4 results about "Morpholino Oligos" patented technology

Described herein are methods and compositions for treating solid or liquid B-cell malignancies using a two-component platform based on morpholino oligonucleotide-linked conjugates to target B-cells and effector cells. The methods described herein may involve two distinct dosing approaches tailored to the type of B-cell malignancy being treated. In some embodiments, solid B-cell tumors are treated using a premixed assembly dosing regimen. In some embodiments, liquid B-cell tumors are treated using a consecutive dosing regimen.

The invention relates to IGF1-BP coupled lipid nanoparticles as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. In order to solve the problem that an endometrial nano-carrier and a corresponding targeting drug are still lacked in the existing preeclampsia prevention and treatment, the invention provides a preparation method of IGF1-BP coupled lipid nanoparticles, which comprises the following steps: respectively preparing an organic phase solution and a water phase solution, assembling the lipid nanoparticles by using the organic phase solution and the water phase solution, and preparing the IGF1-BP coupled lipid nanoparticles. And connecting IGF1-BP to the surface of the lipid nanoparticle through a coupling reaction by virtue of an EDC / NHS technology, so as to obtain the IGF1-BP coupled lipid nanoparticle. According to the IGF1-BP coupled lipid nanoparticles provided by the invention, morpholino oligonucleotide for reducing endometrial APOD expression is delivered to endometrial tissues in a targeted manner, so that not only can the symptoms of preeclampsia be relieved during pregnancy, but also prophylactic treatment can be performed on lying-in women with high risk of preeclampsia during prepregnancy.

The invention relates to a continuous flow preparation method and a continuous flow preparation device of morpholino oligonucleotide, and belongs to the technical field of morpholino oligonucleotide preparation. The invention relates to a continuous flow preparation method of morpholino oligonucleotide. A continuous flow preparation device comprises an automatic synthesizer with a synthesis column; the continuous flow preparation method comprises the following steps: (1) loading morpholino phosphoramidite protected by a protecting group on a solid-phase carrier, filling the solid-phase carrier into a synthetic column, pumping 3-7cv of a deprotection agent into the synthetic column at a first flow rate of 150-240cm / h, and pumping 7-10cv of the deprotection agent into the synthetic column at a second flow rate of 120-150cm / h; the difference between the first flow velocity and the second flow velocity is not less than 30cm / h; (2) pumping a morpholino phosphoramidite monomer reagent and an activating reagent into the synthetic column, heating the synthetic column and the post-column of the synthetic column, keeping the temperature at 30-60 DEG C, and circularly carrying out a coupling reaction; (3) pumping a capping reagent for capping reaction to form a basic group; and (4) circulating the steps (1)-(3) for each basic group to generate the morpholino oligonucleotide. The coupling efficiency is effectively improved, and the purity of the product after ammonolysis is improved.

The application provides a chiral morpholino phosphorus oxychloride monomer and a preparation method and application thereof, and the structure of the monomer is shown in formula I or II: wherein X represents an oxygen atom or a sulfur atom; B represents a base; R 1 is selected from an optionally substituted secondary substituted amine group, an optionally substituted alkoxy group, an optionally substituted phenoxy group, a guanidino group, and a linked nitrogen forming an optionally substituted heterocyclic ring; R 2 is selected from an optionally substituted or unsubstituted tertiary alkyl group, an optionally substituted or unsubstituted benzyl group, an optionally substituted sulfonyl group, and an optionally substituted acyl group. The application can obtain the chiral morpholino phosphorus oxychloride monomer in a stereochemically pure or substantially pure form by using an efficient catalytic asymmetric desymmetrization strategy. And the corresponding morpholino oligonucleotide chain can be synthesized based on the monomer, thereby providing a powerful synthesis platform for developing a new generation of morpholino oligonucleotide drugs with precise stereostructure and optimized performance.