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    INHIBITORY AGENT FOR HUMAN ACQUIRED IMMUNODEFICIENCY SYNDROME VIRUS INFECTION
    2.
    发明专利
    INHIBITORY AGENT FOR HUMAN ACQUIRED IMMUNODEFICIENCY SYNDROME VIRUS INFECTION 失效

    公开(公告)号：JPH06192075A

    公开(公告)日：1994-07-12

    申请号：JP33391192

    申请日：1992-11-20

    申请人： NIPPON KAYAKU KK

    发明人： TOMIYOSHI TSUGIO ,  SHIOZAWA AKIRA ,  HOSHINO KOUROU ,  IKEDA RYUJI

    IPC分类号： A61K31/16 ,  A61P31/12 ,  A61P37/04

    摘要： PURPOSE:To provide the subject inhibitor containing a specific spergualin-related compound as an active ingredient, low in toxicity, and excellent in safety, antitumor activity and immune-enhancing activity. CONSTITUTION:The objective inhibitor contains a spergualin-related compound (salt) of formula I [Gu is guanidino; X0 is (CH2)1-5, (substituted)phenylene; (a) is 3-5; X1 (CH2)0-2-CH(CH00)(CH2)0-2 (R00 is H, OH, OCH3, etc); X2 is NH(CH2)4 NH (CH2)3NH-R02 (R02 is H, the OH-removed residue of the carboxyl group of an amino acid or peptide)] or a spergualin-related compound (salt) of formula II [X is (CH2)1-5, C6H4; (r) is 3-5; R6 is the residue produced by removing one H atom from the alpha-amino group and a hydroxyl group from the alpha-carboxyl group of an amino acid, etc.]. The compound is orally administered at a dose of preferably 5-500mg/kg.day.

    SQUALENE SYNTHASE INHIBITOR AND NEW MALONIC ACID DERIVATIVE
    4.
    发明专利
    SQUALENE SYNTHASE INHIBITOR AND NEW MALONIC ACID DERIVATIVE 失效

    公开(公告)号：JPH10298134A

    公开(公告)日：1998-11-10

    申请号：JP12290697

    申请日：1997-04-28

    申请人： NIPPON KAYAKU KK

    发明人： ICHIKAWA YUICHIRO ,  NIITSUMA SETSUKO ,  ABE MASATOSHI ,  TAKAHASHI WATARU ,  IKEDA RYUJI ,  TAKASHIO KAZUTOSHI

    IPC分类号： A61K31/19 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P31/04 ,  A61P43/00 ,  C07C51/353 ,  C07C59/48

    摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound useful as a treating agent for an infectious disease or a circulatory disease, etc. SOLUTION: A compound of formula I [A and A are each H, a (substituted) aromatic group; X and X are each a (substituted) 1-20C divalent aliphatic hydrocarbon residue; A X and A X cannot be a 1-3C alkyl or benzene at the same time], e.g. 2-dodecyl-2-(5-phenylpentyl)malonic acid. The compound can be obtained, for example, by reacting a malonic acid dialkyl ester of formula II [R is a 1-10C (substituted) alkyl, etc.], with an alkylating agent in the presence of a base (e.g. sodium hydride) in a solvent (e.g. tetrahydrofuran) at 0-100 deg.C for 0.5-48 hr to obtain a dialkylmalonic acid dialkyl ester of formula III and hydrolyzing the ester through the reaction with a base (e.g. sodium hydroxide or potassium hydroxide) in a solvent (e.g. methanol) at -10 to 100 deg.C for 0.5-24 hr to convert the ester moiety into the carboxylic acid.

    NEW TARTARIC ACID DERIVATIVE, ITS USE AND PRODUCTION
    6.
    发明专利
    NEW TARTARIC ACID DERIVATIVE, ITS USE AND PRODUCTION 失效

    公开(公告)号：JPH10298177A

    公开(公告)日：1998-11-10

    申请号：JP12290797

    申请日：1997-04-28

    申请人： NIPPON KAYAKU KK

    发明人： ICHIKAWA YUICHIRO ,  NIITSUMA SETSUKO ,  ABE MASATOSHI ,  TAKAHASHI WATARU ,  IKEDA RYUJI ,  TAKASHIO KAZUTOSHI

    IPC分类号： C07D317/32 ,  A61K31/335 ,  A61K31/357 ,  A61P3/06 ,  A61P9/10 ,  A61P31/04 ,  A61P43/00

    摘要： PROBLEM TO BE SOLVED: To obtain a new tartaric acid derivative having strong activities for inhibiting squalene synthetic enzyme and effectively used as an agent for treating infectious disease such as myocardial disease, and hypercholesterolemia, hyperlipemia, etc. SOLUTION: This tartaric acid derivative is a compound of formula I [A and A are each H or an aromatic ring group; X and X are each a linear or branched 1-20C (un)saturated divalent hydrocarbon residue; with the proviso that both A X and A X are not simultaneously a 1-3C alkyl] or a pharmaceutically acceptable salt thereof, e.g. (4R, 5R)-4,5-dicarboxy-2-dodecyl-2-(5- phenylpentyl)-1,3-dioxolane. The compound of formula I is obtained by reacting a compound of formula II (R is a 1-6C lower alkyl, etc.) with a compound of formula III to provide a compound of formula IV, and converting the compound of formula IV to a carboxylic acid. The tartaric acid derivative is expected to be a medicament such as an anti-Aspergillus agent having high safety.

    NEW PIPERIDINE DERIVATIVE AND ANTIVIRAL AGENT
    8.
    发明专利
    NEW PIPERIDINE DERIVATIVE AND ANTIVIRAL AGENT 失效

    公开(公告)号：JPH072773A

    公开(公告)日：1995-01-06

    申请号：JP16505093

    申请日：1993-06-11

    申请人： NIPPON KAYAKU KK

    发明人： ICHIKAWA YUICHIRO ,  NAGAI MASASHI ,  HOSHINO NAOKO ,  IKEDA RYUJI ,  HOSHINO KOUROU

    IPC分类号： A61K31/445 ,  A61P31/12 ,  A61P31/18 ,  C07D211/56

    摘要： PURPOSE:To obtain a new compound useful as an anti-HIV agent, antiviral agent, etc., having low cell toxicity. CONSTITUTION:A compound of formula I (R is H or protected guanidino; R is alkyl, aryl or acyl; R and R are H, alkyl, aryl or acyl) such as 1- amidino-3-amino-2-methoxypiperidine. The compound of formula I is obtained by reducing a compound of formula III which is obtained by using a compound of formula II (Z is benzyloxycarbonyl) as a starting raw material, in a solvent such as methanol in the presence of a catalytic reduction catalyst such a palladium black in a hydrogen atmosphere.