871839-91-7

Usage

Uses

2-Isopropoxypyridine-5-boronic acid, pinacol ester

InChI:InChI=1/C14H22BNO3/c1-10(2)17-12-8-7-11(9-16-12)15-18-13(3,4)14(5,6)19-15/h7-10H,1-6H3

Upstream product

• 13466-38-1 5-bromopyridin-2(1H)-one 
• 13466-38-1 5-bromopyridin-2-ol 
• 766-11-0 5-bromo-2-fluoropyridine 
• 870521-31-6 5-bromo-2-isopropoxy-pyridine 
• 73183-34-3 bis(pinacol)diborane 

Downstream Products

• 1184174-97-7 C₄₅H₄₇N₅O₅ 
• 1184173-73-6 (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide 
• 1184175-04-9 tert-butyl (S)-3-((3-(6-isopropoxypyridin-3-yl)-1-trityl-1H-indazol-5-yl)carbamoyl)-3-(methylthio)pyrrolidine-1-carboxylate 
• 1184174-14-8 3-(6-isopropoxypyridin-3-yl)-5-nitro-1-trityl-1H-indazole 

Relevant academic research and scientific papers

MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology

The emergence and evolution of new immunological cancer therapies has sparked a rapidly growing interest in discovering novel pathways to treat cancer. Toward this aim, a novel series of pyrrolidine derivatives (compound 5) were identified as potent inhibitors of ERK1/2 with excellent kinase selectivity and dual mechanism of action but suffered from poor pharmacokinetics (PK). The challenge of PK was overcome by the discovery of a novel 3(S)-thiomethyl pyrrolidine analog 7. Lead optimization through focused structure-activity relationship led to the discovery of a clinical candidate MK-8353 suitable for twice daily oral dosing as a potential new cancer therapeutic.

SULFONAMIDE COMPOUNDS AS VOLTAGE-GATED SODIUM CHANNEL MODULATORS

The present invention relates to sulfonamide compounds Formula (I) wherein the substituents are as described herein, and their use in a medicine for the treatment of diseases, disorders associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. It further relates to the compounds herein and their pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof useful in treating diseases, disorders, syndromes and/or conditions associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. The invention also relates to process for the preparation of the compounds of the invention. (I)

SPIROCYCLIC COMPOUNDS

Disclosed herein are spirocyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.

PYRROLIDINONE DERIVATIVES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS

The present invention relates to pyrrolidinone derivatives of formula (I). The pyrrolidinone derivatives of formula (I) are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

COMPOUNDS THAT ARE ERK INHIBITORS

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydopyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

INDOLES USEFUL IN THE TREATMENT OF INFLAMMATION

There is provided a compound of formula (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are