4125-93-3Relevant articles and documents
Preparation method of aspartic acid-1-tert-butyl ester derivative
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Paragraph 0060-0062, (2017/05/02)
The invention relates to a preparation method of an aspartic acid-1-tert-butyl ester derivative and the field of polypeptide synthesis. The preparation method includes following steps: (1), preparing aspartic acid into a mixture of aspartic acid-4-tert-butyl ester and aspartic acid-1-tert-butyl ester; (2), mixing the mixture with salt of transition metal M to obtain a mixture of M[Asp(OtBu)]x and M(Asp-OtBu)x, wherein x is greater than or equal to 1 and less than or equal to 2; (3), enabling the mixture to react with a protection agent, and allowing selective reaction to obtain the aspartic acid-1-tert-butyl ester derivative. The preparation method is few in step, low in cost, high in production time efficiency and easy for industrial mass production.
Conjugates for cancer therapy and diagnosis
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Page/Page column 13, (2010/11/26)
The present invention relates to conjugates of a drug and an amino acid or an amino acid derivative or analog, pharmaceutical compositions that include the conjugates and methods of use thereof. In particular, the present invention relates to conjugates o
Ophthalmic liposomes
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, (2008/06/13)
A liposome composition with enhanced retention on ocular surfaces, for use in ophthalmic drug delivery and dry eye treatment. The liposomes contain about 10-40 mole percent of an amine-derivatized lipid component in which a charged amine group is spaced from a lipid polar head region by a carbon-containing spacer arm at least 3 atoms in length. The liposomes preferably have a close packed lipid structure produced by inclusion of between 20-50 mole percent of cholesterol or an amine-derivatized cholesterol, and/or phospholipids with predominantly saturated acyl chain moieties. The liposomes may be suspended in an aqueous medium containing a high-viscosity polymer, formulated in paste form, or embedded in a polymer matrix, to enhance further the retention of liposomes on a corneal surface.