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    QUINOLINE DERIVATIVE OR SALT THEREOF AND REMEDY FOR CARDIAC DISEASES CONTAINING THE SAME.
    3.
    发明公开
    QUINOLINE DERIVATIVE OR SALT THEREOF AND REMEDY FOR CARDIAC DISEASES CONTAINING THE SAME. 失效
    喹啉或它们的盐和含有心脏病的治疗。

    公开(公告)号：EP0638571A4

    公开(公告)日：1995-04-12

    申请号：EP93911951

    申请日：1993-04-28

    Applicant: KOWA CO

    Inventor： KYOTANI YOSHINORI ,  OGIYA TADAAKI ,  TOMA TSUTOMU ,  KURIHARA YUJI ,  KITAMURA TAKAHIRO ,  YAMAGUCHI TAKASHI ,  ONOGI KAZUHIRO ,  SATO SEICHI ,  SHIGYO HIROMICHI ,  OTA TOMIO ,  KAWADA MITSUO ,  UCHIDA YASUMI

    IPC: C07D491/04 ,  C07D491/048 ,  C07D491/056 ,  A61K31/47

    CPC classification number: C07D491/04

    Abstract: A quinoline derivative represented by general formula (1), a medicinally acceptable salt thereof, and a remedy for cardiac diseases containing the same, wherein ring A represents a furan, dihydrofuran or dioxolane ring, R1 represents hydroxy, carboxy, alkoxycarbonyl, etc., R2s may be the same or different from each other and each represents hydrogen, alkyl, etc., R?3 and R4¿ may be the same or different from each other and each represents hydrogen, halogen, alkyl, amino, alkoxy, etc., R?5, R6, R7 and R8¿ may be the same or different from one another and each represents hydrogen or alkyl, m represents an integer of 0 to 3, and symbol ...... means that there may be a double bond formed by R?6 and R8¿. The compound (1) has a positively inotropic effect on myocardia and an antiarrhythmic effect and can dilate blood vessels without extremely increasing the heart rate. Therefore, a remedy for cardiac diseases containing the same as the active ingredient is remarkably useful for treating cardiac insufficiency, arrhythmia, and so forth.

    Abstract translation: 由通式所表示的喹啉衍生物（1），其药物上可接受的盐，以及用于心脏病含有相同，worin环A darstellt呋喃，二氢呋喃或二氧戊环的补救，R <1> darstellt羟基，羧基，烷氧基羰基， 等，R <2> S可以是相同的或彼此和各darstellt氢，烷基等不同，R <3>和R <4>可以是从彼此，并且每个darstellt氢相同或不同， 卤素，烷基，氨基，烷氧基等，R <5> - [R <6> - [R <7>和R <8>可以相同或彼此不同，分别darstellt氢或烷基，米darstellt成整数 0至3，和符号...... bedeutet，DASS可能存在由R形成双键<6>和R <8>。 的化合物（1）对心肌和抗心律失常效果率的带正性肌力作用和可扩张血管，而不极端地增加的心脏。 因此，对于心脏病含有相同的活性成分的补救可用于治疗心功能不全，心律失常，等等非常有用。

    PRODUCTION OF INDOLE DERIVATIVE
    6.
    发明专利
    PRODUCTION OF INDOLE DERIVATIVE 失效

    公开(公告)号：JPH10204088A

    公开(公告)日：1998-08-04

    申请号：JP1014997

    申请日：1997-01-23

    Applicant: KOWA CO

    Inventor： KYOTANI YOSHINORI ,  KAWAMURA KIYOSHI ,  SATO SEIICHI ,  YAMAGUCHI TAKASHI ,  KITAMURA TAKAHIRO

    IPC: C07D491/048 ,  A61K31/40 ,  A61P9/00

    Abstract: PROBLEM TO BE SOLVED: To obtain a large amount of the subject compound useful as a therapeutic agent for heart diseases under mild conditions in a high yield by treating a specific phthalimide compound with a base. SOLUTION: (2-RS,3-SR)-2,3,5,8,8-Pentamethyl-2-(N-phthaliminomethyl)-2,3,7,8- tetrahydro-6H-furo[2,3-e]indol-7-one of formula I is treated with a base (e.g. methylamine) to give the objective (2-RS,3-SR)-2-aminomethyl-2,3,5,8,8- pentamethyl-2,3,7,8-tetrahydro-6H-furo[2,3-e]indole-7-one of formula II. When an organic amine is used as the base, preferably the compound of formula I is reacted with 1-5 equivalents of the amine at 50-120 deg.C for 1-10 hours. The compound of formula I is preferably obtained by reacting an iodine compound of formula III with a phthalimide alkali salt in an aprotic polar solvent.

