专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

31. 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。

32. 发明授权

US5037976A 2-oxa-isocephem compounds 失效
标题翻译： 2-氧杂 - 异头孢烯化合物
公开(公告)号：US5037976A
公开(公告)日：1991-08-06
申请号：US430539
申请日：1989-11-01
申请人： Setsuro Fujii , Hiroshi Ishikawa , Koichi Yasumura , Koichiro Jitsukawa , Sachio Toyama , Hidetsugu Tsubouchi , Kimio Sudo , Kouichi Tsuji
发明人： Setsuro Fujii , Hiroshi Ishikawa , Koichi Yasumura , Koichiro Jitsukawa , Sachio Toyama , Hidetsugu Tsubouchi , Kimio Sudo , Kouichi Tsuji
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： A 2-oxa-isocephem compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined, pharmaceutically acceptable salts thereof, composition containing the same and processes for preparing the same are disclosed. The compound is useful as an antimicrobial agent.

33. 发明授权

US4999378A Phenylcarboxylic acid derivatives 失效
标题翻译：苯基羧酸衍生物
公开(公告)号：US4999378A
公开(公告)日：1991-03-12
申请号：US372336
申请日：1989-06-20
申请人： Setsuro Fujii , Hiroyuki Kawamura , Shinichi Watanabe
发明人： Setsuro Fujii , Hiroyuki Kawamura , Shinichi Watanabe
IPC分类号： C07C217/22 , C07C217/44 , C07C217/46 , C07C217/84 , C07C217/86 , C07C217/90 , C07C225/22 , C07C229/18 , C07C233/17 , C07C233/18 , C07C233/69 , C07C233/78 , C07C255/25 , C07C275/30 , C07D295/092 , C07D303/22 , C07D317/58 , C07D319/18
CPC分类号： C07D295/088 , C07C217/22 , C07C217/44 , C07C217/46 , C07C217/84 , C07C217/86 , C07C217/90 , C07C225/22 , C07C229/18 , C07C233/17 , C07C233/18 , C07C233/69 , C07C233/78 , C07C255/25 , C07C275/30 , C07D303/22 , C07D317/58 , C07D319/18 , C07C2101/08 , C07C2101/14
摘要： Phenylcarboxylic acid derivatives having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each H, halogen, alkyl, haloalkyl, alkanoyl, cycloalkyl, nitro, amino, --O--D--R.sup.5 (D is alkylene, R.sup.5 is H, amino, morpholino, carboxyl, phthalimido, phenyl, epoxy), substituted or unsubstituted phenoxy, substituted or unsubstituted phenylalkylamino, carboxylalkenyl, or both form alkylenedioxy; R.sup.3 is H, --E--R.sup.6 (E is alkylene, R.sup.6 is H, carboxyl, cyano, OH, phenylalkoxy, or halogen-substituted phenyl, or phenylcarbamoyl), --CO--G--R.sup.7 (G is alkylene, R.sup.7 is H, substituted or unsubstituted phenylcarbamoyl), substituted or unsubstituted benzoyl, alkenyl, carbamoyl, phenyl, or halophenyl; R.sup.4 is H or alkyl; A is alkylene, alkylene condensed with cycloalkyl ring, or alkenylene; B is alkylene or alkenylene; l is 0 or 1. Said compounds have fatty acid synthesis-inhibitory activity, cholesterol synthesis-inhibitory activity and are useful as antilipidemic agent, prophylactic and treating agent of artherosclerosis, prophylactic and treating agent of obesity, antidiabetics.
摘要翻译：具有下式的苯基羧酸衍生物：其中R1和R2各自为H，卤素，烷基，卤代烷基，烷酰基，环烷基，硝基，氨基，-OD-R5（D为亚烷基，R5为H，氨基，吗啉代，羧基苯二甲酰亚氨基，苯基，环氧基），取代或未取代的苯氧基，取代或未取代的苯基烷基氨基，羧基烯基或二者形成亚烷基二氧基; R3是H，-E-R6（E是亚烷基，R6是H，羧基，氰基，OH，苯基烷氧基或卤素取代的苯基或苯基氨基甲酰基），-CO-G-R7（G是亚烷基，R7是H，取代或未取代的苯基氨基甲酰基），取代或未取代的苯甲酰基，烯基，氨基甲酰基，苯基或卤代苯基; R4是H或烷基; A是亚烷基，与环烷基环稠合的亚烷基或亚烯基; B是亚烷基或亚烯基; l是0或1.所述化合物具有脂肪酸合成抑制活性，胆固醇合成抑制活性，可用作抗血脂药物，动脉粥样硬化的预防和治疗剂，肥胖症的预防和治疗剂，抗糖尿病药。

34. 发明授权

US4797502A Sulfonic acid ester derivatives and process for preparing same 失效
标题翻译：磺酸酯衍生物及其制备方法
公开(公告)号：US4797502A
公开(公告)日：1989-01-10
申请号：US4610
申请日：1987-01-20
申请人： Setsuro Fujii , Kazuo Ogawa , Toshihiro Hamakawa , Yoshiyuki Muranaka
发明人： Setsuro Fujii , Kazuo Ogawa , Toshihiro Hamakawa , Yoshiyuki Muranaka
IPC分类号： C07C309/73 , C07C143/68
CPC分类号： C07C309/00
摘要： A sulfonic acid ester derivative represented by the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, A is a group represented by the general formula ##STR2## (wherein R.sub.2 and R.sub.3 are each alkyl having 1 to 4 carbon atoms) or by the general formula ##STR3## (wherein R.sub.4 and R.sub.5 are each alkyl having 1 to 4 carbon atoms or, when taken together with the carbon atom to which they are attached, form cycloalkyl having 4 to 6 carbon atoms), and l is an integer of from 1 to 3, and a process for preparing the derivative.

