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1. 发明授权

US4772553A Method for determination of enzyme activity 失效
标题翻译：测定酶活性的方法
公开(公告)号：US4772553A
公开(公告)日：1988-09-20
申请号：US875161
申请日：1986-06-17
申请人： Setsuro Fujii , Satoshi Sugiyama , Syouzou Sawai
发明人： Setsuro Fujii , Satoshi Sugiyama , Syouzou Sawai
IPC分类号： C07C67/00 , C07C227/00 , C07K5/04 , C07K5/06 , C07K5/083 , C07K5/093 , C07K5/103 , C12Q1/34 , C12Q1/37 , C12Q1/56 , C12N9/99 , C12Q1/38 , C12Q1/44
CPC分类号： C07K5/06026 , C07K5/0808 , C07K5/0819 , C07K5/101 , C12Q1/34 , C12Q1/37 , C12Q1/56 , C12Q2334/30 , C12Q2334/70 , G01N2333/96444 , G01N2333/96455 , G01N2333/968 , G01N2333/9723 , G01N2333/974 , G01N2333/976
摘要： This invention relates to a method for determining an enzyme-, an enzyme inhibitor-, an enzyme activator-, or zymogen-activity, which comprises allowing the enzyme to react with a substrate of the formula ##STR1## (wherein R.sub.1 represents an amino acid of an oligopeptide combined in the form of ester through the C-terminal carboxyl group of said amino acid or oligopeptide and R.sub.2 represents a hydrogen or bromine atom) to hydrolyze the substrate, then allowing the hydrolysis product of the formula ##STR2## to react with a FR-ITR salt [Fast Red-ITR salt (N,N'-diethyl-4-methoxymetanilamide diazonium salt)] to form a pigment, and determining the pigment.
摘要翻译：本发明涉及一种用于测定酶，酶抑制剂，酶活化剂或酶原活性的方法，其包括使酶与下式的底物反应（其中R 1表示通过所述氨基酸或寡肽的C末端羧基以酯的形式结合的寡肽的氨基酸，并且R 2表示氢或溴原子）以水解底物，然后使下式的水解产物与FR-ITR盐[Fast Red-ITR盐（N，N'-二乙基-4-甲氧基甲酰胺重氮盐）]反应，形成颜料，测定颜料。

2. 发明授权

US5162305A Polypeptide derivatives 失效
标题翻译：多肽衍生物
公开(公告)号：US5162305A
公开(公告)日：1992-11-10
申请号：US314018
申请日：1989-02-23
申请人： Setsuro Fujii , Yoshihito Yamamoto , Fumio Shimizu , Masatoshi Inai , Mitsuru Hirohashi
发明人： Setsuro Fujii , Yoshihito Yamamoto , Fumio Shimizu , Masatoshi Inai , Mitsuru Hirohashi
IPC分类号： A61K38/23 , A61K38/00 , A61P5/12 , C07K7/06 , C07K14/575 , C07K14/585
CPC分类号： C07K14/585 , A61K38/00
摘要： Novel synthetic polypeptide derivatives, i.e., novel calcitonin derivatives, having improved basic physiological activities of the corresponding natural calcitonins, i.e., the activity for lowering the blood level of calcium, the activity as an analgesic, as well as the activity for inhibiting the secretion of the gastric juice. Thus these synthetic calcitonins are effective as agents for curing hypercalcemia, analgetic agents, anti-ulcerative agents and the like.

