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1. 发明申请

US20120190672A1 FUSED AMINODIHYDROTHIAZINE DERIVATIVES 有权
标题翻译：熔融氨基二氢卟吩衍生物
公开(公告)号：US20120190672A1
公开(公告)日：2012-07-26
申请号：US13354716
申请日：2012-01-20
申请人： Adrian Hall , Christopher Neil Farthing , Jose Luis Castro Pineiro
发明人： Adrian Hall , Christopher Neil Farthing , Jose Luis Castro Pineiro
IPC分类号： A61K31/542 , A61P25/28 , A61P3/10 , C07D513/04
CPC分类号： C07D513/04
摘要： The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C≡N; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
摘要翻译：本发明涉及式（I）的稠合氨基二氢噻嗪衍生物：其中X是氢或氟; A是CH或N; Y是甲基，乙基，一氟甲基，二氟甲基，三氟甲基，二氟乙基，甲氧基，乙氧基，甲氧基甲基或-C≡N; 及其药学上可接受的盐; 该化合物具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

2. 发明申请

US20120202804A1 FUSED AMINODIHYDRO-OXAZINE DERIVATIVES 有权
标题翻译：熔融氨基二氧杂环丁烷衍生物
公开(公告)号：US20120202804A1
公开(公告)日：2012-08-09
申请号：US13386092
申请日：2010-07-21
申请人： John Mark Ellard , Christopher Neil Farthing , Adrian Hall
发明人： John Mark Ellard , Christopher Neil Farthing , Adrian Hall
IPC分类号： A61K31/5365 , A61P25/28 , C07D498/04
CPC分类号： C07D498/04
摘要： A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
摘要翻译：由通式（I）表示的化合物或其药学上可接受的盐或其溶剂合物，其中环A为C 6-14芳基等，L为-NReCO-等（其中Re为氢原子等），环B为C 6-14芳基等，X为C 1-3亚烷基等，Y为单键等，Z为C1-3亚烷基等 R 1和R 2各自独立地为氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等，具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

3. 发明授权

US09079914B2 Fused aminodihydro-oxazine derivatives 有权
标题翻译：熔融氨基二氢恶嗪衍生物
公开(公告)号：US09079914B2
公开(公告)日：2015-07-14
申请号：US13386092
申请日：2010-07-21
申请人： John Mark Ellard , Christopher Neil Farthing , Adrian Hall
发明人： John Mark Ellard , Christopher Neil Farthing , Adrian Hall
IPC分类号： C07D498/04 , A61K31/5365
CPC分类号： C07D498/04
摘要： A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
摘要翻译：由通式表示的化合物或其药学上可接受的盐或其溶剂化物，其中环A是C 6-14芳基等，L是-NReCO-等（其中Re是氢原子或环）B是C 6-14芳基等，X是C 1-3亚烷基等，Y是单键等，Z是C 1-3亚烷基等，R 1 和R 2各自独立地为氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等，具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

4. 发明授权

US08338407B2 Fused aminodihydrothiazine derivatives 有权
标题翻译：融合氨基二氢噻嗪衍生物
公开(公告)号：US08338407B2
公开(公告)日：2012-12-25
申请号：US13354716
申请日：2012-01-20
申请人： Adrian Hall , Christopher Neil Farthing
发明人： Adrian Hall , Christopher Neil Farthing
IPC分类号： C07D513/04 , A61K31/542
CPC分类号： C07D513/04
摘要： The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C≡N; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
摘要翻译：本发明涉及式（I）的稠合氨基二氢噻嗪衍生物：其中X是氢或氟; A是CH或N; Y是甲基，乙基，一氟甲基，二氟甲基，三氟甲基，二氟乙基，甲氧基，乙氧基，甲氧基甲基或-C≡N; 及其药学上可接受的盐; 该化合物具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

5. 发明申请

US20120202828A1 FUSED AMINODIHYDROPYRIMIDONE DERIVATIVES 有权
标题翻译：熔融的氨基二氢咪唑啉酮衍生物
公开(公告)号：US20120202828A1
公开(公告)日：2012-08-09
申请号：US13386199
申请日：2010-07-21
申请人： Jose Luis Castro Pineiro , Adrian Hall , Andrew Madin , Ngoc-Tri Vo
发明人： Jose Luis Castro Pineiro , Adrian Hall , Andrew Madin , Ngoc-Tri Vo
IPC分类号： A61K31/519 , A61P25/28 , C07D491/048
CPC分类号： C07D491/048
摘要： A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1, R2 and Rx are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
摘要翻译：由通式（I）表示的化合物或其药学上可接受的盐或其溶剂合物，其中环A为C 6-14芳基等，L为-NReCO-等（其中Re为氢原子等），环B为C 6-14芳基等，X为C 1-3亚烷基等，Y为单键等，Z为C1-3亚烷基等 R 1，R 2和R 3各自独立地为氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等，具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

6. 发明申请

US20080249138A1 Pyridine Compounds For The Treatment Of Prostaglandin Mediated Diseases 失效
标题翻译：用于治疗前列腺素介导的疾病的吡啶化合物
公开(公告)号：US20080249138A1
公开(公告)日：2008-10-09
申请号：US11766418
申请日：2007-06-21
申请人： Gerard Martin Paul Giblin , Adrian Hall
发明人： Gerard Martin Paul Giblin , Adrian Hall
IPC分类号： A61K31/44 , C07D213/79 , A61P37/00 , A61P19/00 , A61P25/00 , A61P13/12
CPC分类号： C07D213/79 , C07D213/80 , C07D401/04 , C07D413/12
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein X, Y, Z, R2a, R2b, R3a, R3b, R8, R9, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中X，Y，Z，R 2a，R 2b，R 3a， R 3b，R 8，R 9和R x如本说明书中所定义，其中R 1，R 2，R 3，这些化合物的制备，包含这些化合物的药物组合物和这些化合物在医药中的用途。

