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    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof
    52.
    发明授权
    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof 失效
    三环稠合杂环化合物，其制备方法及其应用

    公开(公告)号：US06700013B2

    公开(公告)日：2004-03-02

    申请号：US10291429

    申请日：2002-11-12

    申请人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    发明人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    IPC分类号： C07C53134

    CPC分类号： C07D405/04 ,  A61K31/31 ,  A61K31/335 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/4353 ,  A61K31/4427 ,  C07D313/14 ,  C07D337/14 ,  C07D407/04 ,  C07D409/04 ,  C07D491/04

    摘要： Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR′ (wherein R and R′ are the same as the above defined R); Y is, for example, CH, CH2 or C═O; Z is, for example, O, S, S═O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.

    摘要翻译： 由式（1）表示的化合物，其中X为例如CH，CH 2，CHR（其中R为低级烷基或取代的低级烷基）或CRR'（其中R和R'与上述定义相同 Y）为例如CH，CH 2或C = O; Z为例如O，S，S = O或SO 2; U为C或N; R 1至R 4各自独立地为例如 氢原子，OR，SR（其中R与上述定义相同）或芳环，取代的芳环或杂环; R 5和R 8中的至少一个是例如OH，剩余的R 5和R 8 各自独立地，例如，氢原子或OH，其旋光异构体，其结合物或其药学上可接受的盐。 这些化合物的特征在于具有广泛的药理作用，例如气管平滑肌的优异的缓解作用，气道超敏反应的抑制和抑制炎症细胞浸润到气道中，另外还具有高安全性。

    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof
    53.
    发明申请
    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof 失效
    三环稠合杂环化合物，其制备方法及其应用

    公开(公告)号：US20030220360A1

    公开(公告)日：2003-11-27

    申请号：US10291429

    申请日：2002-11-12

    申请人： Nippon Suisan Kaisha, Ltd., a Japan corporation

    发明人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    IPC分类号： C07D337/12 ,  C07D337/16 ,  C07D491/02 ,  C07D498/02 ,  A61K031/4743 ,  A61K031/4741 ,  A61K031/335 ,  A61K031/38

    CPC分类号： C07D405/04 ,  A61K31/31 ,  A61K31/335 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/4353 ,  A61K31/4427 ,  C07D313/14 ,  C07D337/14 ,  C07D407/04 ,  C07D409/04 ,  C07D491/04

    摘要： Compounds represented by formula (1), 1 wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRRnull (wherein R and Rnull are the same as the above defined R); Y is, for example, CH, CH2 or CnullO; Z is, for example, O, S, SnullO or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.

    摘要翻译： 由式（1）表示的化合物，其中X为例如CH，CH 2，CHR（其中R为低级烷基或取代的低级烷基）或CRR'（其中R和R'与上述相同 定义R）; Y为例如CH，CH 2或C = O; Z是例如O，S，S = O或SO 2; U是C或N; R 1至R 4各自独立地为例如氢原子，OR，SR（其中R与上述定义相同），或芳香环，取代的芳环或杂环; R5和R8中的至少一个是例如OH，并且R5和R8的剩余部分各自独立地为例如氢原子或OH，其光学异构体，其缀合物或其药学上可接受的盐。 这些化合物的特征在于具有广泛的药理作用，例如气管平滑肌的优异的缓解作用，气道超敏反应的抑制和抑制炎症细胞浸润到气道中，另外还具有高安全性。

    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof
    54.
    发明授权
    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof 失效
    三环稠合杂环化合物，其制备方法及其应用

    公开(公告)号：US06602898B1

    公开(公告)日：2003-08-05

    申请号：US09980581

    申请日：2002-02-26

    申请人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    发明人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    IPC分类号： A61K3138

    CPC分类号： C07D405/04 ,  A61K31/31 ,  A61K31/335 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/4353 ,  A61K31/4427 ,  C07D313/14 ,  C07D337/14 ,  C07D407/04 ,  C07D409/04 ,  C07D491/04

    摘要： Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR′ (wherein R and R′ are the same as the above defined R); Y is, for example, CH, CH2 or C═O; Z is, for example, O, S, S=O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.

