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    • 8. 发明授权
    • Tracheal smooth muscle relaxant
    • 气管平滑肌松弛剂
    • US06180659B2
    • 2001-01-30
    • US09101842
    • 1998-08-31
    • Shinya YamashitaJiro TakeoShuji JinnoYasuyo KogureHiroyuki OnukiTakaaki OkitaJunichiro HataYasuhiro FukudaNaomi Ohtsuka
    • Shinya YamashitaJiro TakeoShuji JinnoYasuyo KogureHiroyuki OnukiTakaaki OkitaJunichiro HataYasuhiro FukudaNaomi Ohtsuka
    • A61K3138
    • C07D337/14A61K31/352A61K31/382C07D313/14Y10S514/826
    • The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient. [In the formula, X and Y each is any group selected from a group consisting of CH2, CHW1 (where W1 is halogen atom, hydroxyl group or lower alkoxy group) and C═O when the bond of X and Y is a single bond while, when it is a double bond, X and Y each is any group selected from a group consisting of CH and COW2 (where W2 is lower alkyl group or lower alkylcarbonyl group); Z is O, S, S═O or SO2; and R1˜R8 each is selected from a group consisting of hydrogen atom, VR9 (where V is O, S, S═O or SO2; and R9 is hydrogen atom, lower alkyl group, hydroxy lower alkyl group, lower acyl group, trihalomethyl group or carboxyl lower alkyl group), carboxyl lower alkyl group, hydroxy lower alkyl group, hydroxy lower alkenyl group, hydroxy lower alkynyl group, halogen atom, lower alkyl group, lower alkyl ketone, trihalomethyl group, trimethylsilylethynyl, nitro group, amino group, N-carbonyl lower alkyl group, lower alkylphenyl group and phenyl group].
    • 本发明提供含有下述式(1)表示的化合物或其药理学上可接受的盐作为有效成分的气管平滑肌松弛剂。[式中,X和Y各自为选自CH 2, CHW1(其中W1为卤原子,羟基或低级烷氧基),当X和Y的键为单键时为C = O,而当为双键时,X和Y各自为选自 由CH和COW 2组成(其中W2是低级烷基或低级烷基羰基); Z是O,S,S = O或SO 2; R1〜R8各自选自氢原子,VR9(其中V为O,S,S = O或SO2; R9为氢原子,低级烷基,羟基低级烷基,低级酰基,三卤甲基 羧基低级烷基,羟基低级烷基,羟基低级烯基,羟基低级炔基,卤素原子,低级烷基,低级烷基酮,三卤代甲基,三甲基甲硅烷基乙炔基,硝基,氨基, N-羰基低级烷基,低级烷基苯基和苯基]。
    • 9. 发明授权
    • Glutamic acid receptor agonist
    • 谷氨酸受体激动剂
    • US5955505A
    • 1999-09-21
    • US894433
    • 1997-08-20
    • Jiro TakeoShinya YamashitaKeiji WadaYoshiyuki Chiba
    • Jiro TakeoShinya YamashitaKeiji WadaYoshiyuki Chiba
    • A61K31/00A61K31/18A61K31/192A61K31/195A61K31/216A61K31/4035A61K31/4406C07C317/28C07C323/49C07C323/56C07C323/62A61K31/44
    • C07C323/62A61K31/00A61K31/18A61K31/192A61K31/195A61K31/216A61K31/4035A61K31/4406C07C317/28C07C323/49C07C323/56
    • A method comprising administering a sulfonamide derivative to a patient requiring activation of glutamate receptors, the sulfonamide derivative represented by the formula ##STR1## wherein A is a napthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 40 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group, and an acetamido group, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group of --OCH.sub.2 -- or a group of --CH.dbd.CH--; X and Y are the same or different, and are each a hydrogen atom or a fluorine atom; R is a carboxy group, an alkoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of ##STR2## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and R.sub.2 is a hydrogen atom, a hydroxyl group, an alkyl group having 1 to 3 carbon atoms, a carboxymethyl group or an alkoxycarbonylmethyl group having 3 to 6 carbon atoms; m is an integer from 0 to 2; and n is an integer from 0 to 3, or an pharmaceutically acceptable salt thereof, as an effective ingredient. The agonist is efficacious in the medical treatment of nerve degenerative disorders.
    • PCT No.PCT / JP96 / 00379 Sec。 371日期1997年8月20日 102(e)日期1997年8月20日PCT提交1996年2月20日PCT公布。 公开号WO96 / 25926 日期:1996年8月29日一种方法,包括向需要谷氨酸受体活化的患者施用磺酰胺衍生物,其中A为萘基,吡啶基,苯基,被1〜 5个选自卤素原子,具有1至40个碳原子的烷基,具有1至4个碳原子的烷氧基,硝基和乙酰氨基,或具有1至20个碳的烷基的基团 原子 B是具有1至3个碳原子的亚烷基,-OCH 2 - 或-CH = CH-的基团; X和Y相同或不同,分别为氢原子或氟原子; R为羧基,碳原子数2〜5的烷氧基羰基,羟甲基或其中R1为氢原子或碳原子数1〜3的烷基的基团。 R2为氢原子,羟基,碳原子数为1〜3的烷基,羧甲基或碳原子数为3〜6的烷氧基羰基甲基。 m为0〜2的整数; n为0〜3的整数,或其药学上可接受的盐作为有效成分。 激动剂在神经退行性疾病的治疗中是有效的。