公开(公告)号：US20140066612A1

公开(公告)日：2014-03-06

申请号：US13964036

申请日：2013-08-09

Applicant: LIFE TECHNOLOGIES CORPORATION

Inventor： Gulilat GEBEYEHU ,  Richard Pires

IPC: C12Q1/68

CPC classification number: C07H21/00 ,  C07B2200/11 ,  C12Q1/68

Abstract: The invention relates to a process for deblocking substantially a blocked, detectably labeled oligonucleotide by contacting the blocked detectably labeled oligonucleotide with an effective amount of a nucleophilic amino compound under conditions that result in substantial deblocking of the oligonucleotide, thereby giving the substantially deblocked oligonucleotide.

Abstract translation: 本发明涉及一种通过使阻断的可检测标记的寡核苷酸与有效量的亲核性氨基化合物在导致寡核苷酸的实际解锁的条件下接触来封闭基本上封闭的可检测标记的寡核苷酸的方法，从而得到基本上解锁的寡核苷酸。

公开(公告)号：US20160024138A1

公开(公告)日：2016-01-28

申请号：US14748930

申请日：2015-06-24

Applicant: LIFE TECHNOLOGIES CORPORATION

Inventor： Gulilat GEBEYEHU ,  Richard Pires

IPC: C07H21/00

CPC classification number: C07H21/00 ,  C07B2200/11 ,  C12Q1/68

Abstract: The invention relates to a process for deblocking substantially a blocked, detectably labeled oligonucleotide by contacting the blocked detectably labeled oligonucleotide with an effective amount of a nucleophilic amino compound under conditions that result in substantial deblocking of the oligonucleotide, thereby giving the substantially deblocked oligonucleotide.

Abstract translation: 本发明涉及一种通过使阻断的可检测标记的寡核苷酸与有效量的亲核性氨基化合物在导致寡核苷酸的实际解锁的条件下接触来封闭基本上封闭的可检测标记的寡核苷酸的方法，从而得到基本上解锁的寡核苷酸。

公开(公告)号：US20150190522A1

公开(公告)日：2015-07-09

申请号：US14336887

申请日：2014-07-21

Applicant: LIFE TECHNOLOGIES CORPORATION

Inventor： Yongliang CHU ,  Malek MASOUD ,  Gulilat GEBEYEHU

IPC: A61K47/48 ,  A61K38/28 ,  A61K38/40 ,  A61K9/16

CPC classification number: A61K47/48046 ,  A61K9/16 ,  A61K31/14 ,  A61K38/28 ,  A61K38/40 ,  A61K47/543 ,  C07C211/21 ,  C07C211/63 ,  C07C211/64 ,  C07C229/26 ,  C07D209/48 ,  C07D241/12 ,  C12N15/88 ,  Y10S435/81

Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i—Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L′-X2—Z or —Z; R1 R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and wherein at least one of R1, R3, R4 and R6 is a straight chain or branched, cyclic, alkyl, alkenyl, alkynyl or aryl group; and anyone of R1, R3, R4 and/or R6 may optionally be covalently linked with each other, with Y or with L when L is C or CH to form a cyclic moiety; Z is selected from the group consisting of amine, spermiyl, carboxyspermiyl, guanidyl, spermidinyl, putricinyl, diaminoalkyl, pyridyl, piperidinyl, pyrrolidinyl, polyamine, amino acid, peptide, and protein; X1 and X2, independently of one another, are selected from the group consisting of NH, O, S, alkylene, and arylene; L′ is selected from the group consisting of alkylene, alkenylene, alkynylene, arylene, alkylene ether, and polyether; D is Q or a bond; A1 and A2, independently of one another, are selected from the group consisting of CH2O, CH2S, CH2NH, C(O), C(NH), C(S) and (CH2)t; X is a physiologically acceptable anion; m, n, r, s, u, v, w and y are 0 or 1, with the proviso that when both m and n are 0 at least one of r, s, u and y is other than 0; i, j, k, l, p and are integers from 0 to about 100; q is an integer from 1 to about 1000; and a is the number of positive charge divided by the valence of the anion.