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1. 发明授权

US4757083A Novel pyrrolidinylamide ester derivatives having anti-prolyl endopeptidase activity and synthesis and use thereof 失效
标题翻译：具有抗脯氨酰内肽酶活性的新型吡咯烷酰胺酯衍生物及其合成和用途
公开(公告)号：US4757083A
公开(公告)日：1988-07-12
申请号：US936445
申请日：1986-12-01
申请人： Naoki Higuchi , Masayuki Saitoh , Masaki Hashimoto , Harukazu Fukami , Takaharu Tanaka
发明人： Naoki Higuchi , Masayuki Saitoh , Masaki Hashimoto , Harukazu Fukami , Takaharu Tanaka
IPC分类号： A61K31/445 , A61K31/40 , A61K31/401 , A61P25/00 , A61P43/00 , C07D295/10 , C07D295/185 , C12N9/99 , C07D295/18
CPC分类号： C07D295/185
摘要： A novel pyrrolidinylamide ester derivative that exhibits inhibitory activity against prolyl endopeptidase, methods for synthesis thereof and its use as an inhibitor against said enzyme are disclosed. The pyrrolidinylamide ester of the invention has the following general formula: ##STR1## wherein n is 0 or an integer of 1 to 7 and R is hydrogen atom or a straight or branched alkyl having 1 to 8 carbon atoms.
摘要翻译：公开了一种对脯氨酰内肽酶具有抑制活性的新型吡咯烷酰胺酯衍生物，其合成方法及其作为对所述酶的抑制剂的用途。本发明的吡咯烷酰胺酯具有以下通式：其中n为0或1〜7的整数，R为氢原子或碳原子数为1〜8的直链或支链烷基。

2. 发明授权

US5198458A Pyrrolidineamide derivatives of acylamino acid and pharmaceutical composition containing the same 失效
标题翻译：酰氨基酸的吡咯烷酰胺衍生物和含有它们的药物组合物
公开(公告)号：US5198458A
公开(公告)日：1993-03-30
申请号：US638148
申请日：1991-01-09
申请人： Naoki Higuchi , Masayuki Saitoh , Masaki Hashimoto , Harukazu Fukami , Takaharu Tanaka
发明人： Naoki Higuchi , Masayuki Saitoh , Masaki Hashimoto , Harukazu Fukami , Takaharu Tanaka
IPC分类号： C07D207/16 , C07D295/185
CPC分类号： C07D295/185 , C07D207/16
摘要： A compound of the general formula: ##STR1## wherein m is an integer of 1 to 7,n is 0 or an integer of 1 to 5,R.sup.1 is the phenyl, a substituted phenyl, the phenoxy, a substituted phenoxy or a saturated or unsaturated straight alkyl having 5 to 18 carbon atoms,R.sup.2 is hydrogen atom,R.sup.3 is hydrogen atom, a branched or unbranched alkyl having 3 to 5 carbon atoms, the phenyl, hydroxyphenyl, benzyloxyphenyl, an alkylthio having 1 to 3 carbon atoms in its alkyl moiety, amino, carboxyl, hydroxy, benzyloxy, indolyl or imidazolyl, or R.sup.2 and R.sup.3 together form a single bond between the carbon atom and the nitrogen atom, and a pharmaceutical composition containing said compound are provided. The compound is effective in curing amnesia because of its anti-prolyl endopeptidase activity.
摘要翻译：一种通式如下的化合物：其中m为1〜7的整数，n为0或1〜5的整数，R 1为苯基，取代苯基，苯氧基，取代的苯氧基或具有5至18个碳原子的饱和或不饱和直链烷基，R 2是氢原子，R 3是氢原子，具有3至5个碳原子的支链或非支链烷基，苯基，羟基苯基，苄氧基苯基，具有1至3个碳原子的烷硫基在其烷基部分中，氨基，羧基，羟基，苄氧基，吲哚基或咪唑基，或R2和R3一起形成碳原子和氮原子之间的单键，并提供含有所述化合物的药物组合物。该化合物由于其抗脯氨酰内肽酶活性而有效地治愈健忘症。