35. 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。

36. 发明授权

US4550076A Rapid assaying method for guanase 失效
标题翻译： guanase快速检测方法
公开(公告)号：US4550076A
公开(公告)日：1985-10-29
申请号：US424182
申请日：1982-09-27
申请人： Nobumoto Chikazawa , Toshiharu Muraoka , Setsuro Fujii
发明人： Nobumoto Chikazawa , Toshiharu Muraoka , Setsuro Fujii
IPC分类号： C12Q1/26 , C12Q1/28 , C12Q1/34
CPC分类号： C12Q1/28 , C12Q1/34 , G01N2333/978
摘要： The guanase activity in body fluids such as blood serum can be rapidly and accurately assayed by (I) decomposing guanine with the guanase in the specimen to xanthine and ammonia at pH 7-9, preferably at pH 8, (II) decomposing the xanthine formed by former step I with xanthine oxidase to uric acid and hydrogen peroxide, (III) reacting the reactant solution of the former step II with 3-methyl-2-benzothiazolinonehydrazone, an aniline derivative such as N,N-di-lower-alkylaniline and peroxidase, and finally measuring the optical absorption of the reactant solution of the step III at 570-600 nm. The all steps can be completed within 15 minutes. Therefore, this assay is adoptable for automatic assay of guanase on usual clinically available automatic analyzers.
摘要翻译：通过（I）将样品中的鸟嘌呤分解为黄嘌呤和氨，pH7-9，优选pH8，（II）分解形成的黄嘌呤的鸟嘌呤，可快速准确地测定体液如血清中的鸟苷酸活性通过前一步骤I将黄嘌呤氧化酶与尿酸和过氧化氢反应，（III）使前一步骤II的反应物溶液与3-甲基-2-苯并噻唑酮腙，苯胺衍生物如N，N-二低级烷基苯胺和过氧化物酶，最后在570-600nm测量步骤III的反应物溶液的光吸收。所有步骤可在15分钟内完成。因此，该测定法可用于通常临床可用的自动分析仪上的鸟苷酸的自动测定。

37. 发明授权

US4503045A 2'-Deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine derivatives, a process for the preparation of the derivatives and anti-tumor agents containing the derivatives 失效
标题翻译： 2'-脱氧-3'，5'-二-O-烷基羰基-5-氟尿苷衍生物，制备衍生物的方法和含有衍生物的抗肿瘤剂
公开(公告)号：US4503045A
公开(公告)日：1985-03-05
申请号：US234569
申请日：1981-02-13
申请人： Setsuro Fujii , Bompei Yasui , Tomohisa Miyamoto , Masatoshi Shiga , Kazuko Ando , Iwao Hashimoto , Masahiro Kawasaki , Yoichiro Kawai , Yuji Mino
发明人： Setsuro Fujii , Bompei Yasui , Tomohisa Miyamoto , Masatoshi Shiga , Kazuko Ando , Iwao Hashimoto , Masahiro Kawasaki , Yoichiro Kawai , Yuji Mino
IPC分类号： C07H19/073 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61P35/00 , C07H19/00 , C07H19/06 , C07H19/08
CPC分类号： C07H19/06
摘要： 2'-Deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine derivatives possessing strong anti-tumor activity with weak toxicity and represented by the general formula: ##STR1## wherein R stands for an alkyl group, an alkoxy group or a halogen atom, m for zero or an integer of 1-3, and n for an integer of 1-14, with the proviso that when m is 2 or 3, R's may be the same or different and that when m is 2 and the adjacent two R's are alkoxy groups, the two alkyl moieties of the alkoxy groups may be combined to form together with the two adjacent oxa bridging members an alkylenedioxy group as a whole. These derivatives are prepared by acylating a 2'-deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine with corresponding benzoyl halides and are useful as active ingredients for anti-tumor agents, especially for oral administration.
摘要翻译： 2'-脱氧-3'，5'-二-O-烷基羰基-5-氟尿苷衍生物具有强的抗肿瘤活性，毒性弱，由以下通式表示：其中R代表烷基，烷氧基基团或卤素原子，m为0或1-3的整数，n为1-14的整数，条件是当m为2或3时，R可以相同或不同，当m为 2并且相邻的两个R是烷氧基，烷氧基的两个烷基部分可以与两个相邻的氧杂桥连成员一起与亚烷基二氧基整体形成。这些衍生物通过用相应的苯甲酰卤酰化2'-脱氧-3'，5'-二-O-烷基羰基-5-氟尿苷来制备，并且可用作抗肿瘤剂的活性成分，特别是用于口服给药。

38. 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。

39. 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。

40. 发明授权

US4490366A 2'-Deoxy-5-fluorouridine derivative and a process for producing the same and an antitumor agent comprising the same 失效
标题翻译： 2'-脱氧-5-氟尿苷衍生物及其制备方法和包含其的抗肿瘤剂
公开(公告)号：US4490366A
公开(公告)日：1984-12-25
申请号：US419014
申请日：1982-09-16
申请人： Setsuro Fujii , Eiichi Sakakibara
发明人： Setsuro Fujii , Eiichi Sakakibara
IPC分类号： C07H19/073 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61P35/00 , C07H19/06
CPC分类号： C07H19/06
摘要： A 2'-deoxy-5-fluorouridine derivative represented by the formula; ##STR1## wherein R represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, an acetyloxy group or a halogen atom, and n is an integer of 1 to 3.
摘要翻译：由下式表示的2'-脱氧-5-氟尿苷衍生物：其中，R表示氢原子，碳原子数1〜5的烷基，碳原子数1〜4的烷氧基，乙酰氧基或卤素原子，n表示1〜3的整数。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式