C07J71/00

Combination of estrogens plus antiprogestins with significant partial agonistic effect as an effective treatment of menopausal symptoms and for prevention of the occurrence of breast cancer

Described herein are compositions and methods for hormone replacement therapy that address the shortcomings of the existing methods. Described herein are pharmaceutically effective partial agonistic antiprogestins. The combined application of estrogens (such as estradiol, estriol and conjugated estrogens) and the disclosed partial agonistic antiprogestins can be used in hormone replacement therapy.

BETULASTATIN COMPOUNDS
20230192759 · 2023-06-22 ·

The present disclosure relates to Betulastatin compounds, pharmaceutical compositions and kits comprising such compounds, and methods for using such compounds or pharmaceutical compositions.

Isoxazolidine derivatives

Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, according to formula (I) according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.

METHOD OF TREATING SHIP1-MEDIATED DISEASES USING PELOROL DERIVATIVES

Provided are compounds of Formula I and pharmaceutically acceptable salt, solvate and/or derivative thereof. Further, provided are methods of treating a disease, disorder or condition mediated or treatable by activation of SHIP1 comprising administering a compound of Formula I or a pharmaceutically acceptable salt, solvate or derivative thereof. The compound of Formula I or a pharmaceutically acceptable salt, solvate or derivative thereof may be used in the treatment of SHIP1 mediated disease, disorder or conditions including inflammatory bowel disease (IBD), Crohn' disease, ulcerative colitis, multiple myeloma, liver injury, acute hepatitis and severe sepsis.

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TACCALONOLIDE MICROTUBULE STABILIZERS

The invention provides epoxytaccalonolide microtubule stabilizers and their use as anti-proliferative microtubule stabilizing agents.

Natural product analogs including an anti-inflammatory cyanoenone pharmacore and methods of use

This invention provides novel compounds comprising the following anti-inflammatory pharmacore: ##STR00001##
wherein X, R.sub.1 and R.sub.2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

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).

6-ALKYL-7-HYDROXY-4-EN-3-ONE STEROIDS AS INTERMEDIATES FOR THE PRODUCTION OF STEROIDAL FXR

The invention relates to compounds of formula (I), wherein R.sup.1, R.sup.2, Y, R.sup.4 and R.sup.5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.

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6.ALPHA.-ALKYL-6,7-DIONE STEROIDS AS INTERMEDIATES FOR THE PRODUCTION OF STEROIDAL FXR MODULATORS

The invention relates to compounds of formula (I), wherein R.sup.1, R.sup.2, Y, R.sup.4 and R.sup.5b are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.

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ROR gamma modulators

The present invention relates to compounds of formula I, or a pharmaceutically acceptable salt thereof, ##STR00001##
for use in the treatment or prevention, suppression or amelioration of a disease mediated by the ROR gamma receptor in a subject in need thereof, in particular diabetes and diabetes-related disorders, specifically type II diabetes, methods of their production, as well as methods of treatment or prevention of such diseases.