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    IMIDAZOHETERO COMPOUND
    1.
    发明专利
    IMIDAZOHETERO COMPOUND 失效

    公开(公告)号：JPH0525169A

    公开(公告)日：1993-02-02

    申请号：JP27172591

    申请日：1991-07-19

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： TAKASUGI HISASHI ,  NISHINO SHIGETAKA ,  INOUE ZENICHI

    IPC: A61K31/435 ,  A61P1/04 ,  C07D471/04

    Abstract: PURPOSE:To provide the subject novel compound useful as an antineoplasmic agent. CONSTITUTION:The objective compound of formula I (R is or lower alkyl; R is H, lower alkyl, halogen or acyl; R is H, lower alkyl, cyclo lower alkyl or lower alkenyl), for example, 5-(3,7-dimethyl-5,6,7,8-tetrahydroimidazo[1,2- a]pyridin-2-yl)-2-methylaminobenzoxazole. This compound can be obtained by catalytic reduction of a compound of formula II pref. using a catalyst such as platinum catalyst, palladium catalyst, nickel catalyst, cobalt catalyst, iron catalyst, or copper catalyst to subject it to hydrogenation.

    DIHYDROPYRIMIDINE DERIVATIVE
    2.
    发明专利
    DIHYDROPYRIMIDINE DERIVATIVE 失效

    公开(公告)号：JPS62252775A

    公开(公告)日：1987-11-04

    申请号：JP633487

    申请日：1987-01-14

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： TAKATANI TAKAO ,  TAKASUGI HISASHI ,  KUNO ATSUSHI ,  INOUE ZENICHI

    IPC: A61K31/505 ,  A61P9/04 ,  C07D211/80 ,  C07D213/00 ,  C07D239/00 ,  C07D239/10 ,  C07D239/22 ,  C07D401/12

    Abstract: NEW MATERIAL:The dihydropyrimidine derivative of formula I (R is H or together with A form a double bond in a ring; R is lower alkyl, lower alkenyl or lower alkynyl; R is lower alkyl or together with A form a double bond in a ring; R is lower alkyl; R is esterified carboxy or phosphonyl; R is H, nitro or lower alkoxy; R is lower alkoxy, lower alkynyloxy or nitro; either one of R and R together with A form a double bond in a ring) or its salt. USE:A medicine having strong cardiotonic activity and, nevertheless, rather decreasing the pulse rate and useful as a cardiotonic agent for the prevention and remedy of cardiopathy such as cardiac insufficiency. PREPARATION:The compound of formula I can be produced e.g. by reacting the compound of formula II (R is H, etc.) with the compound of formula III according to the reaction formula.

    ANTIBACTERIAL AGENT
    6.
    发明专利
    ANTIBACTERIAL AGENT 失效

    公开(公告)号：JPH0578353A

    公开(公告)日：1993-03-30

    申请号：JP18593291

    申请日：1991-02-01

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： TAKASUGI HISASHI ,  KATSURA YOSUKE ,  INOUE ZENICHI ,  FUJI TETSUO

    IPC: A61K31/425 ,  A61P31/04 ,  C07D417/04 ,  C07D417/14

    Abstract: PURPOSE:To provide a new antibacterial agent having especially high antibacterial activity against Gram-negative bacteria. CONSTITUTION:The objective agent contains, as an active component, a compound of formula I [R and R are H, acyl, (halogen-containing) lower alkyl or together form a lower alkylene; R is H or lower alkyl; R is amino, acyl, acylamino, lower alkylisothioureido, heterocyclic amino, heterocyclic group or group of formula IV [(n) is 0 or 1; X is CH or N; R is H, cyano, nitro or acyl; R is H, lower alkyl, lower alkylthio, lower alkoxy or (substituted) amino]; A is lower alkylene, CONH or forms a heterocyclic group in the form of A-R ; Q is H or lower alkyl] or its salt, e.g. 4-(5-acetylaminomethylfuran-2- yl)-2--(diaminomethyleneamino)thiazole. The compound of formula I can be produced by reacting a compound of formula II (Z'' is acid residue) with a compound of formula III in a solvent.

