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    NOVEL ANALOGUES OF OLIGONUCLEOTIDES, METHOD OF OBTAINING THEM AND THEIR APPLICATION AS WELL AS PHARMACEUTIC COMPOSITION
    1.
    发明专利
    NOVEL ANALOGUES OF OLIGONUCLEOTIDES, METHOD OF OBTAINING THEM AND THEIR APPLICATION AS WELL AS PHARMACEUTIC COMPOSITION 未知

    公开(公告)号：PL184920B1

    公开(公告)日：2003-01-31

    申请号：PL31320796

    申请日：1996-03-12

    Applicant: HOECHST AG

    Inventor： PEYMAN ANUSCHIRWAN ,  UHLMANN EUGEN ,  BREIPOHL GERHARD ,  WALLMEIER HOLGER

    IPC: A61K31/66 ,  A01N43/04 ,  A61K31/70 ,  A61K31/7088 ,  A61P31/16 ,  A61P31/18 ,  A61P35/00 ,  A61P43/00 ,  C07F9/38 ,  C07F9/40 ,  C07H19/00 ,  C07H21/00 ,  C07H21/02 ,  C07K14/00 ,  C12Q1/68 ,  C12Q1/70

    Abstract: Oligonucleotide analogues and related cpds. of formula (I) are new, in which n = 0-100; B = H or OH; 1-20C alkyl, 1-20C alkoxy or 1-20C alkylthio opt. substd. by 6-20C aryl; or aryl or heterocyclyl; where alkyl, aryl and heterocyclyl are opt. substd.; or B = a natural or unnatural nucleobase or a label; A = a single bond, CH2, (CR R )pM(CR R )q or (CR R )rM(CR R )sCY'; or A-B = 1-5 D- or L-amino acids condensed on via the carboxyl group; L = N or R N ; R = H or 1-6C alkyl opt. substd. by OH, 1-6C alkoxy, 1-6C alkylthio or NH2; Y' = O, S, CH2, CMe2 or NR ; M = a single bond, O, S or NR ; R and R = H, OH, 1-6C alkoxy, 1-6C alkylthio, NH2, halogen, or 1-6C alkyl opt. substd. by OH, 1-6C alkoxy or 1-6C alkylthio; p, q, r and s = 0-5; D and G = CR R ; R and R = H, 1-6C alkyl, 6-20C aryl, (6-20C)aryl(1-6C)alkyl, OH, 1-6C alkoxy or 1-6C alkylthio, where alkyl and aryl are opt. substd. by SR or NR R ; X = O, S or NR ; Y = O or S; Z = OR , NR R or XQ; R = H, alkyl, alkenyl, alkynyl, aryl or arylalkyl, where alkyl and aryl are opt. substd.; R and R = H, alkyl, alkenyl, alkynyl, aryl or arylalkyl, where alkyl is opt. substd.; or NR R is a 4- to 7-membered ring; Q and Q' = H, R , opt. modified oligonucleotides or conjugates which (a) favourably affect the properties of antisense oligonucleotides, (b) affect the properties of triplex-forming oligonucleotides, (c) serve as DNA probe labels or (d) bind to or crosslink a target nucleic acid during hybridisation; or Q and Q' alone or together are a single bond in a cyclic molecule; or Q and Q', when neither is hydrogen, can be linked together to form a cyclic molecule.

    Phosphonomonoester nucleic acids, process for their preparation, and their use
    2.
    发明专利
    Phosphonomonoester nucleic acids, process for their preparation, and their use 未知

    公开(公告)号：AU706470B2

    公开(公告)日：1999-06-17

    申请号：AU4802896

    申请日：1996-03-12

    Applicant: HOECHST AG

    Inventor： PEYMAN ANUSCHIRWAN ,  UHLMANN EUGEN ,  BREIPOHL GERHARD ,  WALLMEIER HOLGER

    IPC: A61K31/66 ,  A01N43/04 ,  A61K31/70 ,  A61K31/7088 ,  A61P31/16 ,  A61P31/18 ,  A61P35/00 ,  A61P43/00 ,  C07F9/38 ,  C07F9/40 ,  C07H19/00 ,  C07H21/00 ,  C07H21/02 ,  C07K14/00 ,  C12Q1/68 ,  C12Q1/70 ,  C07H21/04

