公开(公告)号：US5326785A

公开(公告)日：1994-07-05

申请号：US040604

申请日：1993-03-31

申请人： Hidetsura Cho ,  Mie Tamaoka ,  Seiitsu Murota ,  Ikuo Morita

发明人： Hidetsura Cho ,  Mie Tamaoka ,  Seiitsu Murota ,  Ikuo Morita

IPC分类号： A61K31/275 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4418 ,  A61P9/00 ,  A61P9/10 ,  C07C255/23 ,  C07C255/41 ,  C07C271/44 ,  C07C323/16 ,  C07C323/18 ,  C07D213/30 ,  C07D233/60 ,  C07D307/42 ,  C07D333/16 ,  C07D521/00 ,  C07D317/08 ,  A61K31/21

CPC分类号： C07D213/30 ,  C07C255/23 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D307/42 ,  C07D333/16

摘要： Described are caffeic acid derivatives represented by the following formula: ##STR1## wherein either one of R.sup.1 and R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a group --CO.sub.2 R.sup.4, or a group --CONR.sup.5 R.sup.6, R.sup.4, R.sup.5 and R.sup.6 being either a hydrogen atom or a particular group, and the other is the group --CO.sub.2 R.sup.4 or the group --CONR.sup.5 R.sup.6, or R.sup.1 and R.sup.2 are coupled together to represent a 5-membered ring so formed, Y represents a particular group or atom, X represents a substituted or unsubstituted C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.12 aralkyl, heterocyclic or heterocyclic ring-alkyl group, m and n stand for particular integers, and R.sup.3 represents a hydrogen atom, a hydroxyl group, a group --OCO.sub.2 R.sup.7, R.sup.7 being a hydrogen atom or a particular group, or a group --OCONR.sup.8 R.sup.9, R.sup.8 representing a C.sub.1 -C.sub.6 alkyl group and R.sup.9 representing a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and pharmaceutically acceptable salts thereof. Therapeutic agents containing the derivatives or salts are effective for diseases of the circulatory system.

摘要翻译： 描述的是由下式表示的咖啡酸衍生物：其中R 1和R 2中的任一个是氢原子，C 1 -C 6烷基，-CO 2 R 4基或-CONR 5 R 6基，R 4，R 5和R 6是 另一个是-CO 2 R 4或-CONR 5 R 6基团，或者R 1和R 2连接在一起以表示如此形成的5元环，Y表示特定的基团或原子，X表示 取代或未取代的C 6 -C 10芳基，C 7 -C 12芳烷基，杂环或杂环环烷基，m和n表示特定整数，R 3表示氢原子，羟基，-OCO 2 R 7基，R 7为氢 或基团-OCONR 8 R 9，R 8表示C 1 -C 6烷基，R 9表示氢原子或C 1 -C 6烷基，及其药学上可接受的盐。 含有衍生物或盐的治疗剂对于循环系统的疾病是有效的。

公开(公告)号：US5063243A

公开(公告)日：1991-11-05

申请号：US344583

申请日：1989-04-28

申请人： Hidetsura Cho ,  Masaru Ueda ,  Mie Tamaoka ,  Mikiko Hamaguchi ,  Seiitsu Murota ,  Ikuo Morita

发明人： Hidetsura Cho ,  Masaru Ueda ,  Mie Tamaoka ,  Mikiko Hamaguchi ,  Seiitsu Murota ,  Ikuo Morita

IPC分类号： C07C255/34

CPC分类号： C07C255/34

摘要： Novel derivatives of caffeic acid of the general formula (I): ##STR1## wherein X is hydrogen atom or hydroxy; R.sup.1 is hydrogen atom, a straight or branched alkyl or alkenyl having 1 to 20 carbon atoms or a group of the formula:--(CH.sub.2).sub.n --Z--R.sup.2wherein n is an integer of 1 to 10; Z is oxygen atom, vinylene residue or a single bond; and R.sup.2 is a substituted or unsubstituted phenyl or heterocyclic residue is provided. These derivatives possess 12-lipoxygenase inhibitory activity and are useful for curing and preventing circulatory diseases. A pharmaceutical composition containing said derivtive is also provided.

公开(公告)号：US5232941A

公开(公告)日：1993-08-03

申请号：US750396

申请日：1991-08-27

申请人： Hidetsura Cho ,  Mie Tamaoka ,  Seiitsu Murota ,  Ikuo Morita

发明人： Hidetsura Cho ,  Mie Tamaoka ,  Seiitsu Murota ,  Ikuo Morita

IPC分类号： A61K31/275 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4418 ,  A61P9/00 ,  A61P9/10 ,  C07C255/23 ,  C07C255/41 ,  C07C271/44 ,  C07C323/16 ,  C07C323/18 ,  C07D213/30 ,  C07D233/60 ,  C07D307/42 ,  C07D333/16 ,  C07D521/00

CPC分类号： C07D213/30 ,  C07C255/23 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D307/42 ,  C07D333/16

