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1. 发明授权

US5384414A Benzopyran derivatives 失效
标题翻译：苯并吡喃衍生物
公开(公告)号：US5384414A
公开(公告)日：1995-01-24
申请号：US107576
申请日：1993-08-18
申请人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
发明人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
IPC分类号： C07D311/72 , C07D311/92 , C07D311/04
CPC分类号： C07D311/92 , C07D311/72
摘要： Benzopyran derivatives of the formula: ##STR1## wherein R.sup.1a is hydrogen, C1-4 alkyl or C1-4 alkoxy; or two R.sup.1a taken together with 7th- and 8th-carbon to which they are attached form a C6 carbocyclic ring;R.sup.2a is hydrogen, C1-4 alkyl or C1-4 alkoxy;R.sup.3a is hydrogen, C2-4 acyl or benzoyl;na is 1-3;Ya is C1-7 alkylene, C2-7 alkenylene or C2-7 alkynylene;Ma isi) bond orii) a group of the formula: --Da--Ba--;Da isi) --O-- orii) --S--;Ba isi) C1-4 alkylene orii) a group of the formula: ##STR2## Za is i) bond,ii) --OCO--,iii) CONR.sup.9a --,iv) --COO--,v) --NR.sup.9a CO--,vi) --O-- orvii) --NH--CO--NH--;Wa is a group of the formula: --W1a--Aa--W2 a--;Aa isi) bond orii) a group of the formula: --Ea-- .circle.Ga --;Ea isi) bond,ii) --O-- oriii) --S--; .circle.Ga is C4-10 carbocyclic or heterocyclic ring; or C4-10 carbocyclic or heterocyclic ring substituted by one to three C1-4 alkyl, C1-4 alkoxy, halogen, a group of the formula: --COOR.sup.7a, trihalomethyl or acetamido;W1a and W2a each, independently, isi) bondii) C1-4 alkylene,iii) C2-4 alkenylene oriv ) C2-4 alkynylene;R.sup.4a is hydrogen or C1-4 alkyl;R.sup.5a is hydrogen, C1-4 alkyl or amino;R.sup.6a is hydrogen, C1-4 alkyl, C1-4 alkoxy, halogen, a group of the formula: --COOR.sup.8a, trihalomethyl or acetoamido;R.sup.7a is hydrogen or C1-4 alkyl;R.sup.8a is hydrogen or C1-4 alkyl;R.sup.9a is hydrogen, C1-4 alkyl or benzyl; with a proviso, and the pharmaceutically acceptable acid addition salts thereof possess the inhibitory activity on Maillard reaction and an antioxidizing effect.
摘要翻译：下式的苯并吡喃衍生物：其中R 1a是氢，C 1-4烷基或C 1-4烷氧基; 或两个R 1a与它们所连接的第七和第八碳一起形成C6碳环; R 2a是氢，C 1-4烷基或C 1-4烷氧基; R3a是氢，C2-4酰基或苯甲酰基; na是1-3; Ya是C 1-7亚烷基，C 2-7亚烯基或C 2-7亚炔基; Ma是i）键或ii）下式的基团：-Da-Ba-; Da为i）-O-或ii）-S-; b）i）C1-4亚烷基或ii）下式的基团：Za是i）键，ii）-OCO-，iii）CONR9a - ，iv）-COO-，v）-NR9aCO-，vi ）-O-或vii）-NH-CO-NH-; Wa是下列基团：-W1a-Aa-W2a-; Aa是i）键或ii）下式的基团：-Ea-＆Cir＆Ga - ; Ea为i）键，ii）-O-或iii）-S-; ＆cir＆Ga是C4-10碳环或杂环; 或被一至三个C 1-4烷基取代的C 4-10碳环或杂环，C 1-4烷氧基，卤素，下式基团：-COOR 7 a，三卤代甲基或乙酰氨基; W1a和W2a各自独立地是i）键合ii）C 1-4亚烷基，iii）C 2-4亚烯基或iv）C 2-4亚炔基; R4a是氢或C1-4烷基; R5a是氢，C1-4烷基或氨基; R 6a是氢，C 1-4烷基，C 1-4烷氧基，卤素，下式基团：-COOR 8 a，三卤甲基或乙酰胺基; R 7a是氢或C 1-4烷基; R 8a是氢或C 1-4烷基; R9a是氢，C1-4烷基或苄基; 并且其药学上可接受的酸加成盐具有对美拉德反应的抑制活性和抗氧化作用。

