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1. 发明申请

US20080182846A1 Preventives or remedies for Alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound 失效
标题翻译：包括含氮杂芳基化合物的阿尔茨海默病或淀粉样蛋白原纤维形成抑制剂的预防或治疗
公开(公告)号：US20080182846A1
公开(公告)日：2008-07-31
申请号：US12068407
申请日：2008-02-06
申请人： Masaki Meguro , Tomichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
发明人： Masaki Meguro , Tomichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
IPC分类号： A61K31/53 , C07D251/18 , A61P25/28
CPC分类号： C07D239/48 , A61K31/50 , A61K31/505 , A61K31/53 , C07D237/20 , C07D237/22 , C07D239/50 , C07D241/20 , C07D251/18 , C07D251/48 , C07D251/52 , C07D251/70
摘要： The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要翻译：本发明涉及阿尔茨海默病的预防药物或补救剂，或淀粉样蛋白原纤维形成抑制剂，其包括作为活性成分的下列通式（I）的化合物或其药理学允许的盐; 以及具有特定取代基的含氮杂芳基衍生物或其药理学上允许的盐，其作为阿尔茨海默氏病的预防剂或治疗剂是有价值的，或作为淀粉样蛋白原纤维形成抑制剂：（其中R 1，和R 2是H或烷基; Z 1和Z 2是H，烷基，烷氧基，卤代烷基或卤代; Z 3 烷氧基，SH，烷硫基，NH 2，单或二烷基氨基，OH或卤素; Z 4和Z 5 >为H或卤素; A为4,6-嘧啶-1,3-二基，1,3,5-三嗪-2,6-二基等）。

2. 发明授权

US08003645B2 Preventives or remedies for Alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound 失效
标题翻译：包括含氮杂芳基化合物的阿尔茨海默病或淀粉样蛋白原纤维形成抑制剂的预防或治疗
公开(公告)号：US08003645B2
公开(公告)日：2011-08-23
申请号：US12068407
申请日：2008-02-06
申请人： Masaki Meguro , Tomichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
发明人： Masaki Meguro , Tomichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
IPC分类号： C07D251/00 , C07D251/18 , C07D251/48
CPC分类号： C07D239/48 , A61K31/50 , A61K31/505 , A61K31/53 , C07D237/20 , C07D237/22 , C07D239/50 , C07D241/20 , C07D251/18 , C07D251/48 , C07D251/52 , C07D251/70
摘要： The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要翻译：本发明涉及阿尔茨海默病的预防药物或补救剂，或淀粉样蛋白原纤维形成抑制剂，其包括作为活性成分的下列通式（I）的化合物或其药理学允许的盐; 以及具有特定取代基的含氮杂芳基衍生物或其药学上允许的盐，其作为阿尔茨海默氏病的预防剂或治疗剂是有价值的，或作为淀粉样蛋白原纤维形成抑制剂：（其中，R 1和R 2为H或烷基; Z 1 Z 2是H，烷基，烷氧基，卤代烷基或卤代; Z 3是烷氧基，SH，烷硫基，NH 2，一或二烷基氨基，OH或卤素; Z 4和Z 5是H或卤素; A是4,6- -1,3-二基，1,3,5-三嗪-2,6-二基等）。

3. 发明申请

US20110275641A1 Preventives or remedies for Alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound 审中-公开
公开(公告)号：US20110275641A1
公开(公告)日：2011-11-10
申请号：US13067111
申请日：2011-05-10
申请人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
发明人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
IPC分类号： A61K31/53 , A61K31/50 , A61P25/28 , A61P25/02 , A61P7/00 , A61P25/00 , A61P35/00 , A61P9/00 , A61K31/505 , A61P3/10
CPC分类号： C07D239/48 , A61K31/50 , A61K31/505 , A61K31/53 , C07D237/20 , C07D237/22 , C07D239/50 , C07D241/20 , C07D251/18 , C07D251/48 , C07D251/52 , C07D251/70
摘要： The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

