The present invention provides a method for producing a hetero-type monodisperse polyethylene glycol, which includes a step (A) of carrying out a nucleophilic substitution reaction between a compound of the formula (2) and a compound of the formula (3) so as to satisfy the requirement of the expression (F1) to obtain a compound of the formula (4), a step (B) of carrying out the Michaels addition reaction of a compound of the formula (5) to the compound of the formula (4) at a temperature condition of 10° C. or lower to obtain a compound of the formula (6), a step (C) of detritylating or debenzylating the compound of the formula (6) to obtain a reaction product containing a compound of the formula (7), a step (D) of purifying the compound of formula (7) from the reaction product, a step (E) of reacting the compound of the formula (7) with phthalimide and performing dephthalimidation to obtain a compound of the formula (8), and a step (F) of subjecting the compound of formula (8) to an acid hydrolysis treatment to obtain a compound represented by the formula (1).

The present disclosure provides conjugates comprising a Factor VIII moiety covalently attached via an oxime-containing linkage to a water-soluble polymer, such as for example, a polyethylene glycol polymer. Methods for preparing and for administering such conjugates, are also provided, as are water-soluble polymer oxyamine reagents useful for preparing the subject conjugates, among other things.

Disclosed herein are glycidol-based polymers, nanoparticles, and methods related thereto useful for drug delivery. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The present disclosure generally relates to a multifunctional additive obtained from the reaction of: (a) an intermediate obtained from the reaction of maleic anhydride and a polyoxyalkylene monoamine; and (b) an amine compound comprising a primary amine group and/or a secondary amine group and its use in a variety of applications, including, but not limited to: as a corrosion inhibitor or friction modifier in aqueous and non-aqueous systems; in fuel deposit control agents; as a dispersant in pigment, asphalt and cement compositions; and as a detergent.

The present invention provides a raw material for bulk drugs and a pharmaceutical additive which provide excellent formulation stability and excellent over-time stability of drug efficacy when used to modify a bulk drug, a polypeptide, a bioactive protein, an enzyme, and the like. The present invention relates to a raw material for bulk drugs or a pharmaceutical additive, containing: a polyether composition (A) represented by formula (1), wherein the polyether composition (A) has a unimodal molecular weight distribution, the polyether composition (A) has a ratio (Mw/Mn) of the weight average molecular weight (Mw) to the number average molecular weight (Mn) of 1.20 or less, and the polyether composition (A) contains a compound in which m is 1 in formula (1) in an amount of 90 wt % or more based on the weight of the polyether composition (A), in formula (1), OR.sup.1, R.sup.2O, R.sup.3O, and R.sup.4O are each independently a C2-C8 oxyalkylene group; when each of these moieties exists in the plural number, each OR.sup.1, each R.sup.2O, each R.sup.3O, and each R.sup.4O may be the same as or different from each other; these moieties may be bonded randomly or in block; a, b, c, and d are each independently an integer of 50 to 1200; X.sup.1 to X.sup.4 are each independently a hydrogen atom, a substituent represented by formula (2), or a substituent represented by formula (3); and m is an integer of 1 to 10.

##STR00001##

The compounds disclosed herein (e.g., compounds of Formula (I), (II), (III), and (IV)) comprise a lipid substructure comprising a hydrophobic moiety and a hydrophilic moiety; and two or more polymeric groups (e.g., two or more polyethylene glycol (PEG) groups). The compounds provided herein can be useful for delivery and expression of mRNA and encoded protein, e.g., as a component of liposomal delivery vehicle, and accordingly can be useful for treating various diseases, disorders and conditions, such as those associated with deficiency of one or more proteins.

##STR00001##

The compounds disclosed herein (e.g., compounds of Formula (I), (II), (III), and (IV)) comprise a lipid substructure comprising a hydrophobic moiety and a hydrophilic moiety; and two or more polymeric groups (e.g., two or more polyethylene glycol (PEG) groups). The compounds provided herein can be useful for delivery and expression of mRNA and encoded protein, e.g., as a component of liposomal delivery vehicle, and accordingly can be useful for treating various diseases, disorders and conditions, such as those associated with deficiency of one or more proteins.

##STR00001##

A stable dispersant and an application thereof in preparing copolymer polyols, the preparation method for the stable dispersant including the steps of 1) contacting a polyol with a dianhydride compound for reaction so as to prepare an adduct; 2) performing a ring-opening addition reaction on the adduct obtained in step 1) and an epoxy compound to prepare a stable dispersant; the dianhydride compound does not contain a double bond that may copolymerize with an olefinically unsaturated monomer, while the epoxy compound contains a double bond that may copolymerize with an olefinically unsaturated monomer, the polyol is a polyester polyol and/or a polyether polyol, preferably being a polyether polyol. The stable dispersant obtained by means of the described preparation method has a multi-active site anchoring function, and is applied to the synthesis of copolymer polyols to obtain copolymer polyols having relatively uniform particle size.

The present invention relates to an amphiphilic block copolymer represented by formula I, a preparation method thereof, and a nanomicelle drug delivery system formed from the copolymer and a poorly soluble drug. The amphiphilic block copolymer includes a hydrophilic chain segment, a hydrophobic chain segment, and a linker for linking the hydrophilic chain segment to the hydrophobic chain segment. The linker contains an unsaturated structure, which can enhance the interaction between the poorly soluble drug and the copolymer to improve the drug loading ability and stability of the nanomicelle. The invention also relates to a nanomicelle drug-loading system, a preparation method thereof, and the use of the nanomicelle drug-loading system for preparing medicines for treating tumors, inflammation, diabetes, central nervous system diseases, cardiovascular diseases, and psychological disorders. ##STR00001##

Disclosed herein are ketal compounds, oligomers, and polyketals that are obtained in both high purity and high yield. These ketals and polyketals are utilized for their ability to readily release small chemical molecules, preferably fragrance molecules. Also disclosed are the utility of ketals and polyketals as delivery vehicles for controlled release of fragrances over time and/or on demand.