477252-20-3

Usage

Uses

Used in Pharmaceutical Industry:
2-(4-Bromopyridin-2-yl)propan-2-ol is used as a key intermediate in the synthesis of pyrazolo[1,5-a]pyridine-derivatives, which are known as TGF-beta receptor inhibitors. These inhibitors play a crucial role in the prevention and treatment of TGF-betaR1 (ALK5)-mediated diseases, such as various types of cancer and fibrosis.

Upstream product

• 75-16-1 methylmagnesium bromide 
• 29681-42-3 methyl 4-bromopyridine-2-carboxylate 
• 676-58-4 methylmagnesium chloride 
• 30766-03-1 4-bromo-2-picolinic acid 
• 62150-47-4 ethyl 4-bromopyridine-2-carboxylate 

Relevant academic research and scientific papers

Growth Factor Receptor antagonists. Preparation method and application thereof

The invention relates to a small molecule antagonist for transforming growth factor β receptors, a method for preparing the small molecule antagonist, and application of the small molecule antagonist in preparation of drugs. The small molecule antagonist for transforming the growth factor β receptor has the application of treating and/or preventing various diseases mediated by ALK5, and has great clinical application potential.

TGF-beta receptor inhibitor

The invention provides a compound shown as a formula (I) and a pharmaceutical composition thereof. The compound shown as the formula (I) of the present invention is useful as a TGF-beta receptor inhibitor, particularly a TGF beta RI inhibitor, for example, in the prevention or treatment of various TGF beta RI (ALK5) mediated related diseases.

ISO-CITRATE DEHYDROGENASE (IDH) INHIBITOR

Disclosed are compounds inhibiting the conversion of α–KG to D-2-HG, pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compound and the pharmaceutical composition c

Aminopyridyloxypyrazole derivative and preparation method and application thereof

The invention relates to an aminopyridyloxypyrazole derivative and a preparation method and application thereof. The structure of the aminopyridyloxypyrazole derivative is shown as a formula (I). The invention provides a brand-new aminopyridyloxypyrazole derivative which has obvious effects of inhibiting TGF [beta] R1 (ALK5) kinase activity and treating cancer or fibrosis related diseases, and the preparation method of the derivative is simple and easy to operate.

SREBP INHIBITOR COMPRISING A THIOPHENE CENTRAL RING

Provided herein is the compound (3-chloro-4-(4-(2-(2-hydroxypropan-2-yl)pyridin-4-yl)thiophen-2-yl)phenyl)(4-hydroxypiperidin-1-yl)methanone (Compound 1), and pharmaceutically acceptable salts, solvates, tautomers, isotopes, or isomers thereof. Also provided herein are methods of inhibiting a component of the sterol regulatory element binding protein (SREBP) pathway, such as an SREBP or SREBP cleavage activating protein (SCAP), using Compound 1, or a pharmaceutically acceptable salt, solvate, tautomer, isotope, or isomer thereof. Further provided are methods of treating a disorder in a subject in need thereof, such as liver disease, non-alcoholic steatohepatitis, insulin resistance, or cancer.

KCNT1 INHIBITORS AND METHODS OF USE

The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.

ARYL-BIPYRIDINE AMINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS

The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula (I): wherein A, X, Y, Z, Q, R1, R2, R3, R4, R5, and n are described herein.

PYRROLOTRIAZINE COMPOUNDS AND METHODS OF INHIBITING TAM KINASES

Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat cancer. (II), or a pharmaceutically acceptable salt thereof, wherein: R1 is pyridin-3-yl, pyridin-4-yl, pyrazol-4-yl, cyclohexyl, or 8-azabicyclo[3.2.1]oct-2- ene-3-yl, wherein R1 is optionally substituted with up to four independently selected substituents; R2 is cyclohexyl substituted with hydroxy and optionally substituted with one or two additional substituents independently selected from C1-C4 alkyl and fluoro, or is 4,5,6,7- tetrahydro-lH-indazolyl optionally substituted with one to three substituents independently selected from C1-C4 alkyl and fluoro; and R3 is -C3-C8 alkyl, -(C2-C6 alkylene)-0-(C1-C6 alkyl), C3-C6 cycloalkyl, or -(C2-C6 alkylene)-C3-C6 cycloalkyl, wherein R3 is optionally substituted with 1-5 substituents inde endentl selected from deuterium, halo, and -OH.

TETRAZOLE CONTAINING COMPOUNDS

The present invention relates to tetrazole containing compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmace

AMINOPYRIDYLOXYPYRAZOLE COMPOUNDS

The present invention relates to novel aminopyridyloxypyrazole compounds that inhibit the activity of transforming growth factor beta receptor 1 (TGFβR1), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, preferably colon cancer, melanoma, hepatocellular carcinoma, renal cancer, glioblastoma, pancreatic cancer, myelodysplastic syndrome, lung cancer, and gastric cancer, and/or fibrosis, preferably liver fibrosis and chronic kidney disease.