摘要： Described are caffeic acid derivatives represented by the following formula: ##STR1## wherein either one of R.sup.1 and R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a group --CO.sub.2 R.sup.4, or a group --CONR.sup.5 R.sup.6, R.sup.4, R.sup.5 and R.sup.6 being either a hydrogen atom or a particular group, and the other is the group --CO.sub.2 R.sub.4 or the group --CONF.sup.5 R.sup.6, or R.sup.1 and R.sup.2 are coupled together to represent a 5-membered ring so formed, Y represents a particular group or atom, X represents a substituted or unsubstituted C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.12 aralkyl, heterocyclic or heterocyclic ring-alkyl group, m and n stand for particular integers, and R.sub.3 represents a hydrogen atom, a hydroxyl group, a group --OCO.sub.2 R.sup.7, R.sup.7 being a hydrogen atom or a particular group, or a group --OCONR.sup.8 R.sup.9, R.sup.8 representing a C.sub.1 -C.sub.6 alkyl group and R.sup.9 representing a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and pharmaceutically acceptable salts thereof. Therapeutic agents containing the derivatives or salts are effective for diseases of the circulatory system.

公开(公告)号：US4673684A

公开(公告)日：1987-06-16

申请号：US719131

申请日：1985-04-02

申请人： Toshio Wakabayashi ,  Makoto Takai ,  Shuji Ichikawa ,  Jun-ichiro Arai ,  Seiitsu Murota

发明人： Toshio Wakabayashi ,  Makoto Takai ,  Shuji Ichikawa ,  Jun-ichiro Arai ,  Seiitsu Murota

IPC分类号： C07C33/46 ,  C07C45/71 ,  C07C47/575 ,  C07C59/64 ,  C07D211/46 ,  C07D213/66 ,  C07D277/16 ,  C07D295/088 ,  C07D295/13 ,  C07D295/185 ,  C07D295/192 ,  C07D295/205 ,  C07D317/60 ,  C07D401/06 ,  C07D417/12 ,  C07D473/08 ,  A61K31/445 ,  C07D405/12

CPC分类号： C07D213/66 ,  C07C33/46 ,  C07C45/71 ,  C07C47/575 ,  C07C59/64 ,  C07D211/46 ,  C07D277/16 ,  C07D295/088 ,  C07D295/13 ,  C07D295/185 ,  C07D295/192 ,  C07D295/205 ,  C07D317/60 ,  C07D401/06 ,  C07D417/12 ,  C07D473/08 ,  Y10S514/826

摘要： According to the invention, there are provided novel amide derivatives and 5-lipoxygenase inhibitors containing the same as an effective ingredient.The above-mentioned compounds of the invention have been demonstrated to posses 5-lipoxygenase-inhibiting activities. These compounds can inhibit the production of leucotrienes such as LTC.sub.4 and LTD.sub.4 which are allergy-inducing factors by inhibiting the activity of 5-lipoxygenase. Accordingly, the amide derivatives can be used as 5-lipoxygenase inhibitors effective for allergic asthma, allergic rhinitis and the like.

摘要翻译： 根据本发明，提供了含有与有效成分相同的酰胺衍生物和5-脂氧合酶抑制剂。 已经证明了本发明的上述化合物具有5-脂氧合酶抑制活性。 这些化合物可通过抑制5-脂氧合酶的活性来抑制作为过敏诱导因子的白三烯如LTC4和LTD4的产生。 因此，酰胺衍生物可以用作对过敏性哮喘，过敏性鼻炎等有效的5-脂氧合酶抑制剂。

公开(公告)号：US5130483A

公开(公告)日：1992-07-14

申请号：US460335

申请日：1990-05-18

申请人： Hiroyuki Ohnishi ,  Shingo Koyama ,  Ryoichi Nanba ,  Syozo Miyaoka ,  Akira Masuda ,  Yoshiyuki Shikata ,  Hideto Ushijima ,  Seiitsu Murota

发明人： Hiroyuki Ohnishi ,  Shingo Koyama ,  Ryoichi Nanba ,  Syozo Miyaoka ,  Akira Masuda ,  Yoshiyuki Shikata ,  Hideto Ushijima ,  Seiitsu Murota

IPC分类号： C07C45/66 ,  C07C45/67 ,  C07C45/72 ,  C07C49/248 ,  C07C49/255 ,  C07C235/34

CPC分类号： C07C235/34 ,  C07C45/66 ,  C07C45/673 ,  C07C45/72 ,  C07C49/248 ,  C07C49/255

摘要： Isoprenoid derivatives represented by the general formula (I) ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, X represents --CH.sub.2 --, --O-- or --NH--, n represents number of the double bond in trans-configuration and is 1 or 2, and m is an integer from 0 to 3.The compounds have a 5-lipoxygenase-inhibiting activity and are useful as a therapeutic agent for such diseases as allergy, nephritis, hepatitis, rheumatism and gastric ulcer.