3. 发明授权

US4826870A Pyrrolidineamide derivative of acylamino acid and pharmaceutical containing the same 失效
标题翻译：酰基氨基酸的吡咯烷酰胺衍生物和含有它们的药物
公开(公告)号：US4826870A
公开(公告)日：1989-05-02
申请号：US10490
申请日：1987-02-03
申请人： Naoki Higuchi , Masayuki Saitoh , Masaki Hashimoto , Harukazu Fukami , Takaharu Tanaka
发明人： Naoki Higuchi , Masayuki Saitoh , Masaki Hashimoto , Harukazu Fukami , Takaharu Tanaka
IPC分类号： C07D207/16 , C07D295/185 , A61K31/40 , C07D207/09
CPC分类号： C07D295/185 , C07D207/16
摘要： A compound of the general formula: ##STR1## wherein m is an integer of 1 to 7, n is 0 or an integer of 1 to 5,R.sup.1 is the phenyl, a substituted phenyl, the phenoxy, a substituted phenoxy or a saturated or unsaturated straight alkyl having 5 to 18 carbon atoms,R.sup.2 is hydrogen atom,R.sup.3 is hydrogen atom, a branched or unbranched alkyl having 3 to 5 carbon atoms, the phenyl, hydroxyphenyl, benzyloxyphenyl, an alkylthio having 1 to 3 carbon atoms in its alkyl moiety, amino, carboxyl, hydroxy, benzyloxy, indolyl or imidazolyl, or R.sup.2 and R.sup.3 together form a single bond between the carbon atom and the nitrogen atom, and a pharmaceutical composition containing said compound are provided. The compound is effective in curing amnesia because of its anti-prolyl endopeptidase activity.
摘要翻译：一种通式如下的化合物：其中m为1〜7的整数，n为0或1〜5的整数，R 1为苯基，取代苯基，苯氧基，取代的苯氧基或具有5至18个碳原子的饱和或不饱和直链烷基，R 2是氢原子，R 3是氢原子，具有3至5个碳原子的支链或非支链烷基，苯基，羟基苯基，苄氧基苯基，具有1至3个碳原子的烷硫基在其烷基部分中，氨基，羧基，羟基，苄氧基，吲哚基或咪唑基，或R2和R3一起形成碳原子和氮原子之间的单键，并提供含有所述化合物的药物组合物。该化合物由于其抗脯氨酰内肽酶活性而有效地治愈健忘症。

4. 发明授权

US4810721A Pyrrolidineamide derivative having anti-prolyl endopeptidase 失效
标题翻译：具有抗脯氨酰内肽酶的吡咯烷酰胺衍生物
公开(公告)号：US4810721A
公开(公告)日：1989-03-07
申请号：US121887
申请日：1987-11-17
申请人： Masayuki Saitoh , Takaharu Tanaka , Naoki Higuchi , Masaki Hashimoto , Harukazu Fukami
发明人： Masayuki Saitoh , Takaharu Tanaka , Naoki Higuchi , Masaki Hashimoto , Harukazu Fukami
IPC分类号： A61K31/40 , A61K31/401 , A61P25/28 , A61P43/00 , C07D207/16 , C12N9/99 , C07D207/00
CPC分类号： C07D207/16
摘要： A novel pyrrolidineamide derivative that exhibits inhibitory activity toward prolyl endopeptidase and its use as an inhibitor against said enzyme are provided. The pyrrolidineamide of the invention has the following general formula: ##STR1## wherein R.sup.1 is benzyloxycarbonyl or a group of the formula: ##STR2## (wherein m is an integer of from 1 to 5) and R.sup.2 is hydroxy, acyloxyy or a group of the formula: ##STR3## (wherein R.sup.3 and R.sup.4 independently are a hydrogen atom, a halogen atom, a lower alkyl or a lower alkoxy).
摘要翻译：提供了对脯氨酰内肽酶具有抑制活性的新型吡咯烷酰胺衍生物及其作为对所述酶的抑制剂的用途。本发明的吡咯烷酰胺具有以下通式：其中R1是苄氧基羰基或下式的基团：其中m是1至5的整数，R2是羟基，酰氧基或下式的基团：其中R 3和R 4独立地是氢原子，卤素原子，低级烷基或低级烷氧基。