4. 发明申请

US20090286809A1 Preventives or remedies for alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound 审中-公开
公开(公告)号：US20090286809A1
公开(公告)日：2009-11-19
申请号：US12458891
申请日：2009-07-27
申请人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
发明人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
IPC分类号： A61K31/4965 , A61K31/505 , C07D239/02 , C07D237/02 , C07D241/02 , A61K31/50 , A61P25/28
CPC分类号： C07D239/48 , A61K31/50 , A61K31/505 , A61K31/53 , C07D237/20 , C07D237/22 , C07D239/50 , C07D241/20 , C07D251/18 , C07D251/48 , C07D251/52 , C07D251/70
摘要： The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

5. 发明授权

US07589105B2 Preventives or remedies for alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound 失效
标题翻译：阿尔茨海默病或淀粉样蛋白原纤维形成抑制剂的预防或补救措施，其包括含氮杂芳基化合物
公开(公告)号：US07589105B2
公开(公告)日：2009-09-15
申请号：US10497183
申请日：2002-11-25
申请人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
发明人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
IPC分类号： A01N43/60 , A01N43/42
CPC分类号： C07D239/48 , A61K31/50 , A61K31/505 , A61K31/53 , C07D237/20 , C07D237/22 , C07D239/50 , C07D241/20 , C07D251/18 , C07D251/48 , C07D251/52 , C07D251/70
摘要： Pharmaceutical compositions and methods of treatment are provided for treating amyloidosis, containing, as an active ingredient, at least one nitrogen-containing heteroaryl compound represented by the following general formula or a pharmacologically permitted salt thereof; together with nitrogen-containing heteroaryl derivatives, and pharmacologically permitted salts thereof: where, R1, R2, Z1-Z5, and A are as defined herein.
摘要翻译：提供药物组合物和治疗方法用于治疗淀粉样变性，其含有至少一种由以下通式表示的含氮杂芳基化合物或其药理学允许的盐作为活性成分; 连同含氮杂芳基衍生物及其药理学允许的盐：其中，R1，R2，Z1-Z5和A如本文所定义。

6. 发明申请

US20050054732A1 Preventives or remidies for alzheimer's disease or amyloid protein fibrosis inhibitors containing nitrogen-containing heteroaryl compounds 失效
标题翻译：含有含氮杂芳基化合物的阿尔茨海默氏病或淀粉样蛋白纤维化抑制剂的预防或保护
公开(公告)号：US20050054732A1
公开(公告)日：2005-03-10
申请号：US10497183
申请日：2002-11-25
申请人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
发明人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
IPC分类号： A61K31/50 , A61K31/505 , A61K31/53 , A61P25/28 , A61P43/00 , C07D237/20 , C07D237/22 , C07D239/48 , C07D239/50 , C07D241/20 , C07D251/18 , C07D251/48 , C07D251/52 , C07D251/70 , A61K31/137
CPC分类号： C07D239/48 , A61K31/50 , A61K31/505 , A61K31/53 , C07D237/20 , C07D237/22 , C07D239/50 , C07D241/20 , C07D251/18 , C07D251/48 , C07D251/52 , C07D251/70
摘要： The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要翻译：本发明涉及阿尔茨海默病的预防药物或补救剂，或淀粉样蛋白原纤维形成抑制剂，其包括作为活性成分的下列通式（I）的化合物或其药理学允许的盐; 以及具有特定取代基的含氮杂芳基衍生物或其药学上允许的盐，其作为阿尔茨海默病的预防剂或治疗药物是有价值的，或作为淀粉样蛋白原纤维形成抑制剂：（其中，R 1和R 2， Z 1和Z 2是H，烷基，烷氧基，卤代烷基或卤代; Z 3是烷氧基，SH，烷硫基，NH 2，一或二烷基氨基，OH或卤素; Z 4和Z 5是H或卤素; A是4,6-嘧啶-1,3-二基，1,3,5-三嗪-2,6-二基等）。

