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    Quinoline-N-oxide derivative and pharmaceutical composition
    2.
    发明授权
    Quinoline-N-oxide derivative and pharmaceutical composition 失效
    喹啉-N-氧化物衍生物和药物组合物

    公开(公告)号：US4657916A

    公开(公告)日：1987-04-14

    申请号：US772693

    申请日：1985-09-05

    申请人： Masayuki Teranishi ,  Koji Suzuki ,  Hiroshi Kase ,  Shigeto Kitamura ,  Katsuichi Shuto ,  Kenji Omori

    发明人： Masayuki Teranishi ,  Koji Suzuki ,  Hiroshi Kase ,  Shigeto Kitamura ,  Katsuichi Shuto ,  Kenji Omori

    IPC分类号： A61K31/47 ,  A61P43/00 ,  C07D215/60 ,  C07D405/12 ,  C07F7/18

    CPC分类号： C07D405/12 ,  C07D215/60

    摘要： A quinoline-N-oxide derivative represented by the formula: ##STR1## wherein X is hydroxy, lower alkoxy, lower alkylthio, unsubstituted or substituted aralkyloxy, or unsubstituted or substituted aralkylthio; Y is a hydrogen atom or halogen atom; R.sub.1 is alkylene or alkenylene having 3 to 15 carbon atom; Z is hydroxymethyl, lower alkoxymethyl, unsubstituted or substituted aryloxymethyl, tetrahydropyranyloxymethyl, tetrahydrofuranyloxymethyl, unsubstituted or substituted arylsulfonyloxymethyl, lower alkylthiomethyl, unsubstituted or substituted arylthiomethyl, lower alkylsulfinylmethyl, unsubstituted or substituted arylsulfinylmethyl, lower alkylsulfonylmethyl, unsubstituted or substituted arylsulfonylmethyl, aminomethyl, --CH.sub.2 NHR.sub.2 (wherein R.sub.2 is lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), --CH.sub.2 NR.sub.3 R.sub.4 (wherein R.sub.3 and R.sub.4 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), --CH.sub.2 N.sup.+ R.sub.5 R.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl, where the counterion is an anion of acid or a hydroxyl ion), --COR.sub.8 (wherein R.sub.8 is a hydrogen atom, lower alkyl or hydroxy), --CH(OR.sub.9).sub.2 (wherein R.sub.9 is lower alkyl), iminomethyl, hydroxyiminomethyl, or a halogen atom and its salts, can very strongly inhibit the lipoxygenase and considerably suppress production and release of its metabolites, and thus are useful as preventive and healing agents for the diseases caused by the lipoxygenase metabolites.

    摘要翻译： 由下式表示的喹啉-N-氧化物衍生物：其中X为羟基，低级烷氧基，低级烷硫基，未取代或取代的芳烷氧基，或未取代或取代的芳烷硫基; Y是氢原子或卤素原子; R1是具有3至15个碳原子的亚烷基或亚烯基; Z是羟甲基，低级烷氧基甲基，未取代或取代的芳氧基甲基，四氢吡喃氧基甲基，四氢呋喃氧基甲基，未取代或取代的芳基磺酰氧基甲基，低级烷硫基甲基，未取代或取代的芳基硫代甲基，低级烷基亚磺酰基甲基，未取代或取代的芳基亚磺酰基甲基，低级烷基磺酰基甲基，未取代或取代的芳基磺酰基甲基，氨基甲基，-CH2NHR2（ 其中R 2是低级烷基，未取代或取代的芳烷基或未取代或取代的芳基），-CH 2 NR 3 R 4（其中R 3和R 4是低级烷基，未取代或取代的芳烷基，或未取代或取代的芳基），-CH 2 N + R 5 R 6 R 7（其中R 5，R 6 ，R 7为低级烷基，未取代或取代的芳烷基或未取代或取代的芳基，其中抗衡离子为酸或羟基离子的阴离子），-COR8（其中R8为氢原子，低级烷基或羟基），-CH （OR 9）2（其中R 9为低级烷基），亚氨基甲基，羟基亚氨基甲基或卤素 原子及其盐可以非常强烈地抑制脂氧合酶，并显着抑制其代谢物的产生和释放，因此可用作由脂氧合酶代谢物引起的疾病的预防和治疗剂。

