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1. 发明授权

US07282521B2 Anti-retroviral moronic acid derivatives 失效
标题翻译：抗逆转录病毒葡萄糖酸衍生物
公开(公告)号：US07282521B2
公开(公告)日：2007-10-16
申请号：US11134904
申请日：2005-05-23
申请人： Kuo-Hsiung Lee , Fang-Rong Chang , Yojiro Sakurai , Chin Ho Chen
发明人： Kuo-Hsiung Lee , Fang-Rong Chang , Yojiro Sakurai , Chin Ho Chen
IPC分类号： A61K31/225 , C07C69/34
CPC分类号： C07J63/008
摘要： The present invention provides moronic acid derivatives of the general formula: which have antiviral activity, along with compositions containing the same and methods of use thereof.
摘要翻译：本发明提供具有抗病毒活性的通式的幽门酸衍生物，以及含有其的组合物及其使用方法。

2. 发明授权

US4686226A Substituted benzo[b]furo- and benzo[b]thieno quinolizines 失效
标题翻译：取代的苯并[b]呋喃和苯并[b]噻吩并喹啉
公开(公告)号：US4686226A
公开(公告)日：1987-08-11
申请号：US771927
申请日：1985-09-03
申请人： Joel R. Huff , John J. Baldwin , Yojiro Sakurai , Joseph P. Vacca , James P. Guare, Jr.
发明人： Joel R. Huff , John J. Baldwin , Yojiro Sakurai , Joseph P. Vacca , James P. Guare, Jr.
IPC分类号： A61K31/435 , A61P1/00 , A61P3/04 , A61P3/08 , A61P7/02 , A61P9/12 , A61P25/02 , A61P25/24 , A61P25/26 , C07D455/06 , C07D471/14 , C07D491/14 , C07D491/147 , C07D495/14 , A61K31/38
CPC分类号： C07D471/14 , C07D455/06 , C07D491/14 , C07D495/14
摘要： Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors and modifiers of gastrointestinal motility.
摘要翻译：取代的六氢芳基喹啉及其药学上可接受的盐是选择性α2-肾上腺素能受体拮抗剂，从而可用作抗抑郁药，抗高血压药，眼用抗高血压药，抗糖尿病药，抗肥胖药和血小板聚集抑制剂和胃肠运动性调节剂。

3. 发明授权

US4182897A Amino- or guanidino-phenylpropionic acid derivatives 失效
标题翻译：氨基或胍基 - 苯基丙酸衍生物
公开(公告)号：US4182897A
公开(公告)日：1980-01-08
申请号：US917232
申请日：1978-06-20
申请人： Setsuro Fujii , Hiroyuki Kawamura , Seizo Taira , Ryoji Matsui , Yojiro Sakurai , Toshiyuki Okutome
发明人： Setsuro Fujii , Hiroyuki Kawamura , Seizo Taira , Ryoji Matsui , Yojiro Sakurai , Toshiyuki Okutome
IPC分类号： C07C205/56 , C07C279/18 , A61K31/24 , C07C101/447 , C07C129/12
CPC分类号： C07C279/18 , C07C205/56 , Y10S514/822
摘要： Amino- or guanidino-phenylpropionic ester derivatives represented by the formula: ##STR1## wherein R is --NH.sub.2 or ##STR2## R.sup.1 is hydrogen or a lower alkyl group, and R.sup.2 is an unsubstituted or a lower-alkyl-, carboxyalkyl-, lower-alkoxy-, lower-alkoxycarbonyl- or halogen-substituted phenyl group or an unsubstituted or a halogen-substituted naphthyl group, and acid addition salts thereof are novel compounds exhibiting a specific enzyme-inhibitory activity to proteolytic enzymes and, therefore, they are useful as the therapeutic agent of diseases induced by abnormal activation of these enzymes. The above-mentioned compounds can be produced by subjecting a nitrocinnamic acid derivative represented by the formula: ##STR3## and a phenol derivative or a naphthol derivative represented by the formula:HO--R.sup.2to an esterification in the conventional manner to obtain a nitrocinnamic ester derivative, then reducing the latter compound to obtain an aminophenylpropionic ester derivative and, if desired, reacting it with cyanamide to obtain a guanidino-phenylpropionic ester derivative and, if desired, further converting the reaction product to an acid addition salt.
摘要翻译：由下式表示的氨基或胍基 - 苯基丙酸酯衍生物：其中R是-NH 2或R 1是氢或低级烷基，R 2是未取代的或低级烷基 - 羧基烷基 - 低级 - 烷氧基 - ，低级烷氧基羰基或卤素取代的苯基或未取代的或卤素取代的萘基，其酸加成盐是对蛋白水解酶具有特异性酶抑制活性的新化合物，因此它们是有用的作为由这些酶的异常活化引起的疾病的治疗剂。上述化合物可以通过将下式所示的硝基肉桂酸衍生物和由式HO-R2表示的酚衍生物或萘酚衍生物以常规方式进行酯化而制得，得到硝基肌氨酸酯衍生物，然后还原后一种化合物以获得氨基苯基丙酸酯衍生物，并且如果需要，可与氰酰胺反应，得到胍基 - 苯基丙酸酯衍生物，如果需要，将反应产物进一步转化成酸加成盐。

