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    TOPOISOMERASE I INHIBITOR
    1.
    发明专利
    TOPOISOMERASE I INHIBITOR 失效

    公开(公告)号：JPH11106338A

    公开(公告)日：1999-04-20

    申请号：JP27098797

    申请日：1997-10-03

    Applicant: SAGAMI CHEM RES

    Inventor： YAZAWA KAZUYOSHI ,  ONIMURA KENJIRO ,  KANO MAYUMI ,  KONDO SEI

    IPC: C07D487/14 ,  A61K31/40 ,  A61P35/00 ,  A61P43/00

    Abstract: PROBLEM TO BE SOLVED: To obtain the subject inhibitor having strong inhibiting activity against DNA topoisomerase I and usable as an antitumor agent by including a mitomycin derivative having docosahexaenoyl group as an active ingredient. SOLUTION: This inhibitor contains a compound of the formula (R is a docosahexaenoyl group) or its pharmaceutically permissible salt as an active ingredient. The compound of the formula can readily be synthesized by using a condensing agent, e.g. from maitomycin C and docosahexaenoic acid. Thereby, cancer chemotherapeutics based on new action mechanism different from well- known antitumor compound can be expected.

    TRIFLUOROMETHYL KETONE DERIVATIVE AND PHOSPHOLIPASE A2 INHIBITOR
    2.
    发明专利
    TRIFLUOROMETHYL KETONE DERIVATIVE AND PHOSPHOLIPASE A2 INHIBITOR 失效

    公开(公告)号：JPH09268153A

    公开(公告)日：1997-10-14

    申请号：JP7997096

    申请日：1996-04-02

    Applicant: SAGAMI CHEM RES

    Inventor： YAZAWA KAZUYOSHI ,  ONIMURA KENJIRO ,  KANO MAYUMI ,  KONDO SEI

    IPC: A61K31/23 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C45/45 ,  C07C49/227

    Abstract: PROBLEM TO BE SOLVED: To obtain the subject compound having uses as a medicine without any adverse effects such as a therapeutic agent, etc., for inflammatory diseases. SOLUTION: This trifluoromethyl ketone derivative is represented by the formula RCOCF3 (RCO is an acyl residue of an n-3-based highly unsaturated fatty acid) and useful as a medicine which is a cytoplasmic phospholipase A2 inhibitor. The compound is obtained by treating the n-3-based highly unsaturated fatty acid with a halogenating agent (e.g. oxalyl chloride), providing an acid halide and then reacting the resultant acid halide with a trifluoroacetic anhydride in the presence of a base (e.g. pyridine). Furthermore, the acyl residue is preferably icosapentaenoyl from the viewpoint of activities.

    1,2,3-THIADIAZOLE DERIVATIVE AND AGROCHEMICAL CONTAINING THE DERIVATIVE
    3.
    发明专利
    1,2,3-THIADIAZOLE DERIVATIVE AND AGROCHEMICAL CONTAINING THE DERIVATIVE 失效

    公开(公告)号：JPH09249665A

    公开(公告)日：1997-09-22

    申请号：JP6078996

    申请日：1996-03-18

    Applicant: SAGAMI CHEM RES ,  DAINIPPON INK & CHEMICALS

    Inventor： KOBORI TAKEO ,  HIRAGA TOMOKO ,  FUJITA MIKAKO ,  KONDO SEI ,  ASADA TORU ,  ONO SATORU ,  TSUBOI HIROYUKI

    IPC: C07D417/12 ,  A01N47/38 ,  C07D417/14

    Abstract: PROBLEM TO BE SOLVED: To obtain the subject new compound low in phytotoxicity, excellent in herbicidal activities against lowland weeds and upland weeds and in fungicidal activities against Pyricularia oryzae, etc., and useful as an active ingredient for agrochemicals such as herbicides and fungicides. SOLUTION: A compound of formula I [X is an alkyl, a (substituted) 6-10C aryl, a (substituted) heterocyclic residue; R , R are each a 1-8C alkyl, a (substituted) 6-10C aryl, R and R may together form a 3-7C polymethylene chain; (n) is 0-2]. For example, 1-(N, N-diethylcarbamoyl)-3-(5-t-butyl-1,2,3- thiadiazol-4-ylthio)-1H-1,2,4-triazole. The compound of formula I is obtained by reacting a compound of formula II or III with a compound of the formula: Cl-CO-N(R )(R ) in the presence of a base and, if necessary, treating the reaction product with an oxidizing agent.