    7.
    发明专利
    失效

    公开(公告)号：JPH05310744A

    公开(公告)日：1993-11-22

    申请号：JP11286392

    申请日：1992-05-01

    Applicant: KOWA CO

    Inventor： KYOTANI YOSHINORI ,  TAIMA TSUTOMU ,  KURIHARA YUJI ,  KITAMURA TAKAHIRO ,  YAMAGUCHI TAKASHI ,  KAMIYA KAZUHIRO ,  ONOKI KAZUHIRO ,  SATO SEIICHI ,  OTA TOMIO ,  UCHIDA YASUYOSHI

    IPC: A61K31/47 ,  A61K31/4741 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  C07D491/052

    Abstract: PURPOSE:To provide a new pyrano[2,3-f]quinoline derivative having excel lent antiarrhythmic action, cardiac action, vasodilative action, etc., and useful as a cardiac disease therapeutic agent represented by cardiac failures. CONSTITUTION:The compound of formula 1 (R is lower alkyl; R is H, halogen, OH, lower alkylsulfonyloxy, lower alkanoyloxy, lower alkoxy, azido, amino; R is H, lower alkyl; R is H, lower alkyl, OH, lower alkylamino, pyrrolidinyl or piperazinyl which may have a substituent; when a double bond exists between the 3,4 positions, the substituent R does not exist), e.g. 3acetoxy-6-methyl-3,4,7,8- tetrahydro-2H-pyrano[2,3-f]quinoline. The compound of formula 1-1 among the compounds of formula 1 is obtained by reacting a quinoline compound with an allyl halide compound, thermally subjecting the obtained compound of formula 3 to a Claisen rearrangement, reacting the reaction product with an aliphatic acid anhydride, reacting the obtained compound of formula 5 with a peracid, and subsequently treating the produced epoxy compound of formula 6 with an alkali halide.

    NOVEL SULFONAMIDE COMPOUND
    10.
    发明专利
    NOVEL SULFONAMIDE COMPOUND 失效

    公开(公告)号：JPH01211567A

    公开(公告)日：1989-08-24

    申请号：JP3394988

    申请日：1988-02-18

    Applicant: KOWA CO

    Inventor： TANABE SOHEI ,  SATO SEIICHI ,  KYOTANI YOSHINORI ,  OTA TOMIO ,  UCHIDA YASUYOSHI

    IPC: C07D295/12 ,  A61K31/495 ,  A61P9/00 ,  C07D213/74 ,  C07D213/75 ,  C07D241/04 ,  C07D295/13

    Abstract: NEW MATERIAL:A sulfonamide compound shown by the formula (R1 is lower alkyl, lower alkoxy or halogen; R2 is H, lower alkyl, aryl or arylalkyl; R3 is aryl or arylalkyl; R4 and R4' may be the same or different and H, lower alkyl or lower alkoxy; m is 0-3; n is 1-8) and an acid addition salt thereof. EXAMPLE:1-Diphenylmethyl-4-(3-benzenesulfonylaminopropyl)piperazine. USE:Useful as a drug for cardiovascular system. PREPARATION:For example, a compound shown by formula II is reacted with a compound shown by formula III in a solvent such as methylene chloride or chloroform at -10-+100 deg.C, preferably in the presence of a base such as sodium hydroxide to give a compound shown by formula I wherein R2 is H. Further this compound is reacted with a compound shown by the formula R2'Y (R2' is R2 except H; Y is halogen, alkylsulfonyloxy, etc.) and converted to a compound shown by formula I wherein R2 is except H.

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