The present inventions provides drug-drug conjugates, drug-porphyrin conjugates, nanoparticles of the conjugates, as well as modified nanoparticles having PEGylated exteriors or encapsulated by red blood cell vesicles. The conjugates, nanoparticles and nanocarriers are useful for treating cancers and other diseases, as well as for imaging diseased tissue or organs.

The present invention relates to a nanoparticle comprising a drug dimer and a use thereof. The nanoparticle comprising a drug dimer of the present invention can increase the drug content and improve the dispersibility of the drug. In addition, the nanoparticle has increased targeting efficiency. Therefore, an effective pharmacological effect can be obtained by using a drug in a less amount, and thus the nanoparticle has excellent commercial applicability.

The disclosure provides a method for preparing drug toxin PNU-159682 (morpholinyl anthracycline derivative) for antibody-conjugated drugs and intermediates involved in the preparation method. The preparation method of the present disclosure improves the stability, practicability and scalability of the process by introducing protecting groups and changing to reagents that are capable to amplify; the preparation method of the present disclosure minimizes the risk and operational difficulty during scale-up production; production and operation is simple and convenient.

Doxorubicin derivatives for targeted activation by Legumain, its preparation method and use. The doxorubicin derivatives are obtained by condensation between the amino group of compound A and the carboxyl group of compound B and have the following structure: ##STR00001##
compounds A and B have the following structures, respectively: ##STR00002##
wherein R.sub.3 in compound B is Leu or absent; R.sub.4 is any one amino acid selected from the group consisting of Ala and Thr; R.sub.5 is any one amino acid selected from the group consisting of Ala, Thr and Asn; R.sub.6 is ##STR00003##
wherein n=1-20; or ##STR00004##
wherein R.sub.7 is substituted or unsubstituted, linear or branched, saturated or unsaturated C1-C20 fatty hydrocarbon, or substituted or unsubstituted C6-C20 aromatic hydrocarbon. The doxorubicin derivatives of the present invention are specifically tumor-targeted and have a long in vivo metabolic half-life, as compared with doxorubicin. They exhibit an efficient and safe anti-tumor effect and could be used to prepare an anti-tumor drug.

Doxorubicin derivatives for targeted activation by Legumain, its preparation method and use. The doxorubicin derivatives are obtained by condensation between the amino group of compound A and the carboxyl group of compound B and have the following structure: ##STR00001##
compounds A and B have the following structures, respectively: ##STR00002##
wherein R.sub.3 in compound B is Leu or absent; R.sub.4 is any one amino acid selected from the group consisting of Ala and Thr; R.sub.5 is any one amino acid selected from the group consisting of Ala, Thr and Asn; R.sub.6 is ##STR00003##
wherein n=1-20; or ##STR00004##
wherein R.sub.7 is substituted or unsubstituted, linear or branched, saturated or unsaturated C1-C20 fatty hydrocarbon, or substituted or unsubstituted C6-C20 aromatic hydrocarbon. The doxorubicin derivatives of the present invention are specifically tumor-targeted and have a long in vivo metabolic half-life, as compared with doxorubicin. They exhibit an efficient and safe anti-tumor effect and could be used to prepare an anti-tumor drug.

The present invention provides engineered glycosyltransferase (GT) enzymes, polypeptides having GT activity, and polynucleotides encoding these enzymes, as well as vectors and host cells comprising these polynucleotides and polypeptides. The present invention provides engineered sucrose synthase (SuS) enzymes, polypeptides having SuS activity, and polynucleotides encoding these enzymes, as well as vectors and host cells comprising these polynucleotides and polypeptides. The present invention also provides compositions comprising the GT enzymes and methods of using the engineered GT enzymes to make products with β-glucose linkages. The present invention further provides compositions and methods for the production of rebaudiosides (e.g., rebaudioside M, rebaudioside A, rebaudioside I, and rebaudioside D). The present invention also provides compositions comprising the SuS enzymes and methods of using them. Methods for producing GT and SuS enzymes are also provided.

The present invention provides engineered glycosyltransferase (GT) enzymes, polypeptides having GT activity, and polynucleotides encoding these enzymes, as well as vectors and host cells comprising these polynucleotides and polypeptides. The present invention provides engineered sucrose synthase (SuS) enzymes, polypeptides having SuS activity, and polynucleotides encoding these enzymes, as well as vectors and host cells comprising these polynucleotides and polypeptides. The present invention also provides compositions comprising the GT enzymes and methods of using the engineered GT enzymes to make products with β-glucose linkages. The present invention further provides compositions and methods for the production of rebaudiosides (e.g., rebaudioside M, rebaudioside A, rebaudioside I, and rebaudioside D). The present invention also provides compositions comprising the SuS enzymes and methods of using them. Methods for producing GT and SuS enzymes are also provided.

A non-aqueous electrolytic solution includes a phosphoric acid diester salt, which can suppress deterioration of charge-discharge characteristics of a power storage element, and can suppress the rise in internal resistance after storage at high temperature. The phosphoric acid diester salt is represented by the following chemical formula (1): ##STR00001##
in which M.sup.n+ represents a hydrogen ion, an alkali metal ion, an alkali earth metal ion, an aluminum ion, a transition metal ion, or an onium ion, R.sup.1 and R.sup.2 are different from each other and represent a hydrocarbon group having 1 to 10 carbon atoms, or a hydrocarbon group having 1 to 10 carbon atoms and having at least one of a halogen atom, a heteroatom, and an unsaturated bond, and n represents a valence.

A non-aqueous electrolytic solution includes a phosphoric acid diester salt, which can suppress deterioration of charge-discharge characteristics of a power storage element, and can suppress the rise in internal resistance after storage at high temperature. The phosphoric acid diester salt is represented by the following chemical formula (1): ##STR00001##
in which M.sup.n+ represents a hydrogen ion, an alkali metal ion, an alkali earth metal ion, an aluminum ion, a transition metal ion, or an onium ion, R.sup.1 and R.sup.2 are different from each other and represent a hydrocarbon group having 1 to 10 carbon atoms, or a hydrocarbon group having 1 to 10 carbon atoms and having at least one of a halogen atom, a heteroatom, and an unsaturated bond, and n represents a valence.

The present disclosure relates to processes for preparing functionalized cyclooctenes and the synthetic intermediates prepared thereby.