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1. 发明授权

US5462934A Condensed heterocyclic ketone derivatives and their use 失效
标题翻译：缩合杂环酮衍生物及其用途
公开(公告)号：US5462934A
公开(公告)日：1995-10-31
申请号：US026041
申请日：1993-03-04
申请人： Giichi Goto , Masaomi Miyamoto , Yuji Ishihara
发明人： Giichi Goto , Masaomi Miyamoto , Yuji Ishihara
IPC分类号： C07D209/08 , C07D215/08 , C07D223/16 , C07D225/06 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D417/12 , C07D471/10 , A61K31/55 , C07D401/10 , C07D403/10
CPC分类号： C07D223/16 , C07D209/08 , C07D215/08 , C07D225/06 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D417/12 , C07D471/10
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is H or an optionally substituted hydrocarbon or acyl group; ring A is an optionally further substituted benzene ring; n is an integer of 1 to 10; R.sup.2, R.sup.3 and R.sup.4 are H or an optionally substituted hydrocarbon group; R.sup.3 and R.sup.4 may form an optionally substituted heterocyclic group, taken together with the adjacent nitrogen atom; k is an integer of 0 to 3; and m is an integer of 1 to 8; provided that when k=0 and m=2, n is an integer of not less than 2 or a pharmaceutically acceptable salt thereof, exhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic/prophylactic medicaments of senile dementia.
摘要翻译：下式的化合物：其中R 1是H或任选取代的烃或酰基; 环A是任选进一步取代的苯环; n为1〜10的整数。 R2，R3和R4是H或任选取代的烃基; R 3和R 4可以与相邻的氮原子一起形成任选取代的杂环基; k为0〜3的整数， m为1〜8的整数。条件是当k = 0且m = 2时，n是不小于2的整数或其药学上可接受的盐，其具有优异的胆碱酯酶抑制活性和单胺再摄取抑制活性，因此可用作老年性痴呆的治疗/预防药物。

2. 发明授权

US5441967A Cyclic amine compounds and their use 失效
标题翻译：环胺化合物及其用途
公开(公告)号：US5441967A
公开(公告)日：1995-08-15
申请号：US171163
申请日：1993-12-22
申请人： Giichi Goto , Hidefumi Yukimasa , Tetsuji Imamoto
发明人： Giichi Goto , Hidefumi Yukimasa , Tetsuji Imamoto
IPC分类号： C12N9/99 , A61K31/00 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/4465 , A61K31/451 , A61P9/00 , A61P25/28 , C07D211/26 , C07D211/32 , C07D211/70 , C07D213/36 , C07D213/38 , C07D213/50 , C07D521/00 , C07D401/04
CPC分类号： C07D231/12 , C07D211/26 , C07D211/32 , C07D211/70 , C07D213/38 , C07D213/50 , C07D233/56 , C07D249/08
摘要： 1. A cyclic amine compound of the formula ##STR1## wherein B means a saturated or unsaturated 5- to 7-membered aza-heterocyclic group which may be substituted; A means a bond or an alkylene or alkenylene group which may be substituted by hydrocarbon residues, oxo, hydroxyimino, and/or hydroxy, .sub.-- means either a single bond or a double bond (provided that when A means a bond, .sub.-- means a single bond); R.sub.2 and R.sub.3 independently mean a hydrogen atom or a hydrocarbon residue which may be substituted (provided that both of R.sub.2 and R.sub.3 are not hydrogen atoms) or jointly form a cyclic amino group together with the adjacent nitrogen atom, n is 0, 1 or 2 and p is 1 or 2 or a physiologically acceptable salt thereof.The compounds are useful for therapy of cerebral edema, acute symptoms in cerebral apoplexy and protection of brain and nerve cell, or useful as anticholinesterase or as brain function-improving agent.
摘要翻译： 1.下式的环胺化合物其中B表示可被取代的饱和或不饱和的5-至7-元氮杂杂环基; A表示可以被烃残基，氧代，羟基亚氨基和/或羟基取代的键或亚烷基或亚烯基， - 表示单键或双键（条件是当A表示键时， - 表示单键键）; R2和R3独立地表示氢原子或可被取代的烃残基（条件是R2和R3都不是氢原子）或与相邻的氮原子一起形成环氨基，n是0,1或2 和p为1或2或其生理上可接受的盐。该化合物可用于治疗脑水肿，脑中风的急性症状和保护脑和神经细胞，或用作抗胆碱酯酶或脑功能改善剂。