    CONTAINER
    3.
    发明申请
    CONTAINER 审中-公开
    容器

    公开(公告)号：US20100219094A1

    公开(公告)日：2010-09-02

    申请号：US12302006

    申请日：2007-05-22

    申请人： Masashi Moteki ,  Minoru Honda ,  Kenji Omori

    发明人： Masashi Moteki ,  Minoru Honda ,  Kenji Omori

    IPC分类号： B65D73/00

    CPC分类号： A61J1/10 ,  A61J1/2024 ,  A61J1/2093 ,  B32B7/05 ,  B32B15/08 ,  B32B27/306 ,  B32B27/32 ,  B32B27/34 ,  B32B27/365 ,  B32B2255/10 ,  B32B2255/20 ,  B32B2255/205 ,  B32B2307/7244 ,  B32B2439/46 ,  B32B2439/80 ,  B32B2535/00 ,  B65D81/24 ,  B65D81/3266

    摘要： A drug container with no need to peel a gas-barrier film or with no need to contain a desiccant, an oxygen absorbent or the like, in which the contents therein can be seen by the naked eyes. The container (10) comprises a front sheet (20) and a rear sheet (22), the front sheet (20) and the rear sheet (22) being fusion-bonded each other so as to form a space (14) therebetween, wherein the front sheet is constituted of a multilayered film having a linear-polyolefin layer as the outermost layer, wherein the rear sheet is constituted of a multilayered film having at least one selected from a group consisting of a metal foil, a vapor-deposited metal layer and a vapor-deposited inorganic layer, and wherein a transparent covering sheet (24) comprising a film having a vapor-deposited metal oxide layer is fusion-bonded to the front sheet so that the entire outer surface of at least a part of the front sheet which forms the space can be covered with the transparent covering sheet (24).

    摘要翻译： 不需要剥离阻气膜的药物容器，也可以不含有通过肉眼可以看到内容物的干燥剂，氧吸收剂等。 容器（10）包括前片（20）和后片（22），前片（20）和后片（22）彼此熔合以在其间形成间隙（14） 其特征在于，所述前片由具有直链状聚烯烃层作为最外层的多层膜构成，所述后片由具有选自金属箔，气相沉积金属 层和气相沉积无机层，并且其中将包含具有气相沉积金属氧化物层的膜的透明覆盖片（24）熔融粘合到前片，使得至少一部分的整个外表面 可以用透明覆盖片（24）覆盖形成空间的前片。

    Cyclic compounds
    5.
    发明申请
    Cyclic compounds 审中-公开
    环状化合物

    公开(公告)号：US20080027037A1

    公开(公告)日：2008-01-31

    申请号：US11889749

    申请日：2007-08-16

    申请人： Koichiro Yamada ,  Kenji Matsuki ,  Kenji Omori ,  Kohei Kikkawa

    发明人： Koichiro Yamada ,  Kenji Matsuki ,  Kenji Omori ,  Kohei Kikkawa

    IPC分类号： A61K31/495 ,  A61K31/40 ,  A61K31/496 ,  A61K31/497 ,  A61K31/53 ,  A61K31/553 ,  A61P9/00 ,  C07D239/02 ,  C07D401/02 ,  C07D498/14 ,  C07D498/04 ,  C07D413/02 ,  C07D403/02 ,  C07D253/065 ,  C07D207/44 ,  A61P5/00 ,  A61K31/535 ,  A61K31/505 ,  A61K31/4965 ,  A61K31/44

    CPC分类号： C07D401/12 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/56 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07F9/65583

    摘要： 1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, —O—, —CH═N—, —N═CH—, —N═N—, —CH═CH—, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring. The compound of the present invention has excellent selective PDE V inhibitory activity and therefore, is useful as a therapeutic or prophylactic drug for treating various diseases due to functional disorders on cGMP-signaling.

