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    104.
    发明专利
    未知

    公开(公告)号：NO179614C

    公开(公告)日：1996-11-13

    申请号：NO905521

    申请日：1990-12-20

    Applicant: HOECHST AG

    Inventor： PEYMAN ANUSCHIRWAN ,  UHLMANN EUGEN ,  WINKLER IRVIN ,  HELSBERG MATTHIAS ,  MEICHSNER CHRISTOPH

    IPC: A61K31/66 ,  A61K31/662 ,  A61K31/675 ,  A61K31/685 ,  A61P31/12 ,  A61P31/18 ,  C07F9/38 ,  C07F9/40 ,  C07F9/58 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/6558 ,  C07F9/6571

    Abstract: The compound of the formula I in which R represents an aldehyde group or a group which can be converted into an aldehyde, R and R represent alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, hydrogen, sodium, potassium, calcium, magnesium, aluminium, lithium, ammonium or triethylammonium or R and R together form a cyclic diester, R and R represent alkyl, alkenyl, alkynyl, cycloalkyl, hydrogen, alkoxy or halogen, R and R represent alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, alkoxy, phenyl, cyanide, hydroxyl or hydrogen, X, Y or Z represent oxygen or sulphur, or prodrug forms of the compound of the formula I can be used for treatment of diseases caused by viruses. The preparation of these compounds and pharmaceutical preparations which contain them and also their use are described.

    OLIGONUCLEOTIDE ANALOGUES AND PHARMACEUTICAL COMPOSITIONS
    105.
    发明专利
    OLIGONUCLEOTIDE ANALOGUES AND PHARMACEUTICAL COMPOSITIONS 未知

    公开(公告)号：NZ245721A

    公开(公告)日：1995-09-26

    申请号：NZ24572193

    申请日：1993-01-20

    Applicant: HOECHST AG

    Inventor： UHLMANN EUGEN ,  PEYMAN ANUSCHIRWAN ,  O'MALLEY GERARD ,  HELSBERG MATTHIAS ,  WINKLER IRVIN

    IPC: A61K31/70 ,  A61K31/7125 ,  A61K48/00 ,  A61P31/12 ,  A61P35/00 ,  C07F9/24 ,  C07F9/44 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/68 ,  C07H19/00 ,  C07H19/20 ,  C07H19/10 ,  C07F9/02

    Abstract: Oligonucleotide analogs (I) and their physiologically tolerable salts. Oligonucleotide analogs and their physiologically tolerable salts of formula (I) are new. R = H, a substituent or -P(=W)ZZ'; R = H, OH, 1-18C alkoxy, halo, azido or amino; B = nucleotide base residue; A = oxy or methylene; d, e, f = 0-50; i = 1-10; r = 0 or 1; W = oxo, selenoxo or thioxo; V = oxy, sulfandiyl or imino; Y = oxy, sulfandiyl, imino or methylene; Y' = oxy, sulfandiyl, imino, (CH2)m or V(CH2)m; m = 1-18; X = OH or SH; U, R , R = substituents; p = 1-100; q = 0-18; R = H or functional group; Sp = a (3',5'-) spacer group of formula (i); g, g' = 0 or 1; h = 0-10; G = 1-12C alkylene (optionally substituted), (6-14C)aryldi-(1-8C)alkylene, 6-18C arylene, (CH2CH2V) alpha CH2CH2, (CH2V) alpha CH2, -(G-Y-P(=W)(U)-Y'-) beta or a group of formula (ii); alpha = 1-11; beta = 1-6; Z, Z' = OH, (seleno)thio or a substituent; provided that r is 0 when V is Y' and is 1 if i is greater than 1. Positions of R and the adjacent phosphoryl residue can be reversed; each nucleoside had D- or L-configuration and each B has alpha or beta configuration. Independent claims are also included for: (1) a method for producing (I); (2) the phosphitylation reagent of formula DMTr-X'-G'-Y''-P(U')(NR R ); and (3) a pharmaceutical composition containing at least one compound (I) and optionally auxiliary, carrier and/or other active agents. R , R = 1-12C alkyl or together form a 5-6 membered ring; DMTr = dimethoxytrityl; X', Y'' = oxy or sulfandiyl; U' = 1-4C alkyl or protected OH; G' = (CH2CH2O) alpha CH2CH2 or CH2CH(OR')CH2; and R' = 1-18C alkyl, 6-14C aryl or 6-14C aryl(1-8C) alkyl.

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