5. 发明授权

US5205855A Herbicidally active phenoxyalkanecarboxylic acid derivatives 失效
标题翻译：除草活性苯氧亚硬脂酸衍生物
公开(公告)号：US5205855A
公开(公告)日：1993-04-27
申请号：US578254
申请日：1990-09-06
申请人： Harukazu Fukami , Naoki Higuchi , Naoko Kawaguchi , Masaki Hashimoto , Kinya Ide , Toshio Takahashi
发明人： Harukazu Fukami , Naoki Higuchi , Naoko Kawaguchi , Masaki Hashimoto , Kinya Ide , Toshio Takahashi
IPC分类号： A01N39/02 , A01N39/04 , A01N41/06 , A01N43/40 , A01N47/12 , A01N47/24 , C07C69/712 , C07C205/38 , C07D213/64 , C07D213/643
CPC分类号： C07D213/643 , A01N39/02 , A01N39/04 , A01N41/06 , A01N43/40 , A01N47/12 , A01N47/24 , C07C205/38 , C07C69/712
摘要： A compound of the formula: ##STR1## wherein Q.sup.1 is CH or N; R is H or C.sub.1 -C.sub.5 alkyl; X is H, halogen, CF.sub.3, or NO.sub.2 ; Y is H or halogen; Z is --O-- or --NH--; A is ##STR2## wherein Q.sup.2, and Q.sup.3 are each CH or N; R.sup.1 and R.sup.2 are each H, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, or C.sub.2 -C.sub.6 alkoxycarbonyl; R.sup.3, R.sup.4, and R.sup.5 are each H or C.sub.1 -C.sub.5 alkyl; R.sup.6 is H, halogen, or C.sub.1 -C.sub.5 alkyl; R.sup.7, R.sup.8, R.sup.9, and R.sup.10 are each H or C.sub.1 -C.sub.5 alkyl; R.sup.11 is H, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.2 -C.sub.6 alkenyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.15 aryloxyalkyl, or C.sub.7 -C.sub.15 aralkyl; R.sup.12 and R.sup.13 are each H or C.sub.1 -C.sub.5 alkyl; R.sup.14 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.5 -C.sub.10 aryl, or C.sub.7 -C.sub.15 aralkyl; or R.sup.13 and R.sup.14 taken together form C.sub.3 -C.sub.4 alkylene, V.sup.1 and V.sup.2 and are each H, halogen, NO.sub.2, CN, or CF.sub.3 ; V.sup.3 is halogen or CF.sub.3 ; W.sup.1 is --O-- or --NH--; W.sup.2 is --(CH.sub.2).sub.n -- wherein n is 0 or 1, or CO; X.sup.1 is halogen, or a salt thereof, which is effective as a herbicidal agent.
摘要翻译：下式的化合物：其中Q 1是CH或N; R是H或C 1 -C 5烷基; X是H，卤素，CF 3或NO 2; Y为H或卤素; Z是-O-或-NH-; A是其中Q2和Q3各自为CH或N; R 1和R 2各自为H，C 1 -C 5烷基，C 1 -C 5烷氧基或C 2 -C 6烷氧基羰基; R 3，R 4和R 5各自为H或C 1 -C 5烷基; R6是H，卤素或C1-C5烷基; R 7，R 8，R 9和R 10各自为H或C 1 -C 5烷基; R11是H，C1-C5烷基，C1-C5烷氧基，C2-C6烯基，C6-C10芳基，C7-C15芳氧基烷基或C7-C15芳烷基; R 12和R 13各自为H或C 1 -C 5烷基; R14是C1-C5烷基，C2-C6烯基，C5-C10芳基或C7-C15芳烷基; 或R 13和R 14一起形成C 3 -C 4亚烷基，V 1和V 2，各自为H，卤素，NO 2，CN或CF 3; V3是卤素或CF 3; W1是-O-或-NH-; W2是 - （CH2）n-，其中n是0或1，或CO; X1是作为除草剂有效的卤素或其盐。

