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    TETRAHYDROCARBAZOLE-1-ALKANOIC ACIDS FOR CYCLOSPRIN REMEDY
    22.
    发明专利
    TETRAHYDROCARBAZOLE-1-ALKANOIC ACIDS FOR CYCLOSPRIN REMEDY 失效

    公开(公告)号：JPH01110625A

    公开(公告)日：1989-04-27

    申请号：JP18047688

    申请日：1988-07-21

    Applicant: MERCK FROSST CANADA INC

    Inventor： ANSONII DABURIYU FUOODOOHATSUC

    IPC: A61K31/40 ,  A61K31/403 ,  A61K31/41 ,  A61P43/00 ,  C07D209/86 ,  C07D209/88 ,  C07D209/94

    Abstract: PURPOSE: To inhibit nephrotoxicity induced by cyclosporin. CONSTITUTION: A compound (salt) of formula I R to R are each H, a 1-6C alkyl, a 2-6C alkenyl or the formula (CH2 )n M [(n) is 0-3; M is OR , a halogen, etc., (R is H, a 1-6C alkyl, etc.)]; R is H or a 1-6C alkyl; R is H or a 1-6C alkyl; R is H, OH, etc.; R is COOH, CHO, etc.; (r) is 1-6}, for example, 9-p- chlorobenzyl-6-fluoro-1,2,3,4-tetrahydrocarbazol-1-yl acetate. This compound of formula I is obtained by reaction between a compound of formula II and a ketone compound of formula III (R is a 1-6C alkyl, benzyl, etc.) in an alcohol solution followed by hydrolysis using NaOH, KOH or the like.

    IMPROVEMENT FOR CYCLOSPORIN REMEDY
    23.
    发明专利
    IMPROVEMENT FOR CYCLOSPORIN REMEDY 失效

    公开(公告)号：JPS6461425A

    公开(公告)日：1989-03-08

    申请号：JP18047388

    申请日：1988-07-21

    Applicant: MERCK FROSST CANADA INC

    Inventor： ANSONII DABURIYU FUOODOOHATSUC

    IPC: A61K45/06 ,  A61K38/00 ,  A61K38/13 ,  A61P7/02 ,  A61P29/00 ,  A61P33/02 ,  A61P37/06 ,  A61P43/00

    Abstract: PURPOSE: To provide an improvement of treating method of cyclosporine decreasing nephrotoxicity which is an adverse reaction of the cyclosporine treatment by auxiliary-administering an effective amount of cyclosporine and an effective amount of antithromboxane A2 agent to a mammal. CONSTITUTION: This cyclosporine, especially, cyclosporine A is orally administered in daily dose of 1 or 5 to 50mg/kg divided into 1 to 3 times a day. The antithromboxane A2 is administered in a dose rate of 0.002 to 100mg/kg, preferably 0.02 to 30mg/kg in oral, endorectal, percutaneous, parenteral, intramuscular, intravenous administration. 3-(Hydroxymethyl) dibenzo[b,f] thiepin 5,5-dioxide, etc., are manifested as the antithromboxane A2 agent. Cyclosporine has immunosuppression, antiinflammatory, antiparasitic action and restricts nephrotoxicity induced by the cyclosporine in transplant surgery area by auxiliary-administering the antithromboxane A2 .

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