C07D493/08

HYBRID AMIDE DERIVATIVES OF AMPHOTERICIN B
20230016424 · 2023-01-19 ·

Disclosed are C16 amide derivatives of C2′-epi-amphotericin B (C2′epiAmB) and amphotericin B (AmB), characterized by improved clinical efficacy with reduced toxicity compared to AmB. Also disclosed are pharmaceutical compositions comprising either type of the C16 amide derivatives, and therapeutic methods of using either type of the C16 amide derivatives; and methods of making the C16 amide derivatives of C2′-epi-amphotericin B.

PEGYLATED PRODRUGS OF PHENOLIC TRPV1 AGONISTS
20230219901 · 2023-07-13 ·

Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity.

PEGYLATED PRODRUGS OF PHENOLIC TRPV1 AGONISTS
20230219901 · 2023-07-13 ·

Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity.

METHODS OF PREPARING SYNTHETIC CANNABICHROMENE AND CANNABICITRAN AND DERIVATIVES THEREOF
20230219916 · 2023-07-13 ·

The present disclosure relates to the preparation of synthetic cannabinoid derivatives of Formulae I and II, and compositions made therefrom.

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METHODS OF PREPARING SYNTHETIC CANNABICHROMENE AND CANNABICITRAN AND DERIVATIVES THEREOF
20230219916 · 2023-07-13 ·

The present disclosure relates to the preparation of synthetic cannabinoid derivatives of Formulae I and II, and compositions made therefrom.

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Safe, Environmentally Friendly and Controllable Method for Preparing Cycloaliphatic Diepoxides
20230212133 · 2023-07-06 ·

The present disclosure relates to the field of epoxide synthesis, and particularly to a safe, environmentally friendly and controllable method for preparing cycloaliphatic diepoxides. The method comprises the steps of: mixing a diene compound, a carboxylic acid, an alkaline salt, and a solvent, and cooling; dropwise adding a hydrogen peroxide solution thereto over 1-12 h; standing for layering to obtain an underlayer of an organic phase 1, washing the organic phase 1 with a washing liquid, and standing for layering to obtain an underlayer of an organic phase 2; and purifying the organic phase 2. The reaction system of the present disclosure is simple, environmentally friendly, safe and controllable, and the production cost is low, which can meet the technical and economic requirements. The obtained cycloaliphatic diepoxides have high purity, high yield, low solvent content, low chroma and low halogen content, which are suitable for large-scale industrial production.

LACTAMS AS CBL-B INHIBITORS SELECTIVE OVER C-CBL

A compound, of formula (I):

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suitable for treating a cancer wherein the cancer is susceptible to inhibition of Cbl-B.

LACTAMS AS CBL-B INHIBITORS SELECTIVE OVER C-CBL

A compound, of formula (I):

##STR00001##

suitable for treating a cancer wherein the cancer is susceptible to inhibition of Cbl-B.

Heterocyclic compounds, preparation methods therefor, and methods of uses thereof

Provided herein are novel heterocyclic compounds, for example, compounds having Formula I. Also provided herein are methods of preparing the compounds and methods of using the same, for example, in inhibiting TGF-beta mediated signaling and/or for treating cancer. ##STR00001##

Heterocyclic compounds, preparation methods therefor, and methods of uses thereof

Provided herein are novel heterocyclic compounds, for example, compounds having Formula I. Also provided herein are methods of preparing the compounds and methods of using the same, for example, in inhibiting TGF-beta mediated signaling and/or for treating cancer. ##STR00001##