http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0552767-B1

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filingDate 1993-01-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2002-05-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c270e2f31e176b041428a0054d315c08
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2a36585a5ebfd5af175d128eb0be0e03
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_74190ca234941567e680c41f0aadeb8b
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_952843f006c93e6567c01babbbbcd1af
publicationDate 2002-05-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0552767-B1
titleOfInvention 3'-derivatised oligonucleotide analogues with non-nucleotidic groups, their preparation and use
abstract Oligonucleotide analogs (I) and their physiologically tolerable salts. Oligonucleotide analogs and their physiologically tolerable salts of formula (I) are new. R<1> = H, a substituent or -P(=W)ZZ'; R<2> = 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<3>, R<4> = substituents; p = 1-100; q = 0-18; R<11> = 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<2> 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<5>R<6>); and (3) a pharmaceutical composition containing at least one compound (I) and optionally auxiliary, carrier and/or other active agents. R<5>, R<6> = 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.
priorityDate 1992-01-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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