    GUANIDINE DERIVATIVE
    7.
    发明专利
    GUANIDINE DERIVATIVE 失效

    公开(公告)号：JP2000001486A

    公开(公告)日：2000-01-07

    申请号：JP12937699

    申请日：1999-05-11

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： TAKENAKA KOHEI ,  INOUE ZENICHI ,  AKAHA ATSUSHI ,  MACHITANI KOJI ,  NAKAMURA TAKASHI

    IPC: C07D333/28 ,  A61K31/00 ,  A61K31/165 ,  A61K31/166 ,  A61K31/38 ,  A61K31/381 ,  A61P3/00 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P13/00 ,  A61P13/12 ,  A61P43/00

    Abstract: PROBLEM TO BE SOLVED: To obtain a new compound having strong inhibiting action on Na+/H+ exchange in a human or animal cell and having further high effect as a medicine such as preventing and therapeutic agent for cardiovascular diseases. SOLUTION: This compound is represented by formula I [R1 is a group of formula II or III (R5 and R6 are each H, a lower alkyl or the like; X is carbonyl or sulfonyl); R2 is an arylyl or heterocycle; (n) is 1-6] and its salt, e.g. [3-(2,5-dichlorothiophen-3-yl)-5-[2-(methylaminoethyl)- aminocarbonyl]benzoyl]guanidine dihydrochloride. The compound of formula I is obtained by reacting a compound of formula IV, its derivative or a salt thereof with a compound of formula V, its derivative or a salt thereof. The reaction is usually carried out in water and an organic solvent under cooling or under heating. Furthermore, when the compound of formula V is used in a form of a free acid or its salt, the reaction is preferably carried out in the presence of a condensing agent.

    CEPHEM COMPOUND
    8.
    发明专利
    CEPHEM COMPOUND 失效

    公开(公告)号：JPH01242589A

    公开(公告)日：1989-09-27

    申请号：JP6891388

    申请日：1988-03-22

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： TAKASUGI HISASHI ,  INOUE ZENICHI

    IPC: C07D501/22

    Abstract: NEW MATERIAL:A compound (salt) expressed by the formula (R is amino or aminoacyl; R is carboxyl or protected carboxyl). EXAMPLE:7-acetamide-3-vinyl-2-cephem-4-carboxylic acid p-nitrobenzyl ester. USE:An antibacterial agent against wide pathogenic fungi containing Gram-posi tive and Gram-negative bacteria. PREPARATION:For example, 7-acetamide-3-vinyl-3-cephem-4-carboxylic acid and p-nitrobenzyl chloride are added to dimethyl sulfoxide and reacted in the presence of triethylamine at 40-45 deg.C for 4.5hr. The reaction mixture is then poured into a large amount of water and the resultant precipitate is filtered and purified using the column chromatography, etc., thus obtaining the objective compound of the formula.

    NOVEL FURYLTHIAZOLE DERIVATIVE AND PRODUCTION THEREOF
    10.
    发明专利
    NOVEL FURYLTHIAZOLE DERIVATIVE AND PRODUCTION THEREOF 失效

    公开(公告)号：JPH0272177A

    公开(公告)日：1990-03-12

    申请号：JP20880189

    申请日：1989-08-11

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： TAKASUGI HISASHI ,  KATSURA YOSUKE ,  INOUE ZENICHI ,  FUJI TETSUO

    IPC: A61K31/425 ,  A61K31/44 ,  A61K31/505 ,  A61K31/54 ,  A61P1/04 ,  A61P43/00 ,  C07D417/04 ,  C07D417/14

    Abstract: NEW MATERIAL:A compound expressed by formula I [R and R are H, alkyl which may have a substituent group (acyl or halogen) or mutually link to form alkylene; R is H or alkyl; R is NH2, acyl, acylamino, heterocyclic group or formula II (n is 0 or 1; X is CH or N; R is H, CN, NO2, etc., R is H, alkyl, alkylthio, etc.), etc.; A is alkylene or CONH or A-R is heterocyclic group: Q is H or alkyl] and salts thereof. EXAMPLE:4- [5-(2-Amino-2-sulfamoyliminoethyl)furan-2-yl] -2-(diaminomethyl- eneamino)thiazole. USE:Having antitumor and H2-receptor antagonistic activity and useful for treating gastritis, ulcer, reflux esophagitis, upper gastrointestinal hemorrhage, etc. PREPARATION:For example, a compound expressed by formula III (Z is acid residue) or salt thereof is reacted with a compound expressed by formula IV to afford the compound expressed by formula I.

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