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    91.
    发明专利
    未知

    公开(公告)号：NO911081D0

    公开(公告)日：1991-03-19

    申请号：NO911081

    申请日：1991-03-19

    Applicant: HOECHST AG

    Inventor： JAEHNE GERHARD ,  ROESNER MANFRED ,  WINKLER IRVIN ,  HELSBERG MATTHIAS ,  SCHOLL THOMAS

    IPC: A61K31/52 ,  A61K31/522 ,  A61P31/12 ,  A61P31/22 ,  C07D473/00 ,  C07D473/04 ,  C07D473/16 ,  C07D473/18 ,  C07D473/20 ,  C07D473/22 ,  C07D473/24 ,  C07D473/28 ,  C07D473/32 ,  C07D473/34 ,  C07D473/36 ,  C07D473/40 ,  C07D

    Abstract: Purine derivs. of formula (I) and their salts are new. R1 = H, halo, NH3, OH, 1-6C alkoxy, -O-CH2Ph, -OPh, SH, 1-6C alkylthio, -S-CH2Ph, -SPh, NH2, 1-6C alkylamino, -NH-CH2Ph, -NH-Ph, 2-12C dialkylamino, -N(CH2Ph)2, cyclic dialkylamino, -N(Ph)2, 1-8C acylamino, 2-16C diacylamino, (N-alkyl-2-pyrrolidin-yliden)amino or 2-10C dialkylaminomethylidenamino; R2 = H, halo, N3, OH, SH, NH2, 1-6C alkylamino, 2-12C dialkylamino, -NH-CH2Ph, -N-(CH2Ph)2, cyclic dialkylamino, -NH-Ph, -N(Ph)2, 1-8C acylamino or thioacylamino, 2-16C diacylamino or di(thioacyl)amino; R3 = H, 1-6C alkyl (opt. substd.) or R8, where R8 is a phosphate ester-contg. gp.; R4 = H, 1-6C alkyl, OH, SH, NH2, halo, N3, 1-6C alkoxy, alkylthio or alkylamino, 2-12C dialkylamino, -O-CH2Ph, -S-CH2Ph, -NH-CH2Ph, -N(CH2Ph)2, -NHPh, -N(Ph)2, -OPh, -SPh, 1-8C acyloxy, 1-8C acylthio, 1-8C acylamino, 2-16C diacylamino, -O-(1-4C alkyl)-P(O)(OR6)(OR7) or -O(1-4C alkyl)-P(1-6C alkyl)(=O)(OR6); R5 = H, 1-6C alkyl (opt. substd.). A number of provisos are given in the specification.

    92.
    发明专利
    未知

    公开(公告)号：FI911310A0

    公开(公告)日：1991-03-18

    申请号：FI911310

    申请日：1991-03-18

    Applicant: HOECHST AG

    Inventor： JAEHNE GERHARD ,  ROESNER MANFRED ,  WINKLER IRVIN ,  HELSBERG MATTHIAS ,  SCHOLL THOMAS

    IPC: A61K31/52 ,  A61K31/522 ,  A61P31/12 ,  A61P31/22 ,  C07D473/00 ,  C07D473/04 ,  C07D473/16 ,  C07D473/18 ,  C07D473/20 ,  C07D473/22 ,  C07D473/24 ,  C07D473/28 ,  C07D473/32 ,  C07D473/34 ,  C07D473/36 ,  C07D473/40 ,  C07D

    Abstract: Purine derivs. of formula (I) and their salts are new. R1 = H, halo, NH3, OH, 1-6C alkoxy, -O-CH2Ph, -OPh, SH, 1-6C alkylthio, -S-CH2Ph, -SPh, NH2, 1-6C alkylamino, -NH-CH2Ph, -NH-Ph, 2-12C dialkylamino, -N(CH2Ph)2, cyclic dialkylamino, -N(Ph)2, 1-8C acylamino, 2-16C diacylamino, (N-alkyl-2-pyrrolidin-yliden)amino or 2-10C dialkylaminomethylidenamino; R2 = H, halo, N3, OH, SH, NH2, 1-6C alkylamino, 2-12C dialkylamino, -NH-CH2Ph, -N-(CH2Ph)2, cyclic dialkylamino, -NH-Ph, -N(Ph)2, 1-8C acylamino or thioacylamino, 2-16C diacylamino or di(thioacyl)amino; R3 = H, 1-6C alkyl (opt. substd.) or R8, where R8 is a phosphate ester-contg. gp.; R4 = H, 1-6C alkyl, OH, SH, NH2, halo, N3, 1-6C alkoxy, alkylthio or alkylamino, 2-12C dialkylamino, -O-CH2Ph, -S-CH2Ph, -NH-CH2Ph, -N(CH2Ph)2, -NHPh, -N(Ph)2, -OPh, -SPh, 1-8C acyloxy, 1-8C acylthio, 1-8C acylamino, 2-16C diacylamino, -O-(1-4C alkyl)-P(O)(OR6)(OR7) or -O(1-4C alkyl)-P(1-6C alkyl)(=O)(OR6); R5 = H, 1-6C alkyl (opt. substd.). A number of provisos are given in the specification.

    98.
    发明专利
    未知

    公开(公告)号：NO308609B1

    公开(公告)日：2000-10-02

    申请号：NO930200

    申请日：1993-01-21

    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.

    99.
    发明专利
    未知

    公开(公告)号：NO308215B1

    公开(公告)日：2000-08-14

    申请号：NO930199

    申请日：1993-01-21

    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 ,  C07F9/22 ,  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.

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