C07H13/12

Mebendazole prodrugs with enhanced solubility and oral bioavailability

Prodrugs of mebendazole and methods for their use in treating a disease, disorder, or disorder, including cancer, are disclosed.

Mebendazole prodrugs with enhanced solubility and oral bioavailability

Prodrugs of mebendazole and methods for their use in treating a disease, disorder, or disorder, including cancer, are disclosed.

Crystalline form of Remdesivir

The present invention provides a novel crystalline form of remdesivir, remdesivir Form APO-I, including remdesivir and dimethyl sulfoxide, compositions and processes for the preparation thereof, the use of this crystalline form in the treatment of a viral infection, and methods of treating viral infections using the same, and in particular, a viral infection caused by Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2).

Crystalline form of Remdesivir

The present invention provides a novel crystalline form of remdesivir, remdesivir Form APO-I, including remdesivir and dimethyl sulfoxide, compositions and processes for the preparation thereof, the use of this crystalline form in the treatment of a viral infection, and methods of treating viral infections using the same, and in particular, a viral infection caused by Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2).

Large scale preparation of pseudo-trisaccharide aminoglycosides and of intermediates thereof

Synthetic pathways for preparing pseudo-trisaccharide aminoglycoside compounds represented by Formula I or Ia as defined in the specification and donor and acceptor compounds useful for preparing such compounds are provided. A process of stereoselectively preparing compounds represented by Formula III as defined in the specification, while avoiding chromatographic separation of stereoisomers are also provided. Compounds prepared by the described processes and uses thereof are also provided.

Liposomes useful for drug delivery

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

NOVEL BENZIMIDAZOLE DERIVATIVES, PREPARATION METHOD THEREOF AND USE THEREOF AS ANTI-CANCER AGENT COMPRISING THE SAME
20210300959 · 2021-09-30 ·

According to the present invention, there are provided a benzimidazole carbamate-sugar compound conjugate compound represented by the following Chemical Formula 1, a preparation method thereof, and a use thereof as an anti-cancer agent:

##STR00001## Wherein, R.sub.1, R.sub.2, R.sub.3 and X are as defined in the specification and claims.

Triazole antimicrobial derivative, pharmaceutical composition and use thereof

The present disclosure provides a triazole antibacterial derivative and a pharmaceutical composition thereof and a use thereof and in particular relates to a compound represented by the following formula (I), and a racemate, a stereoisomer, a tautomer, an oxynitride or a pharmaceutically acceptable salt thereof: ##STR00001## The compound of the present disclosure has a desirable water solubility and can be formulated into an injection for use without adding a cosolvent having a potential safety risk (such as hydroxypropyl-β-cyclodextrin, sulfobutylether-β-cyclodextrin, and the like), facilitating drug administration for patients, and greatly improving clinical safety. The drug can be used even by patients with moderate or severe renal impairment, thereby expanding the application scope of the drug.

Liposomes Useful for Drug Delivery

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

New potent sialyltransferase inhibitors

The present invention relates to a new class of sialyltransferase inhibitors. The class features a carbamate or similar moiety on the amine of a neuraminic acid derivative. Such inhibitors are suitable for use as a medicament, for example for treating, preventing, or delaying bacterial infection, viral infection, cancer, a disorder of sialic acid metabolism, or an autoimmune disease.