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1. 发明授权

US07504437B2 Benzylamine analogues 失效
标题翻译：苄胺类似物
公开(公告)号：US07504437B2
公开(公告)日：2009-03-17
申请号：US10629108
申请日：2003-07-28
申请人： Kazuo Koyama , Shinji Marumoto , Narihiro Toda , Keiko Suzuki
发明人： Kazuo Koyama , Shinji Marumoto , Narihiro Toda , Keiko Suzuki
IPC分类号： A61K31/136 , C07C211/03
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 represents C1–C6 alkyl, amino(C1–C6 alkyl)amino, di(C1–C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and represent hydrogen or C1–C6 alkyl; Ra represents C1–C6 alkyl or C2–C6 alkenyl or together with R2 represents a C1–C3 alkylene; Arom represents aryl or heteroaryl; A represents a C1–C6 alkylene; E represents a single bond, oxygen, sulfur or R4NR4—, wherein R4 is hydrogen or C1–C7 alkenoyl; X1 and X2 are the same or different and represent oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof. The compound has superior acetylcholinesterase inhibitory action and selective serotonin reuptake inhibitory action, and is useful for treating or preventing Alzheimer's disease, depression, Huntington's chorea, Pick's disease, tardive dyskinesia, compulsive disorders or panic disorders.
摘要翻译：式（I）的化合物：其中R1表示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，表示氢或C1-C6烷基; R a表示C 1 -C 6烷基或C 2 -C 6烯基或与R 2表示C 1 -C 3亚烷基; 芳基表示芳基或杂芳基; A表示C1-C6亚烷基; E表示单键，氧，硫或R 4 NR 4 - ，其中R 4是氢或C 1 -C 7链烯酰基; X1和X2相同或不同，代表氧或硫; 或其药理学上可接受的盐或酯。该化合物具有优异的乙酰胆碱酯酶抑制作用和选择性5-羟色胺再摄取抑制作用，可用于治疗或预防阿尔茨海默病，抑郁症，亨廷顿舞蹈病，皮克病，迟发性运动障碍，强迫症或恐慌症。

2. 发明申请

US20090149444A1 Benzylamine analogues 审中-公开
标题翻译：苄胺类似物
公开(公告)号：US20090149444A1
公开(公告)日：2009-06-11
申请号：US12322173
申请日：2009-01-29
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 , A61P25/28 , C07D223/16 , C07C271/44 , A61K31/27
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 represents a C1-C6 alkyl, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and represent hydrogen or a C1-C6 alkyl; Ra represents hydrogen, C1-C6 alkyl or C2-C6 alkenyl or together with R2 represents a C1-C3 alkylene; Arom represents a heteroaryl; A represents a C1-C6 alkylene; E represents a single bond, oxygen, sulphur or R4NR4—, wherein R4 is hydrogen or C1-C7 alkenoyl; X1 and X2 both represent oxygen; X2 is attached at the 3-position or the 4-position; or a pharmacologically acceptable salt or ester thereof. The compound has superior acetylcholinesterase inhibitory action and selective serotonin reuptake inhibitory action, and is useful for treating Alzheimer's disease, depression, Huntington's chorea, Pick's disease, tardive dyskinesia, compulsive disorders or panic disorders.
摘要翻译：式（I）的化合物：其中R1表示C1-C6烷基，（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，表示氢或C1-C6烷基; R a表示氢，C 1 -C 6烷基或C 2 -C 6烯基或与R 2表示C 1 -C 3亚烷基; Arom表示杂芳基; A表示C1-C6亚烷基; E表示单键，氧，硫或R 4 NR 4 - ，其中R 4是氢或C 1 -C 7链烯酰基; X1和X2都代表氧; X2位于3位或4位; 或其药理学上可接受的盐或酯。该化合物具有优异的乙酰胆碱酯酶抑制作用和选择性5-羟色胺再摄取抑制作用，可用于治疗阿尔茨海默病，抑郁症，亨廷顿氏舞蹈病，皮克病，迟发性运动障碍，强迫症或恐慌症。

3. 发明申请

US20070037795A1 Benzylamine analogues 失效
公开(公告)号：US20070037795A1
公开(公告)日：2007-02-15
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： C07D333/22 , C07D215/38 , C07D277/00 , C07D275/02 , A61K31/55 , C07D263/34 , C07D261/02 , A61K31/50 , A61K31/4965
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 (1): 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.

4. 发明申请

US20070037793A1 Benzylamine analogues 失效
公开(公告)号：US20070037793A1
公开(公告)日：2007-02-15
申请号：US11583404
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： A61K31/55 , C07D223/16
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 group, an amino group, a (C1-C6 alkyl)amino group, a di(C1-C6 alkyl)amino group or a nitrogen-containing saturated heterocyclic group; R3 is a hydrogen atom or a C1-C6 alkyl group; Arom is an unsubstituted or substituted aryl group or an unsubstituted or substituted heteroaryl group; wherein the substituted aryl group is substituted at 1 to 5 positions and the substituted heteroaryl group is substituted at 1 to 3 positions; and wherein the substituents of the aryl group and of the heteroaryl group are independently selected from the group consisting of halogen atom, 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 and carboxyl; A is a C1-C6 alkylene group; Ra together with R2 is a C2-C3 alkylene group containing a double bond; E is a single bond, an oxygen atom, a sulfur atom or a group of the formula: —NR4—, wherein R4 is a hydrogen atom or a C1-C7 alkanoyl group; X1 and X2 are the same or different and are an oxygen atom or a sulfur atom, or a pharmacologically acceptable salt or ester thereof.

5. 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。

6. 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。

7. 发明授权

US07504393B2 Benzylamine analogues 失效
标题翻译：苄胺类似物
公开(公告)号：US07504393B2
公开(公告)日：2009-03-17
申请号：US11583404
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： A61K31/55 , A61K31/4704 , C07D215/06 , C07D223/04
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 group, an amino group, a (C1-C6 alkyl)amino group, a di(C1-C6 alkyl)amino group or a nitrogen-containing saturated heterocyclic group; R3 is a hydrogen atom or a C1-C6 alkyl group; Arom is an unsubstituted or substituted aryl group or an unsubstituted or substituted heteroaryl group; wherein the substituted aryl group is substituted at 1 to 5 positions and the substituted heteroaryl group is substituted at 1 to 3 positions; and wherein the substituents of the aryl group and of the heteroaryl group are independently selected from the group consisting of halogen atom, 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 and carboxyl; A is a C1-C6 alkylene group; Ra together with R2 is a C2-C3 alkylene group containing a double bond; E is a single bond, an oxygen atom, a sulfur atom or a group of the formula: —NR4—, wherein R4 is a hydrogen atom or a C1-C7 alkanoyl group; X1 and X2 are the same or different and are an oxygen atom or a sulfur atom, 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组; R3是氢原子或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，取代的杂芳基在1至3个位置被取代; 并且其中芳基和杂芳基的取代基独立地选自卤素原子，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，C 2 -C 7烷氧基羰基，氨基，C 1 -C 7烷酰氨基，羟基，巯基，氰基，硝基和羧基; A是C1-C6亚烷基; R a与R 2一起是含有双键的C 2 -C 3亚烷基; E是单键，氧原子，硫原子或式-NR4-基团，其中R4是氢原子或C1-C7烷酰基; X1和X2相同或不同，为氧原子或硫原子，或其药理学上可接受的盐或酯。

8. 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）。

9. 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).

10. 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）。

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