3. 发明授权

US5273974A Condensed heterocyclic compounds, their production and use 失效
标题翻译：稠合杂环化合物，其生产和使用
公开(公告)号：US5273974A
公开(公告)日：1993-12-28
申请号：US796430
申请日：1991-11-22
申请人： Giichi Goto , Yuji Ishihara , Masaomi Miyamoto
发明人： Giichi Goto , Yuji Ishihara , Masaomi Miyamoto
IPC分类号： A61K31/445 , A61K31/335 , A61K31/38 , A61K31/395 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/452 , A61K31/47 , A61K31/55 , A61P25/28 , A61P43/00 , C07D211/04 , C07D401/06 , C07D401/14 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/00 , C07D493/00 , C07D495/00 , C07D401/10 , C07D405/10 , C07D409/10
CPC分类号： C07D401/06 , C07D401/14 , C07D405/06 , C07D409/06 , Y02P20/55
摘要： A condensed heterocyclic derivative of the formula (I): ##STR1## wherein X is an oxygen atom, a sulfur atom or R.sup.1 --N

4. 发明授权

US5180746A Aralkylamine compounds 失效
标题翻译： ARALKYLAMINE化合物
公开(公告)号：US5180746A
公开(公告)日：1993-01-19
申请号：US480564
申请日：1990-02-15
申请人： Giichi Goto , Akinobu Nagaoka , Yuji Ishihara
发明人： Giichi Goto , Akinobu Nagaoka , Yuji Ishihara
IPC分类号： C12N9/99 , A61K31/00 , A61K31/33 , A61K31/357 , A61K31/36 , A61K31/40 , A61P25/00 , A61P25/28 , C07C211/30 , C07C217/58 , C07C217/74 , C07C225/12 , C07C225/18 , C07D295/112 , C07D295/12 , C07D317/70 , C07D521/00
CPC分类号： C07D295/112 , C07C217/74 , C07C225/18 , C07D317/70 , C07C2102/08
摘要： An aralkylamine compound of the formula ##STR1## wherein R.sup.1 means a hydrogen atom or a lower alkyl group; R.sup.2 means an aromatic group which may be substituted; R.sup.3 means a hydrogen atom, a lower alkyl group or an aromatic group which may be substituted; n means an integer of 0 to 7; ring A means a five-through eight-membered cyclic group which may be substituted and may contain one or two hetero atom(s) of O and S atoms as the ring-constituents; and ring B means a benzene ring which may be substituted, or a salt thereof, which is useful as an cholinesterase inhibitor and a cerebral function ameliorating agent.
摘要翻译：式IMA的芳烷基胺化合物，其中R 1表示氢原子或低级烷基; R2表示可以被取代的芳基; R3表示氢原子，低级烷基或可被取代的芳基; n表示0〜7的整数，环A表示可以被取代的五元至八元环基，并且可以含有一个或两个O原子和S原子作为环组成的杂原子; 环B表示作为胆碱酯酶抑制剂和脑功能改善剂有用的可被取代的苯环或其盐。

5. 发明授权

US5177087A Cyclic amine compounds and their use 失效
标题翻译：循环胺化合物及其用途
公开(公告)号：US5177087A
公开(公告)日：1993-01-05
申请号：US461114
申请日：1990-01-04
申请人： Giichi Goto , Hidefumi Yukimasa , Tetsuji Imamoto
发明人： Giichi Goto , Hidefumi Yukimasa , Tetsuji Imamoto
IPC分类号： C12N9/99 , A61K31/00 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/4465 , A61K31/451 , A61P9/00 , A61P25/28 , C07D211/26 , C07D211/32 , C07D211/70 , C07D213/36 , C07D213/38 , C07D213/50 , C07D521/00
CPC分类号： C07D231/12 , C07D211/26 , C07D211/32 , C07D211/70 , C07D213/38 , C07D213/50 , C07D233/56 , C07D249/08
摘要： There is provided a cyclic amine compound of the formula ##STR1## wherein B means a saturated or unsaturated 5- to 7-membered aza-heterocyclic group which may be substituted; A means a bond or an alkylene or alkenylene group which may be substituted by hydrocarbon residues, oxo, hydroxyimino, and/or hydroxy, means either a single bond or a double bond (provided that when A means a bond, means a single bond); R.sub.2 and R.sub.3 independently mean a hydrogen atom or a hydrocarbon residue which may be substituted (provided that both of R.sub.2 and R.sub.3 are not hydrogen atoms) or jointly form a cyclic amino group together with the adjacent nitrogen atom, n is 0, 1 or 2 and p is 1 or 2 or a physiologically acceptable salt thereof.The compounds are useful for therapy of cerebral edema, acute symptoms in cerebral apoplexy and protection of brain and nerve cell, or useful as anticholinesterase or as brain function-improving agent.