    摘要翻译： 1.式（I）的环状化合物或其药理学上可接受的盐，其中X是-CH-或-N-，Y是-NH-，-NR 4 - ， - S- ，-O - ， - CH-N - ， - N-CH - ， - N - ， - CH-CH-等，R 1是低级烷氧基，氨基， 含有N原子的杂环或被含有N原子（各自任选被取代的）的杂环取代的羟基，R 2是任选地是低级烷基氨基 被芳基取代，任选被芳基取代的低级烷氧基，被含有N原子的芳族杂环取代的低级烷氧基，R 3是芳基， 含有N原子，低级烷基，低级烷氧基，环低级烷氧基，被含有N原子的杂环取代的羟基或氨基的杂环（各自为 任选取代的）和R 3和Y中的取代基可以组合形成 内酯环。 本发明的化合物具有优异的选择性PDE V抑制活性，因此可用作治疗或预防药物，用于治疗由于cGMP信号传导的功能紊乱引起的各种疾病。

    Aromatic nitrogen-containing 6-membered cyclic compounds
    6.
    发明授权
    Aromatic nitrogen-containing 6-membered cyclic compounds 有权
    芳香族含氮6元环状化合物

    公开(公告)号：US06797709B2

    公开(公告)日：2004-09-28

    申请号：US10426884

    申请日：2003-05-01

    申请人： Koichiro Yamada ,  Kenji Matsuki ,  Kenji Omori ,  Kohei Kikkawa

    发明人： Koichiro Yamada ,  Kenji Matsuki ,  Kenji Omori ,  Kohei Kikkawa

    IPC分类号： C07D24110

    CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07F9/6512 ,  C07F9/65583

    摘要： An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, —NH—Q—R3 (R3 is a substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or —NH—R4 (R4 is a substituted or unsubstituted cycloalkyl group); R2 is a substituted or unsubstituted aryl group; one of Y and Z is ═CH—, and the other is ═N—, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.

    摘要翻译： 式（I）的芳香族含氮6元环状化合物：其中环A是取代或未取代的含氮杂环基; R 1是取代或未取代的低级烷基，-NH-QR 3（R 3是取代或未取代的含氮杂环基，Q是低级亚烷基或单键）或 - NH-R 4（R 4是取代或未取代的环烷基）; R 2是取代或未取代的芳基; Y和Z之一是= CH-，另一个是= N-或其药学上可接受的盐，这些化合物表现出优异的选择性PDE V抑制活性，因此可用于预防或治疗阴茎勃起功能障碍， 等等

    Aromatic nitrogen-containing 6-membered cyclic compounds
    8.
    发明授权
    Aromatic nitrogen-containing 6-membered cyclic compounds 有权
    芳香族含氮6元环状化合物

    公开(公告)号：US06656935B2

    公开(公告)日：2003-12-02

    申请号：US09925892

    申请日：2001-08-10

    申请人： Koichiro Yamada ,  Kenji Matsuki ,  Kenji Omori ,  Kohei Kikkawa

    发明人： Koichiro Yamada ,  Kenji Matsuki ,  Kenji Omori ,  Kohei Kikkawa

    IPC分类号： C07D23948

    CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07F9/6512 ,  C07F9/65583

    摘要： An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, —NH—Q—R3 (R3 is a substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or —NH—R4 (R4 is a substituted or unsubstituted cycloalkyl group); R2 is a substituted or unsubstituted aryl group; one of Y and Z is ═CH—, and the other is ═N—, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.

    摘要翻译： 式（I）的芳香族含氮6元环状化合物：其中环A是取代或未取代的含氮杂环基; R 1是取代或未取代的低级烷基，-NH-QR 3（R 3是取代或未取代的含氮杂环基，Q是低级亚烷基或单键）或 - NH-R 4（R 4是取代或未取代的环烷基）; R 2是取代或未取代的芳基; Y和Z之一是= CH-，另一个是= N-或其药学上可接受的盐，这些化合物表现出优异的选择性PDE V抑制活性，因此可用于预防或治疗阴茎勃起功能障碍， 等等