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1. 发明授权

US06972287B1 Method of inhibiting amyloid protein aggregation and imaging amyloid deposits 失效
标题翻译：抑制淀粉样蛋白聚集和成像淀粉样沉积物的方法
公开(公告)号：US06972287B1
公开(公告)日：2005-12-06
申请号：US10009611
申请日：2000-05-31
申请人： Corinne Elizabeth Augelli-Szafran , Mark Robert Barvian , Christopher Franklin Bigge , Shelly Ann Glase , Shunichiro Hachiya , John Steven Kiely , Takenori Kimura , Yingjie Lai , Annette Theresa Sakkab , Mark James Suto , Larry Craswell Walker , Tomoyuki Yasunaga , Nian Zhuang
发明人： Corinne Elizabeth Augelli-Szafran , Mark Robert Barvian , Christopher Franklin Bigge , Shelly Ann Glase , Shunichiro Hachiya , John Steven Kiely , Takenori Kimura , Yingjie Lai , Annette Theresa Sakkab , Mark James Suto , Larry Craswell Walker , Tomoyuki Yasunaga , Nian Zhuang
IPC分类号： A61K31/196 , A61K31/402 , A61K31/4164 , C07C229/58 , C07C229/62 , C07C229/64 , C07C233/43 , C07C311/51 , C07D209/44 , C07D213/82 , C07D217/02 , C07D233/88 , C07D257/04 , C07D295/135 , C07D317/58 , C07D413/06 , C07D401/10 , A61K31/41 , A61P25/28 , C07D403/10 , C07D413/10
CPC分类号： C07D213/82 , A61K31/196 , A61K31/402 , A61K31/4164 , C07C229/58 , C07C229/62 , C07C229/64 , C07C233/43 , C07C311/51 , C07D209/44 , C07D217/02 , C07D233/88 , C07D257/04 , C07D295/135 , C07D317/58 , C07D413/06
摘要： The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).
摘要翻译：本发明提供使用式（I）的化合物治疗阿尔茨海默病的方法。还提供了使用式（I）化合物和淀粉样沉积物成像方法以及式（I）的新化合物抑制淀粉样蛋白聚集的方法。

2. 发明授权

US5384425A Diurea derivatives useful as medicaments and processes for the preparation thereof 失效
标题翻译：用作药物的二脲衍生物及其制备方法
公开(公告)号：US5384425A
公开(公告)日：1995-01-24
申请号：US64850
申请日：1993-10-07
申请人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
发明人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
IPC分类号： C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07D213/75 , C07C69/017
CPC分类号： C07D213/75 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07C2101/14 , C07C2101/18
摘要： Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## wherein, R.sup.1 and R.sup.2 are the same or different, and each represents C.sup.1 -10 alkyl group, a C.sup.3 -18 cycloalkyl group, or a lower alkyl group substituted by cycloalkyl radical(s);R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and each represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, hydrocarbyl aralkyl group, a pyridyl group, or an unsubstituted or substituted phenyl group, the substituents of the phenyl group being selected from a group consisting of lower alkyl radical, halogen atom-substituted lower alkyl radical, halogen atom, nitro radical, amino radical, mono- or di-lower alkylamino radical, lower acylamino radical, hydroxyl radical, lower alkoxy radical and lower acyloxy radical;X represents an oxygen atom or a sulfur atom, and n.sup.1 and n.sup.2 represent an integer of 1 to 6; and wherein at least one of R.sup.3 -R.sup.6 is a phenyl substituted by acyloxy.
摘要翻译：提供了可由以下通式表示的二脲衍生物及其盐：其中，R 1和R 2相同或不同，各自表示C 1-10烷基，C 3-18环烷基或低级被环烷基取代的烷基; R 3，R 4，R 5和R 6相同或不同，各自表示氢原子，低级烷基，环烷基，烃基芳烷基，吡啶基或未取代或取代的苯基，苯基基团选自低级烷基，卤素原子取代的低级烷基，卤原子，硝基，氨基，一或二低级烷基氨基，低级酰基氨基，羟基，低级烷氧基和低级烷基酰氧基; X表示氧原子或硫原子，n1和n2表示1〜6的整数，并且其中R 3 -R 6中的至少一个是被酰氧基取代的苯基。