6. 发明授权

US5116861A Nitrosothiol derivatives and their use 失效
标题翻译：硝基苯酚衍生物及其用途
公开(公告)号：US5116861A
公开(公告)日：1992-05-26
申请号：US562626
申请日：1990-08-03
申请人： Giichi Goto , Shigenori Ohkawa , Shoji Fukumoto
发明人： Giichi Goto , Shigenori Ohkawa , Shoji Fukumoto
IPC分类号： A61K38/00 , C07C381/00 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/093
CPC分类号： C07K5/0819 , C07C381/00 , C07K5/0215 , C07K5/0606 , A61K38/00
摘要： Novel nitrosothiol derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrogen atom, an acyl group or a hydrocarbon residue which may be substituted; X.sup.1 is a hydrogen atom, an acyl group, a lower alkoxy group or a hydrocarbon residue which may be substituted; X.sup.2 is an acyl group or a carboxyl group which may be esterified or which may form an amide; with proviso that when X.sup.2 is a carboxyl group X.sup.1 is not a hydrogen atom or acetyl group and that when both R.sup.1 and R.sup.2 are hydrogen atoms X.sup.1 is not acetyl group or .gamma.-glutamyl group, and salts thereof, show excellent hypotensive action, antiarrhythmic action, anti-anginal action, cardiotonic action or coronary vasodilation, thus being useful as therapeutic or prophylactic agents for the cardiovascular diseases such as hypertension and angina pectoris.

7. 发明授权

US5059627A Nerve growth factor secretion inducing composition 失效
标题翻译：神经生长因子分泌诱导组成
公开(公告)号：US5059627A
公开(公告)日：1991-10-22
申请号：US487249
申请日：1990-03-02
申请人： Giichi Goto , Kyozo Hayashi
发明人： Giichi Goto , Kyozo Hayashi
IPC分类号： A61K31/05 , A61K31/047 , A61K31/085 , A61K31/09 , A61K31/12 , A61K31/122 , A61K31/215 , A61K31/44 , A61K31/66 , A61P25/00 , A61P25/28 , A61P43/00
CPC分类号： A61K31/12
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group; R.sup.2 is a hydrogen atom or an alkyl or alkenyl group which may be substituted; R.sup.3 and R.sup.4 each independently means a lower alkyl or lower alkoxy group or, taken together, mean a butadienylene group; and X.sup.1 and X.sup.2 each means a free hydroxy group or an esterified or etherified hydroxy group, has nerve growth factor secretion inducing activity, and a mammal suffering from degenerative nervous system disorders such as senile dementia, Alzheimer's disease, etc. is treated by administering said compound to said mammal.
摘要翻译：下式的化合物：其中R1是低级烷基;其中R1是低级烷基; R2是氢原子或可被取代的烷基或烯基; R 3和R 4各自独立地表示低级烷基或低级烷氧基，或者一起表示丁二烯基; X1和X2各自表示游离羟基或酯化或醚化的羟基，具有神经生长因子分泌诱导活性，并且通过施用所述的方法治疗患有退行性神经系统疾病如老年痴呆，阿尔茨海默氏病等的哺乳动物，与所述哺乳动物复合。