    摘要翻译： 由式（1）表示的化合物，其中X为例如CH，CH 2，CHR（其中R为低级烷基或取代的低级烷基）或CRR'（其中R和R'与上述定义相同 Y）为例如CH，CH 2或C = O; Z为例如O，S，S = O或SO 2; U为C或N; R 1至R 4各自独立地为例如 氢原子，OR，SR（其中R与上述定义相同）或芳环，取代的芳环或杂环; R 5和R 8中的至少一个是例如OH，剩余的R 5和R 8 各自独立地，例如，氢原子或OH，其旋光异构体，其结合物或其药学上可接受的盐。 这些化合物的特征在于具有广泛的药理作用，例如气管平滑肌的优异的缓解作用，气道超敏反应的抑制和抑制炎症细胞浸润到气道中，另外还具有高安全性。

    Anti-neurodegeneratively active 10-aminoaliphatyl-dibenzi �b,f! oxepines
    55.
    发明授权
    Anti-neurodegeneratively active 10-aminoaliphatyl-dibenzi �b,f! oxepines 失效
    抗神经变性活性的10-氨基二苯基二苯并（B，F）氧杂七环素

    公开(公告)号：US5780500A

    公开(公告)日：1998-07-14

    申请号：US844135

    申请日：1997-04-18

    申请人： Claudia Betschart ,  Kaspar Zimmermann

    发明人： Claudia Betschart ,  Kaspar Zimmermann

    IPC分类号： A61K31/335 ,  A61K31/4025 ,  A61K31/4523 ,  A61K31/5377 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07D313/14

    CPC分类号： C07D313/14

    摘要： Base-substituted debenz�b,f!oxepines of formula I ##STR1## wherein alk is a divalent aliphatic radical, R is an amino group that is unsubstituted or mono- or di-substituted by monovalent aliphatic and/or araliphatic radicals or disubstituted by divalent aliphatic radicals, and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, and pharmaceutically acceptable salts thereof, may be used as anti-neurodegenerative active ingredients of medicaments. The invention relates also to novel compounds of formula I.

    摘要翻译： 式I的碱取代的脱苄基[b，f]氧杂七环素其中alk是二价脂族基团，R是未被取代的或被一价脂族和/或芳脂族基团单取代或二取代的氨基 或二价脂族基团二取代，R 1，R 2，R 3和R 4各自独立地为氢，低级烷基，低级烷氧基，卤素或三氟甲基及其药学上可接受的盐，可用作抗神经变性活性成分 的药物。 本发明还涉及式I的新化合物。

    Anti-oxidative tricyclic, condensed heterocyclic compound
    56.
    发明授权
    Anti-oxidative tricyclic, condensed heterocyclic compound 失效
    抗氧化三环，稠合杂环化合物

    公开(公告)号：US5734067A

    公开(公告)日：1998-03-31

    申请号：US809001

    申请日：1997-03-04

    申请人： Shuji Jinno ,  Yasuyo Kogure ,  Hiroyuki Onuki ,  Takaaki Okita

    发明人： Shuji Jinno ,  Yasuyo Kogure ,  Hiroyuki Onuki ,  Takaaki Okita

    IPC分类号： C07D313/14 ,  C07D337/14 ,  C07D493/04

    CPC分类号： C07D493/04 ,  C07D313/14 ,  C07D337/14

    摘要： Providing a novel tricyclic, condensed heterocyclic compound having an anti-oxidative action and being promising for use in pharmaceutical agents, cosmetics, chemical products and the like. By chemical synthesis, a novel anti-oxidative, tricyclic, condensed heterocyclic compound represented by the following formula: ##STR1## (wherein X--Y represents CH.sub.2 --C.dbd.O, CH.sub.2 --CH.sub.2 or CH.dbd.CH; Z represents O, S, or S.dbd.O; R.sub.1 to R.sub.8 represent independently those selected from the group consisting of hydrogen atom, a hydroxyl group, a halogen group, a lower alkyl group, a lower alkoxyl group, a lower alkyl ketone group and CF.sub.3 ; and at least two of R.sub.1 to R.sub.4 are hydroxyl groups); and the salts thereof are provided. The compound has an anti-oxidative activity at the same degree as or higher than the activity of .alpha.-tocopherol, so the compound is promising as a therapeutic drug for a variety of diseases, such as cancer, arteriosclerosis, or liver diseases, in which it is believed that biological lipid peroxides may be involved.

