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1. 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。

2. 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。

3. 发明授权

US5885990A Substituted amidinonaphthyl ester derivative 失效
标题翻译：取代的脒基萘酯衍生物
公开(公告)号：US5885990A
公开(公告)日：1999-03-23
申请号：US849761
申请日：1997-06-12
申请人： Toyoo Nakayama , Hiroyuki Kawamura , Hiroyuki Uchiyama
发明人： Toyoo Nakayama , Hiroyuki Kawamura , Hiroyuki Uchiyama
IPC分类号： C07C257/18 , C07C279/18 , C07D233/50 , C07D277/18 , C07D295/13 , C07D295/155 , C07D295/28 , A61K31/245 , C07D233/24 , C07D295/14
CPC分类号： C07D295/32 , C07C257/18 , C07C279/18 , C07D233/50 , C07D277/18 , C07D295/13 , C07D295/155
摘要： Substituted amidinonaphthyl ester compounds effective for treatment of thrombosis are represented by the following formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1## wherein R.sub.1 represents (4,5-dihydro-1H-imidazol-2-yl)amino group, (4,5-dihydro-1,3-thiazol-2-yl)amino group, amidino group, morpholinomethyl group, nitro group, amino group, dimethylamino group, ##STR2## R.sub.3 represents hydrogen, methoxy group, hydroxyl group, acetylamino group, morpholino group, piperidino group, 1-pyrrolidinyl group or dimethylamino group,m represents 0-4,R.sub.4 represents hydrogen or methyl group,R.sub.2 represents NH.sub.2 CO(CH.sub.2).sub.n --, 2-(carbamoyl)vinyl group or R.sub.5 OOC(CH.sub.2).sub.n --,R.sub.5 represents dimethylcarbamoylmethyl group, hydrogen or lower alkyl group, andn represents 0-2.
摘要翻译： PCT No.PCT / JP95 / 02723 Sec。 371日期：1997年6月12日 102（e）日期1997年6月12日PCT 1995年12月27日PCT PCT。公开号WO96 / 20917 日期：1996年7月11日有效治疗血栓形成的取代脒基萘酯化合物由下式（I）及其药学上可接受的酸加成盐表示：其中R1表示（4,5-二氢-1H-咪唑 -2-基）氨基，（4,5-二氢-1,3-噻唑-2-基）氨基，脒基，吗啉代甲基，硝基，氨基，二甲基氨基，R 3表示氢，甲氧基，羟基，乙酰氨基，吗啉代基，哌啶子基，1-吡咯烷基或二甲基氨基，m表示0-4，R4表示氢或甲基，R2表示NH2CO（CH2）n-，2-（氨基甲酰基）乙烯基或R5OOC（CH2）n-，R5代表二甲基氨基甲酰基甲基，氢或低级烷基，n代表0-2。

4. 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。

5. 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。

6. 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。

7. 发明授权

US4454338A Amidine compound 失效
标题翻译：脒化合物
公开(公告)号：US4454338A
公开(公告)日：1984-06-12
申请号：US300534
申请日：1981-09-09
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 , 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 pharmaceuticlly 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，可用作强效的抗胰蛋白胨，抗血浆素，抗激肽释放酶和抗凝血酶剂。具有强大的抗C1（C1＆upbar＆r，C1＆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将式（ⅩⅧ）代表的羧酸化合物与6-脒基-2-萘酚进行常规的酯化反应来制备，如果需要，可以将其转化成其药学上可接受的酸加成盐。

8. 发明授权

US5532267A Amidinonaphthyl furancarboxylate derivatives and acid addition salts therof 失效
标题翻译：脒基萘基呋喃羧酸酯衍生物和酸加成盐
公开(公告)号：US5532267A
公开(公告)日：1996-07-02
申请号：US215785
申请日：1994-03-22
申请人： Toyoo Nakayama , Seizo Taira , Hiroyuki Kawamura , Masaoki Shibuya , Masahiro Iwaki
发明人： Toyoo Nakayama , Seizo Taira , Hiroyuki Kawamura , Masaoki Shibuya , Masahiro Iwaki
IPC分类号： C07D307/68 , C07D407/12 , A61K31/335 , A61K31/34 , C07D307/46 , C07D317/14
CPC分类号： C07D407/12 , C07D307/68
摘要： Amidinonaphthyl furancarboxylate derivatives of the formula I ##STR1## wherein A is a single bond or A denotes (a) a phenyl group, cyclopentyl group, or cyclohexyl group,(b) an alkenylphenyl group, alkylphenyl group, phenylalkenyl group, or phenylalkyl group wherein alkyl is C.sub.1 to C.sub.7 alkyl and alkenyl is C.sub.2 to C.sub.7 alkenyl,(c) a C.sub.1 to C.sub.18 alkyl or C.sub.2 to C.sub.7 alkenyl group which may be substituted by one or two substituents selected from C.sub.1 to C.sub.5 alkyl groups and quanidino groups, wherein an alkyl substituent together with the carbon atom to which it is attached may form a cycloalkyl ring having from 3 to 6 carbon atoms, or said C.sub.1 to C.sub.5 alkyl may itself be substituted by a C.sub.3 to C.sub.6 cycloalkyl ring, or(d) --(CH.sub.2).sub.n --NH--CO--(CH.sub.2).sub.n' wherein n and n' may be the same or different and represent an integer from 1 to 4; andwherein R denotes(e) a hydroxyl group,(f) a C.sub.1 to C.sub.7 alkoxy group which may be mono- or disubstituted by C.sub.1 to C.sub.5 alkyl,(g) a phenyl-C.sub.1 -C.sub.4 alkoxy group,(h) --OAl(OH).sub.2,(i) an amino group,(j) ##STR2## or (k) ##STR3## and pharmaceutically acceptable acid addition salts thereof, useful as pharmaceuticals.
摘要翻译：其中A是单键或A表示（a）苯基，环戊基或环己基，（b）烯基苯基，烷基苯基，苯基烯基，（C 1 -C 6）烷氧基羰基，或苯基烷基，其中烷基是C1-C7烷基，烯基是C2-C7链烯基，（c）C1-C18烷基或C2-C7烯基，其可以被一个或两个选自C1-C5烷基和喹啉基的取代基取代基团，其中烷基取代基与其所连接的碳原子一起可以形成具有3至6个碳原子的环烷基环，或所述C1至C5烷基本身可以被C 3至C 6环烷基环取代，或（d ） - （CH 2）n -NH-CO-（CH 2）n'，其中n和n'可以相同或不同，表示1至4的整数; 并且其中R表示（e）羟基，（f）可被C1至C5烷基单或二取代的C1至C7烷氧基，（g）苯基-C1-C4烷氧基，（h）-OAl（ OH）2，（i）可用作药物的氨基，（j）和/或其药学上可接受的酸加成盐。

9. 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）

10. 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.

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