公开(公告)号：ZA93423B

公开(公告)日：1993-09-09

申请号：ZA93423

申请日：1993-01-21

Applicant: HOECHST AG

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

IPC: A61K31/70 ,  A61K31/7125 ,  A61K48/00 ,  A61P31/12 ,  A61P35/00 ,  C07F9/24 ,  C07F9/44 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/68 ,  C07H ,  C12Q ,  A61K

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.

公开(公告)号：PT98167A

公开(公告)日：1993-08-31

申请号：PT9816791

申请日：1991-07-01

Applicant: HOECHST AG

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

IPC: A61K31/505 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61P31/12 ,  A61P31/22 ,  C07D239/36 ,  C07D239/47 ,  C07D239/52 ,  C07D239/54 ,  C07D239/553 ,  C07D405/04 ,  C07D409/04 ,  C07H19/06

公开(公告)号：CA2087817A1

公开(公告)日：1993-07-23

申请号：CA2087817

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 ,  C07F9/48 ,  C07F9/553

Abstract: HOE 92/F 013 of the disclosure 2'-derivatized oligonucleotide analogs with nonnucleotidic groupings, their preparation and use The present invention relates to novel oligonucleotide analogs with valuable physical, biological and pharmacological properties, and a process for their preparation.

公开(公告)号：HUT57764A

公开(公告)日：1991-12-30

申请号：HU92891

申请日：1991-03-20

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 ,  C07D473/02

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.

公开(公告)号：AU617115B2

公开(公告)日：1991-11-21

申请号：AU2017988

申请日：1988-07-29

Applicant: HOECHST AG

Inventor： SCHRINNER ELMAR ,  WINKLER IRVIN ,  MEICHSNER CHRISTOPH ,  HELSBERG MATTHIAS

IPC: C07D473/06 ,  A61K20060101 ,  A61K31/52 ,  A61K31/70 ,  A61K31/715 ,  A61P31/12 ,  C07D20060101 ,  C07D473/04 ,  C08B20060101 ,  C08B37/00 ,  A61K31/735

Abstract: The preparation contains or consists of… a) at least one sulphated polysaccharide and… b) at least one xanthine derivative. The preparation is suitable for the control and prophylaxis of viral diseases, especially those caused by retroviruses.

公开(公告)号：NO911081A

公开(公告)日：1991-09-23

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

CPC classification number: C07D473/04 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  C07D473/32 ,  C07D473/40

公开(公告)号：IE904625A1

公开(公告)日：1991-07-17

申请号：IE462590

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.

公开(公告)号：AU3793389A

公开(公告)日：1990-01-11

申请号：AU3793389

申请日：1989-07-07

Applicant: HOECHST AG

Inventor： KLOSA JOSEF ,  SCHRINNER ELMAR ,  HELSBERG MATTHIAS ,  WINKLER IRVIN ,  MEICHSNER CHRISTOPH ,  KROGER HANS

IPC: A61K31/52 ,  A61P31/12 ,  C07D473/38

公开(公告)号：DK338389D0

公开(公告)日：1989-07-07

申请号：DK338389

申请日：1989-07-07

Applicant: HOECHST AG

Inventor： KLOSA JOSEF ,  KROEGER HANS ,  MEICHSNER CHRISTOPH ,  WINKLER IRVIN ,  HELSBERG MATTHIAS ,  SCHRINNER ELMAR

IPC: A61K31/52 ,  A61P31/12 ,  C07D473/38

公开(公告)号：AU2017988A

公开(公告)日：1989-02-02

申请号：AU2017988

申请日：1988-07-29

Applicant: HOECHST AG

Inventor： SCHRINNER ELMAR ,  WINKLER IRVIN ,  MEICHSNER CHRISTOPH ,  HELSBERG MATTHIAS

IPC: C07D473/06 ,  A61K20060101 ,  A61K31/52 ,  A61K31/70 ,  A61K31/715 ,  A61P31/12 ,  C07D20060101 ,  C07D473/04 ,  C08B20060101 ,  C08B37/00

Abstract: The preparation contains or consists of… a) at least one sulphated polysaccharide and… b) at least one xanthine derivative. The preparation is suitable for the control and prophylaxis of viral diseases, especially those caused by retroviruses.