6. 发明授权

US4976773A Herbicidally active phenoxyalkanecarboxylic acid derivatives 失效
标题翻译：除草活性苯氧亚硬脂酸衍生物
公开(公告)号：US4976773A
公开(公告)日：1990-12-11
申请号：US230481
申请日：1988-08-10
申请人： Harukazu Fukami , Naoki Higuchi , Naoko Kawaguchi , Masaki Hashimoto , Kinya Ide , Toshio Takahashi
发明人： Harukazu Fukami , Naoki Higuchi , Naoko Kawaguchi , Masaki Hashimoto , Kinya Ide , Toshio Takahashi
IPC分类号： A01N37/02 , A01N37/18 , A01N37/24 , A01N39/02 , A01N39/04 , A01N41/06 , A01N43/40 , A01N47/12 , A01N47/24 , C07C69/712 , C07C205/38 , C07C255/54 , C07C311/39 , C07D213/64 , C07D213/643 , C07D213/84 , C07D213/85
CPC分类号： C07D213/643 , A01N39/02 , A01N39/04 , A01N41/06 , A01N43/40 , A01N47/12 , A01N47/24 , C07C205/38 , C07C255/54 , C07C311/39
摘要： A compound of the formula: ##STR1## wherein Q.sup.1 is CH or N; R is H or C.sub.1 -C.sub.5 alkyl; X is H, halogen, CF.sub.3, or NO.sub.2 ; Y is H or halogen; Z is --O-- or --NH--; A is ##STR2## wherein Q.sup.2, and Q.sup.3 are each CH or N; R.sup.1 and R.sup.2 are each H, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, or C.sub.2 -C.sub.6 alkxoycarobnyl; R.sup.3, R.sup.4, and R.sup.5 are each H or C.sub.1 -C.sub.5 alkyl; R.sup.6 is H, halogen, or C.sub.1 -C.sub.5 alkyl; R.sup.7, R.sup.8, R.sup.9, and R.sup.10 are each H or C.sub.1 -C.sub.5 alkyl; R.sup.11 is H, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.2 -C.sub.6 alkenyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.15 aryloxyalkyl, or C.sub.7 -C.sub.15 aralkyl; R.sup.12 and R.sup.13 are each H or C.sub.1 -C.sub.5 alkyl; R.sup.14 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.5 -C.sub.10 aryl, or C.sub.7 -C.sub.15 aralkyl; or R.sup.13 and R.sup.14 taken together form C.sub.3 -C.sub.4 alkylene, V.sup.1 and V.sup.2 are each H, halogen, NO.sub.2, CN, or CF.sub.3 ; V.sup.3 is halogen or CF.sub.3 ; W.sup.1 is --O-- or --NH--; W.sup.2 is --(CH.sub.2).sub.n -- wherein n is 0 or 1, or CO; X.sup.1 is halogen, or a salt thereof, which is effective as a herbicidal agent.
摘要翻译：下式的化合物：其中Q 1是CH或N; R是H或C 1 -C 5烷基; X是H，卤素，CF 3或NO 2; Y为H或卤素; Z是-O-或-NH-; A是，其中Q 2和Q 3各自为CH或N; R 1和R 2各自为H，C 1 -C 5烷基，C 1 -C 5烷氧基或C 1 -C 5烷氧基羰基; R 3，R 4和R 5各自为H或C 1 -C 5烷基; R 6是H，卤素或C 1 -C 5烷基; R 7，R 8，R 9和R 1各自为H或C 1 -C 5烷基; R 1是H，C 1 -C 5烷基，C 1 -C 5烷氧基，C 2 -C 6烯基，C 6 -C 10芳基，C 7 -C 15芳氧基烷基或C 7 -C 15芳烷基; R 1，R 2和R 3各自为H或C 1 -C 5烷基; R 1为C 1 -C 5烷基，C 2 -C 6烯基，C 5 -C 10芳基或C 7 -C 15芳烷基; 或R 1 3和R 1 4。一起形成C 3 -C 4亚烷基，V 1和V 2各自为H，卤素，NO 2，CN或CF 3; V 3是卤素或CF 3; W 1是-O-或-NH-; W 2为 - （CH 2）n - ，其中n为0或1，或CO; X 1是作为除草剂有效的卤素或其盐。