4. 发明申请

US20060004097A1 Anti-retroviral moronic acid derivatives 失效
标题翻译：抗逆转录病毒葡萄糖酸衍生物
公开(公告)号：US20060004097A1
公开(公告)日：2006-01-05
申请号：US11134904
申请日：2005-05-23
申请人： Kuo-Hsiung Lee , Fang-Rong Chang , Yojiro Sakurai , Chin Chen
发明人： Kuo-Hsiung Lee , Fang-Rong Chang , Yojiro Sakurai , Chin Chen
IPC分类号： A61K31/225 , C07C235/54
CPC分类号： C07J63/008
摘要： The present invention provides moronic acid derivatives of the general formula: which have antiviral activity, along with compositions containing the same and methods of use thereof.
摘要翻译：本发明提供具有抗病毒活性的通式的幽门酸衍生物，以及含有其的组合物及其使用方法。

5. 发明授权

US4634783A Novel amidine compound 失效
标题翻译：新型脒化合物
公开(公告)号：US4634783A
公开(公告)日：1987-01-06
申请号：US573268
申请日：1984-01-23
申请人： Setsuro Fujii , Toyoo Nakayama , Shigeki Nunomura , Ryoji Matsui , Shin-ichi Watanabe , Kimio Sudo , Toshiyuki Okutome , Masateru Kurumi , Yojiro Sakurai , Takuo Aoyama
发明人： Setsuro Fujii , Toyoo Nakayama , Shigeki Nunomura , Ryoji Matsui , Shin-ichi Watanabe , Kimio Sudo , Toshiyuki Okutome , Masateru Kurumi , Yojiro Sakurai , Takuo Aoyama
IPC分类号： A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/4465 , A61K31/454 , A61K31/455 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/5377 , A61K31/54 , A61K31/541 , A61K31/5415 , A61P1/00 , A61P7/04 , A61P29/00 , A61P37/08 , A61P43/00 , C07D207/16 , C07D207/337 , C07D207/34 , C07D209/08 , C07D209/18 , C07D209/30 , C07D209/42 , C07D211/62 , C07D213/55 , C07D213/79 , C07D213/80 , C07D215/48 , C07D215/50 , C07D215/54 , C07D233/54 , C07D233/60 , C07D233/61 , C07D235/06 , C07D235/28 , C07D235/30 , C07D241/24 , C07D261/18 , C07D263/34 , C07D263/42 , C07D277/68 , C07D279/22 , C07D279/36 , C07D307/16 , C07D307/24 , C07D307/54 , C07D307/68 , C07D307/71 , C07D307/85 , C07D311/12 , C07D333/24 , C07D333/38 , C07D333/70 , C12N9/99 , C07D307/56 , C07D307/64 , C07D307/66
CPC分类号： C07D213/79 , C07D207/16 , C07D207/34 , C07D209/08 , C07D209/18 , C07D209/42 , C07D211/62 , C07D213/55 , C07D215/48 , C07D233/54 , C07D233/64 , C07D235/06 , C07D241/24 , C07D261/18 , C07D263/34 , C07D277/68 , C07D279/22 , C07D307/54 , C07D307/68 , C07D307/71 , C07D307/85 , C07D311/12 , C07D333/24 , C07D333/38 , C07D333/70
摘要： Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.
摘要翻译：式“IMAGE”的脒化合物及其药学上可接受的酸加成盐是新的化合物，可用作强抗胰蛋白酶，抗纤溶酶，抗激肽释放酶和抗凝血酶剂。它们也可用作强大的抗补体剂。

6. 发明授权

US4496584A Amidine derivatives with anti-complement activity 失效
标题翻译：具有抗补体活性的脒衍生物
公开(公告)号：US4496584A
公开(公告)日：1985-01-29
申请号：US370647
申请日：1982-04-21
申请人： Setsuro Fujii , Takashi Yaegashi , Toyoo Nakayama , Shigeki Nunomura , Yojiro Sakurai , Toshiyuki Okutome
发明人： Setsuro Fujii , Takashi Yaegashi , Toyoo Nakayama , Shigeki Nunomura , Yojiro Sakurai , Toshiyuki Okutome
IPC分类号： A61K31/215 , A61K31/155 , A61K31/22 , A61K31/23 , A61K31/27 , A61P1/00 , A61P7/00 , A61P13/02 , A61P15/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C69/035 , C07C239/00 , C07C257/18 , C07C279/14 , C11C3/04
CPC分类号： C07C257/18
摘要： Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsin, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-Cl activity and anti-complement activity, they are also useful as anti-complement agents. These amidino compounds are prepared by reacting carboxylic compounds represented by the formulaR.sub.1 --COOHor their reactive intermediates with amidinonaphthol represented by the formula ##STR2## and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.
摘要翻译：由式＆lt; IMAGE＆gt;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，可用作强抗胰蛋白酶，抗血浆素，抗激肽释放酶和抗凝血酶剂。具有强的抗C1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使由式R 1 -COOH表示的羧酸化合物或其反应性中间体与由式“IMAGE”表示的脒基萘酚反应并且如果需要可以转化成其药学上可接受的酸加成盐来制备。