3. 发明授权

US5047521A 5-fluorouracil derivatives 失效
标题翻译： 5-氟尿嘧啶衍生物
公开(公告)号：US5047521A
公开(公告)日：1991-09-10
申请号：US150407
申请日：1988-02-09
申请人： Setsuro Fujii , Mitsuru Hirohashi , Yoshihito Yamamoto , Yutaka Kojima
发明人： Setsuro Fujii , Mitsuru Hirohashi , Yoshihito Yamamoto , Yutaka Kojima
IPC分类号： A61K31/505 , A61K31/70 , C07D239/54 , C07D239/553 , C07D401/12 , C07D409/06 , C07D409/14 , C07H19/06 , C07H19/073 , H01S4/00
CPC分类号： C07D239/553 , C07D401/12 , C07D409/14 , C07H19/06
摘要： This invention relates to a novel 5-fluorouracil derivative represented by the formula ##STR1## wherein R.sup.y is a hydrogen atom or a specific acyl group, Z is a phenyl-lower alkoxy-lower alkyl group, thienyl-lower alkyl group optionally substituted with halogen atom on the thienyl ring, or a group ##STR2## wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a specific acyl group, phenyl-lower alkyl group having a group R.sup.x OCO-- on the phenyl ring, or a group --(A).sub.n B, R.sup.x being a specific organic group, A being a lower alkylene group, n being 0 or 1, and B being a 5- or 6-membered unsaturated heterocyclic group having 1 to 4 hetero-atoms selected from N, O and S and optionally having a benzene ring, naphthalene ring or pyridine ring condensed therewith, with the proviso that R.sup.1 and R.sup.2 are not hydrogen atoms or specific acyl groups at the same time; to a process for preparing the same; and to an anticancer composition comprising the same as an effective ingredient.
摘要翻译： PCT No.PCT / JP87 / 00275 Sec。 371日期1988年2月9日 102（e）1988年2月9日PCT PCT公开1987年4月30日PCT公布。公开号WO87 / 06582 日本公开日：1987年11月5日。本发明涉及由式（1）表示的新型5-氟尿嘧啶衍生物，其中R y为氢原子或特定酰基，Z为苯基 - 低级烷氧基 - 低级烷基任选被噻吩基环上的卤素原子取代的噻吩基 - 低级烷基，或其中R 1和R 2各自为氢原子，特定酰基，具有基团R xOCO-的苯基 - 低级烷基基团环，或基团 - （A）nB，Rx是特定的有机基团，A是低级亚烷基，n是0或1，B是具有1〜4个杂原子的5或6元不饱和杂环基，选自N，O和S且任选具有苯环的原子，萘环或与其缩合的吡啶环，条件是R1和R2不同时为氢原子或特定酰基; 一个制备它的过程; 以及包含其作为有效成分的抗癌组合物。

4. 发明授权

US4652570A Anti-cancer composition for delivering 5-fluorouracil 失效
标题翻译：用于递送5-氟尿嘧啶的抗癌组合物
公开(公告)号：US4652570A
公开(公告)日：1987-03-24
申请号：US645165
申请日：1984-08-28
申请人： Setsuro Fujii , Norio Unemi , Setsuo Takeda
发明人： Setsuro Fujii , Norio Unemi , Setsuo Takeda
IPC分类号： A61K31/505 , C07D239/54 , C07D239/553
CPC分类号： C07D239/553 , A61K31/505 , Y10S514/922
摘要： An anti-cancer composition for treating cancers sensitive to 5-fluorouracil therapy in warm-blooded animals, comprising 5-fluorouracil and uracil.
摘要翻译：一种用于治疗温血动物中对5-氟尿嘧啶治疗敏感的癌症的抗癌组合物，其包含5-氟尿嘧啶和尿嘧啶。

5. 发明授权

US4570006A Amidine compound, process for producing same and anti-complement agent comprising same 失效
标题翻译：脒化合物，其制备方法和包含其的抗补体剂
公开(公告)号：US4570006A
公开(公告)日：1986-02-11
申请号：US664261
申请日：1984-10-24
申请人： Setsuro Fujii , Takashi Yaegashi , Toyoo Nakayama , Yojiro Sakurai , Shigeki Nunomura , Toshiyuki Okutome
发明人： Setsuro Fujii , Takashi Yaegashi , Toyoo Nakayama , Yojiro Sakurai , Shigeki Nunomura , Toshiyuki Okutome
IPC分类号： A61K31/155 , A61K31/215 , A61K31/24 , C07C45/54 , C07C271/06 , C07C271/22 , C07C279/18 , C07C335/22 , C07D317/68 , C07C119/00 , A61K31/22 , A61K31/235
CPC分类号： C07C255/00 , C07C271/22 , C07C279/18 , C07C335/22 , C07C45/54 , C07D317/68
摘要： Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsine, anti-plasmin, anti-kallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with amidinophenol compound (III) and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof. ##STR2##
摘要翻译：由式（I）表示的脒基化合物及其药学上可接受的酸加成盐是新型化合物，可用作强抗胰蛋白酶，抗纤溶酶，抗激肽释放酶和抗凝血酶剂。具有强大的抗Cl（Cl＆upbar＆r，Cl＆upbar＆s）活性和抗补体活性，它们也可用作抗补体剂。这些脒基化合物通过通式（II）R 1 -COOH（II）表示的羧酸化合物与脒基苯酚化合物（III）的酯化反应制备，如果需要，可以将其转化为其药学上可接受的酸加成盐。（三）