7. 发明授权

US5039696A Maleimide derivatives and fungicides for agriculture and horticulture containing the same 失效
标题翻译：用于农业和园艺的马来酰亚胺衍生物和杀真菌剂
公开(公告)号：US5039696A
公开(公告)日：1991-08-13
申请号：US473632
申请日：1990-02-01
申请人： Shinjiro Niwata , Harukazu Fukami , Masaki Hashimoto , Norio Ohtsuka , Fumio Fujita
发明人： Shinjiro Niwata , Harukazu Fukami , Masaki Hashimoto , Norio Ohtsuka , Fumio Fujita
IPC分类号： C07D207/452 , A01N37/46 , C07D207/44 , C07D207/456
CPC分类号： C07D207/456 , A01N37/46
摘要： A maleimide derivative useful as an active agent for a fungicide for agriculture and horticulture, having the formula (I): ##STR1## wherein X and Y each independently represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aralkyloxy group or a trifluoromethyl group,Z represents a chlorine atom or bromine atom,and R represents a straight or branched alkyl group having 1 to 15 carbon atoms, an alkenyl group having 2 to 5 carbon atoms, an alkynyl group having 2 to 5 carbon atoms, an alkoxyalkyl group having 2 to 5 carbon atoms, an oxoalkyl group having 3 to 6 carbon atoms or a phenyl group or a phenyl alkyl group which may be substituted.

8. 发明授权

US5424310A Substituted 1,2,4-triazine-3,5-dione derivative and anticoccidial drug composition containing the same as active component 失效
标题翻译：取代的1,2,4-三嗪-3,5-二酮衍生物和含有活性成分的抗球虫药物组合物
公开(公告)号：US5424310A
公开(公告)日：1995-06-13
申请号：US79925
申请日：1993-06-23
申请人： Harukazu Fukami , Masaki Hashimoto , Shinjiro Niwata , Jun Imose , Harumoto Kawaguchi , Toshio Takahashi
发明人： Harukazu Fukami , Masaki Hashimoto , Shinjiro Niwata , Jun Imose , Harumoto Kawaguchi , Toshio Takahashi
IPC分类号： A61K31/53 , A61P33/02 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D253/075
CPC分类号： C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： A substituted 1,2,4-triazine-3,5-dione derivative having the formula (I) or a salt thereof: ##STR1## wherein R represents a 5- or 6-membered heterocyclic group which may have at least one substituent selected from the group consisting of a halogen, a lower alkyl group and a halogenated lower alkyl group, and an anticoccidial drug composition containing the same as an active component.
摘要翻译：具有式（I）的取代的1,2,4-三嗪-3,5-二酮衍生物或其盐：其中R表示可以具有至少5或6元杂环基选自卤素，低级烷基和卤代低级烷基的一个取代基和含有它们作为活性组分的抗球虫药物组合物。