2. 发明授权

US5169957A Benzopyran derivatives 失效
标题翻译：苯并吡喃衍生物
公开(公告)号：US5169957A
公开(公告)日：1992-12-08
申请号：US736321
申请日：1991-07-26
申请人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
发明人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
IPC分类号： C07D311/72 , C07D311/92
CPC分类号： C07D311/72 , C07D311/92
摘要： Benzopyran derivatives of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof possess the inhibitory activity on Maillard reaction and an antioxidizing effect, and therefore, are useful for the prevention and treatment of several diabetic complications, diseases induced by aging and several diseases caused by formation of peroxidized fat.
摘要翻译：具有下式的苯并吡喃衍生物及其药学上可接受的酸加成盐对美拉德反应具有抑制活性和抗氧化作用，因此可用于预防和治疗几种糖尿病并发症，由老化和由过氧化脂肪形成引起的几种疾病。

3. 发明授权

US5055598A Benzopyran derivatives 失效
标题翻译： BENZOPYRAN衍生物
公开(公告)号：US5055598A
公开(公告)日：1991-10-08
申请号：US491876
申请日：1990-03-12
申请人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
发明人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
IPC分类号： A61K31/00 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/355 , A61P3/00 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/02 , A61P15/00 , A61P25/18 , A61P27/02 , A61P35/00 , A61P43/00 , C07D311/72 , C07D311/92 , C07D405/06
CPC分类号： C07D311/92 , C07D311/72
摘要： Benzopyran derivatives of the formula: ##STR1## wherein the variables are defined in the specification and the pharmaceutically acceptable acid addition salts thereof possess the inhibitory activity on Maillard reaction and an antioxidizing effect, and therefore, are useful for the prevention and treatment of several diabetic complications, diseases induced by aging and several diseases caused by formation of peroxidized fat.

4. 发明授权

US5508450A Benzopyran derivatives 失效
标题翻译：苯并吡喃衍生物
公开(公告)号：US5508450A
公开(公告)日：1996-04-16
申请号：US316332
申请日：1994-09-30
申请人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
发明人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
IPC分类号： C07D311/72 , C07D311/92 , C07D311/04
CPC分类号： C07D311/92 , C07D311/72
摘要： Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.
摘要翻译：本文描述了对美拉德反应具有抑制作用以及抗氧化作用的苯并吡喃衍生物。这些衍生物可用于治疗和/或预防糖尿病并发症，例如冠心病，周围循环功能不全或失败，脑血管障碍，神经源性糖尿病，肾病，动脉硬化，关节动脉硬化，白内障和视网膜病变。此外，衍生物还可以用于治疗和/或预防由老化引起的疾病和治疗和/或预防由形成过氧化脂肪引起的疾病。

5. 发明授权

US5266709A Benzopyran derivatives 失效
标题翻译：苯并吡喃衍生物
公开(公告)号：US5266709A
公开(公告)日：1993-11-30
申请号：US936285
申请日：1992-08-28
申请人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
发明人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
IPC分类号： C07D311/72 , C07D311/92 , C07D311/04
CPC分类号： C07D311/92 , C07D311/72
摘要： Benzopyran derivatives of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof possess the inhibitory activity on Maillard reaction and an antioxidizing effect, and therefore, are useful for the prevention and treatment of several diabetic complications, diseases induced by aging and several diseases caused by formation of peroxidized fat.
摘要翻译：具有下式的苯并吡喃衍生物及其药学上可接受的酸加成盐对美拉德反应具有抑制活性和抗氧化作用，因此可用于预防和治疗几种糖尿病并发症，由老化和由过氧化脂肪形成引起的几种疾病。

6. 发明授权

US5411974A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US5411974A
公开(公告)日：1995-05-02
申请号：US265734
申请日：1994-06-27
申请人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
发明人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
IPC分类号： C07D207/08 , C07D277/04 , C07D405/04 , C07D417/06 , A61K31/425
CPC分类号： C07D207/08 , C07D277/04 , C07D405/04 , C07D417/06
摘要： Heterocyclic compounds of the general formula: ##STR1## wherein, Z represents methylene group or sulfur atom, R represents a general formula:G--E--D--B--A--.
摘要翻译：具有以下通式的杂环化合物：其中Z表示亚甲基或硫原子，R表示通式：G-E-D-B-A-。

