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    OLIGONUCLEOTIDE ANALOGUES
    83.
    发明专利
    OLIGONUCLEOTIDE ANALOGUES 未知

    公开(公告)号：HU9300162D0

    公开(公告)日：1993-04-28

    申请号：HU9300162

    申请日：1993-01-21

    Applicant: HOECHST AG

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

    IPC: A61K31/70 ,  A61K31/7125 ,  A61K48/00 ,  A61P31/12 ,  A61P35/00 ,  C07F9/22 ,  C07F9/24 ,  C07H1/00 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/68

    Abstract: The invention relates to compounds of the formula I in which R is H, alkyl, acyl, aryl or a phosphate residue; R is H, OH, alkoxy, NH2 or halogen; B is a base customary in nucleotide chemistry; a is O or CH2; n is an integer from 1 to 100; W is O, S or Se; V is O, S or NH; Y is O, S, NH or CH2; Y' is O, S, NH or alkylene; X is OH or SH; U is OH, SH, SeH, alkyl, aryl or amine, and Z is OH, SH, SeH, an optionally substituted radical from the series comprising alkyl, aryl, heteroaryl, alkoxy or amino or a group which favours intracellular uptake or as labelling of a DNA probe or which on hybridisation interacts with the target nucleic acid, where if Z is OH, SH, CH3 or OC2H5, at least one of the groups X, Y, Y', V, W is not equal to OH or O, or R is not equal to H; process for their preparation and their use as inhibitors of gene expression, as probes for detecting nucleic acids and as aids in molecular biology.

    84.
    发明专利
    未知

    公开(公告)号：FI930221A0

    公开(公告)日：1993-01-20

    申请号：FI930221

    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

    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.

    86.
    发明专利
    未知

    公开(公告)号：PT96626A

    公开(公告)日：1991-10-15

    申请号：PT9662691

    申请日：1991-01-31

    Applicant: HOECHST AG

    Inventor： UHLMANN EUGEN ,  BUDT KARL-HEINZ ,  KNOLLE JOCHEN ,  PEYMAN ANUSCHIRWAN ,  WINKLER IRVIN ,  HELSBERG MATTHIAS

    IPC: A61P31/12 ,  A61K31/66 ,  C07F9/38 ,  C07F9/40 ,  C07F9/6574 ,  A61K31/16

    Abstract: The use of a compound of the formula I I in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R1 and R2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R1 and R2 together form a cyclic diester, R3 and R4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.

    89.
    发明专利
    未知

    公开(公告)号：NO905521L

    公开(公告)日：1991-06-24

    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.

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