公开(公告)号：PT552767E

公开(公告)日：2002-10-31

申请号：PT93100893

申请日：1993-01-21

Applicant: HOECHST AG

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

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.

公开(公告)号：FI102280B1

公开(公告)日：1998-11-13

申请号：FI906268

申请日：1990-12-19

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：PL172245B1

公开(公告)日：1997-08-29

申请号：PL29751693

申请日：1993-01-22

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.

公开(公告)号：NO179614B

公开(公告)日：1996-08-05

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.

公开(公告)号：IE67439B1

公开(公告)日：1996-04-03

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：NZ245720A

公开(公告)日：1995-12-21

申请号：NZ24572093

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 ,  C07F9/22 ,  C07F9/24 ,  C07H1/00 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/68 ,  C07H19/00 ,  C07F9/02

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.

公开(公告)号：CA2135591A1

公开(公告)日：1995-05-13

申请号：CA2135591

申请日：1994-11-10

Applicant: HOECHST AG

Inventor： PEYMAN ANUSCHIRWAN ,  UHLMANN EUGEN ,  MAG MATTHIAS ,  KRETZSCHMAR GERHARD ,  HELSBERG MATTHIAS ,  WINKLER IRVIN

IPC: C12N15/09 ,  A61K31/70 ,  A61K31/7088 ,  A61P31/12 ,  A61P31/22 ,  A61P35/00 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/70 ,  C12Q1/68

Abstract: of the disclosure: Stabilized oligonucleotides and their use The invention relates to novel stabilized oligonucleotides in which at least one non-terminal pyrimidine nucleoside is modified, and to their use as a diagnostic or pharmaceutical for the treatment of viral infections, cancer or diseases in which integrins or cell-cell adhesion receptors are active.

公开(公告)号：CA2132265A1

公开(公告)日：1995-03-18

申请号：CA2132265

申请日：1994-09-16

Applicant: HOECHST AG

Inventor： PEYMAN ANUSCHIRWAN ,  UHLMANN EUGEN ,  MAG MATTHIAS ,  KRETZSCHMAR GERHARD ,  HELSBERG MATTHIAS ,  WINKLER IRVIN

IPC: C12N15/09 ,  A61K31/70 ,  A61P31/12 ,  A61P31/22 ,  C07H21/00 ,  C07H21/04 ,  C12N15/113 ,  A61K48/00 ,  A61K47/48

Abstract: of the disclosure Novel antisense oligonucleotides against HSV 1, and their preparation The invention relates to novel antisense oligonucleotides having the sequences AO1 (Herp099): 5'-G C G G G G C T C C A T G G G G G T C G-3' AO2 (Herp018): 5'-G C A G G A G G A T G C T G A G G A G G-3' AO3 (Herp002): 5'-G G G G C G G G G C T C C A T G G G G G-3' AO4 (Herp112): 5'-G G C G G G G C T C C A T G G G G G T C-3' AO5 (Herp034): 5'-G G G G C T C C A T G G G G G T C G T A-3' AO6 (Herp024): 5'-A A G A G G T C C A T T G G G T G G G G-3' or AO7 (Herp028): 5'-G G C C C T G C T G T T C C G T G G C G-3' and their mixtures, homologs or modified forms, against HSV 1.

公开(公告)号：HU208400B

公开(公告)日：1993-10-28

申请号：HU36591

申请日：1991-02-01

Applicant: HOECHST AG

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

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

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.

公开(公告)号：AU3545093A

公开(公告)日：1993-09-30

申请号：AU3545093

申请日：1993-03-26

Applicant: HOECHST AG

Inventor： JAHNE GERHARD ,  HELSBERG MATTHIAS ,  WINKLER IRVIN ,  GROSS GERHARD ,  SCHOLL THOMAS

IPC: A61K31/52 ,  A61P31/12 ,  C07D473/00 ,  C07D473/32

Abstract: Compounds of the formula 1 in which the radicals R and/or R independently of one another represent acyl radicals of the formula -C(=O)-R (2> where R denotes C1-C3-alkyl and one of the radicals R and R can also denote hydrogen, and their physiologically tolerable salts have an antiviral action.