    Abstract: Oligonucleotide analogues and related cpds. of formula (I) are new, in which n = 0-100; B = H or OH; 1-20C alkyl, 1-20C alkoxy or 1-20C alkylthio opt. substd. by 6-20C aryl; or aryl or heterocyclyl; where alkyl, aryl and heterocyclyl are opt. substd.; or B = a natural or unnatural nucleobase or a label; A = a single bond, CH2, (CR R )pM(CR R )q or (CR R )rM(CR R )sCY'; or A-B = 1-5 D- or L-amino acids condensed on via the carboxyl group; L = N or R N ; R = H or 1-6C alkyl opt. substd. by OH, 1-6C alkoxy, 1-6C alkylthio or NH2; Y' = O, S, CH2, CMe2 or NR ; M = a single bond, O, S or NR ; R and R = H, OH, 1-6C alkoxy, 1-6C alkylthio, NH2, halogen, or 1-6C alkyl opt. substd. by OH, 1-6C alkoxy or 1-6C alkylthio; p, q, r and s = 0-5; D and G = CR R ; R and R = H, 1-6C alkyl, 6-20C aryl, (6-20C)aryl(1-6C)alkyl, OH, 1-6C alkoxy or 1-6C alkylthio, where alkyl and aryl are opt. substd. by SR or NR R ; X = O, S or NR ; Y = O or S; Z = OR , NR R or XQ; R = H, alkyl, alkenyl, alkynyl, aryl or arylalkyl, where alkyl and aryl are opt. substd.; R and R = H, alkyl, alkenyl, alkynyl, aryl or arylalkyl, where alkyl is opt. substd.; or NR R is a 4- to 7-membered ring; Q and Q' = H, R , opt. modified oligonucleotides or conjugates which (a) favourably affect the properties of antisense oligonucleotides, (b) affect the properties of triplex-forming oligonucleotides, (c) serve as DNA probe labels or (d) bind to or crosslink a target nucleic acid during hybridisation; or Q and Q' alone or together are a single bond in a cyclic molecule; or Q and Q', when neither is hydrogen, can be linked together to form a cyclic molecule.

    Phosphonomonoester nucleic acids, process for their preparation, and their use
    3.
    发明专利
    Phosphonomonoester nucleic acids, process for their preparation, and their use 未知

    公开(公告)号：AU4802896A

    公开(公告)日：1996-09-26

    申请号：AU4802896

    申请日：1996-03-12

    Applicant: HOECHST AG

    Inventor： PEYMAN ANUSCHIRWAN ,  UHLMANN EUGEN ,  BREIPOHL GERHARD ,  WALLMEIER HOLGER

    IPC: A61K31/66 ,  A01N43/04 ,  A61K31/70 ,  A61K31/7088 ,  A61P31/16 ,  A61P31/18 ,  A61P35/00 ,  A61P43/00 ,  C07F9/38 ,  C07F9/40 ,  C07H19/00 ,  C07H21/00 ,  C07H21/02 ,  C07K14/00 ,  C12Q1/68 ,  C12Q1/70 ,  C07H21/04

    Abstract: Oligonucleotide analogues and related cpds. of formula (I) are new, in which n = 0-100; B = H or OH; 1-20C alkyl, 1-20C alkoxy or 1-20C alkylthio opt. substd. by 6-20C aryl; or aryl or heterocyclyl; where alkyl, aryl and heterocyclyl are opt. substd.; or B = a natural or unnatural nucleobase or a label; A = a single bond, CH2, (CR R )pM(CR R )q or (CR R )rM(CR R )sCY'; or A-B = 1-5 D- or L-amino acids condensed on via the carboxyl group; L = N or R N ; R = H or 1-6C alkyl opt. substd. by OH, 1-6C alkoxy, 1-6C alkylthio or NH2; Y' = O, S, CH2, CMe2 or NR ; M = a single bond, O, S or NR ; R and R = H, OH, 1-6C alkoxy, 1-6C alkylthio, NH2, halogen, or 1-6C alkyl opt. substd. by OH, 1-6C alkoxy or 1-6C alkylthio; p, q, r and s = 0-5; D and G = CR R ; R and R = H, 1-6C alkyl, 6-20C aryl, (6-20C)aryl(1-6C)alkyl, OH, 1-6C alkoxy or 1-6C alkylthio, where alkyl and aryl are opt. substd. by SR or NR R ; X = O, S or NR ; Y = O or S; Z = OR , NR R or XQ; R = H, alkyl, alkenyl, alkynyl, aryl or arylalkyl, where alkyl and aryl are opt. substd.; R and R = H, alkyl, alkenyl, alkynyl, aryl or arylalkyl, where alkyl is opt. substd.; or NR R is a 4- to 7-membered ring; Q and Q' = H, R , opt. modified oligonucleotides or conjugates which (a) favourably affect the properties of antisense oligonucleotides, (b) affect the properties of triplex-forming oligonucleotides, (c) serve as DNA probe labels or (d) bind to or crosslink a target nucleic acid during hybridisation; or Q and Q' alone or together are a single bond in a cyclic molecule; or Q and Q', when neither is hydrogen, can be linked together to form a cyclic molecule.

