13636results about How to "Good water solubility" patented technology

Activated polymeric bicine derivatives such as,as well as conjugates made therewith are disclosed. Methods of making and using the bicine derivatives are also disclosed.

PEG and related polymer derivatives having weak, hydrolytically unstable linkages near the reactive end of the polymer are provided for conjugation to drugs, including proteins, enzymes, small molecules, and others. These derivatives provide a sufficient circulation period for a drug-PEG conjugate, followed by hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that demonstrate reduced activity when permanently coupled to PEG maintain a therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG derivatives of the invention can be used to impart improved water solubility, increased size, a slower rate of kidney clearance, and reduced immunogenicity to a conjugate formed by attachment thereto. Controlled hydrolytic release of the bound molecule into an aqueous environment can then enhance the drug's delivery profile by providing a delivery system which employs such polymers and utilizes the teachings provided herein.

The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Calcium-strontium-hydroxyphosphate (strontium-apatite-) cement preparations are described, comprising a powder mixture, which contains molar quantities of the components calcium (Ca), strontium (Sr) and phosphate (P) in the mixture in the ranges 1.00<Ca / P≦1.50 and 0<Sr / P<1.5, together with an alkali salt or an ammonium salt of phosphoric acid, and with water and / or an aqueous solution. The powder mixture particularly contains, as the Ca-component, Ca3(PO4)2 (TCP), and as the Sr-component SrHPO4 and / or Sr3(PO4)2 and optionally additional SrCO3. As the aqueous mixing solution for the formation of the strontium-apatite cement, an aqueous solution of an alkali salt or an ammonium salt of the phosphoric acid is suitable.

Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.

The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Modified human interferon polypeptides and uses thereof are provided.

The present invention discloses cell penetrating peptides and conjugates of a cell penetrating peptide and a cargo molecule.

Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.

The invention provides a functional oil microencapsulation and a manufacturing method thereof and relates to a microencapsulation, and the functional oil microencapsulation has the advantages of high stability and immobilized proteinaceous pellicle. The oil microencapsulation is prepared from the following raw materials: functional oil, plant oil, an antioxidant, aqueous-phase main-wall materials, aqueous-phase auxiliary-wall materials, bio-enzyme protein and water. The plant oil serving as a carrier is mixed with the functional oil, then the antioxidant is added, and then the materials are heated and dissolved in water bath, thus obtaining an oil-phase core material solution; the aqueous-phase main-wall materials and the aqueous-phase auxiliary-wall materials are added into deionized water, and then the materials are heated and dissolved in water bath, thus obtaining an aqueous-phase wall material solution; the oil-phase core material solution is added in the aqueous-phase wall material solution, the mixture is sheared and emulsified by a shearing machine, and then is homogenized by a homogenizer, thus obtaining a nanometer-level solution with uniform oil drop diameter; and bio-enzyme is added into the nanometer-level solution, the mixture is placed in hot-water bath for heating and stirring reaction, temperature is raised after the reaction so as to enable the bio-enzyme to be inactivated, and drying is carried out, thus obtaining the functional oil microencapsulation.

The invention discloses a high-efficiency multielement compound foliage selenium fertilizer which aims to increase selenium artificially. The high-efficiency multielement compound foliage selenium fertilizer comprises the following components: macroelements, medium elements, microelements, chelator, selenium, rare-earth elements, active organic substances, growth regulator and surfactant. The high-efficiency multielement compound foliage selenium fertilizer is especially suitable for producing selenium-rich tea, selenium-rich rice, selenium-rich corn and other selenium-rich agricultural products in low-selenium or selenium-deficient regions. The invention has the advantages of favorable raw material compatibility, scientific proportion, scientific technique and diversified and compounded nutrient elements, and can effectively solve the nutrient deficiency symptom of the crop, thereby achieving the goal of sufficiently supplementing insufficient soil nutrients.

Modified human plasma polypeptides or Fc and uses thereof are provided.

The present invention aims to provide a supporting material for supporting the shape of a photofabrication model on photofabrication in ink-jet three dimensional printing method in which the photocured product is excellent in solubility in water and is easy to remove after photofabrication, and the like. A modeling material for forming a photofabrication model in ink-jet three dimensional printing method containing a curable resin component with a weighted average of SP value of 9.0 to 10.3; and a supporting material for supporting the shape of a photofabrication model on photofabrication in ink-jet three dimensional printing method containing a water-soluble monofunctional ethylenically unsaturated monomer (F), polyoxypropylene glycol with a number average molecular weight of 100 to 5,000 and / or water (G), and a photopolymerization initiator (D).

The present invention provides compounds that inhibit Factor XIa and methods of preventing or treating undesired thrombosis by administering a compound of the invention to a mammal. The invention also provides three-dimensional structures of Factor XIa and methods for designing or selecting additional Factor XIa inhibitors using these structures.