    摘要翻译： PCT No.PCT / JP95 / 01975 Sec。 371日期1997年3月4日 102（e）1997年3月4日PCT PCT 1995年9月28日PCT公布。 WO96 / 10021 PCT出版物 日期1996年4月4日提供具有抗氧化作用的新型三环稠合杂环化合物，并且有希望用于药剂，化妆品，化学产品等。 通过化学合成，由下式表示的新型抗氧化三环稠合杂环化合物：其中XY表示CH 2 -C = O，CH 2 -CH 2或CH = CH; Z表示O，S或S = O; R 1〜R 8分别独立地表示选自氢原子，羟基，卤素基，低级烷基，低级烷氧基，低级烷基酮基和CF 3的化合物; R 1〜 R4为羟基）; 并提供其盐。 该化合物具有与α-生育酚活性相同或更高的抗氧化活性，因此该化合物作为各种疾病如癌症，动脉硬化或肝脏疾病的治疗药物是有希望的，其中 相信可能涉及生物脂质过氧化物。

    Tricyclic aromatic compounds
    57.
    发明授权
    Tricyclic aromatic compounds 失效
    三环芳香族化合物

    公开(公告)号：US4923892A

    公开(公告)日：1990-05-08

    申请号：US356884

    申请日：1989-05-23

    申请人： O. William Lever, Jr. ,  Harry J. Leighton

    发明人： O. William Lever, Jr. ,  Harry J. Leighton

    IPC分类号： C07C229/38 ,  C07D313/12 ,  C07D313/14

    CPC分类号： C07D313/12 ,  C07C229/38 ,  C07D313/14 ,  C07C2103/32 ,  Y10S514/826

    摘要： The present invention relates to compounds of formula I ##STR1## or a salt, ester or amide thereof; wherein R.sup.1 is --CH.sub.2 --CH.sub.2 --, CH.sub.2 --O-- or --O--CH.sub.2 --; R.sup.2 and R.sup.3 are the same or different and are each hydrogen, C.sub.1-4 alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members; R.sup.4 is a single bond or a C.sub.1-7 bivalent aliphatic hydrocarbon group and may be joined to the aromatic ring system at the 2,3,8 or 9 positions; n is 0 to 3, and their use as antihistamine and antiasthma agents.

    摘要翻译： 本发明涉及式Ⅰ化合物或其盐，酯或酰胺; 其中R1是-CH2-CH2-，CH2-O-或-O-CH2-; R2和R3相同或不同，各自为氢，C1-4烷基或与氮一起包含含有4-6个环成员的含氮杂环; R4是单键或C1-7二价脂族烃基，并且可以在2,3,8或9位连接到芳环体系; n为0〜3，用作抗组胺药和止喘药。

    Analgesic dibenz[b,f]oxepins
    59.
    发明授权
    Analgesic dibenz[b,f]oxepins 失效
    止痛二苯并[b，f] oxepins

    公开(公告)号：US4496582A

    公开(公告)日：1985-01-29

    申请号：US560717

    申请日：1983-12-12

    申请人： Helen H. Ong ,  Matthew J. Flynn

    发明人： Helen H. Ong ,  Matthew J. Flynn

    IPC分类号： C07D313/06 ,  A61K31/335 ,  A61P25/04 ,  C07D313/14 ,  C07D407/12

    CPC分类号： C07D407/12 ,  C07D313/14

    摘要： There are described analgesic dibenz[b,f]oxepins having the general formula ##STR1## wherein n is an odd integer 1-7 inclusive; R is --CO.sub.2 R.sub.1 or --CH.sub.2 OR.sub.2 where R.sub.1 is H, C.sub.1-5 lower alkyl, aralkyl, ##STR2## R.sub.3 being C.sub.1-5 lower alkyl; X and Y are each independently hydrogen, halogen, trifluoromethyl, C.sub.1-5 lower alkoxy, C.sub.1-5 lower alkyl, C.sub.1-5 lower alkylthio, or hydroxy; and the dotted line may be a bond or nothing.

    摘要翻译： 描述了具有通式为“IMAGE”的镇痛二苯并[b，f]氧杂七环素，其中n为整数1-7; R是-CO 2 R 1或-CH 2 OR 2，其中R 1是H，C 1-5低级烷基，芳烷基，R 3是C 1-5低级烷基; X和Y各自独立地为氢，卤素，三氟甲基，C 1-5低级烷氧基，C 1-5低级烷基，C 1-5低级烷硫基或羟基; 而虚线可能是一个债券或一无所有。