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    Quinolonecarboxylic acid derivatives or salts thereof
    3.
    发明授权
    Quinolonecarboxylic acid derivatives or salts thereof 有权
    喹诺酮羧酸衍生物或其盐

    公开(公告)号：US06335447B1

    公开(公告)日：2002-01-01

    申请号：US09647763

    申请日：2000-10-05

    申请人： Kazuya Hayashi ,  Tokunori Kito ,  Junichi Mitsuyama ,  Tetsumi Yamakawa ,  Hiroshi Kuroda ,  Hiroyo Kawafuchi

    发明人： Kazuya Hayashi ,  Tokunori Kito ,  Junichi Mitsuyama ,  Tetsumi Yamakawa ,  Hiroshi Kuroda ,  Hiroyo Kawafuchi

    IPC分类号： C07D45302

    CPC分类号： C07D401/04 ,  Y02P20/55

    摘要： Novel quinolonecarboxylic acid derivatives of general formula (1) or salts thereof which have potent antibacterial effects on gram-positive bacteria in particular Propionibacterium acnes (wherein R1 represents a hydrogen atom or a carboxyl-protective group; R2 represents an optionally substituted cycloalkyl group; R3 represents a hydrogen atom, a halogen atom, an optionally substituted alkyl, alkoxy or alkylthio group, an optionally protected hydroxyl or amino group, or a nitro group; R4 represents an optionally substituted alkyl or alkoxy group; and Z represents a pyridin-4-yl or pyridin-3-yl group which is optionally substituted with at least one group selected from a halogen atom, an optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio or amino group and an optionally protected hydroxyl or amino group).

    摘要翻译： 对革兰氏阳性细菌特别是痤疮丙酸杆菌（其中R1表示氢原子或羧基保护基团; R2表示任选取代的环烷基; R3表示任意取代的环烷基）的革兰氏阳性细菌具有强效抗菌作用的通式（1）的新型喹诺酮羧酸衍生物或其盐 表示氢原子，卤素原子，任选取代的烷基，烷氧基或烷硫基，任选保护的羟基或氨基或硝基; R 4表示任选取代的烷基或烷氧基; Z表示吡啶-4-基， 吡啶-3-基或任选被至少一个选自卤素原子，任选取代的烷基，烯基，环烷基，烷氧基，烷硫基或氨基的基团取代的吡啶-3-基，以及任意保护的羟基或氨基。

    Triazole derivatives and salts thereof, and antifungal agent containing the same
    4.
    发明授权
    Triazole derivatives and salts thereof, and antifungal agent containing the same 失效
    三唑衍生物及其盐，以及含有它们的抗真菌剂

    公开(公告)号：US5605921A

    公开(公告)日：1997-02-25

    申请号：US261952

    申请日：1994-06-17

    申请人： Hiroyuki Imaizumi ,  Tetsuya Kajita ,  Kenichi Takashima ,  Minako Yotsuji ,  Keiko Takakura ,  Akira Yotsuji ,  Junichi Mitsuyama ,  Katsumi Shimizu ,  Hiroshi Sakai ,  Hirokazu Narita

    发明人： Hiroyuki Imaizumi ,  Tetsuya Kajita ,  Kenichi Takashima ,  Minako Yotsuji ,  Keiko Takakura ,  Akira Yotsuji ,  Junichi Mitsuyama ,  Katsumi Shimizu ,  Hiroshi Sakai ,  Hirokazu Narita

    IPC分类号： A61K31/41 ,  A61P31/04 ,  A61P31/10 ,  C07D249/08 ,  C07D401/12 ,  C07D417/06 ,  C07D521/00 ,  A01N43/653

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The present invention relates to a compound represented by the general formula (1) or its salt, a process for producing the same, and an antifungal agent comprising the same as an effective component: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group bonded through a carbon atom in the ring to the main chain; R.sup.2 presents a hydrogen atom, a fluorine atom or a substituted or unsubstituted alkyl group; and R.sup.3 represents a cyano group, a thioamido group or a group represented by the formula ##STR2## in which R.sup.4 is a hydroxyl group or a group of the formula ##STR3## (R.sup.7 and R.sup.8, which may be the same or different, are hydrogen atoms or substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, amino, alkoxy, hydroxyl or heterocyclic groups, and may form a substituted or unsubstituted heterocyclic group together with the nitrogen atom to which R.sup.7 and R.sup.8 attach), R.sup.5 is a substituted or unsubstituted alkoxy group or a group of the formula ##STR4## (R.sup.7 and R.sup.8 are as defined above), and R.sup.6 is a hydrogen atom or a substituted or unsubstituted alkyl group.

