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    ANTI-AIDS AGENT CONTAINING OLIGODEOXYRIBONUCLEOTIDE CONTAINING MODIFIED NUCLEOSIDE, OR THE LIKE
    1.
    发明专利
    ANTI-AIDS AGENT CONTAINING OLIGODEOXYRIBONUCLEOTIDE CONTAINING MODIFIED NUCLEOSIDE, OR THE LIKE 失效

    公开(公告)号：JP2000302684A

    公开(公告)日：2000-10-31

    申请号：JP11440899

    申请日：1999-04-22

    申请人： SANKYO CO

    发明人： KOIZUMI MAKOTO ,  KANEKO MASAKATSU ,  OMINE HISANORI ,  FURUKAWA HIDEHIKO ,  NISHIGAKI TAKASHI

    IPC分类号： C07H21/04 ,  A61K31/00 ,  A61K31/70 ,  A61K31/7088 ,  A61P31/00 ,  A61P31/18

    摘要： PROBLEM TO BE SOLVED: To obtain an anti-AIDS agent having a specific inhibitory activity against an AIDS virus, capable of efficiently controlling proliferation of the virus in an infected cell by making the anti-AIDS agent include a specific oligodeoxyribonucleotide (salt). SOLUTION: This anti-AIDS agent contains an oligodeoxyribonucleotide of formula I (B1 is a group of formula II, a group of formula III, or the like; B2 and B3 are each a group of formula II to formula V: (m) is 0-7; (z) is 0-9; S1 and S2 are each H, a 1-4C alkyl, a 1-4C alkoxy or a halogen) such as cyanoethyl =2-N-methyl-6-O-diphenylcarbamyl-2'-deoxy-5'-O-(4,4'-dimethoxytrityl) guanosin-3'-O-yl-N,N-diisopropylphosphoramidite and its pharmacologically acceptable salt. A daily dose of the compound of formula I is preferably 10-1,000 mg per adult in the case of oral administration.

    METHOD FOR SYNTHESIZING OLIGONUCLEOTIDE
    3.
    发明专利
    METHOD FOR SYNTHESIZING OLIGONUCLEOTIDE 失效

    公开(公告)号：JPH0753587A

    公开(公告)日：1995-02-28

    申请号：JP11328194

    申请日：1994-05-27

    申请人： SANKYO CO

    发明人： KOIZUMI MAKOTO ,  KANEKO MASAKATSU

    IPC分类号： A61K31/70 ,  A61K31/7088 ,  A61P31/12 ,  A61P31/18 ,  C07H21/04

    摘要： PURPOSE:To simply obtain the subject compound having an anti-AIDS viral action at a low cost and in high purity by synthesizing a substituent-having oligonucleotide on the 3'-terminal hydroxyl group of an oligonucleotide having a basic sequence through phosphorous acid using a DNA synthesizing machine. CONSTITUTION:A compound of formula I [R -R are each H, a 1-4C alkoxy; X is S', S'O, etc.; A is (CH2)h ((h) is 1-6), etc.; Y is hydroxyl group, phenyloxy, etc.,] is reacted with a polymeric substance of formula II (X is oxygen atom, sulfur atom, etc.,), and a DNA chain is elongated on the obtained polymeric substance of formula III using a DNA-synthesizing machine to obtain the objective compound of formula IV [R -R are each H, a 1-4C alkyl, etc.; Z is C, silicon, etc.,); R is H, a 1-4C aralkyl; Y is O2, sulfur atom, etc.; Y is O2, NH group, etc.; X is O2, etc., D is oligonucleotide having a chain length of 2-30].

    GRISEOLIC ACID ANALOG AND LAK INHIBITOR CONTAINING THE SAME
    4.
    发明专利
    GRISEOLIC ACID ANALOG AND LAK INHIBITOR CONTAINING THE SAME 失效

    公开(公告)号：JPH04210920A

    公开(公告)日：1992-08-03

    申请号：JP220391

    申请日：1991-01-11

    申请人： SANKYO CO

    发明人： KANEKO ISAO ,  OTSUKI MASAHIKO ,  KANEKO MASAKATSU ,  KAMOGARI MAKOTO ,  YASUMOTO TAKASHI

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61P37/06 ,  C07H19/16

    摘要： PURPOSE:To provide a new griseolic acid analog having excellent LAK and CTL activity inhibiting action and expected to be useful as an excellent low- toxic immunosuppressive agent, etc. CONSTITUTION:The compound of formula I {one of R and R is group of formula II [B is 1-25C alkylene, 2-25C alkenylene or 2-25C alkynylene; R is H, halogen, halogenomethyl, NH, OH, SH or aryl; B may be interrupted with a group selected from -OCO-, -O-, -S-, -SS-, -SCO-, -NHCO-, -NHCOO- and -NR - (R is lower alkyl)] and the other is H or group of formula II}, its ester derivative and their salts, for example, O '-palmitoylgriseolic acid. The compound can be produced by protecting the 7'-OH and 9'-COOH groups of griseolic acid of formula III by conventional method, esterifying the 8'-COOH group and reacting the 2'-OH group of the resultant compound of formula IV with a compound of formula R -B-CO-X (X is leaving group).

