A61P3/04

N-[8-(2-HYDROXYBENZOYL)AMINO]POTASSIUM OCTANOATE CRYSTAL POLYMORPH, AND PREPARATION METHOD THEREFOR AND USE THEREOF

Disclosed in the present application is a crystal polymorph of potassium N-[8-(2-hydroxybenzoyl)amino]octanoate, wherein the crystal polymorph of potassium N-[8-(2-hydroxybenzoyl)amino]octanoate is crystal Form I, and the crystal Form I has at least an X-ray powder diffraction pattern with characteristic peaks represented by 2θ° of 7.83±0.2, 26.64±0.2 and 18.89±0.2. The crystal polymorph of potassium N-[8-(2-hydroxybenzoyl)amino]octanoate provided by the present application has four crystal forms, has high solubility and strong stability, can deliver drugs more effectively, increases the permeability of the delivered drugs in the gastrointestinal tract, and is beneficial to the preparation of oral preparations, such that preventive and/or therapeutic drugs can be better delivered into the body to achieve the effect of improving the bioavailability.

NOVEL COMPOUND USEFUL AS TOLL-LIKE RECEPTOR 7 ACTIVATION INHIBITOR

CB-7 exhibits a weak TLR7 inhibiting effect in normal mice. The present invention provides a novel compound with a stronger TLR7 inhibiting effect than CB-7, a pharmaceutically acceptable salt of said compound, or a prodrug of said compound or salt. The present invention also provides a drug for the prevention or treatment of diseases associated with the activation of TLR7, said drug including the aforementioned TLR7 activation inhibitor.

ACC INHIBITOR AND USE THEREOF

The present invention provides a compound suitable for use as an acetyl CoA carboxylase (ACC) inhibitor, specifically, a thienopyridine derivative, and use of the compound in the preparation of drugs for treating metabolic disorders, cancers or other proliferative disorders, and nonalcoholic steatohepatitis (NASH).

COMPOUND AS SHP2 INHIBITOR AND USE THEREOF

The present invention falls within the field of medical chemistry and relates to a class of compounds as SHP2 inhibitors and the use thereof. Specifically, the present invention provides a compound represented by formula (I), or an isomer, a pharmaceutically acceptable salt, a solvate, a crystal or a prodrug thereof, a preparation method therefor, a pharmaceutical composition comprising the compounds, and the use of the compounds or the composition for treating a disease mediated by SHP2.

AMORPHOUS FORM OF NITROGEN-CONTAINING TRICYCLIC COMPOUND AND USE THEREOF

An amorphous form of a nitrogen-containing tricyclic compound and a use thereof, a pharmaceutical composition containing the compound in the amorphous form, and the use of the compound in the amorphous form or the pharmaceutical composition in the preparation of a drug for preventing, treating or alleviating FXR-mediated diseases in a patient.

NOVEL FATTY ACID MODIFIED UROCORTIN 2 DERIVATIVES AND THE USES THEREOF

Ucn2 derivatives comprising a peptide and a substituent with high potency, high physical and high chemical stability, suitable for administration to humans, and their medical use in treatment and/or prevention of obesity and/or diabetes.

LONG-ACTING GDF15 FUSION PROTEIN AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

A fusion protein including a GDF15 variant having increased physiological activity and in vivo stability, and a pharmaceutical composition containing the same are disclosed. The GDF15 variant or long-acting GDF15 fusion protein is superior to conventional GDF15 variants in terms of in vitro efficacy, binding affinity for GDF15 receptors, and body weight loss effect. Therefore, a pharmaceutical composition containing, as an active ingredient, the GDF15 variant, the long-acting GDF15 fusion protein, or a dimer of the fusion protein, causes appetite suppression, and thus can be effectively used as a therapeutic agent for metabolic diseases or obesity. Furthermore, the pharmaceutical composition can be used in combination therapy or the like with chemical drugs and other therapeutic agents for metabolic diseases, and can be effectively used in combination therapy with conventional therapeutic agents for metabolic diseases or obesity.

THERAPEUTIC COMBINATIONS OF DRUGS AND METHODS OF USING THEM
20230002377 · 2023-01-05 ·

Provided are therapeutic combinations or formulations of drugs comprising triple monoamine reuptake inhibitors, melanin concentrating hormone receptor 1 (MCHRT) antagonists and diazoxide or its formulations and various combinations thereof, these in combination with other drugs or active agents. Provided are methods for the treatment of various conditions, including genetic confirmed syndromes, and diseases, using therapeutic combinations and formulations of drugs as provided herein. Provided are methods for administering triple monoamine reuptake inhibitors (TRIs), melanin concentrating hormone receptor 1 (MCHRT) antagonists and diazoxide or diazoxide or its formulations, whose dosages are determined using a method as provided herein including empirical methods for safe and predictable titration and to determine the initial therapeutic dose; model-based methods for safe and predictable titration and to determine the initial therapeutic dose and to determine the lowest therapeutic dose or to determine an optimal effective dose, including use of Bayesian pharmacometric models.

Double-acylated GLP-1 derivatives

The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1: HOOC—(CH.sub.2).sub.x—CO—*, and Chem. 2: HOOC—C.sub.6H.sub.4—O—(CH.sub.2).sub.y—CO—*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH.sub.2).sub.q—CH[(CH.sub.2).sub.w—NR.sub.1R.sub.2]—CO—*, which is connected at its CO—* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R.sub.1 and R.sub.2 independently represent *—H or *—CH.sub.3, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptide and linker intermediates. The derivatives are potent, stable, protracted, and suitable for oral administration.

Methods and compositions of bile acids and salts for reduction of fat
11517576 · 2022-12-06 · ·

The present invention relates to compositions and methods for treating fat deposit accumulation in a subject. The invention provides a non-surgical method for reducing fat deposits comprising administering an effective amount of a fat-lysing concentration of one or more of cholate and chenodeoxycholate in a pharmaceutically acceptable formulation to the subject in need thereof.