors 审中-公开
标题翻译： 8-喹啉黄嘌呤和8-异喹啉黄嘌呤衍生物作为PDE 5抑制剂
公开(公告)号：US20060173181A1
公开(公告)日：2006-08-03
申请号：US11274030
申请日：2005-11-15
申请人： Gurdip Bhalay , Stephen Collingwood , Robin Fairhurst , Sylvie Gomez , Reto Naef , David Sandham
发明人： Gurdip Bhalay , Stephen Collingwood , Robin Fairhurst , Sylvie Gomez , Reto Naef , David Sandham
IPC分类号： C07D473/04 , A61K31/522
CPC分类号： C07D239/545 , A61K31/522 , C07D473/04 , C07D473/06
摘要： A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.
摘要翻译：式（I）R 1的化合物是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基，烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基，其中其芳基环任选地与5元杂环基稠合，或任选被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基，氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基，R 3是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基，R 0 任选地与5元杂环基稠合并且任选地被一个或多个选自卤素，氰基，羟基，烷基，羟基烷基，烷氧基烷基，烷硫基的取代基取代的喹啉基，异喹啉基或氧代二氢异喹啉基烷基，烷氧基，烷硫基，烯基，烷氧基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个选自卤素或烷氧基的取代基或具有5或6个环原子通过环碳原子连接到指定碳原子的杂芳基，R 6和R 7各自独立地任选被羟基或烷氧基取代的氢或烷基或R 6和R 7中的一个是氢，另一个是酰基或R 6和 R 7与它们所连接的氮原子一起表示5-或6-元杂环基。

4. 发明申请

US20160068546A1 TREATING DISEASES MEDIATED BY BLOCKADE OF THE EPITHELIAL SODIUM CHANNEL WITH PYRAZINE-2-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：用吡嗪-2-羧酰胺衍生物治疗由上皮细胞通道引起的疾病
公开(公告)号：US20160068546A1
公开(公告)日：2016-03-10
申请号：US14847262
申请日：2015-09-08
申请人： Gurdip BHALAY , Emma BUDD , Graham Charles BLOOMFIELD , Stephen Paul COLLINGWOOD , Andrew DUNSTAN , Lee EDWARDS , Peter GEDECK , Catherine HOWSHAM , Peter HUNT , Thomas Anthony HUNT , Paul OAKLEY , Nichola SMITH
发明人： Gurdip BHALAY , Emma BUDD , Graham Charles BLOOMFIELD , Stephen Paul COLLINGWOOD , Andrew DUNSTAN , Lee EDWARDS , Peter GEDECK , Catherine HOWSHAM , Peter HUNT , Thomas Anthony HUNT , Paul OAKLEY , Nichola SMITH
IPC分类号： C07D519/00 , A61K31/497
CPC分类号： C07D519/00 , A61K31/497 , C07D403/12 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：式Ⅰ化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11具有说明书中所述的含义，可用于治疗疾病，对上皮钠通道的阻断作出反应。还描述了含有化合物的药物组合物和用于制备化合物的方法。

5. 发明授权

US08697687B2 Treating diseases mediated by blockade of the epithelial sodium channel with pyrazine-2-carboxamide derivatives 有权
标题翻译：用吡嗪-2-甲酰胺衍生物治疗由上皮钠通道阻断介导的疾病
公开(公告)号：US08697687B2
公开(公告)日：2014-04-15
申请号：US13613495
申请日：2012-09-13
申请人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
发明人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
IPC分类号： A01N43/62 , A61K31/55 , A61K31/4965 , A61K31/535 , C07D237/00 , C07D239/00 , C07D241/00 , C07D413/00 , C07D243/08
CPC分类号： C07D519/00 , A61K31/497 , C07D403/12 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：式Ⅰ化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11具有说明书中所述的含义，可用于治疗疾病，对上皮钠通道的阻断作出反应。还描述了含有化合物的药物组合物和用于制备化合物的方法。

6. 发明授权

US08168654B2 Quinuclidine derivatives binding to mucarinic M3 receptors 失效
标题翻译：奎宁环衍生物与粘蛋白M3受体结合
公开(公告)号：US08168654B2
公开(公告)日：2012-05-01
申请号：US12582291
申请日：2009-10-20
申请人： Stephen P Collingwood , Brian Cox , Urs Baettig , Gurdip Bhalay , Nicholas J Devereux
发明人： Stephen P Collingwood , Brian Cox , Urs Baettig , Gurdip Bhalay , Nicholas J Devereux
IPC分类号： A01N43/90 , A61K31/44 , C07D453/02 , C07D241/02
CPC分类号： C07D453/02
摘要： Compounds of formula I in salt or zwitterionic form wherein, wherein R1, R2, R3, and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：盐或两性离子形式的式I化合物，其中R1，R2，R3和R4具有说明书中所示的含义，可用于治疗由毒蕈碱M3受体介导的病症。还描述了含有化合物的药物组合物和制备该化合物的方法。

