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    DIAZA CYCLIC COMPOUND
    5.
    发明专利
    DIAZA CYCLIC COMPOUND 失效

    公开(公告)号：JPH08231516A

    公开(公告)日：1996-09-10

    申请号：JP1640696

    申请日：1996-02-01

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： NAGANO MASANOBU ,  TAKENAKA KOHEI ,  KATO TAKESHI ,  KOBAYASHI YUIKO

    IPC: C12N9/99 ,  A61K31/55 ,  A61P9/00 ,  A61P9/12 ,  A61P43/00 ,  C07D243/02 ,  C07D405/12

    Abstract: PURPOSE: To obtain a new compound having an activity for inhibiting neutral endpeptidase and angiotensin transferase, and useful for hypertension, cardiac failure, angina pectoris, renal failure, periodic edema, aldosteronism, hypercalcemia, glaucoma, asthma, inflammation, ache, epilepsia, etc. CONSTITUTION: A compound of formula I [R is an acyl; a (protected)mercapto; R is H, a (substituted)aryl; R is a (substituted)acyl lower alkyl; R is a lower alkyl, a cyclo lower alkyl, a (substituted)aryl; X is a lower alkylene; Y is a single bond, C(=O); Z is a lower alkylene; R is H, a lower alkyl; R is H, or R and R are combined with each other to form a single bond]. For example, [(S)-6-((S)-2-acetylthio-3-phenylpropionyl)amino-4,5,6,7-tetrahydro-7- oxo-3- phenyl-1H-1,2-diazepin-1-yl]acetic acid ethyl ester. The compound of formula I is obtained by reacting a compound of formula II with a compound of formula III.

    QUINAZOLINE DERIVATIVE
    8.
    发明专利
    QUINAZOLINE DERIVATIVE 失效

    公开(公告)号：JPS5695174A

    公开(公告)日：1981-08-01

    申请号：JP17045980

    申请日：1980-12-03

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： UEDA IKUO ,  KATOU MASAYUKI ,  NAGANO MASANOBU

    IPC: C07D239/94 ,  A61K31/505 ,  A61K31/517 ,  A61P37/08 ,  C07D239/95 ,  C07D405/12 ,  C07D487/04 ,  C07D487/14

    Abstract: NEW MATERIAL:A compound shown by the formula I [Ra and Rb are esterified carboxyl group; R and R are H, alkyl, halogen, nitro, amino, alkoxy, etc.; A' is a group shown by the formula II (R is H, alkyl, OH, dialkylamino, etc.), or a group shown by the formula III (R is alkyl or alkenyl)], a pyrimidoquinazoline compound shown by the formula IV (R is H, carboxy, etc.; A is a group shown by the formula III, etc.), or their pharmaceutically acceptable salts. EXAMPLE:Diethyl [(6-pivalamide-4-quinazolinylamino)methylene]-propanedioate. USE:An antiallergic agent, e.g., a drug for allergic asthma. PROCESS:A compound shown by the formula V is reacted with a compound shown by the formula VI (R is alkoxy) to give a compound shown by the formula I.

    9.
    发明专利
    失效

    公开(公告)号：JPH05294946A

    公开(公告)日：1993-11-09

    申请号：JP20154191

    申请日：1991-05-09

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： UEDA IKUO ,  KATO MASAYUKI ,  NAGANO MASANOBU

    IPC: A61K31/505 ,  A61K31/517 ,  A61P37/08 ,  C07D239/74 ,  C07D239/80 ,  C07D239/94 ,  C07D239/95 ,  C07D239/96 ,  C07D265/26 ,  C07D405/12 ,  C07D487/04 ,  C07D487/14

    Abstract: PURPOSE:To provide the subject new compound exhibiting a strong antiallergic effect and useful as a low-toxic antiallergic agent. CONSTITUTION:A compound of formula I [R a and R b are each an esterified carboxyl or a group of formula II may be formed in combination of R a with R b; R and R are each H, an alkyl, a halogen, nitro, amino, etc.; A' is formula III (R is H, an alkyl, hydroxyl, etc.) or formula IV (R is an alkyl)], e.g. diethyl[(4-quinazolinylamino)-methylene] propanedioate. The compound of formula I is obtained by reacting a compound of formula V with a compound of formula VI (R is an alkoxy) in a solvent such as N,N-dimethylformamide under cooling or heating. Useful for allergic asthma, allergic rhinitis, uticaria, pollinosis, allergic conjunctivitis, atopic dermatitis, colitis ulcerosa, alimentary allergy, etc.

    IMIDAZOPYRIDINE COMPOUND AND PRODUCTION THEREOF
    10.
    发明专利
    IMIDAZOPYRIDINE COMPOUND AND PRODUCTION THEREOF 失效

    公开(公告)号：JPS63146881A

    公开(公告)日：1988-06-18

    申请号：JP29718287

    申请日：1987-11-25

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： SHIOKAWA YOICHI ,  NAGANO MASANOBU ,  ITANI HIROMICHI

    IPC: C07D471/04 ,  A61K31/44 ,  A61P1/04 ,  C07D20060101

    Abstract: NEW MATERIAL:The compound of formula I [R is lower alkynyl (oxy lower alkyl) or N,N-di-lower alkylamine lower alkynyl; R is lower alkyl; R is cyano, trihalo-lower alkyl, carbamoyl, protected amino, (protected) COOH, OH, (protected) hydroxy-lower alkyl, substituted ar-lower alkyl, etc.; R is H or lower alkyl] and its salt. EXAMPLE:8-(2-Methoxycabonylamine-6-methylbenzyloxy)-2-methyl-3-(2-prop ynyl) imidazo[1,2-1]pyridine. USE:An antiulcer agent. PREPARATION:A compound of formula II or its salt is made to react with a compound of formula III or its reactive derivative at the OH group.

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