公开(公告)号：US6008398A

公开(公告)日：1999-12-28

申请号：US595264

申请日：1996-02-01

申请人： Robert Gerard Gentles ,  Alan F. Cook ,  Morris Jonathan Rudolph ,  Reza Fathi

发明人： Robert Gerard Gentles ,  Alan F. Cook ,  Morris Jonathan Rudolph ,  Reza Fathi

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 ,  C07F9/40

CPC分类号： C07F9/6578 ,  C07B59/004 ,  C07F9/1411 ,  C07F9/1414 ,  C07F9/143 ,  C07F9/144 ,  C07F9/145 ,  C07F9/2408 ,  C07F9/2416 ,  C07F9/242 ,  C07F9/5728 ,  C07F9/582 ,  C07F9/588 ,  C07F9/65062 ,  C07F9/650958 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/6561 ,  C07F9/65616 ,  C40B40/00 ,  Y02P20/55

摘要： A phosphorus ester oligomer having the structure: 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, substituted or unsubstituted alkylamino, substituted or unsubstituted arylamino and aminoalkyl; B.sub.1 and B.sub.2 can be the same or different and each is independently selected from hydrogen, lower alkyl, a labeling group, a protecting group, a phosphoramidate or a phosphomonoester; R.sub.1 can be the same or different in each monomeric unit, and in at least one of the non-nucleotide monomeric units, R.sub.1 is independently selected from the group consisting of (i) a non-vicinal diol attached to a hydrogen bond donor functionality; (ii) a hydrogen bond acceptor selected from an ether; (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 two. Preferred R.sub.1 moieties include condensation products of alicyclic diols and polycyclic diols; also the non-nucleotide monomers thereof, and the use of the oligomers as selective target-binding compounds.

摘要翻译： 具有以下结构的磷酯低聚物：其中A可以在每个单体单元中相同或不同，并且各自独立地选自氧，硫，低级烷基，取代或未取代的烷基氨基，取代或未取代的芳基氨基和氨基烷基; B1和B2可以相同或不同，各自独立地选自氢，低级烷基，标记基团，保护基，氨基磷酸酯或磷酸酯酯; R 1可以在每个单体单元中相同或不同，并且在至少一个非核苷酸单体单元中，R 1独立地选自（i）与氢键供体官能团连接的非连接二醇; （ii）选自醚的氢键受体; （iii）连接到疏水官能团的非连位二醇或连接到脂族或脂环族疏水官能团的连位二醇（iv）连接到环取代的阴离子官能团上的二醇和（v）连接到非邻位的阳离子部分 或脂环族二醇，其中任何一种可进一步包括可检测标记，并且n为至少两个。 优选的R1部分包括脂环族二醇和多环二醇的缩合产物; 也是其非核苷酸单体，以及低聚物作为选择性靶结合化合物的用途。

公开(公告)号：US5919965A

公开(公告)日：1999-07-06

申请号：US374040

申请日：1995-01-18

申请人： Robert Gerard Gentles ,  Alan F. Cook ,  Morris Jonathan Rudolph ,  Reza Fathi

发明人： Robert Gerard Gentles ,  Alan F. Cook ,  Morris Jonathan Rudolph ,  Reza Fathi

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 ,  C07F9/06 ,  C07D241/04

CPC分类号： C07F9/6578 ,  C07B59/004 ,  C07F9/1411 ,  C07F9/1414 ,  C07F9/143 ,  C07F9/144 ,  C07F9/145 ,  C07F9/2408 ,  C07F9/2416 ,  C07F9/242 ,  C07F9/5728 ,  C07F9/582 ,  C07F9/588 ,  C07F9/65062 ,  C07F9/650958 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/6561 ,  C07F9/65616 ,  C40B40/00 ,  Y02P20/55

摘要： A phosphorus ester oligomer having the structure: ##STR1## 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; B.sub.1 and B.sub.2 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; R.sub.1 can be the same or different in each monomeric unit, and in at least one of the non-nucleotide monomeric units, R.sub.1 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 R.sub.1 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.

摘要翻译： 具有以下结构的磷酯低聚物：其中A可以在每个单体单元中相同或不同，并且各自独立地选自氧，硫，低级烷基，烷基或芳基取代的氨基和氨基烷基; B1和B2可以相同或不同，各自独立地选自氢，低级烷基，标记基团，保护基，氨基磷酸酯或磷酸酯酯; R 1可以在每个单体单元中相同或不同，并且在至少一个非核苷酸单体单元中，R 1独立地选自以下组中的缩合产物：（i）连接于氢的非连位二醇 债券供体功能; （ii）选自醚，嘌呤或嘧啶取代的1,2-二醇或二取代杂环的氢键受体; （iii）连接到疏水官能团的非连位二醇或连接到脂族或脂环族疏水官能团的连位二醇（iv）连接到环取代的阴离子官能团上的二醇和（v）连接到非邻位的阳离子部分 或脂环族二醇，其中任何一种可以进一步包括可检测标记，并且n是至少一个。 优选的R1部分包括杂环二醇，脂环族二醇和多环二醇的缩合产物。 还有其非核苷酸单体，低聚物的组合文库混合物以及低聚物作为选择性靶结合化合物的用途。