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    Method of treating congestive heart failure using carbostyril derivatives
    1.
    发明授权
    Method of treating congestive heart failure using carbostyril derivatives 失效
    使用喹诺酮衍生物治疗充血性心力衰竭的方法

    公开(公告)号：US5266577A

    公开(公告)日：1993-11-30

    申请号：US734958

    申请日：1991-07-24

    申请人： Takafumi Fujioka ,  Shuji Teramoto ,  Michiaki Tominaga ,  Yoichi Yabuuchi

    发明人： Takafumi Fujioka ,  Shuji Teramoto ,  Michiaki Tominaga ,  Yoichi Yabuuchi

    IPC分类号： A61K31/47 ,  C07D215/22 ,  C07D215/227 ,  C07D215/54 ,  C07D401/12 ,  C07D409/12 ,  C07D215/16

    CPC分类号： C07D215/227 ,  A61K31/47 ,  C07D215/54 ,  C07D401/12 ,  C07D409/12

    摘要： Method for the treatment of congestive heart failure or paroxymal frequent heart pulse using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of -A-NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition for prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.

    摘要翻译： 使用下式的喹诺酮衍生物治疗充血性心力衰竭或阵发性频繁心脏脉搏的方法：其中R1是H或CN，R2和R3各自为H，任选地被OH，环烷基，烯基，苯基， 在烷基部分上具有烷氧基烷氧基，卤素，烷氧基，NO2，烷基，CN，烷硫基或烷基亚磺酰基的任意取代基的苯基烷基，在苯环上具有任选烷氧基取代基的苯基磺酰基烷基，苯硫基烷基，具有卤素取代基的苯基亚磺酰基烷基 或苯基环上的烷氧基，在苯环上具有卤素或烷氧基的任意取代基的苯氧基烷基，在吡啶环上具有卤素或烷氧基的任意取代基的吡啶基烷基，噻吩烷基，苯甲酰基烷基，苯硫基硫代羰基，苯甲酰基，吡啶基，苯基烯基或-A-NR4R5基团（ R4和R5各自为苯基上的烷基或具有卤素或烷氧基的任意取代基的苯基，A为a 可被O取代的亚烷基及其盐，以及新的喹诺酮衍生物，以及用于预防和治疗含有所述新型喹诺酮衍生物的心脏病的药物组合物。

    Carbostyril derivatives
    2.
    发明授权
    Carbostyril derivatives 失效
    卡波他汀衍生物

    公开(公告)号：US5436254A

    公开(公告)日：1995-07-25

    申请号：US125667

    申请日：1993-11-02

    申请人： Hidenori Ogawa ,  Hisashi Miyamoto ,  Kazumi Kondo ,  Hiroshi Yamashita ,  Kenji Nakaya ,  Michiaki Tominaga ,  Yoichi Yabuuchi

    发明人： Hidenori Ogawa ,  Hisashi Miyamoto ,  Kazumi Kondo ,  Hiroshi Yamashita ,  Kenji Nakaya ,  Michiaki Tominaga ,  Yoichi Yabuuchi

    IPC分类号： C07D215/22 ,  C07D215/227 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07D521/00 ,  C07H15/26 ,  A61K31/47 ,  C07D217/00

    CPC分类号： C07D215/227 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07H15/26

    摘要： Novel carbostyril derivatives of the formula: ##STR1## wherein R.sup.1 is H, NO.sub.2, alkoxy, alkoxycarbonyl, alkyl, halogen, optionally substituted amino, OH, CN, COOH, alkanoyloxy, hydrazinocarbonyl; q is 1 to 3, and R is a group of the formula: ##STR2## [wherein R.sup.2 is H, alkoxycarbonyl, optionally substituted phenoxycarbonyl, phenylalkenyl--CO--, optionally substituted phenylalkanoyl, alkanoyl, alkenyl--CO--, optionally substituted phenyl--SO.sub.2 --, --CONR.sup.8 R.sup.9, optionally substituted heterocyclic group--CO--, naphthyl--CO--, thienylalkanoyl, tricyclo[3.3.1.1]alkanoyl, ##STR3## (R.sup.13 is OH, optionally substituted alkoxy, --NR.sup.32 R.sup.33, --O--A--(E).sub.l --NR.sup.4 R.sup.5, --(B).sub.l --NR.sup.6 R.sup.7, etc.), n is 1 or 2, m is 0 or 1 to 3, R.sup.3 is alkyl, R.sup.10 is --(CO).sub.l --NR.sup.11 R.sup.12 ], and the bond between 3- and 4-position of carbostyril nucleus is single or double bond, which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.