7. 发明申请

US20110275640A1 Preventives or remedies for alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound 审中-公开
标题翻译：阿尔茨海默病或淀粉样蛋白原纤维形成抑制剂的预防或补救措施，其包括含氮杂芳基化合物
公开(公告)号：US20110275640A1
公开(公告)日：2011-11-10
申请号：US13067110
申请日：2011-05-10
申请人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
发明人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
IPC分类号： A61K31/53 , A61K31/50 , A61P25/28 , A61P3/10 , A61P25/02 , A61P13/12 , A61P25/00 , A61P35/00 , A61P9/00 , A61K31/505 , A61P7/00
CPC分类号： C07D239/48 , A61K31/50 , A61K31/505 , A61K31/53 , C07D237/20 , C07D237/22 , C07D239/50 , C07D241/20 , C07D251/18 , C07D251/48 , C07D251/52 , C07D251/70
摘要： The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要翻译：本发明涉及阿尔茨海默病的预防药物或补救剂，或淀粉样蛋白原纤维形成抑制剂，其包括作为活性成分的下列通式（I）的化合物或其药理学允许的盐; 以及具有特定取代基的含氮杂芳基衍生物或其药学上允许的盐，其作为阿尔茨海默氏病的预防剂或治疗剂是有价值的，或作为淀粉样蛋白原纤维形成抑制剂：（其中，R 1和R 2为H或烷基; Z 1 Z 2是H，烷基，烷氧基，卤代烷基或卤代; Z 3是烷氧基，SH，烷硫基，NH 2，一或二烷基氨基，OH或卤素; Z 4和Z 5是H或卤素; A是4,6- -1,3-二基，1,3,5-三嗪-2,6-二基等）。

8. 发明申请

US20090286794A1 Preventives or remedies for alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound 审中-公开
标题翻译：阿尔茨海默病或淀粉样蛋白原纤维形成抑制剂的预防或补救措施，其包括含氮杂芳基化合物
公开(公告)号：US20090286794A1
公开(公告)日：2009-11-19
申请号：US12458890
申请日：2009-07-27
申请人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
发明人： Masaki Meguro , Tomiichiro Oda , Yasuhiro Nakagami , Shinji Marumoto , Kazuo Koyama , Isao Kaneko
IPC分类号： A61K31/53 , C07D251/18 , C07D241/10 , A61K31/4965 , C07D239/02 , C07D239/42
CPC分类号： C07D239/48 , A61K31/50 , A61K31/505 , A61K31/53 , C07D237/20 , C07D237/22 , C07D239/50 , C07D241/20 , C07D251/18 , C07D251/48 , C07D251/52 , C07D251/70
摘要： The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要翻译：本发明涉及阿尔茨海默病的预防药物或补救剂，或淀粉样蛋白原纤维形成抑制剂，其包括作为活性成分的下列通式（I）的化合物或其药理学允许的盐; 以及具有特定取代基的含氮杂芳基衍生物或其药学上允许的盐，其作为阿尔茨海默氏病的预防剂或治疗剂是有价值的，或作为淀粉样蛋白原纤维形成抑制剂：（其中，R 1和R 2为H或烷基; Z 1 Z 2是H，烷基，烷氧基，卤代烷基或卤代; Z 3是烷氧基，SH，烷硫基，NH 2，一或二烷基氨基，OH或卤素; Z 4和Z 5是H或卤素; A是4,6- -1,3-二基，1,3,5-三嗪-2,6-二基等）。

