Patent classifications
C07H15/18
BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF HYPERCHOLEMIA AND CHOLESTATIC LIVER DISEASE
Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
Functionalized n-acetylgalactosamine analogs
Embodiments of the present application relate to functionalized N-acetylgalactosamine-analogs, methods of making, and uses of the same. In particular, mono or trivalent N-acetylgalactosamine analogs may be prepared by utilizing a wide variety of linkers containing functional groups. These functionalized N-acetylgalactosamine-analogs may be used in the preparation of targeted delivery of oligonucleotide-based therapeutics.
COMPOSITIONS AND METHODS FOR ASCAROSIDE MODIFICATION OF MAMMALIAN MICROBIOTA
Described herein are composition of ascarosides, methods of using them, and the like for inhibiting bacterial population growth or for altering the relative ratio of sub-populations of first and second bacteria in a mixed population of bacteria. The invention is particularly useful, for example, for modifying a microbiome of a patient (e.g., for treatment of gut microbiome dysfunction).
TUCARESOL DERIVATIVES AND USES THEREOF
Disclosed herein are tucaresol derivative compound and composition containing the same. Also disclosed herein are methods of enhancing immune response in a subject by administering the tucaresol derivative compound or by co-administering the tucaresol derivative compound and one or more additional agents. Also disclosed herein are use of the tucaresol derivative compound and composition containing the same in the manufacture of a medicament for treating cancer or enhancing immune response in a subject.
TUCARESOL DERIVATIVES AND USES THEREOF
Disclosed herein are tucaresol derivative compound and composition containing the same. Also disclosed herein are methods of enhancing immune response in a subject by administering the tucaresol derivative compound or by co-administering the tucaresol derivative compound and one or more additional agents. Also disclosed herein are use of the tucaresol derivative compound and composition containing the same in the manufacture of a medicament for treating cancer or enhancing immune response in a subject.
Brartemicin analogues
The invention relates to brartemicin analogues of Formula (IV) and their uses. These compounds are potent Mincle agonists and Th1-stimulating vaccine adjuvants. ##STR00001##
Brartemicin analogues
The invention relates to brartemicin analogues of Formula (IV) and their uses. These compounds are potent Mincle agonists and Th1-stimulating vaccine adjuvants. ##STR00001##
SYNTHETIC AGONISTS OF TLR4 RECEPTOR
The present invention relates to new synthetic molecules with agonist activity of human Toll-like Receptor 4 (TLR4), compositions comprising them and uses thereof for the treatment of diseases in which it is useful to induce or increase an immune response. The compounds have general formula (1), wherein R.sub.1 is a saturated C.sub.8-C.sub.16 aliphatic chain having a ═0 on C.sub.1, said chain being free from —OH substituents on C.sub.3, wherein R.sub.2 is a saturated C.sub.8-C.sub.16 aliphatic chain having a ═O on C.sub.1, said chain being free from —OH substituents on C.sub.3, wherein R.sub.3 is a saturated C.sub.8-C.sub.16 aliphatic chain having a ═O on C.sub.1, said chain being free from —OH substituents on C.sub.3; wherein R.sub.4 is a hydrogen atom (H) or a phosphate group (PO.sub.4.sup.2−).
##STR00001##
Lactuloside compounds and preparation and use thereof
The present disclosure relates to the field of pharmaceutical chemistry, and particularly to a compound represented by Formula (I), a preparation method and medical use thereof. In the compound represented by Formula (I), a lactulosyl group is connected to a heteroatom of genin (G) via a glycosidic bond, wherein the genin (G) is a group formed by removing one hydrogen atom from a heteroatom of an active pharmaceutical molecule, and “” indicates that the lactulosyl group is connected to the heteroatom of the genin (G) via an α-glycosidic bond or a β-glycosidic bond. Pharmacokinetic experiments prove that the lactuloside compound according to the present disclosure can pass through the gastrointestinal tract of a mammal without being absorbed significantly by the gastrointestinal tract and hydrolyzed significantly by endogenous enzymes of a mammal host. Therefore, the lactuloside compound can arrive at the colon site of the mammal, and release an active drug in the colon under the action of colon flora. The lactuloside compound has a function of colon-localized drug release, and can be used for preventing or treating an intestinal disease. ##STR00001##
FUNCTIONALIZED N-ACETYLGALACTOSAMINE ANALOGS
Embodiments of the present application relate to functionalized N-acetylgalactosamine-analogs, methods of making, and uses of the same. In particular, mono or trivalent N-acetylgalactosamine analogs may be prepared by utilizing a wide variety of linkers containing functional groups. These functionalized N-acetylgalactosamine-analogs may be used in the preparation of targeted delivery of oligonucleotide-based therapeutics.