    摘要翻译： 其中R1是H，NO2，烷氧基，烷氧基羰基，烷基，卤素，任选取代的氨基，OH，CN，COOH，烷酰氧基，肼基羰基; q为1至3，并且R为下式的基团：其中R 2为H，烷氧基羰基，任选取代的苯氧基羰基，苯基烯基-CO-，任选取代的苯基烷酰基，烷酰基，烯基-CO-， 任选取代的苯基-SO 2 - ，-CONR 8 R 9，任选取代的杂环基-CO-，萘基-CO-，噻吩基烷酰基，三环[3.3.1.1]烷酰基，（R 13是OH，任选取代的烷氧基，-NR 32 R 33，-OA - （E）1-NR4R5， - （B）1-NR6R7等），n为1或2，m为0或1至3，R3为烷基，R10为 - （CO）1-NR11R12] 喹诺酮核的3-和4-位之间的键是单键或双键，其具有优异的加压素拮抗活性，并且可用作血管扩张剂，降血压剂，水利尿剂，血小板凝集抑制剂和含有该化合物的血管加压素拮抗剂组合物 有效成分。

    Compositions for treating glaucoma containing a carbostyril
    3.
    发明授权
    Compositions for treating glaucoma containing a carbostyril 失效
    用于治疗含有喹诺酮类青光眼的组合物

    公开(公告)号：US4309432A

    公开(公告)日：1982-01-05

    申请号：US109057

    申请日：1980-01-02

    申请人： Nobuyuki Tanaka ,  Yoichi Nishinakamura ,  Kazuyuki Nakagawa

    发明人： Nobuyuki Tanaka ,  Yoichi Nishinakamura ,  Kazuyuki Nakagawa

    IPC分类号： A61K31/47

    CPC分类号： A61K31/47 ,  Y10S514/913

    摘要： This invention provides a glaucoma treating composition comprising at least one of carbostyril derivatives represented by the formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or lower alkenyl, R.sup.2 is hydrogen or a group ##STR2## wherein R.sup.4 is lower alkyl, cycloalkyl, or lower alkyl substituted by phenyl with or without a lower alkoxy substituent on the phenyl nucleus, R.sup.3 is a group ##STR3## wherein R.sup.4 is as defined above when R.sup.2 is hydrogen, or R.sup.3 is hydrogen, hydroxyl, ureido, lower alkynyloxy, lower alkoxy having a lower alkanoyl substitutent, lower alkanoylamino or lower alkenyloxy when R.sup.2 is ##STR4## and the carbon-to-carbon bond between the 3-position and the 4-position of the carbostyril skeleton is a single bond or double bond, and pharmacologically acceptable acid addition salts thereof; and a method of treating glaucoma comprising administering said composition to a patient with glaucoma.

    摘要翻译： 本发明提供了一种青光眼治疗组合物，其包含由下式表示的喹诺酮衍生物中的至少一种：其中R1是氢，低级烷基或低级烯基，R2是氢或基团，其中R4是低级烷基，环烷基或 被苯基上具有或不具有低级烷氧基取代基的苯基取代的低级烷基，R3是一个基团，其中当R2是氢时R4如上所定义，或R3是氢，羟基，脲基，低级炔氧基，低级烷氧基， 当R2为“IMAGE”时，低级烷酰基取代基，低级烷酰基氨基或低级烯氧基，喹诺酮骨架3位和4位之间的碳 - 碳键为单键或双键，以及药理学上可接受的酸 其加成盐; 以及治疗青光眼的方法，包括将所述组合物给予患有青光眼的患者。