9. 发明授权

US4945104A Maleimide derivatives and use thereof in agricultural and horticultural fungicides 失效
标题翻译：马来酰亚胺衍生物及其在农业和园艺杀真菌剂中的应用
公开(公告)号：US4945104A
公开(公告)日：1990-07-31
申请号：US370800
申请日：1989-06-23
申请人： Harukazu Fukami , Masaki Hashimoto , Shinjiro Niwata , Norio Ohtsuka , Fumio Fujita
发明人： Harukazu Fukami , Masaki Hashimoto , Shinjiro Niwata , Norio Ohtsuka , Fumio Fujita
IPC分类号： C07D207/452 , A01N37/32 , A01N39/00 , A01N43/36 , C07D207/44 , C07D207/456
CPC分类号： C07D207/456 , A01N39/00
摘要： A maleimide derivative having the formula (I): ##STR1## wherein R.sub.1 represents a lower alkyl group having 1 to 4 carbon atoms, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently represent a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a phenyl group which may be substituted, or an aralkyl group having 7 to 10 carbon atoms, and X.sub.1 and X.sub.2 independently represent a hydrogen atom or a halogen atom, and a production process thereof as well as a agricultural and horticultural fungicide containing, as an active ingredient, the maleimide derivative.

10. 发明授权

US08017587B2 2-O- (β-D-glucopyranosyl) ascorbic acid, process for its production, and foods and cosmetics containing compositions comprising it 有权
标题翻译： 2-O-（＆bgr--D-吡喃葡萄糖基）抗坏血酸，其生产方法，以及含有组合物的组合物的食品和化妆品
公开(公告)号：US08017587B2
公开(公告)日：2011-09-13
申请号：US11898121
申请日：2007-09-10
申请人： Mitsuru Maeda , Masahiro Nakao , Harukazu Fukami
发明人： Mitsuru Maeda , Masahiro Nakao , Harukazu Fukami
IPC分类号： A01N43/04 , A01N43/08
CPC分类号： A61K8/676 , A23L33/105 , A23L33/15 , A23V2002/00 , A61K8/602 , A61K31/375 , A61K2800/52 , A61Q17/04 , A61Q19/00 , A61Q19/02 , C07H1/08 , C07H17/04 , C12P19/60 , A23V2250/708
摘要： The present invention provides a novel ascorbic acid derivative as a provitamin C with improved stability in the body and prolonged life in the body compared to conventionally known 2-O-(α-D-glucopyranosyl)ascorbic acid.The composition comprising the novel compound 2-O-(β-D-glucopyranosyl)ascorbic acid has been extracted from plants such as from Ningxia Lycium barbarum L. and/or Lycium chinense Mill. The compositions comprising 2-O-(β-D-glucopyranosyl)ascorbic acid may be enzymatically synthesized using β-D-glucosyltransferase. Pure 2-O-(β-D-glucopyranosyl)ascorbic acid may be produced from such compositions. Alternatively, 2-O-(β-D-glucopyranosyl)ascorbic acid may be produced by chemical synthesis. The 2-O-(β-D-glucopyranosyl)ascorbic acid results in higher stability and a prolonged life of vitamin C when ingested in the body compared to the corresponding α-D-glucopyranosyl derivative, and is therefore highly suitable as a provitamin C to be used in cosmetics and foods.
摘要翻译：与常规已知的2-O-（α-D-吡喃葡萄糖基）抗坏血酸相比，本发明提供了一种新型抗坏血酸衍生物作为维生素C，具有改善体内的稳定性和延长的身体寿命。从宁夏枸杞子和/或枸杞子植物提取含有新化合物2-O-（＆bgr-D-吡喃葡萄糖基）抗坏血酸的组合物。可以使用β-葡萄糖基转移酶酶法合成包含2-O-（β-谷氨酰-D-吡喃葡萄糖基）抗坏血酸的组合物。可以从这样的组合物制备纯2-O-（＆bgr-D-吡喃葡萄糖基）抗坏血酸。或者，可通过化学合成制备2-O-（＆bgr-D-吡喃葡萄糖基）抗坏血酸。与对应的α-D-吡喃葡萄糖基衍生物相比，2-O-（＆bgr-D-吡喃葡萄糖基）抗坏血酸在身体摄取时导致更高的稳定性和更长的维生素C的使用寿命，因此非常适合作为维生素 C用于化妆品和食品。

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