9. 发明授权

US07514475B2 Benzylamine analogues 失效
标题翻译：苄胺类似物
公开(公告)号：US07514475B2
公开(公告)日：2009-04-07
申请号：US11583499
申请日：2006-10-19
申请人： Kazuo Koyama , Shinji Marumoto , Narihiro Toda , Hiroshi Kogen , Keiko Suzuki
发明人： Kazuo Koyama , Shinji Marumoto , Narihiro Toda , Hiroshi Kogen , Keiko Suzuki
IPC分类号： A61K31/137 , C07C205/04
CPC分类号： C07C219/30 , C07C271/44 , C07C323/20 , C07C323/25 , C07C333/04 , C07D213/64 , C07D213/68 , C07D215/20 , C07D317/58 , C07D333/38
摘要： A compound of the formula (I): wherein R1 is a C1-C6 alkyl, an amino, a (C1-C6 alkyl)amino, a di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and are a hydrogen or a C1-C6 alkyl; Arom is an unsubstituted or substituted aryl or an unsubstituted or substituted heteroaryl; wherein the substituted aryl is substituted at 1 to 5 positions and the substituted heteroaryl is substituted at 1 to 3 positions; wherein the heteroaryl is furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; and wherein the substituents of the substituted aryl and of the substituted heteroaryl are independently halogen, C1-C6 alkyl, halogeno C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C3 alkylenedioxy, C1-C7 alkanoyl, C2-C7 alkyloxycarbonyl, amino, C1-C7 alkanoylamino, hydroxyl, mercapto, cyano, nitro or carboxyl; A is an ethylene or propylene; Ra is a hydrogen, a C1-C6 alkyl or a C2-C6 alkenyl; E is a single bond, an oxygen, a sulfur or —NR4—, wherein R4 is a hydrogen or a C1-C7 alkanoyl; X1 and X2 are the same or different and are an oxygen or a sulfur, or a pharmacologically acceptable salt or ester thereof.
摘要翻译：式（I）的化合物：其中R1是C1-C6烷基，氨基，（C1-C6烷基）氨基，二（C1-C6烷基）氨基或含氮饱和杂环; R2和R3相同或不同，为氢或C1-C6烷基; Arom是未取代或取代的芳基或未取代或取代的杂芳基; 其中取代的芳基在1至5个位置被取代，并且取代的杂芳基在1至3个位置被取代; 吡唑基，咪唑基，恶唑基，异恶唑基，噻唑基，异噻唑基，1,2,3-恶二唑基，吡喃基，吡啶基，哒嗪基，嘧啶基，吡嗪基或喹啉基;其中杂芳基为呋喃基，噻吩基，吡咯基，并且其中取代的芳基和取代的杂芳基的取代基独立地为卤素，C 1 -C 6烷基，卤代C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6烷硫基，C 1 -C 3亚烷基二氧基，C 1 -C 7烷酰基， C7烷氧基羰基，氨基，C1-C7烷酰基氨基，羟基，巯基，氰基，硝基或羧基; A是乙烯或丙烯; R a是氢，C 1 -C 6烷基或C 2 -C 6烯基; E是单键，氧，硫或-NR4-，其中R4是氢或C1-C7烷酰基; X1和X2相同或不同，为氧或硫，或其药理学上可接受的盐或酯。

10. 发明申请

US20080255095A1 Benzylamine analogues 审中-公开
标题翻译：苄胺类似物
公开(公告)号：US20080255095A1
公开(公告)日：2008-10-16
申请号：US11820218
申请日：2007-06-18
申请人： Kazuo Koyama , Shinji Marumoto , Narihiro Toda , Hiroshi Kogen , Keiko Suzuki
发明人： Kazuo Koyama , Shinji Marumoto , Narihiro Toda , Hiroshi Kogen , Keiko Suzuki
IPC分类号： A61K31/55 , C07D333/22 , C07D215/38 , C07D263/34 , A61K31/50 , A61P25/28 , A61K31/4965 , C07D261/02 , C07D277/00 , C07D275/02
CPC分类号： C07C219/30 , C07C271/44 , C07C323/20 , C07C323/25 , C07C333/04 , C07D213/64 , C07D213/68 , C07D215/20 , C07D317/58 , C07D333/38
摘要： A compound of the formula (I): wherein R1 is C1-C6 alkyl, amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are hydrogen or C1-C6 alkyl; Arom is phenyl, idenyl, napthyl, phenanthrenyl, furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; A is C1-C6 alkylene; Ra is hydrogen, C1-C6 alkyl or C2-C6 alkenyl; E is a single bond, oxygen, sulfur or —NR4—, wherein R4 is hydrogen or C1-C7 alkanoyl; X1 and X2 are oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof.
摘要翻译：式（I）的化合物：其中R 1是C 1 -C 6烷基，氨基，（C 1）（C 1 -C 6烷基）氨基或含氮饱和杂环基;（C 1 -C 6烷基）氨基， R 2和R 3是氢或C 1 -C 6烷基; 芳基是苯基，烯基，萘基，菲基，呋喃基，噻吩基，吡咯基，氮杂基，吡唑基，咪唑基，恶唑基，异恶唑基，噻唑基，异噻唑基，1,2,3-恶二唑基，吡喃基，吡啶基，哒嗪基，嘧啶基，吡嗪基或喹啉基。 A是C 1 -C 6亚烷基; R a是氢，C 1 -C 6烷基或C 2 -C 6烷基或C 2 -C 6 - 链烯基; E是单键，氧，硫或-NR 4 - ，其中R 4是氢或C 1 -C 7 烷酰基; X 1和X 2是氧或硫; 或其药理学上可接受的盐或酯。

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