    摘要翻译： 本发明涉及由通式（1）表示的化合物或其盐，其制备方法和含有该化合物的有效成分的抗真菌剂：有或无取代的芳基或取代或未取代的杂环基 通过环中的碳原子键合到主链上; R2表示氢原子，氟原子或取代或未取代的烷基; 并且R 3表示氰基，硫代酰氨基或由下式表示的基团：其中R 4是羟基或式（R 3和R 8）可以相同或不同， 氢原子或取代或未取代的烷基，烯基，炔基，环烷基，芳基，氨基，烷氧基，羟基或杂环基，并且可以与R7和R8连接的氮原子一起形成取代或未取代的杂环基），R5是 取代或未取代的烷氧基或式的基团（R 7和R 8如上定义），R 6为氢原子或取代或未取代的烷基。

    Triazole derivatives and salts thereof and antifungal agent containing the same
    5.
    发明授权
    Triazole derivatives and salts thereof and antifungal agent containing the same 失效
    三唑衍生物及其盐和含有它们的抗真菌剂

    公开(公告)号：US5366989A

    公开(公告)日：1994-11-22

    申请号：US986800

    申请日：1992-12-08

    申请人： Hiroyuki Imaizumi ,  Tetsuya Kajita ,  Kenichi Takashima ,  Minako Yotsuji ,  Keiko Takakura ,  Akira Yotsuji ,  Junichi Mitsuyama ,  Katsumi Shimizu ,  Hiroshi Sakai ,  Hirokazu Narita

    发明人： Hiroyuki Imaizumi ,  Tetsuya Kajita ,  Kenichi Takashima ,  Minako Yotsuji ,  Keiko Takakura ,  Akira Yotsuji ,  Junichi Mitsuyama ,  Katsumi Shimizu ,  Hiroshi Sakai ,  Hirokazu Narita

    IPC分类号： A61K31/41 ,  A61P31/04 ,  A61P31/10 ,  C07D249/08 ,  C07D401/12 ,  C07D417/06 ,  C07D521/00 ,  A01N43/653

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The present invention relates to a compound represented by the general formula (1) or its salt, a process for producing the same, and an antifungal agent comprising the same as an effective component: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group bonded through a carbon atom in the ring to the main chain; R.sup.2 presents a hydrogen atom, a fluorine atom or a substituted or unsubstituted alkyl group; and R.sup.3 represents a cyano group, a thioamido group or a group represented by the formula ##STR2## in which R.sup.4 is a hydroxyl group or a group of the formula ##STR3## (R.sup.7 and R.sup.8, which may be the same or different, are hydrogen atoms or substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, amino, alkoxy, hydroxyl or heterocyclic groups, and may form a substituted or unsubstituted heterocyclic group together with the nitrogen atom to which R.sup.7 and R.sup.8 attach), R.sup.5 is a substituted or unsubstituted alkoxy group or a group of the formula ##STR4## (R.sup.7 and R.sup.8 are as defined above), and R.sup.6 is a hydrogen atom or a substituted or unsubstituted alkyl group.