    PRODUCTION OF ALKYNYLSILANES
    4.
    发明专利
    PRODUCTION OF ALKYNYLSILANES 失效

    公开(公告)号：JPH09194484A

    公开(公告)日：1997-07-29

    申请号：JP534896

    申请日：1996-01-17

    Applicant: SAGAMI CHEM RES

    Inventor： KONDO SEI ,  SUGITA HIKARI ,  HIYAMA TAMEJIROU ,  HATANAKA YASUO

    IPC: B01J27/138 ,  C07B61/00 ,  C07F7/08 ,  C07F7/14

    Abstract: PROBLEM TO BE SOLVED: To efficiently produce alkynylsilanes useful as an organic synthetic reactant, etc., such as a protecting group or an alkynylating agent by reacting a specific halosilane with a 1-alkyne in the coexistence of metallic samarium and a zinc salt. SOLUTION: A halosilane represented by formula I [R is H, an alkyl, an aryl, an alkenyl or an alkynyl having no acetylenic hydrogen; X is a halogen; (n) is an integer of 0-3] (e.g. chlorotrimethylsilane) is reacted with a 1-alkyne represented by formula II (R is an alkyl, a cycloalkyl, an aryl, an alkenyl, an alkynyl having no acetylenic hydrogen, an alkoxy, silyl or an acyl) (e.g. phenylethynye) in the coexistence of metallic samarium and a zinc salt to thereby efficiently afford the objective alkynylsilane represented by formula III and useful as an organic synthetic reactant, etc., such as a protecting group or an alkynylating agent [e.g. trimethyl(phenylethynyl)silane].

    GENE CODING FOR BIOSYNTHETIC ENZYME GROUP FOR EICOSAPENTAENOIC ACID AND PRODUCTION OF EICOSAPENTAENOIC ACID
    6.
    发明专利
    GENE CODING FOR BIOSYNTHETIC ENZYME GROUP FOR EICOSAPENTAENOIC ACID AND PRODUCTION OF EICOSAPENTAENOIC ACID 失效

    公开(公告)号：JPH08242867A

    公开(公告)日：1996-09-24

    申请号：JP348596

    申请日：1996-01-12

    Applicant: SAGAMI CHEM RES

    Inventor： YAZAWA KAZUYOSHI ,  YAMADA AKIKO ,  KONDO SEI ,  KATO MASASHI

    IPC: C12N15/09 ,  A61K31/20 ,  A61P7/02 ,  C07H21/04 ,  C12N1/21 ,  C12N9/00 ,  C12P7/64 ,  C12R1/19

    Abstract: PURPOSE: To obtain a new gene, having a specific base sequence, coding for a biosynthetic enzyme for eicosapentaenoic acid, having various physiological activities and useful for production, etc., of the biosynthetic enzyme for the eicosapentaenoic acid useful as a raw material, etc., for medicines, foods, feeds, etc. CONSTITUTION: Thus new gene codes for a biosynthetic enzyme for eicosapentaenoic acid with a base sequence containing a base sequence of the formula and producing the biosynthetic enzyme for the eicosapentaenoic acid, playing an important role as a constituent component of a biomembrane, having suppressing actions on blood platelet agglutination, lowering actions on neutral fats and cholesterol in blood, vasodepressor actions, etc., and useful as medicines, foods, feeds, etc., according to a genetic recombination method. The gene is obtained by culturing a microorganism, belonging to the Shewanella and having the ability to produce the eicosapentaenoic acid, then collecting the microbial cell, extracting a chromosomic DNA from the collected microbial cell, preparing a DNA library using the resultant chromosomic DNA and recovering the DNA from a clone having the productivity for the eicosapentaenoic acid.

    PHYSIOLOGICALLY ACTIVE PEPTIDE-BASED COMPOUND
    8.
    发明专利
    PHYSIOLOGICALLY ACTIVE PEPTIDE-BASED COMPOUND 失效

    公开(公告)号：JPH0770098A

    公开(公告)日：1995-03-14

    申请号：JP3241593

    申请日：1993-01-29

    Applicant: SAGAMI CHEM RES

    Inventor： U SEITAI ,  TSUJI TOMOKO ,  KONDO SEI

    IPC: A61K31/335 ,  A61K31/336 ,  A61P19/10 ,  A61P43/00 ,  C07D303/48 ,  C12P17/02 ,  C12R1/645

    Abstract: PURPOSE:To obtain the subject compound useful as a therapeutic agent effective for osteoporosis caused by dissolution of collagen, having excellent inhibitory action on cathepsin L. CONSTITUTION:A physiologically active peptide-based compound of formula I (R is H or -OH) such as cathestatin A of formula II. Cathestatin A has the following physical properties. Appearance: white powder. Molecular formula: C17H23N3O5. Molecular weight: 349. Mass spectrum: (SI-Mass)350(M+H) . Solubility: soluble in water, DMSO and acetic acid, insoluble in benzene, ethyl acetate and chloroform. Color reaction: positive to ninhydrin, etc. The compound of formula I is obtained by culturing a strain SCRC-OB16 (FERM-P-13,390), a newly separated one from a sponge in a sea area of Misaki at Yokosuka city in Kanagawa Prefecture, Japan, under an aerobic condition at pH6-7 at 20-30 deg.C for 2-10 days.

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