6. 发明授权

US4532255A Amidine compounds and anticomplement agent comprising same 失效
标题翻译：脒化合物和包含其的抗补体剂
公开(公告)号：US4532255A
公开(公告)日：1985-07-30
申请号：US572269
申请日：1984-01-20
申请人： Setsuro Fujii , Toshiyuki Okutome , Toyoo Nakayama , Takashi Yaegashi , Masateru Kurumi
发明人： Setsuro Fujii , Toshiyuki Okutome , Toyoo Nakayama , Takashi Yaegashi , Masateru Kurumi
IPC分类号： C07C249/02 , A61K31/155 , C07C257/18 , C07C279/18 , C07D317/68 , C07C101/00 , A61K31/34 , C07C101/48
CPC分类号： C07D317/68 , C07C279/18
摘要： Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-C1 (C1r, C1s) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula ##STR2## with 6-amidino-2-naphthol and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.

7. 发明授权

US4514416A Amidine compound, process for producing same and anti-complement agent comprising same 失效
标题翻译：脒化合物，其制备方法和包含其的抗补体剂
公开(公告)号：US4514416A
公开(公告)日：1985-04-30
申请号：US611937
申请日：1984-05-21
申请人： Setsuro Fujii , Takashi Yaegashi , Toyoo Nakayama , Yojiro Sakurai , Shigeki Nunomura , Toshiyuki Okutome
发明人： Setsuro Fujii , Takashi Yaegashi , Toyoo Nakayama , Yojiro Sakurai , Shigeki Nunomura , Toshiyuki Okutome
IPC分类号： A61K31/155 , A61K31/215 , A61K31/24 , C07C45/54 , C07C271/06 , C07C271/22 , C07C279/18 , C07C335/22 , C07D317/68 , C07C119/00 , A61K31/22 , A61K31/235
CPC分类号： C07C255/00 , C07C271/22 , C07C279/18 , C07C335/22 , C07C45/54 , C07D317/68
摘要： Amidino compounds represented by the formula (I) ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with amidinophenol compound (III) and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof. ##STR2##
摘要翻译：由式（I）表示的脒基化合物及其药学上可接受的酸加成盐是新的化合物，可用作强效的抗胰蛋白酶，抗血纤维蛋白酶，抗激肽释放酶和抗凝血酶剂。具有强大的抗Cl（Cl＆upbar＆r，Cl＆upbar＆s）活性和抗补体活性，它们也可用作抗补体剂。这些脒基化合物通过通式（II）R 1 -COOH（II）表示的羧酸化合物与脒基苯酚化合物（III）的酯化反应制备，如果需要，可以将其转化为其药学上可接受的酸加成盐。（三）

