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    Carbostyril derivatives and pharmaceutical preparations containing same
    6.
    发明授权
    Carbostyril derivatives and pharmaceutical preparations containing same 失效
    卡波他汀衍生物和含有它们的药物制剂

    公开(公告)号：US4824840A

    公开(公告)日：1989-04-25

    申请号：US25193

    申请日：1987-03-12

    申请人： Kazuo Banno ,  Takafumi Fujioka ,  Yasuo Oshiro ,  Kazuyuki Nakagawa

    发明人： Kazuo Banno ,  Takafumi Fujioka ,  Yasuo Oshiro ,  Kazuyuki Nakagawa

    IPC分类号： C07D215/06 ,  A61K31/4704 ,  A61K31/495 ,  A61P25/00 ,  A61P25/20 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D205/06 ,  C07D215/16 ,  C07D215/22 ,  C07D215/227 ,  C07D215/26 ,  C07D215/28 ,  C07D241/04 ,  C07D243/08 ,  C07D295/04 ,  C07D403/12 ,  C07D405/12 ,  C07D403/02

    CPC分类号： C07D215/227 ,  C07D215/16 ,  C07D215/22 ,  C07D215/28

    摘要： Carbostyril derivatives having antihistaminic action and central nervous controlling action are useful as antihistaminic agents or central nervous controlling agents. The derivatives are represented by the general formula, ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms or a phenylalkyl group, an alkylene group containing 1 to 4 carbon atoms; R.sup.2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or a phenyl group; R.sup.3 is a hydrogen atom, a hydroxy group, an alkyl group having 1 to 4 carbon atoms, an alkanoyloxy group having 1 to 4 carbon atoms or a 3,4,5-trimethoxybenzoyloxy group; R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; R.sup.5 is a cycloalkyl group having 3 to 8 carbon atoms, a phenyl group (which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, alkyl groups having 1 to 4 carbon atoms and alkoxy groups having 1 to 4 carbon atoms), an alkyl group having 1 to 4 carbon atoms (having one substituted group such as a hydroxy group, a phenyl group or an alkanoyloxy group having 1 to 4 carbon atoms), an alkanoyl group having 1 to 4 carbon atoms or benzoyl group; X is a halogen atom; n is 0, or an integer of 1 or 2; Q is an integer of 2 or 3, l and m are respectively an integer of 0 to 1-6, but the sum of l and m should not exceed 6; the carbon-carbon bond at the 3- and 4-positions in the carbostyril skeleton is a single or double bond and; the substituted position of the side chain of ##STR2## is any one of the 4-, 5-, 6-, 7- or 8-positions.

    摘要翻译： 具有抗组胺作用和中枢神经控制作用的卡波他特尔衍生物可用作抗组胺剂或中枢神经控制剂。 衍生物由通式（1）表示，其中R 1是氢原子，具有1至6个碳原子的烷基，具有2至4个碳原子的烯基，具有2至4个碳原子的炔基 原子或苯基烷基，含有1至4个碳原子的亚烷基; R2是氢原子，碳原子数1〜4的烷基或苯基; R3是氢原子，羟基，碳原子数1〜4的烷基，碳原子数1〜4的烷酰氧基或3,4,5-三甲氧基苯甲酰氧基。 R4是氢原子或碳原子数1〜4的烷基。 R5是具有3-8个碳原子的环烷基，苯基（其可以具有1至3个选自卤素原子，具有1至4个碳原子的烷基和具有1至4个碳原子的烷氧基的取代基） ），碳原子数1〜4的烷基（具有羟基，苯基或碳原子数1〜4的烷酰氧基的一个取代基），碳原子数1〜4的烷酰基或苯甲酰基; X是卤原子; n为0或1或2的整数; Q为2或3的整数，l和m分别为0至1-6的整数，但l和m之和不应超过6; 喹诺酮骨架中3-和4-位的碳 - 碳键是单键或双键， “IMAGE”侧链的取代位置是4-，5-，6-，7-或8-位中的任何一个。

    Hydrofluorene derivatives
    7.
    发明授权
    Hydrofluorene derivatives 失效
    氢氟芴衍生物

    公开(公告)号：US5017724A

    公开(公告)日：1991-05-21

    申请号：US532341

    申请日：1990-06-04

    申请人： Yasuo Oshiro ,  Tatsuyoshi Tanaka ,  Yoji Sakurai ,  Seiji Sato

    发明人： Yasuo Oshiro ,  Tatsuyoshi Tanaka ,  Yoji Sakurai ,  Seiji Sato

    IPC分类号： C07D207/09 ,  C07D207/26 ,  C07D207/27 ,  C07D211/26 ,  C07D211/58 ,  C07D213/38 ,  C07D213/82 ,  C07D295/096 ,  C07D295/15

    CPC分类号： C07D207/27 ,  C07D207/09 ,  C07D211/26 ,  C07D211/58 ,  C07D213/38 ,  C07D213/82 ,  C07D295/096 ,  C07D295/15 ,  C07C2103/18

