1.
    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

    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
    3.
    发明专利

    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

    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.

    TWITCH PREVENTIVE AGENT
    8.
    发明专利

    公开(公告)号:JPH02255614A

    公开(公告)日:1990-10-16

    申请号:JP7497089

    申请日:1989-03-29

    Applicant: KOWA CO

    Inventor: UCHIDA YASUYOSHI

    Abstract: PURPOSE:To obtain a preventive agent against twitch complicated with laser arterioplasty containing nipradilol as an active ingredient. CONSTITUTION:The objective substance obtained by containing nipradilol, one of racemic modifications thereof, one of optical isomers or a mixture thereof, preferably (2'R).(3R)-nipradilol as an active ingredient, suitably blending the active ingredient with normally used pharmaceutical raw materials and preparing a pharmaceutical according to a conventional method. The preventive agent is preferably intravenously administered; however, the agent can be prepared into a dosage form for oral or rectal administration. The agent is administered in an amount of 0.001-100mg, preferably 0.1-10mg expressed in terms of the nipradilol 5min to 1hr before cautery. The nipradilol is a compounded of a chemical name 3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1- benzopyran.

    NOVEL RACEMIC COMPOUND AND ITS CONVERSION

    公开(公告)号:JPS60181083A

    公开(公告)日:1985-09-14

    申请号:JP3617884

    申请日:1984-02-29

    Applicant: KOWA CO

    Abstract: NEW MATERIAL:The racemic compound (351-A) consisting of 3,4-dihydro-8-(2- hydroxy-3-isopropylamino)propoxy-3-nitroxy-2H-1-benzopyran (2S), (3S) and (2R), (3R), and the racemic compound (351-B) consisting of (2R), (3S) and (2S), (3R). USE:A beta-blocker and vasodilator. PREPARATION:One of the above racemic compounds is made to react with the compound of formula I [R is (cyclo)alkyl, aryl or aralkyl] or its reactive derivative to obtain the compound of formula II, which is converted to the oxazolinium ion of formula III with a conversion reagent (e.g. thionyl chloride). The ion is treated with an acid and hydrolyzed to obtain the other racemic compound.

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