8. 发明授权

US4452813A Sulfonate derivatives, process for preparing same and antilipemic compositions containing the derivative 失效
标题翻译：磺酸衍生物，其制备方法和含有衍生物的抗血小板组合物
公开(公告)号：US4452813A
公开(公告)日：1984-06-05
申请号：US377074
申请日：1982-05-11
申请人： Setsuro Fujii , Toshihiro Hamakawa , Kazuo Ogawa , Yoshiyuki Muranaka , Sadao Hashimoto
发明人： Setsuro Fujii , Toshihiro Hamakawa , Kazuo Ogawa , Yoshiyuki Muranaka , Sadao Hashimoto
IPC分类号： A61K31/255 , C07C45/63 , C07C45/64 , C07C45/78 , C07C62/24 , C07C245/14 , C07C303/00 , C07C309/65 , C07C143/68
CPC分类号： C07C245/14 , C07C309/00 , C07C45/63 , C07C45/64 , C07C45/78 , C07C62/24
摘要： A sulfonate derivative represented by the formula ##STR1## wherein R.sub.1 is lower alkyl, lower alkoxy or halogen, l is an integer of from 0 to 3, n is 0 or 1, A is straight-chain or branched-chain alkylene having 1 to 4 carbon atoms, and R.sub.2 is hydrogen or lower alkyl but, when n is 0 or 1 and A is straight-chain alkylene with 1 to 4 carbon atoms, is not hydrogen and the method for preparing the same.
摘要翻译：式中，R 1为低级烷基，低级烷氧基或卤素，l为0〜3的整数，n为0或1的磺酸酯衍生物，A为直链或支链的亚烷基，具有1〜 4个碳原子，R2为氢或低级烷基，但当n为0或1且A为具有1至4个碳原子的直链亚烷基时，不是氢及其制备方法。

9. 发明授权

US4224342A Guanidinobenzoic acid compounds and process for preparing the same 失效
标题翻译：胍基苯甲酸化合物及其制备方法
公开(公告)号：US4224342A
公开(公告)日：1980-09-23
申请号：US959276
申请日：1978-11-09
申请人： Setsuro Fujii , Tsuyoshi Watanabe , Masashi Shiota , Okumoto Itsuo , Naohiro Kayama
发明人： Setsuro Fujii , Tsuyoshi Watanabe , Masashi Shiota , Okumoto Itsuo , Naohiro Kayama
IPC分类号： A61K31/245 , A61P1/00 , A61P7/04 , C07C279/18 , A61K31/155 , C07C129/12
CPC分类号： C07C279/18 , Y02P20/55
摘要： Guanidinobenzoic acid compounds represented by the formula ##STR1## wherein R and Z are as defined hereinafter, having anti-plasmin and anti-trypsin activities and processes for preparing the same as well as a pharmaceutical composition and a method of inhibiting the activity of plasmin and a trypsin is disclosed.
摘要翻译：由下式表示的胍基苯甲酸化合物，其中R和Z如下文所定义，具有抗纤溶酶和抗胰蛋白酶活性及其制备方法以及药物组合物和抑制活性的方法的纤溶酶和胰蛋白酶。

10. 发明授权

US4030977A Method for purification of physiologically active substance using enzyme-enzyme inhibitor system 失效
标题翻译：使用酶 - 酶抑制剂系统纯化生理活性物质的方法
公开(公告)号：US4030977A
公开(公告)日：1977-06-21
申请号：US668378
申请日：1976-03-19
申请人： Setsuro Fujii , Yasumichi Kajita , Seizi Hiraku , Heizo Kira , Hideki Aishita , Keiko Muryobayashi , Hiroshi Terashima , Akira Akimoto , Ken Taniguchi , Minoru Wada
发明人： Setsuro Fujii , Yasumichi Kajita , Seizi Hiraku , Heizo Kira , Hideki Aishita , Keiko Muryobayashi , Hiroshi Terashima , Akira Akimoto , Ken Taniguchi , Minoru Wada
IPC分类号： C12N9/00 , C12N11/02 , C12D13/10
CPC分类号： C12N11/02 , C12N9/00
摘要： A method for isolating and purifying a physiologically active substance contained in a tissue or a body fluid using an insoluble type naturally occurring proteolytic enzyme inhibitor or an insoluble type proteolytic enzyme alone or in combination with the insoluble type naturally occurring proteolytic enzyme inhibitor is disclosed.
摘要翻译：公开了使用不溶型天然蛋白水解酶抑制剂或不溶型蛋白水解酶单独或与不溶型天然存在的蛋白水解酶抑制剂组合来分离和纯化包含在组织或体液中的生理活性物质的方法。

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