    PRODUCTION OF GRISEOLIC ACID DERIVATIVE
    5.
    发明专利
    PRODUCTION OF GRISEOLIC ACID DERIVATIVE 失效

    公开(公告)号：JPS6230797A

    公开(公告)日：1987-02-09

    申请号：JP25195985

    申请日：1985-11-12

    申请人： SANKYO CO

    发明人： KANEKO MASAKATSU ,  KIMURA MISAKO ,  MUROFUSHI YOSHINOBU

    IPC分类号： C07H19/16 ,  C07H19/02

    摘要： PURPOSE:To obtain the titled nontoxic compound useful as an ameliorant of cerebral function and cardiovascular agent, etc., in high yield and a short process, by reacting a griseolic acid derivative which is a starting raw material with an alkylating agent and heating the formed compound. CONSTITUTION:A compound expressed by formula I (R is H or protecting group of OH; R2 is H or OH which can be protected; R3 and R4 are H or protecting group of COOH; R5 and R6 are H or together form single bond) is first reacted with an alkylating or aralkylating agent expressed by the formula R7-X (R7 is lower alkyl or aralkyl; X is halogen, arylsulfonyloxy, etc.) normally in an inert solvent to give a compound, which is then heated in a solvent. The protecting groups are, as necessary, removed to give the aimed compound expressed by formula II. The above-mentioned heat treatment is preferably carried out by a method for distilling away the solvent from the reaction mixture of the compound expressed by formula I with the compound expressed by the formula R7-X, dissolving the resultant residue in a buffer solution at 4-12pH and heating the resultant solution, etc.

    NEW 3'-4' CROSSLINKED NUCLEOSIDE AND OLIGONUCLEOTIDE ANALOGUE
    9.
    发明专利
    NEW 3'-4' CROSSLINKED NUCLEOSIDE AND OLIGONUCLEOTIDE ANALOGUE 失效

    公开(公告)号：JP2001064296A

    公开(公告)日：2001-03-13

    申请号：JP2000187448

    申请日：2000-06-22

    申请人： SANKYO CO

    发明人： KANEKO MASAKATSU ,  MORITA KOJI ,  IMANISHI TAKESHI

    IPC分类号： C07H19/06 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/712 ,  A61K48/00 ,  A61P31/12 ,  C07H19/16 ,  C07H21/00

    摘要： PROBLEM TO BE SOLVED: To obtain a new 3'-4' crosslinked nucleoside useful as an intermediate for producing an oligonucleotide analogue used as an antiviral drug, an anti- sense or anti-gene drug, or the like, which are stable and excellent. SOLUTION: This new compound is represented by formula I (R1 and R2 are each H, phosphate group; A is a 1-4C alkylene; B is purin-9-yl, or the like) and is preferably 3'-O,4'-C-ethylene-5-methyluridine. The compound of formula I is obtained by reacting a compound of formula II (X and Y are each a protecting group) with an eliminable group-introducing reagent such as p- toluenesulfonylchloride, an acid anhydride such as acetic anhydride and a trimethylsilylation product corresponding to a purine or pyrimidine capable of containing a desired substituent in order, and then eliminating a protecting group Y of a produced compound of formula III (R9 is a group for forming an eliminable group together in association with oxygen; Z is an acryl; B1 is purin-9-yl, or the like) and simultaneously performing cyclization reaction of a deprotected 3'OH and a group of OR9.

    NEW NUCLEOSIDE AND OLIGONUCLEOTIDE ANALOG
    10.
    发明专利
    NEW NUCLEOSIDE AND OLIGONUCLEOTIDE ANALOG 失效

    公开(公告)号：JP2000297097A

    公开(公告)日：2000-10-24

    申请号：JP2000034560

    申请日：2000-02-14

    申请人： SANKYO CO

    发明人： KANEKO MASAKATSU ,  MORITA KOJI ,  IMANISHI TAKESHI

    IPC分类号： C12N15/09 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7076 ,  A61K31/7088 ,  A61K31/712 ,  A61K48/00 ,  A61P31/12 ,  A61P35/00 ,  A61P43/00 ,  C07H19/06 ,  C07H19/067 ,  C07H19/10 ,  C07H19/16 ,  C07H19/167 ,  C07H19/20 ,  C07H21/00 ,  C07H21/02

    摘要： PROBLEM TO BE SOLVED: To obtain a new compound having an intramolecular ether bond and useful for an antisense or antigene medicine, a primer for a detecting agent for a specific gene or for initiating the amplification and an intermediate for producing the primer. SOLUTION: This compound is represented by formula I R1 and R2 are each H, a protecting group of OH, a (protected)phosphate group, P(R3)R4 [R3 and R4 are each a (protected)OH, a (protected)amino or the like]; A is a 1-4C alkylene; B is a (substituted)purin-9-yl or a (substituted)2-oxo-pyrimidin-1-yl), e.g. 5 '-O-dimethoxytrityl -2'-O, 4'-C-ethylene-4 -N -benzoylcytidine-3' -O-(2- cyanoethyl N,N-diisopropyl)phosphoramidite. The compound represented by formula I is produced by a method, etc., for using, e.g. a compound represented by formula II (X and Y are each a protecting group) as a starting substance, passing the compound represented by formula II through a compound represented by formula III (R7 is a group capable of forming a leaving group), etc., and providing a compound represented by formula IV (B1 is purin-9-yl or the like).