C07H17/04

Furaneone glycoside compound, pharmaceutical composition thereof, preparation method therefor, and application thereof
11673909 · 2023-06-13 · ·

Disclosed are a furaneone glycoside compound, a pharmaceutical composition thereof, a preparation method therefor, and an application thereof. Specifically disclosed are a compound as represented by formula A-1, a pharmaceutically acceptable salt thereof or a crystal form thereof. Also disclosed is a pharmaceutical composition, which comprises the compound as represented by formula A-1, the pharmaceutically acceptable salt thereof, and a pharmaceutical adjuvant. Also disclosed is an application of the compound as represented by formula A-1, the pharmaceutically acceptable salt thereof, the crystal form thereof, or the pharmaceutical composition in the preparation of drugs. The drugs are drugs for treating inflammatory bowel diseases. The furaneone glycoside compound has a good effect of treating inflammatory bowel diseases, particularly ulcerative colitis. ##STR00001##

Furaneone glycoside compound, pharmaceutical composition thereof, preparation method therefor, and application thereof
11673909 · 2023-06-13 · ·

Disclosed are a furaneone glycoside compound, a pharmaceutical composition thereof, a preparation method therefor, and an application thereof. Specifically disclosed are a compound as represented by formula A-1, a pharmaceutically acceptable salt thereof or a crystal form thereof. Also disclosed is a pharmaceutical composition, which comprises the compound as represented by formula A-1, the pharmaceutically acceptable salt thereof, and a pharmaceutical adjuvant. Also disclosed is an application of the compound as represented by formula A-1, the pharmaceutically acceptable salt thereof, the crystal form thereof, or the pharmaceutical composition in the preparation of drugs. The drugs are drugs for treating inflammatory bowel diseases. The furaneone glycoside compound has a good effect of treating inflammatory bowel diseases, particularly ulcerative colitis. ##STR00001##

1,4,7,10-TETRAZACYCLODODECANE BASED AGENTS TO TARGET BACTERIA AND ITS USE

The present invention relates to new compounds comprising a siderophore moiety as well as a core structure able to chelate a metal ion. Optionally, the compounds may have additionally a moiety with a functional element including a marker molecule, a bioactive agent, an activity based probe suitable to monitor the aberrant expression or activity of proteins involved in the initiation and progression of bacterial infection, or a compound useful for bacterial inhibition. In a further aspect, the present invention provides a pharmaceutical composition containing said compound, for example, said pharmaceutical composition is an antibiotic. Additionally, the present invention relates to the use of said compounds in diagnostic methods, in particular, imaging methods including SPEC, PET or MRI. In an embodiment of the present invention, the compound is part of a theranostic composition having both, therapeutic as well as diagnostic activities.

1,4,7,10-TETRAZACYCLODODECANE BASED AGENTS TO TARGET BACTERIA AND ITS USE

The present invention relates to new compounds comprising a siderophore moiety as well as a core structure able to chelate a metal ion. Optionally, the compounds may have additionally a moiety with a functional element including a marker molecule, a bioactive agent, an activity based probe suitable to monitor the aberrant expression or activity of proteins involved in the initiation and progression of bacterial infection, or a compound useful for bacterial inhibition. In a further aspect, the present invention provides a pharmaceutical composition containing said compound, for example, said pharmaceutical composition is an antibiotic. Additionally, the present invention relates to the use of said compounds in diagnostic methods, in particular, imaging methods including SPEC, PET or MRI. In an embodiment of the present invention, the compound is part of a theranostic composition having both, therapeutic as well as diagnostic activities.

Compound isolated from Pseudolysimachion rotundum var. subintegrum, the composition comprising the same for treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease and the use thereof

A compound (3R,5S,5aS,6R,7S,8R,8aS)-8-chloro-8a-hydroxy-5-(2-hydroxy acetoxy) hexahydro-1H-3,6-methanocyclopenta[e][1,3]dioxepin-7-yl 3,4-dihydroxybenzoate (KS534), the isomer thereof, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease (COPD)

Selective glycosidase inhibitors and uses thereof

The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac. ##STR00001##

Selective glycosidase inhibitors and uses thereof

The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac. ##STR00001##

CANNABINOID GLYCOSIDES AND USES THEREOF

The present invention provides tetrahydrocannabinol glycoside and cannabidiol glycoside prodrugs and pharmaceutical compositions comprising these compounds, and their use for the site specific delivery of tetrahydrocannabinol or cannabidiol. Also provided are processes for the preparation of purified tetrahydrocannabinol glycoside and cannabidiol glycoside prodrugs.

HEPARANASE COMPOUNDS AND METHODS OF USE

The invention relates to compounds that interact with heparanase, uses in heparanase screening, uses in in vitro and in vivo imaging (e g , positron emission tomography (PET) and magnetic resonance imaging (MRI)), methods of synthesis, methods of modulating heparanase activity, and methods of treating disease and disorders associated with heparanase. The compounds of the invention are also useful in treating one or more diseases or disorders associated with the function of heparanase.

METABOLITES OF GLP1R AGONISTS

The present invention provides metabolites of Compound 1 or a compound of Formula I or III, including compositions and salts thereof, which are useful in the prevention and/or treatment of a disease or disorder such as T2DM, obesity, or NASH, as well as analytical methods related to the administration of Compound 1 or a compound of Formula I or III.