8. 发明授权

US06271266B1 Use of idebenone and analogues against &bgr; amyloid induced cytotoxicity 失效
标题翻译：使用艾地苯醌和类似物对β淀粉样蛋白诱导的细胞毒性
公开(公告)号：US06271266B1
公开(公告)日：2001-08-07
申请号：US09180463
申请日：1998-11-09
申请人： Masaomi Miyamoto , Keisuke Hirai , Giichi Goto
发明人： Masaomi Miyamoto , Keisuke Hirai , Giichi Goto
IPC分类号： A61K31185
CPC分类号： A61K31/047 , A61K31/122
摘要： A compound of the formula: wherein R1 represents a lower alkyl; R2 represents H, an optionally substituted alkyl or an optionally substituted alkenyl; R3 and R4 each represents an optionally substituted lower alkyl or a lower alkoxy, or R3 and R4 form, taken together, an optionally substituted butadienylene; and X1 and X2 each represents an optionally esterified or etherified hydroxy, or a salt thereof is useful for protecting cells from the cytotoxicity of &bgr;-amyloid protein.
摘要翻译：下式的化合物：其中R 1表示低级烷基; R 2表示H，任选取代的烷基或任选取代的烯基; R 3和R 4各自表示任选取代的低级烷基或低级烷氧基，或者R 3和R 4一起形成任选取代的亚二烯基; 并且X 1和X 2各自表示任选酯化或醚化的羟基，或其盐可用于保护细胞免受β-淀粉样蛋白的细胞毒性。

9. 发明授权

US5580883A Aminobenzene compounds to prevent nerve cell degradation 失效
标题翻译：氨基苯化合物防止神经细胞降解
公开(公告)号：US5580883A
公开(公告)日：1996-12-03
申请号：US266614
申请日：1994-06-28
申请人： Giichi Goto , Hidefumi Yukimasa , Masaomi Miyamoto
发明人： Giichi Goto , Hidefumi Yukimasa , Masaomi Miyamoto
IPC分类号： C07D211/46 , C07D211/58 , C07D401/12 , A61K31/445 , A61K31/38 , A61K31/44 , A61K31/535
CPC分类号： C07D401/12 , C07D211/46 , C07D211/58
摘要： A compound useful for central antioxidant having inhibitory activity of degeneration and necrocytosis of cerebral cells of the formula (I): ##STR1## wherein A and B are independently (1) a group of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are independently hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted heterocyclic group, or R.sub.1 together with R.sub.2 and the nitrogen atom to which they are bound may form a cyclic amino group, provided that both R.sub.1 and R.sub.2 are not hydrogen atom at the same time, or (2) a group of the formula: ##STR3## wherein D is O or S, R.sub.3 is hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group, m is 1, 2, or 3 and n is 0, 1, 2, 3 or 4;p is 1 or 2, provided that both A may be the same or different when p is 2; andR.sub.4, R.sub.5 and R.sub.6 are independently hydrogen atom, a lower alkyl or a lower alkoxy, or R.sub.5 and R.sub.6 may bond together to form --CH.dbd.CH--CH.dbd.CH--, or a salt thereof.
摘要翻译：可用于具有式（I）的脑细胞的变性和坏死细胞增多抑制活性的中枢抗氧化剂的化合物：其中R 1和R 2独立地为氢原子，任选取代的烃残基或任选取代的杂环基，或R 1与R 2一起并且与它们结合的氮原子可以形成环状氨基，条件是R 1和R 2不得同时为氢原子，或（2）式：其中D是O或S，R 3是氢原子，任选取代的烃残基或任选取代的酰基，m是1,2或3，n是0,1,2,3或4; p为1或2，条件是当p为2时，A可以相同或不同; 并且R 4，R 5和R 6独立地为氢原子，低级烷基或低级烷氧基，或者R 5和R 6可以键合在一起形成-CH = CH-CH = CH-或其盐。

10. 发明授权

US5273978A Optically active isoindoline derivatives, their production and use 失效
标题翻译：光活性异吲哚啉衍生物，其生产和使用
公开(公告)号：US5273978A
公开(公告)日：1993-12-28
申请号：US992004
申请日：1992-12-17
申请人： Giichi Goto , Naohisa Fukuda
发明人： Giichi Goto , Naohisa Fukuda
IPC分类号： C07D471/04 , C07D519/00 , A61K31/40 , C07D209/46
CPC分类号： C07D471/04
摘要： The present invention provides an optically active isoindoline derivative represented by the formula: ##STR1## which is useful as an improving, therapeutic and preventive agent for anxiety-associated nervous symptoms, and an intermediate for synthesis thereof.
摘要翻译：本发明提供了可用作焦虑相关神经症状的改善，治疗和预防剂及其合成中间体的由下式表示的光学活性异二氢吲哚衍生物：。

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