    PHOSPHONO-MONOESTER-NUCLEINIC ACIDS, PROCESS FOR PRODUCING THEM, AND THEIR USE
    10.
    发明专利
    PHOSPHONO-MONOESTER-NUCLEINIC ACIDS, PROCESS FOR PRODUCING THEM, AND THEIR USE 未知

    公开(公告)号：HU9600647A2

    公开(公告)日：1997-05-28

    申请号：HU9600647

    申请日：1996-03-13

    Applicant: HOECHST AG

    Inventor： BREIPOHL GERHARD ,  PEYMAN ANUSCHIRWAN ,  UHLMANN EUGEN ,  WALLMEIER HOLGER

    IPC: A61K31/66 ,  A01N43/04 ,  A61K31/70 ,  A61K31/7088 ,  A61P31/16 ,  A61P31/18 ,  A61P35/00 ,  A61P43/00 ,  C07F9/38 ,  C07F9/40 ,  C07H19/00 ,  C07H21/00 ,  C07H21/02 ,  C07K14/00 ,  C12Q1/68 ,  C12Q1/70 ,  A61K51/00 ,  C07H1/00 ,  C12N7/06

    Abstract: Oligonucleotide analogues and related cpds. of formula (I) are new, in which n = 0-100; B = H or OH; 1-20C alkyl, 1-20C alkoxy or 1-20C alkylthio opt. substd. by 6-20C aryl; or aryl or heterocyclyl; where alkyl, aryl and heterocyclyl are opt. substd.; or B = a natural or unnatural nucleobase or a label; A = a single bond, CH2, (CR R )pM(CR R )q or (CR R )rM(CR R )sCY'; or A-B = 1-5 D- or L-amino acids condensed on via the carboxyl group; L = N or R N ; R = H or 1-6C alkyl opt. substd. by OH, 1-6C alkoxy, 1-6C alkylthio or NH2; Y' = O, S, CH2, CMe2 or NR ; M = a single bond, O, S or NR ; R and R = H, OH, 1-6C alkoxy, 1-6C alkylthio, NH2, halogen, or 1-6C alkyl opt. substd. by OH, 1-6C alkoxy or 1-6C alkylthio; p, q, r and s = 0-5; D and G = CR R ; R and R = H, 1-6C alkyl, 6-20C aryl, (6-20C)aryl(1-6C)alkyl, OH, 1-6C alkoxy or 1-6C alkylthio, where alkyl and aryl are opt. substd. by SR or NR R ; X = O, S or NR ; Y = O or S; Z = OR , NR R or XQ; R = H, alkyl, alkenyl, alkynyl, aryl or arylalkyl, where alkyl and aryl are opt. substd.; R and R = H, alkyl, alkenyl, alkynyl, aryl or arylalkyl, where alkyl is opt. substd.; or NR R is a 4- to 7-membered ring; Q and Q' = H, R , opt. modified oligonucleotides or conjugates which (a) favourably affect the properties of antisense oligonucleotides, (b) affect the properties of triplex-forming oligonucleotides, (c) serve as DNA probe labels or (d) bind to or crosslink a target nucleic acid during hybridisation; or Q and Q' alone or together are a single bond in a cyclic molecule; or Q and Q', when neither is hydrogen, can be linked together to form a cyclic molecule.

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