C07D237/04

COVALENT INHIBITORS OF KRAS G12C
20190389796 · 2019-12-26 ·

Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.

COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS

The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS

The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

Synthesis of 6-oxo-1,4,5,6-tetrahydropyridizin-3-carboxylic acid

A method for producing 6-oxo-1,4,5,6-tetrahydropyridazine-3-carboxylic acid is disclosed that includes steps of adding hydrazine sulfate with 2-ketoglutaric acid in a container as a solid, adding water to the solid creating a heterogenous mixture of the hydrazine sulfate, 2-ketoglutaric acid and water, blending the heterogenous mixture for at least one hour, and measuring the heterogenous mixture to confirm that it has converted into 6-oxo-1,4,5,6-tetrahydropyridazine-3-carboxylic acid. Hydrazine sulfate can be added to the 2-ketoglutaric acid in the container at a ratio of greater than 1.1. The compound 6-oxo-1,4,5,6-tetrahydropyridazine-3-carboxylic acid (PCA) has many uses. It has been used for medical applications and as a building block and for medical applications. The compound is also a product of the remediation of hydrazine using 2-ketogluraric acid.

Synthesis of 6-oxo-1,4,5,6-tetrahydropyridizin-3-carboxylic acid

A method for producing 6-oxo-1,4,5,6-tetrahydropyridazine-3-carboxylic acid is disclosed that includes steps of adding hydrazine sulfate with 2-ketoglutaric acid in a container as a solid, adding water to the solid creating a heterogenous mixture of the hydrazine sulfate, 2-ketoglutaric acid and water, blending the heterogenous mixture for at least one hour, and measuring the heterogenous mixture to confirm that it has converted into 6-oxo-1,4,5,6-tetrahydropyridazine-3-carboxylic acid. Hydrazine sulfate can be added to the 2-ketoglutaric acid in the container at a ratio of greater than 1.1. The compound 6-oxo-1,4,5,6-tetrahydropyridazine-3-carboxylic acid (PCA) has many uses. It has been used for medical applications and as a building block and for medical applications. The compound is also a product of the remediation of hydrazine using 2-ketogluraric acid.

6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives as PDE3A and PDE3B inhibitors for treating cancer

The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I): The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I): ##STR00001##

6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives as PDE3A and PDE3B inhibitors for treating cancer

The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I): The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I): ##STR00001##

Compositions, methods, and systems for the synthesis and use of imaging agents

The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

Compositions, methods, and systems for the synthesis and use of imaging agents

The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

Use of Sanglifehrin Macrocyclic Analogues as Anticancer Compounds

The present invention relates to uses of sanglifehrin macrocyclic analogues in treatment of cancer, especially liver cancer.