7. 发明申请

US20120071479A1 PYRAZINE DERIVATIVES AS ENAC BLOCKERS 有权
标题翻译：作为ENAC阻隔剂的吡嗪衍生物
公开(公告)号：US20120071479A1
公开(公告)日：2012-03-22
申请号：US13232175
申请日：2011-09-14
申请人： Gurdip Bhalay , Lee Edwards , Catherine Howsham , Peter Hunt , Nichola Smith
发明人： Gurdip Bhalay , Lee Edwards , Catherine Howsham , Peter Hunt , Nichola Smith
IPC分类号： A61K31/497 , A61P37/08 , A61P11/12 , A61P29/00 , C07D471/10 , A61K31/5377
CPC分类号： C07D241/26 , C07D403/12 , C07D487/10
摘要： Compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：式I化合物及其药学上可接受的盐和溶剂合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9和R10具有说明书中所示的含义，可用于治疗由阻断上皮钠通道。还描述了含有化合物的药物组合物和用于制备化合物的方法。

8. 发明授权

US07754758B2 Pyrrolidine derivatives acting as CCR3-receptor antagonists 失效
标题翻译：作为CCR3受体拮抗剂的吡咯烷衍生物
公开(公告)号：US07754758B2
公开(公告)日：2010-07-13
申请号：US10585615
申请日：2005-01-28
申请人： Gurdip Bhalay , Andrew Dunstan , Angela Glen , Trevor John Howe , Clive McCarthy
发明人： Gurdip Bhalay , Andrew Dunstan , Angela Glen , Trevor John Howe , Clive McCarthy
IPC分类号： C07D207/12 , A61K31/40
CPC分类号： C07D207/12 , C07D211/26
摘要： Compounds of formula I in free or salt form, wherein T, X, Y, U, R1, R2, m, n and p have the meanings as indicated in the specification, are useful for treating conditions mediated by CCR3. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：游离或盐形式的式I化合物，其中T，X，Y，U，R 1，R 2，m，n和p具有说明书中所示的含义，可用于治疗由CCR3介导的病症。还描述了含有化合物的药物组合物和用于制备化合物的方法。

9. 发明授权

US08546416B2 3-spirocyclic piperidine derivatives as ghrelin receptor agonists 有权
标题翻译： 3-螺环哌啶衍生物作为生长素释放肽受体激动剂
公开(公告)号：US08546416B2
公开(公告)日：2013-10-01
申请号：US13479596
申请日：2012-05-24
申请人： Ameet Vijay Ambarkhane , Gurdip Bhalay , Martin Beckett , James Dale , Ahmed Hamadi , Alessandro Mazzacani , Jeffrey McKenna , Christopher Thomson
发明人： Ameet Vijay Ambarkhane , Gurdip Bhalay , Martin Beckett , James Dale , Ahmed Hamadi , Alessandro Mazzacani , Jeffrey McKenna , Christopher Thomson
IPC分类号： C07D211/00 , C07D213/00 , C07D215/00 , C07D219/00 , C07D221/00 , C07D217/00
CPC分类号： C07D471/10 , A61K31/407 , A61K31/435 , A61K31/55 , A61K45/06 , C07D487/10
摘要： The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
摘要翻译：本发明涉及式（I）的衍生物，其中取代基如说明书中所定义; 制备此类衍生物的方法; 包含这些衍生物的药物组合物; 这种衍生物作为药物; 用于治疗疾病或由生长素释放肽受体介导的疾病的衍生物。

10. 发明申请

US20130012500A1 ORGANIC COMPOUNDS 有权
标题翻译：有机化合物
公开(公告)号：US20130012500A1
公开(公告)日：2013-01-10
申请号：US13613495
申请日：2012-09-13
申请人： Gurdip BHALAY , Emma BUDD , Graham Charles BLOOMFIELD , Stephen Paul COLLINGWOOD , Andrew DUNSTAN , Lee EDWARDS , Peter GEDECK , Catherine HOWSHAM , Peter HUNT , Thomas Anthony HUNT , Paul OAKLEY , Nichola SMITH
发明人： Gurdip BHALAY , Emma BUDD , Graham Charles BLOOMFIELD , Stephen Paul COLLINGWOOD , Andrew DUNSTAN , Lee EDWARDS , Peter GEDECK , Catherine HOWSHAM , Peter HUNT , Thomas Anthony HUNT , Paul OAKLEY , Nichola SMITH
IPC分类号： C07D403/12 , C07D471/10 , C07D413/14 , A61K31/5377 , A61P29/00 , A61P11/00 , A61P11/08 , A61P11/06 , A61P35/00 , A61P27/02 , A61K31/497 , A61K31/551
CPC分类号： C07D519/00 , A61K31/497 , C07D403/12 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：式Ⅰ化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11具有说明书中所述的含义，可用于治疗疾病，对上皮钠通道的阻断作出反应。还描述了含有化合物的药物组合物和用于制备化合物的方法。

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