    摘要： Novel hydrofluorene derivatives and salts thereof represented by the formula (1) which possess excellent activities for improving anoxemic and hypoxic symptoms and syndromes accompanied therewith, therefore said derivatives are useful as cerebral activators, preventive agents for arrhythmia and heart failure caused by the shortage of oxygen and others. Furthermore, said hydrofluorene derivatives and salts thereof possess actions for scavenging active oxygen radicals, therefore, the derivatives are useful prophylactic and treating agents for various disturbances and diseases caused by the excessive formation of active oxygen radicals. In addition to the above, the hydrofluorene derivatives are useful as anti-oxidative agents for fats and oils.Yet, further, the hydrofluorene derivatives and salts thereof accelerate the uptaking of high-affinity choline in the central nerve system and/or the releasing of acetylcholine therefrom, therefore, the hydrofluorene derivatives and salts thereof are useful cholinergic nerve system activating agents.

    摘要翻译： 由式（1）表示的新型氢芴衍生物及其盐，其具有改善缺氧症和缺氧症状及伴随症状的优异活性，因此所述衍生物可用作脑激活剂，由氧气不足引起的心律失常和心力衰竭的预防剂 和别的。 此外，所述氢芴衍生物及其盐具有清除活性氧自由基的作用，因此，该衍生物是用于由过度形成活性氧自由基引起的各种紊乱和疾病的预防和治疗剂。 除了上述之外，氢芴衍生物可用作脂肪和油的抗氧化剂。 此外，氢芴衍生物和其盐加速了中枢神经系统中高亲和力胆碱的吸收和/或乙酰胆碱的释放，因此，氢芴衍生物及其盐是有用的胆碱能神经系统活化剂。

    Carbostyril derivatives for inhibiting skin erythema and/or skin pigmentation
    9.
    发明授权
    Carbostyril derivatives for inhibiting skin erythema and/or skin pigmentation 失效
    用于抑制皮肤红斑和/或皮肤色素沉着的碳青霉烯衍生物

    公开(公告)号：US06133264A

    公开(公告)日：2000-10-17

    申请号：US485454

    申请日：2000-02-10

    申请人： Yasuo Oshiro ,  Takao Nishi ,  Keiichi Kuwahara ,  Kozo Watanabe

    发明人： Yasuo Oshiro ,  Takao Nishi ,  Keiichi Kuwahara ,  Kozo Watanabe

    IPC分类号： C07D215/22 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P17/00 ,  C07D215/227 ,  C07D215/26 ,  C07D405/12 ,  A61K31/5377 ,  A61D17/00 ,  C07D401/02

    CPC分类号： C07D215/227 ,  C07D215/26 ,  C07D405/12

    摘要： The present invention provides an agent for inhibiting skin erythema and/or skin pigmentation, containing at least one selected from the group consisting of the carbostyril derivative and salt thereof represented by the general formula, ##STR1## (wherein R.sup.1 is a hydrogen atom, a lower alkyl group or the like; R.sup.2 is a hydrogen atom, a lower alkyl group, a lower alkoxy group or the like; R.sup.3 and R.sup.4 are lower alkyl groups which may have hydroxyl groups as substituents or the like; the carbon--carbon bond between 3- and 4-positions in the carbostyril skeleton is a single bond or double bond).

    摘要翻译： PCT No.PCT / JP98 / 03657 Sec。 371日期2000年2月10日 102（e）日期2000年2月10日PCT提交1998年8月18日PCT公布。 第WO99 /​​ 09011号公报 日期1999年2月25日本发明提供一种抑制皮肤红斑和/或皮肤色素沉着的药剂，其含有选自由通式表示的喹诺酮衍生物及其盐的至少一种（其中，R 1为氢原子 ，低级烷基等; R 2为氢原子，低级烷基，低级烷氧基等; R 3和R 4为可具有羟基作为取代基的低级烷基等;碳 - 碳 喹诺酮骨架中3-和4-位之间的键是单键或双键）。

    Carbostyril derivatives
    10.
    发明授权
    Carbostyril derivatives 失效
    卡波他汀衍生物

    公开(公告)号：US5006528A

    公开(公告)日：1991-04-09

    申请号：US424719

    申请日：1989-10-20

    申请人： Yasuo Oshiro ,  Seiji Sato ,  Nobuyuki Kurahashi

    发明人： Yasuo Oshiro ,  Seiji Sato ,  Nobuyuki Kurahashi

    IPC分类号： C07D215/22 ,  C07D215/227

    CPC分类号： C07D215/227

    摘要： A novel carbostyril derivative and salt thereof represented by the formula (1) ##STR1## (wherein R is a group of the formula ##STR2## ((wherein R.sup.1 is a C.sub.1- C.sub.3 alkoxy group)), a group of the formula ##STR3## ((wherein R.sup.2 and R .sup.3 are each, at the same time, a chlorine atom, a bromine atom; and R.sup.4 is a hydrogen atom or a chlorine atom)), 2-methyl-3-nitrophenyl group, 3,5-dichlorophenyl group, or a group of the formula ##STR4## ((wherein R.sup.5 is a chlorine atom or a bromine atom; and R.sup.6 is a methyl group)); the carbon-carbon bond between 3- and 4-position in the carbostyril skeleton is a single or double bond).