公开(公告)号：US5053498A

公开(公告)日：1991-10-01

申请号：US421917

申请日：1989-10-16

申请人： Yusei Shiraga ,  Chikara Fukaya ,  Toshiaki Akira ,  Masakazu Iwai ,  Kazumasa Yokoyama ,  Mamoru Tabata ,  Hiroshi Fukui ,  Shigeo Tanaka ,  Yoshiro Iga ,  Tadakazu Suyama ,  Kanemichi Okano

发明人： Yusei Shiraga ,  Chikara Fukaya ,  Toshiaki Akira ,  Masakazu Iwai ,  Kazumasa Yokoyama ,  Mamoru Tabata ,  Hiroshi Fukui ,  Shigeo Tanaka ,  Yoshiro Iga ,  Tadakazu Suyama ,  Kanemichi Okano

IPC分类号： A61K31/12 ,  A61K31/70 ,  A61K36/54 ,  C07C49/242 ,  C07C49/255 ,  C07C49/647 ,  C07C49/743 ,  C07H15/18 ,  C07H15/203 ,  C07H15/207

CPC分类号： C07C403/08 ,  C07C403/10 ,  C07C403/12 ,  C07H15/18 ,  C07H15/203 ,  C07C2101/16 ,  Y10S514/927

摘要： A therapeutic and prophylactic agent for peptic ulcers which contains as an active ingredient a compound of the general formula (I): ##STR1## wherein R.sub.1 represents hydrogen or .dbd.O; R.sub.2 represents hydrogen or --OR.sub.5 ; R.sub.3 represents hydrogen or --OR.sub.5 ; R.sub.4 represents --OR.sub.7 in the case of the absence of double bond; R.sub.5, R.sub.6 and R.sub.7 each represents hydrogen or an organic residue;X represents group (A);.dbd.C.dbd.CH--COR.sub.8 (A)or group (B): ##STR2## wherein R.sub.8 represents alkyl, and R.sub.9 and R.sub.10 each represents hydrogen or an organic residue; with the proviso that when X represents group (A), then R.sub.1 and R.sub.3 both represent hydrogen, R.sub.2 represents --OR.sub.5, R.sub.4 represents OR.sub.7 and the bond between the carbon atom to which X is attached and the carbon atom to which R.sub.4 is attached is a single bond, and when X represents group (B), then R.sub.1 represents .dbd.O, R.sub.2 represents hydrogen, R.sub.3 represents --OR.sub.6 and the bond between the carbon atom to which X is attached and the carbon atom to which R.sub.4 is attached is a double bond, or a pharmaceutically acceptable salt thereof, or a compound of the general formula (II): ##STR3## wherein R.sub.11 represents hydrogen or an organic residue, and R.sub.12, R.sub.13 and R.sub.14 each represents an organic residue, or and a pharmaceutically acceptable salt thereof. The compounds of the general formulae (I) and (II) can be derived from compounds contained in a hot water extract of cinnamon.

公开(公告)号：US4560556A

公开(公告)日：1985-12-24

申请号：US572750

申请日：1984-01-23

申请人： Yoshio Kagitani ,  Kenji Tanaka ,  Yasuo Ueda ,  Yusei Shiraga ,  Tunetaka Nakajima ,  Takuji Doi ,  Takao Ohmura ,  Satoshi Funakoshi ,  Tadakazu Suyama

发明人： Yoshio Kagitani ,  Kenji Tanaka ,  Yasuo Ueda ,  Yusei Shiraga ,  Tunetaka Nakajima ,  Takuji Doi ,  Takao Ohmura ,  Satoshi Funakoshi ,  Tadakazu Suyama

IPC分类号： C07K14/705 ,  A61K31/40 ,  A61K31/43 ,  A61K31/545 ,  A61K31/70 ,  A61K38/00 ,  A61K38/16 ,  A61K38/22 ,  A61K47/48 ,  C07K14/435 ,  C07K14/78 ,  C07K19/00 ,  A61K35/16 ,  A61K37/04

CPC分类号： C07K14/78 ,  A61K47/48292 ,  A61K38/00 ,  Y10S530/829 ,  Y10S530/83

摘要： Physiologically active substances such as antibiotics can preferentially be carried to a morbid part, for example, injured tissue and neoplastic cell proliferation site by administering its complex with fibronectin to repair the morbid part. The complex is prepared by the reaction between the physiologically active substance and the fibronectin with or without intervention of a protein cross-linking agent.