3. 发明授权

US6133258A Inhibitor of kainic acid neurotoxicity and pyridothiazine derivative 失效
标题翻译：红藻氨酸神经毒性抑制剂和吡啶并噻嗪衍生物
公开(公告)号：US6133258A
公开(公告)日：2000-10-17
申请号：US68534
申请日：1998-05-13
申请人： Jun-ichi Shishikura , Hiroshi Inami , Tomoyuki Yasunaga , Masaaki Hirano , Shuichi Sakamoto , Kazushige Ohno , Masamichi Okada , Shin-ichi Tsukamoto
发明人： Jun-ichi Shishikura , Hiroshi Inami , Tomoyuki Yasunaga , Masaaki Hirano , Shuichi Sakamoto , Kazushige Ohno , Masamichi Okada , Shin-ichi Tsukamoto
IPC分类号： A61K31/5415 , A61K31/542 , C07D513/04
CPC分类号： A61K31/5415
摘要： Neuroprotective agents based on inhibition of kainic acid neurotoxicity and compounds useful as neuroprotective agents based on inhibition of kainic acid neurotoxicity. An inhibitors of kainic acid neurotoxicity, comprising as an active ingredient a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof, and a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein symbols in the formula have the following respective meanings: the ring A: a pyridine ring; ##STR2## R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or a lower alkyl, cycloalkyl, alkenyl, aryl, carboxyl or lower alkoxycarbonyl group which may have substituent(s), or are not present, with the proviso that R.sup.2 and R.sup.3 may together form a nitrogen-containing heterocyclic group which may have nitrogen atoms as another hetero atom, may be fused with a benzene ring and may have a lower alkyl group as a substituent.
摘要翻译： PCT No.PCT / JP96 / 03339 Sec。 371日期1998年5月13日 102（e）日期1998年5月13日PCT 1996年11月14日PCT PCT。出版物WO97 / 17970 日期1997年5月22日基于抑制红藻氨酸神经毒性的神经保护剂和基于抑制红藻氨酸神经毒性作用的神经保护剂的化合物。作为活性成分的红藻氨酸神经毒性抑制剂，含有下述通式（I）所示的吡哆噻嗪衍生物或其药学上可接受的盐，以及下述通式（I）表示的吡哒嗪衍生物或其药学上可接受的盐其中式中的符号具有以下各自的含义：环A：吡啶环; R 1，R 2，R 3，R 4和R 5可以相同或不同，各自表示氢原子或可以具有取代基或不存在的低级烷基，环烷基，烯基，芳基，羧基或低级烷氧基羰基，条件是R2和R3可以一起形成可以具有氮原子作为另一个杂原子的含氮杂环基，可以与苯环稠合并且可以具有低级烷基作为取代基。

4. 发明授权

US5227492A Diurea derivatives useful as medicaments and processes for the preparation thereof 失效
标题翻译：用作药物的二脲衍生物及其制备方法
公开(公告)号：US5227492A
公开(公告)日：1993-07-13
申请号：US906735
申请日：1992-06-30
申请人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
发明人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
IPC分类号： C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07D213/75
CPC分类号： C07D213/75 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07C2101/14 , C07C2101/18
摘要： Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## Illustrative derivatives include 1,3-bis[[1-cycloheptyl-3-(3-pyridyl)ureido]-methyl]benzene, 1,3-bis[[1-cycloheptyl-3-(2-pyridyl)ureido]-methyl]benzene, and 1,3-bis[[1-cycloheptyl-3-(4-pyridyl)ureido]-methyl]benzene.The above compounds inhibit acyl-coenzyme A cholesterol acyltransferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.
摘要翻译：提供二脲衍生物，其可以由以下通式及其盐表示：示例性衍生物包括1,3-双[[1-环庚基-3-（3-吡啶基）脲基] - 甲基]苯，苯，1,3-双[[1-环庚基-3-（4-吡啶基）脲基] - 甲基]苯。上述化合物抑制酰基辅酶A胆固醇酰基转移酶（ACAT酶），从而控制胆固醇酯对血管中动脉壁平滑肌的积累。

5. 发明授权

US5166429A Diurea derivatives useful as medicaments and processes for the preparation thereof 失效
标题翻译：用作药物的二脲衍生物及其制备方法
公开(公告)号：US5166429A
公开(公告)日：1992-11-24
申请号：US764617
申请日：1991-09-24
申请人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
发明人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
IPC分类号： C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07D213/75
CPC分类号： C07D213/75 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07C2101/14 , C07C2101/18
摘要： Diurea Derivatives represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A chloresterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.
摘要翻译：由以下通式表示的二脲衍生物及其盐：上述化合物抑制酰基辅酶A氯韦斯醇醇酰基转移酶（ACAT酶），从而控制胆固醇酯对血液中动脉壁平滑肌的积累船只。

6. 发明授权

US5091419A Diurea derivatives useful as medicaments and processes for the preparation thereof 失效
标题翻译：作为其制剂的药物和方法有用的DIUREA衍生物
公开(公告)号：US5091419A
公开(公告)日：1992-02-25
申请号：US593516
申请日：1990-10-02
申请人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
发明人： Noriki Ito , Tomoyuki Yasunaga , Yuichi Iizumi , Tomio Araki
IPC分类号： A61K31/17 , C07C211/26 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/06 , C07C335/14 , C07C335/16 , C07D213/75
CPC分类号： C07D213/75 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C335/14 , C07C2101/14 , C07C2101/18
摘要： Diurea derivatives are provided which are represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A cholesterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester on the smooth muscle of arterial wall in the blood vessels.

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