Complementary dna and toxins

Details Complementary dna and toxins Complementary dna and toxins

C - Chemistry, Metallurgy

07

C

C07C 317/18 (2006.01) C07C 323/12 (2006.01) C07F 9/06 (2006.01) C07F 9/24 (2006.01) C07F 9/28 (2006.01) C07H 21/00 (2006.01) C12N 15/10 (2006.01) G01N 33/543 (2006.01) C07B 61/00 (2006.01)

Patent

CA 2190145

This invention relates to new derivatized solid supports and compounds having formula (I) wherein S may be a solid support; L may be a chemical bond or a suitable inorganic or organic linker; Z may be -SO2- or -S-S-; R may be -OH, an H-phosphonate, an alkane-phosphonate, a phosphotriester, a phosphite triester, a phosphite diester, a phosphorothioate, a phosphorodithioate, a phosphoroamidate, a phosphoroamidite, -OR1, -SR1, a nucleotide, N, which may be substituted or modified in its sugar, phosphate or base, or an oligonucleotide of the formula -(N)g -R2, wherein N is as defined above which may be the same or different; g is an integer from one to two hundred; R1 is a suitable protecting group; and R2 may be an H-phosphonate, an alkane- phosphonate, a phosphotriester, a phosphite triester, a phosphite diester, a phosphorothioate, a phosphorodithioate, a phosphoroamidate, a phosphoroamidite, -OH, -OR1, -SR1, or -O-P(OCH2CH2CN)-O-CH2CH2ZCH2CH2OR1. Furthermore, this invention provides methods for preparing 3'-phosphate oligonucleotides, 5'-phosphate oligonucleotides, (3',5')-diphosphate oligonucleotides, 3'-phosphate oligonucleotide conjugates, 5'-phosphate oligonucleotide conjugates, and (3',5')-diphosphate oligonucleotide conjugates.

L'invention porte sur de nouveaux dérivés sur supports solides et composés de formule (I) où S peut être un support solide; L, peut être une liaison chimique ou un liant approprié organique ou inorganique; Z peut être -SO¿2? ou -S-S-; R peut être -OH, H-phosphonate, alcane-phosphonate, phosphotriester, phosphitetriester, phosphitediester, phosphorothioate, phosphorodithioate, phosphoroamidate, phosphoroamidite, OR?1¿, -SR?1¿, un nucléotide N pouvant être substitué ou modifié dans ses sucres, ses phosphates ou bases, ou un oligonucléotide de formule -(N)¿g?-R?2¿, où N est tel que ci-dessus avec possibilités de changement; g est un entier entre 1 et 200; R?2¿ peut être H-phosphonate, alcane-phosphonate, phosphotriester, phosphitetriester, phosphitediester, phosphorothioate, phosphorodithioate, phosphoroamidate, phosphoroamidite, -OH, -OR?1¿, -SR?1¿ ou -O-P(OCH¿2?CH¿2?CN)-O-CH¿2?CH¿2?ZCH¿2?CH¿2?OR?1¿. L'invention porte en outre sur des procédés de préparation de 3'-phosphateoligonucléotides, de 5'-phosphateoligonucléotides, de (3',5')-diphosphateoligonucléotides, et de leurs conjugués.

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