摘要翻译： 生理活性物质如抗生素可以优先通过给予其与纤连蛋白的复合物来修复病态部分而被携带到病态部分，例如损伤组织和肿瘤细胞增殖部位。 该复合物通过蛋白质交联剂的介导或不涉及生理活性物质与纤连蛋白之间的反应来制备。

公开(公告)号：US4888417A

公开(公告)日：1989-12-19

申请号：US867169

申请日：1986-05-27

申请人： Yusei Shiraga ,  Chikara Fukaya ,  Toshiaki Akira ,  Masakazu Iwai ,  Kazumasa Yokoyama ,  Mamoru Tabata ,  Hiroshi Fukui ,  Shigeo Tanaka ,  Yoshiro Iga ,  Tadakazu Suyama ,  Kanemichi Okano

发明人： Yusei Shiraga ,  Chikara Fukaya ,  Toshiaki Akira ,  Masakazu Iwai ,  Kazumasa Yokoyama ,  Mamoru Tabata ,  Hiroshi Fukui ,  Shigeo Tanaka ,  Yoshiro Iga ,  Tadakazu Suyama ,  Kanemichi Okano

IPC分类号： A61K31/12 ,  A61K31/70 ,  A61K36/54 ,  C07C49/242 ,  C07C49/255 ,  C07C49/647 ,  C07C49/743 ,  C07H15/18 ,  C07H15/203 ,  C07H15/207

CPC分类号： C07C403/08 ,  C07C403/10 ,  C07C403/12 ,  C07H15/18 ,  C07H15/203 ,  C07C2101/16 ,  Y10S514/927

摘要： A therapeutic and prophylactic agent for peptic ulcers which contains as an active ingredient a compound of the general formula (I): ##STR1## wherein R.sub.1 represents hydrogen or =O; R.sub.2 represents hydrogen or --OR.sub.5 ; R.sub.3 represents hydrogen or --OR.sub.6 ; R.sub.4 represents --OR.sub.7 in the case of the absence of double bond; R.sub.5, R.sub.6 and R.sub.7 each represents hydrogen or an organic residue;X represents group (A):.dbd.C.dbd.CH--COR.sub.8 (A) or group (B): ##STR2## wherein R.sub.8 represents alkyl, and R.sub.9 and R.sub.10 each represents hydrogen or an organic residue; with the proviso that when X represents group (A), then R.sub.1 and R.sub.3 both represent hydrogen, R.sub.2 represents --OR.sub.5 ; R.sub.4 represents OR.sub.7 and the bond between the carbon atoms to which X is attached and the carbon atom to which R.sub.4 is attached is a single bond, and when X represents group (B), then R.sub.1 represents .dbd.O, R.sub.2 represents hydrogen, R.sub.3 represents --OR.sub.6 and the bond between the carbon atom to which X is attached and the carbon atom to which R.sub.4 is attached is a double bond, or a pharmaceutically acceptable salt thereof, or a compound of the general formula (II): ##STR3## wherein R.sub.11 represents hydrogen or an organic residue, and R.sub.12, R.sub.13 and R.sub.14 each represents an organic residue, or a pharmaceutically acceptable salt thereof. The compounds of the general formulae (I) and (II) can be derived from compounds contained in a hot water extract of cinnamon.

摘要翻译： 含有作为活性成分的通式（I）的化合物的消化性溃疡的治疗和预防剂：其中R1表示氢或= O; R2代表氢或-OR5; R3表示氢或-OR6; 在不存在双键的情况下，R4代表-OR7; R5，R6和R7各自表示氢或有机残基; X表示基团（A）：= C = CH-COR 8（A）或基团（B）：其中R 8表示烷基，R 9和R 10各自表示氢或有机残基; 条件是当X表示基团（A）时，则R1和R3都表示氢，R2表示-OR5; R4表示OR7，X所连接的碳原子和与R4连接的碳原子之间的键为单键，当X表示基团（B）时，则R 1表示= O，R 2表示氢，R 3表示 -OR 6和X所连接的碳原子和与R 4连接的碳原子之间的键是双键，或其药学上可接受的盐或通式（II）的化合物：（ II）其中R 11表示氢或有机残基，R 12，R 13和R 14各自表示有机残基或其药学上可接受的盐。 通式（I）和（II）的化合物可以衍生自肉桂热水提取物中所含的化合物。

公开(公告)号：US4587052A

公开(公告)日：1986-05-06

申请号：US578032

申请日：1984-02-08

申请人： Yasuo Ueda ,  Yusei Shiraga ,  Satoshi Morimoto ,  Yoshio Kagitani ,  Satoshi Funakoshi ,  Tadakazu Suyama

发明人： Yasuo Ueda ,  Yusei Shiraga ,  Satoshi Morimoto ,  Yoshio Kagitani ,  Satoshi Funakoshi ,  Tadakazu Suyama

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Benzodiazepine derivative represented by the following general formula or pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 is --COR.sup.4 (R.sup.4 is a carboxylic acid residue) or an alkyl or aralkyl group (these groups have a substituent selected from a carboxyl group, an amino group and a cyano group), R.sup.2 is a lower alkyl group and R.sup.3 is a hydrogen atom or a lower alkyl group.The above compound is low in toxicity and has an antitumor activity.

摘要翻译： 由下列通式表示的苯并二氮杂衍生物或其药学上可接受的盐：其中R 1为-COR 4（R 4为羧酸残基）或烷基或芳烷基（这些基团具有选自羧基，氨基 基和氰基），R2是低级烷基，R3是氢原子或低级烷基。 上述化合物的毒性低，具有抗肿瘤活性。