7. 发明申请

US20050239802A1 (2-((2-alkoxy)-phenyl)-cyclopent-1enyl) aromatic carbo and heterocyclic acid and derivatives 失效
标题翻译：（2 - （（2-烷氧基） - 苯基） - 环戊-1-烯基）芳族碳和杂环酸及其衍生物
公开(公告)号：US20050239802A1
公开(公告)日：2005-10-27
申请号：US10508761
申请日：2003-04-07
申请人： Gerard Martin Giblin , Adrian Hall , David Hurst , Ian Kilford , Xiao Lewell , Alan Taylor , Riccardo Novelli
发明人： Gerard Martin Giblin , Adrian Hall , David Hurst , Ian Kilford , Xiao Lewell , Alan Taylor , Riccardo Novelli
IPC分类号： C07D295/14 , A61K31/19 , A61K31/192 , A61K31/196 , A61K31/4015 , A61K31/435 , A61K31/44 , A61K31/45 , A61K31/455 , A61K31/465 , A61K31/495 , A61K31/4965 , A61K31/505 , A61K31/5375 , A61P3/14 , A61P13/00 , A61P13/12 , A61P19/00 , A61P19/02 , A61P25/04 , A61P25/28 , A61P29/00 , A61P37/00 , A61P43/00 , C07C65/28 , C07C69/94 , C07C229/56 , C07C229/64 , C07C233/00 , C07C233/54 , C07C255/57 , C07C311/00 , C07C311/08 , C07C317/46 , C07C323/62 , C07D207/26 , C07D207/263 , C07D207/27 , C07D211/76 , C07D213/00 , C07D213/79 , C07D213/80 , C07D213/89 , C07D229/00 , C07D237/24 , C07D239/00 , C07D239/28 , C07D241/24 , C07D241/26 , C07D265/28 , C07D295/155 , A61K31/537
CPC分类号： C07D207/27 , C07C65/28 , C07C229/64 , C07C233/54 , C07C255/57 , C07C311/08 , C07C2601/10 , C07D211/76 , C07D213/79 , C07D213/80 , C07D213/89 , C07D237/24 , C07D239/28 , C07D241/24 , C07D241/26 , C07D295/155
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2, Rx, R8, R9 and n are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中A，R 1，R 2，R x，X， 8，R 9和n如说明书中所定义，制备这些化合物的方法，包含这些化合物的药物组合物以及这些化合物在医药中的用途。

8. 发明申请

US20090298866A1 Indole Compounds 审中-公开
标题翻译：吲哚化合物
公开(公告)号：US20090298866A1
公开(公告)日：2009-12-03
申请号：US12373315
申请日：2007-07-09
申请人： Adrian Hall , David Nigel Hurst , Tiziana Scoccitti , Pamela Joan Theobald
发明人： Adrian Hall , David Nigel Hurst , Tiziana Scoccitti , Pamela Joan Theobald
IPC分类号： A61K31/437 , C07D277/28 , C07D277/24 , C07D417/14 , C07D471/04 , A61K31/427 , A61K31/44 , A61P37/04
CPC分类号： C07D417/04 , C07D413/04
摘要： The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein X, R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：本申请涉及式（I）化合物或其药学上可接受的衍生物：其中X，R 1，R 2和R 3如说明书中所定义的式（I），制备这些化合物的方法，药物组合物，包含这些化合物和这些化合物在医药中的应用。

9. 发明申请

US20090281152A1 Indole Compounds Having Affinity to the EP1 Receptor 审中-公开
标题翻译：具有与EP1受体亲和性的吲哚化合物
公开(公告)号：US20090281152A1
公开(公告)日：2009-11-12
申请号：US12373319
申请日：2007-07-09
申请人： Gerard Martin Paul Giblin , Mairi Gibson , Adrian Hall
发明人： Gerard Martin Paul Giblin , Mairi Gibson , Adrian Hall
IPC分类号： A61K31/422 , C07D413/04 , C07D417/04 , A61K31/427 , A61P25/00
CPC分类号： C07D413/04 , C07D417/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein R1, R2 and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中R 1，R 2和R 3如说明书中所定义的式（I），制备这些化合物的方法，包含这些化合物的药物组合物和这些化合物的用途在医学上。

10. 发明申请

US20090099177A1 PYRIDYL COMPOUNDS 审中-公开
标题翻译：吡啶化合物
公开(公告)号：US20090099177A1
公开(公告)日：2009-04-16
申请号：US12299120
申请日：2007-05-02
申请人： Gerard Martin Paul Giblin , Adrian Hall , David Nigel Hurst , Tiziana Scoccitti
发明人： Gerard Martin Paul Giblin , Adrian Hall , David Nigel Hurst , Tiziana Scoccitti
IPC分类号： A61K31/5377 , C07D213/74 , A61K31/44 , C07D413/14 , C07D473/00 , A61K31/52
CPC分类号： C07D213/81 , C07D213/50 , C07D213/74 , C07D213/75 , C07D213/82 , C07D401/04 , C07D401/12 , C07D405/12 , C07D471/04 , C07D473/00 , C07D487/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein R1, and R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中R1和R2和R3如说明书中所定义，制备这些化合物的方法，包含这些化合物的药物组合物以及这些化合物在药物中的用途。

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