7. 发明授权

US5340832A Prolinal derivatives useful for treating amnesia 失效
标题翻译：用于治疗遗忘症的脯氨酸衍生物
公开(公告)号：US5340832A
公开(公告)日：1994-08-23
申请号：US107314
申请日：1993-08-17
申请人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
发明人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
IPC分类号： A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P25/28 , C07D207/08 , C07D401/12 , C07D405/12 , C07D409/12 , A61K31/52
CPC分类号： C07D207/08 , C07D405/12
摘要： A novel prolinal derivative of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms, R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.
摘要翻译：一种新颖的通式如下的流延衍生物：其中A表示1至8个碳原子的亚烷基或亚烯基或3至7个碳原子的饱和烃环，R表示氢原子苯基，苄基，1〜8个碳原子的烷基或3〜7个碳原子的环烷基，B表示1〜8个未被取代或被苯基取代或被苯基取代的亚烷基，苄基或单键，D表示未被取代或被1至3个卤素原子，1至4个碳原子的烷基或烷氧基，硝基或三氟甲基取代的碳环或杂环。]具有抑制性对脯氨酰内肽酶的活性，因此可用于治疗和/或预防药物作为遗忘。

8. 发明授权

US5254550A Prolinal derivatives and pharmaceutical compositions thereof 失效
标题翻译：脯氨酸衍生物及其药物组合物
公开(公告)号：US5254550A
公开(公告)日：1993-10-19
申请号：US803421
申请日：1991-12-06
申请人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
发明人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
IPC分类号： C07D207/08 , C07D405/12 , A61K31/495 , C07D401/12
CPC分类号： C07D207/08 , C07D405/12
摘要： A novel prolinal derivative of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms,R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group]posses inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent for amnesia.
摘要翻译：一种新颖的通式如下的流延衍生物：其中A表示1至8个碳原子的亚烷基或亚烯基或3至7个碳原子的饱和烃环，R表示氢原子苯基，苄基，1〜8个碳原子的烷基或3〜7个碳原子的环烷基，B表示1〜8个未被取代或被苯基取代或被苯基取代的亚烷基，苄基或单键，D表示未被取代或被1至3个卤素原子，1至4个碳原子的烷基或烷氧基，硝基或三氟甲基取代的碳环或杂环]具有抑制活性在脯氨酰内肽酶上，因此可用于治疗和/或预防健忘症药物。

9. 发明授权

US5545657A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US5545657A
公开(公告)日：1996-08-13
申请号：US354899
申请日：1994-12-09
申请人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
发明人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
IPC分类号： C07D207/08 , C07D277/04 , C07D405/04 , C07D417/06 , C07D207/416 , A61K31/40
CPC分类号： C07D207/08 , C07D277/04 , C07D405/04 , C07D417/06
摘要： Heterocyclic compounds of the general formula: ##STR1## wherein, Z represents methylene group or sulfur atom, R represents a general formula:G--E--D--B--A--L represents a group of general formula:--CO--COR.sup.2--CO--R.sup.4--CO--CH.sub.2 --COR.sup.2--CO--CF.sub.2 --COR.sup.2--CO--CO--NR.sup.5 R.sup.6or--CO--CH.sub.2 --CO--NR.sup.5 R.sup.6and non-toxic salt or hydrate thereof possess an inhibitory activity on propyl endopeptidase, and therefore useful, for prevention and/or treatment of amnesia.
摘要翻译：具有以下通式的杂环化合物：其中Z表示亚甲基或硫原子，R表示通式：GEDBAL表示通式-CO-COR 2 -CO-R 4 -CO-CH 2 - COR2 -CO-CF2-COR2 -CO-CO-NR5R6或-CO-CH2-CO-NR5R6及其无毒盐或水合物对丙基内肽酶具有抑制活性，因此可用于预防和/或治疗健忘症。

10. 发明授权

US5112847A Prolinal derivatives having inhibitory activity on prolyl endopeptidase 失效
标题翻译：具有抑制活性的PROLLAL衍生物在PROLYL ENDOPEPTIDASE
公开(公告)号：US5112847A
公开(公告)日：1992-05-12
申请号：US536830
申请日：1990-06-12
申请人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
发明人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
IPC分类号： C07D207/08
CPC分类号： C07D207/08
摘要： Prolinal derivatives of the formula ##STR1## wherein A is a group of the general formula ##STR2## wherein one of R.sup.1 and R.sup.2 is a hydrogen atom and the other is an alkyl group of from 2 to 5 carbon atoms, alkoxy group of from 1 to 5 carbon atom(s), phenyl group, benzyl group, cycloalkyl group of from 4 to 6 carbon atoms or (cycloalkyl group of from 4 to 6 carbon atoms)--methyl group or R.sup.1 and R.sup.2 each represent the same or different alkyl group of from 1 to 4 carbon atom(s) or a group of the formula ##STR3## wherein m represents an integer of from 3 to 6, n represents an integer of from 3 to 10, D represents a specified heterocyclic ring which is unsubstituted or substituted. These derivatives possess inhibitory activity on prolyl endopeptidase and therefor are useful as treating and/or preventing agents for amnesia.

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