7. 发明授权

US4490388A Amidine compound 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：US4490388A
公开(公告)日：1984-12-25
申请号：US350964
申请日：1982-02-22
申请人： Setsuro Fujii , Takuo Aoyama , Yojiro Sakurai , Toyoo Nakayama , Shigeki Nunomura , Takashi Yaegashi , Toshiyuki Okutome
发明人： Setsuro Fujii , Takuo Aoyama , Yojiro Sakurai , Toyoo Nakayama , Shigeki Nunomura , Takashi Yaegashi , Toshiyuki Okutome
IPC分类号： C07C271/22 , C07C279/18 , C07D317/60 , C07D317/68 , C07C101/00 , A61K31/215
CPC分类号： C07D317/68 , C07C271/22 , C07C279/18 , C07D317/60
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 4-(.beta.-amidinoethenyl)phenol represented by the formula (III) ##STR2## and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.
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由式（II）R1-COOH（II）表示的羧酸化合物与由式（III）表示的4-（β-脒基乙烯基）苯酚（III）进行常规酯化而制备，如果必需的，可以转化成其药学上可接受的酸加成盐。

8. 发明授权

US4563527A Amidine compounds 失效
标题翻译：脒化合物
公开(公告)号：US4563527A
公开(公告)日：1986-01-07
申请号：US632350
申请日：1984-07-19
申请人： Setsuro Fujii , Toyoo Nakayama , Shigeki Nunomura , Kimio Sudo , Shin-ichi Watanabe , Toshiyuki Okutome , Yojiro Sakurai , Masateru Kurumi , Takuo Aoyama
发明人： Setsuro Fujii , Toyoo Nakayama , Shigeki Nunomura , Kimio Sudo , Shin-ichi Watanabe , Toshiyuki Okutome , Yojiro Sakurai , Masateru Kurumi , Takuo Aoyama
IPC分类号： C07D307/68 , C07D307/85 , C07D333/38 , C07D405/12 , C07D307/54
CPC分类号： C07D405/12 , C07D307/68 , C07D307/85 , C07D333/38
摘要： Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.
摘要翻译：式“IMAGE”的脒化合物及其药学上可接受的酸加成盐是新的化合物，可用作强抗胰蛋白酶，抗纤溶酶，抗激肽释放酶和抗凝血酶剂。它们也可用作强大的抗补体剂。

9. 发明授权

US4214093A Amino- or guanidino-1,2,3,4-tetrahydro-1-naphthoic esters 失效
标题翻译：氨基或胍基-1,2,3,4-四氢-1-萘甲酸酯
公开(公告)号：US4214093A
公开(公告)日：1980-07-22
申请号：US30594
申请日：1979-04-16
申请人： Setsuro Fujii , Yojiro Sakurai , Toyoo Nakayama , Ryoji Matsui
发明人： Setsuro Fujii , Yojiro Sakurai , Toyoo Nakayama , Ryoji Matsui
IPC分类号： A61K31/00 , A61K31/13 , A61K31/215 , A61K31/24 , C07C101/48
摘要： Amino- or guanidino-1,2,3,4-tetrahydro-1-naphthoic esters represented by the formula, ##STR1## wherein R.sub.1 is --NH.sub.2 or ##STR2## R.sub.3 is --H, --R.sub.4, --O--R.sub.4, --NHCOCH.sub.3, a halogen, --CN, ##STR3## --COOH, --COOR.sub.4, ##STR4## or --(CH.sub.2).sub.n --COOCH.sub.2 --CO--R.sub.5 ; R.sub.5 is --O--R.sub.4, --NH.sub.2 or ##STR5## n is 0, 1 or 2, and R.sub.4 is a lower alkyl, or pharmaceutically acceptable acid addition salts thereof. Owing to their inhibitory activity on proteolytic enzymes the said esters and acid addition salts thereof are useful in the therapy of diseases caused by such enzymes.
摘要翻译：由下式表示的氨基或胍基-1,2,3,4-四氢-1-萘甲酸酯，其中R 1是-NH 2或者R 3是-H，-R 4， -O-R 4，-NHCOCH 3，卤素，-CN，-COOH，-COOR 4，或者 - （CH 2）n -COOH CH 2 -CO-R 5; R5是-O-R4，-NH2或n是0,1或2，R4是低级烷基或其药学上可接受的酸加成盐。由于其对蛋白水解酶的抑制活性，所述酯和其酸加成盐可用于治疗由这些酶引起的疾病。

10. 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）

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