    摘要翻译： 本发明涉及由通式（1）表示的化合物或其盐，其制备方法和含有该化合物的有效成分的抗真菌剂：有或无取代的芳基或取代或未取代的杂环基 通过环中的碳原子键合到主链上; R2表示氢原子，氟原子或取代或未取代的烷基; 并且R 3表示氰基，硫代酰氨基或由下式表示的基团：其中R 4是羟基或式（R 3和R 8）可以相同或不同， 氢原子或取代或未取代的烷基，烯基，炔基，环烷基，芳基，氨基，烷氧基，羟基或杂环基，并且可以与R7和R8连接的氮原子一起形成取代或未取代的杂环基），R5是 取代或未取代的烷氧基或式6的基团是氢原子或取代或未取代的烷基。

    4-{3-[4-(3-{4-[amino (butoxycarbonylimino) methyl] phenoxy} propyl)-1-piperidinyl] propoxy}-N'-(butoxycarbonyl) benzamidine crystals
    6.
    发明授权
    4-{3-[4-(3-{4-[amino (butoxycarbonylimino) methyl] phenoxy} propyl)-1-piperidinyl] propoxy}-N'-(butoxycarbonyl) benzamidine crystals 失效
    4- {3- [4-（3- {4- [氨基（丁氧基羰基亚氨基）甲基]苯氧基}丙基）-1-哌啶基]丙氧基} -N' - （丁氧基羰基）苄脒晶体

    公开(公告)号：US08158800B2

    公开(公告)日：2012-04-17

    申请号：US12667179

    申请日：2008-07-02

    申请人： Junichi Mitsuyama ,  Naokatsu Aoki

    发明人： Junichi Mitsuyama ,  Naokatsu Aoki

    IPC分类号： C07D211/26

    CPC分类号： C07D211/22

    摘要： To provide novel crystals of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}-N′-(butoxycarbonyl)benzamidine.Means for Solving the ProblemsThe type II crystal, the type III crystal and the type IV crystal of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}-N′-(butoxycarbonyl)benzamidine are useful as excellent drug substances of antifungal agents.

    摘要翻译： 为了提供4- {3- [4-（3- {4- [氨基（丁氧基羰基亚氨基）甲基]苯氧基}丙基）-1-哌啶基]丙氧基} -N' - （丁氧基羰基）苄脒的新晶体。 解决问题的手段4- {3- [4-（3- {4- [氨基（丁氧基羰基亚氨基）甲基]苯氧基}丙基）-1-哌啶基]的II型晶体，III型晶体和IV型晶体 丙氧基} -N' - （丁氧基羰基）苄脒可用作抗真菌剂的优异药物。

    NOVEL 4-{3-[4-(3-{4-[AMINO (BUTOXYCARBONYLIMINO) METHYL] PHENOXY} PROPYL)-1-PIPERIDINYL] PROPOXY]-N'-(BUTOXYCARBONYL) BENZAMIDINE CRYSTALS
    7.
    发明申请
    NOVEL 4-{3-[4-(3-{4-[AMINO (BUTOXYCARBONYLIMINO) METHYL] PHENOXY} PROPYL)-1-PIPERIDINYL] PROPOXY]-N'-(BUTOXYCARBONYL) BENZAMIDINE CRYSTALS 失效
    新的4- {3- [4-（3- {4- [氨基（羧基苄基）甲基]苯氧基}丙基）-1-哌啶基]丙氧基] -N' - （二氧代羰基）苯甲酰胺晶体

    公开(公告)号：US20110046381A1

    公开(公告)日：2011-02-24

    申请号：US12667179

    申请日：2008-07-02

    申请人： Junichi Mitsuyama ,  Naokatsu Aoki

    发明人： Junichi Mitsuyama ,  Naokatsu Aoki

    IPC分类号： C07D211/26

    CPC分类号： C07D211/22

    摘要： Problems To provide novel crystals of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}-N′-(butoxycarbonyl)benzamidine.Means for Solving the Problems The type II crystal, the type III crystal and the type IV crystal of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}-N′-(butoxycarbonyl)benzamidine are useful as excellent drug substances of antifungal agents.

    摘要翻译： 问题提供4- {3- [4-（3- {4- [氨基（丁氧基羰基亚氨基）甲基]苯氧基}丙基）-1-哌啶基]丙氧基} -N' - （丁氧基羰基）苄脒的新晶体。 解决问题的手段4- {3- [4-（3- {4- [氨基（丁氧基羰基亚氨基）甲基]苯氧基}丙基）-1-哌啶基]的II型晶体，III型晶体和IV型晶体 丙氧基} -N' - （丁氧基羰基）苄脒可用作抗真菌剂的优异药物。