发明公开
- 专利标题: NON-NUCLEOTIDE PHOSPHORUS ESTER OLIGOMERS
- 专利标题(中): 非核苷酸亚磷酸酯低聚物
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申请号: EP96905134申请日: 1996-01-03
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公开(公告)号: EP0804443A4公开(公告)日: 1998-04-29
- 发明人: GENTLES ROBERT GERARD , COOK ALAN F , RUDOLPH MORRIS JONATHAN , FATHI REZA
- 申请人: PHARMAGENICS INC
- 专利权人: PHARMAGENICS INC
- 当前专利权人: PHARMAGENICS INC
- 优先权: US37404095 1995-01-18
- 主分类号: C07B59/00
- IPC分类号: C07B59/00 ; C07B61/00 ; C07D233/60 ; C07F9/141 ; C07F9/143 ; C07F9/144 ; C07F9/145 ; C07F9/24 ; C07F9/572 ; C07F9/58 ; C07F9/6506 ; C07F9/6509 ; C07F9/6539 ; C07F9/655 ; C07F9/6561 ; C07F9/6574 ; C07F9/6578 ; C07F9/09 ; C07F9/117 ; C07F9/12
摘要:
A phosphorus ester oligomer having structure (I) wherein A can be the same or different in each monomeric unit and each is independently selected from the group consisting of oxygen, sulfur, lower alkyl, alkyl- or aryl-substituted amino and aminoalkyl; B1 and B2 can be the same or different and each is independently selected from hydrogen, lower alkyl, a labelling group, a protecting group, a phosphoramidate or a phosphomonoester; R1 can be the same or different in each monomeric unit, and in at least one of the non-nucleotide monomeric units, R1 is independently selected from the group consisting of a condensation product of (i) a non-vicinal diol attached to a hydrogen bond donor functionality; (ii) a hydrogen bond acceptor selected from an ether, a purine or pyrimidine substituted 1,2-diol or a disubstituted heterocycle; (iii) a non-vicinal diol attached to a hydrophobic functionality or a vicinal diol attached to an aliphatic or alicyclic hydrophobic functionality; (iv) a diol attached to a ring substituted anionic functionality and (v) a cationic moiety attached to a non-vicinal or alicyclic diol, any of which can further include a detectable label, and n is at least one. Preferred R1 moieties include condensation products of heterocyclic diols, alicyclic diols, and polycyclic diols. Also the non-nucleotide monomers thereof, combinatorial library mixtures of the oligomers and the use of the oligomers as selective target-binding compounds.
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