C07J71/0031

BUDESONIDE 21-PHOSPHATE SALTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

The present invention relates to salts of budesonide 21-phosphate with β2 adrenergic agonists, preferably with formoterol, pharmaceutical compositions containing the same and the use thereof in the treatment of respiratory inflammatory pathologies, obstructive pathologies and allergen-induced airway dysfunctions. The invention further relates to the process for preparing said salts.

Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof

The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

Use of steroidal glycosides, pharmaceutical formulations, use of <i>Furcraea foetida </i>plant extracts, process for producing <i>Furcraea foetida </i>plant extracts and method for treating skin disorders
11427611 · 2022-08-30 ·

The present invention relates, in its broadest aspects, to steroidal glycosides useful in the treatment of skin disorders. Particularly, the invention relates to the use of certain steroidal glucosides, per se, or in the form aglycona, derivatives of spirostanol, of its precursor furastanol, or mixtures thereof, used in the treatment of skin disorders, for instance, psoriasis. The invention further relates to formulations containing steroidal glycosides, the process of obtaining extract from the Furcraea foetida plant, and a method of treating skin disorders.

GLUCOCORTICOID RECEPTOR AGONISTS

The present invention provides a compound of Formula I:

##STR00001##

wherein R is hydrogen, —P(═O)(OH).sub.2,

##STR00002##

or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is useful for treating autoimmune and inflammatory diseases, such as atopic dermatitis, rheumatoid arthritis, systemic lupus erythematosus, lupus nephritis, and inflammatory bowel disease.

CARBOXY SUBSTITUTED GLUCOCORTICOID RECEPTOR AGONISTS
20220306681 · 2022-09-29 ·

The present invention provides a compound of Formula I:

##STR00001##

wherein R.sup.1 is H, halogen, C1-C3 alkyl, or C1-C3 alkoxy;
R.sup.2 is H or halogen; and
X is O, OCH.sub.2, or CH.sub.2, or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is useful for treating autoimmune and inflammatory diseases, such as atopic dermatitis, rheumatoid arthritis, and lupus nephritis.

Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof

The present invention further provides method of preparing nanocrystals or microcrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

COMPOUND AND PREPARATION METHOD AND APPLICATION THEREOF
20210388007 · 2021-12-16 · ·

The present disclosure relates to a compound and a preparation method and application thereof, the compound having a chemical structure formula of:

##STR00001##

wherein M in the formula is selected from a group consisting of CF.sub.3 or CF.sub.2H, and R.sub.1, R.sub.2, and R.sub.3 are each independently selected from a group consisting of aryl, heteroaryl, and alkyl. The compound provided by the present disclosure can be used as a trifluoroethanolation reagent or difluoroethanolation reagent as synthetic intermediates of many organic compounds, and some of the compounds have pharmaceutical activity. The preparation steps of such compounds are simplified, with mild synthesis conditions and wide applicability of substrates.

XYLOGLUCAN-CONTAINING PRODRUGS AND METHODS OF MANUFACTURE AND USE THEREOF

The present application provides compounds, compositions and methods to reduce, alleviate or treat various enteric diseases and disorders, such as inflammatory bowel disease. The compounds are xyloglucan-containing prodrugs, referred to herein as glyco-caged prodrugs, of formula (I) or (II), xyloglucan-β-O—R.sup.D (I), xyloglucan-β-O-L.sup.SI-R.sup.D (II).

Timosaponin compounds

Provided herein are timosaponin compounds of Formula I, II, III, I′, II′ and III′, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are uses of said timosaponin compounds for preparing medicament for the treatment of diseases associated with beta-amyloid in hosts or subjects in need thereof.

Steroids and protein-conjugates thereof

Described herein are protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.