C07H15/26

Method for preparation of derivatives of gram-positive bacteria surface capsular polysaccharide
11603416 · 2023-03-14 · ·

The present disclosure discloses a method for preparation of derivatives of gram-positive bacteria surface capsular polysaccharide, and belongs to the field of carbohydrate chemistry. The present disclosure takes glucose as a glycosyl donor to obtain a target β-glucosidic bond, then successfully synthesizes a disaccharide building block through a method of redox of a glucose C-2 site, and then takes the disaccharide building block as a repeat unit to synthesize a target oligosaccharide structure such as a derivative [.fwdarw.3)-α-D-Manp-(1.fwdarw.4)-β-D-Rhap-(1.fwdarw.].sub.5-Linker of gram-positive bacteria cell wall capsular polysaccharide. A reduction end of decose is linked with a linker to be linked with a protein to make glycoconjugates for immunological studies. The method provided by the present disclosure is simple, time-saving, labor-saving and low-cost, and the resultant derivatives of the gram-positive bacteria surface capsular polysaccharide may be used for development and preparation of medicine related to autism.

PHYTOSPHINGOSINE DERIVATIVES AS ADJUVANTS IN IMMUNE STIMULATION

Phytosphingosine derivatives suitable as adjuvants in immune stimulation, pharmaceutical compositions comprising such compounds and the medical use of the compounds and/or compositions in therapeutic or prophylactic methods of immune stimulation in a subject, and for use in the treatment of a disease, for which stimulation of an immune response in a subject produces a therapeutic benefit. The phytosphingosine derivative may also be used as adjuvants in vaccinating a subject. The phytosphingosine derivative may also be used in stimulating antibody production, stimulating an immune response against infection, stimulating an immune response against a cancer, or preventing and/or treating septic shock. Methods for the manufacture of the derivatives comprising an Ugi-4-component reaction (Ugi-4CR) is also disclosed.

Mannose derivatives for treating bacterial infections

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: ##STR00001## The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

Mannose derivatives for treating bacterial infections

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: ##STR00001## The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

Method for improving the oral bioavailability of a drug

The invention is in the field of medical sciences. It provides new pharmaceutical methods and preparations. In particular, the invention relates to a method for increasing the oral bioavailability of drugs. The invention also provides new compositions comprising a drug covalently attached to a saccharide as in formula (I) below. More in particular, the invention relates to a method for increasing the oral bioavailability of a drug by covalently attaching a sugar-linked, N-substituted or unsubstituted carbamoylalkylidene moiety to a hydroxyl or thiol group of a drug, wherein the substituents are as defined in the claims. ##STR00001##

Method for improving the oral bioavailability of a drug

The invention is in the field of medical sciences. It provides new pharmaceutical methods and preparations. In particular, the invention relates to a method for increasing the oral bioavailability of drugs. The invention also provides new compositions comprising a drug covalently attached to a saccharide as in formula (I) below. More in particular, the invention relates to a method for increasing the oral bioavailability of a drug by covalently attaching a sugar-linked, N-substituted or unsubstituted carbamoylalkylidene moiety to a hydroxyl or thiol group of a drug, wherein the substituents are as defined in the claims. ##STR00001##

VACCINE AGAINST KLEBSIELLA PNEUMONIAE

The present invention relates to a synthetic saccharide of general formula (I) that is related to Klebsiella pneumoniae serotype O1, O2, O2ac, and O8 O-polysaccharide and carbapenem-resistant Klebsiella pneumoniae ST258 O-polysaccharide and conjugate thereof. Said synthetic saccharide, said conjugate and pharmaceutical composition containing said synthetic saccharide or said conjugate are useful for prevention and/or treatment of diseases associated with Klebsiella pneumoniae. Furthermore, the synthetic saccharide of general formula (I) is useful as marker in immunological assays for detection of antibodies against Klebsiella pneumoniae bacteria.

VACCINE AGAINST KLEBSIELLA PNEUMONIAE

The present invention relates to a synthetic saccharide of general formula (I) that is related to Klebsiella pneumoniae serotype O1, O2, O2ac, and O8 O-polysaccharide and carbapenem-resistant Klebsiella pneumoniae ST258 O-polysaccharide and conjugate thereof. Said synthetic saccharide, said conjugate and pharmaceutical composition containing said synthetic saccharide or said conjugate are useful for prevention and/or treatment of diseases associated with Klebsiella pneumoniae. Furthermore, the synthetic saccharide of general formula (I) is useful as marker in immunological assays for detection of antibodies against Klebsiella pneumoniae bacteria.

Ribose Cationic Lipids
20220323355 · 2022-10-13 ·

Disclosed are cationic lipids which are compounds of Formula (I′). Cationic lipids 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##

GPR119 AGONISTS
20230061736 · 2023-03-02 ·

This disclosure is directed, at least in part, to GPR119 agonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the GPR119 agonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.