113984-76-2

Upstream product

• 459-56-3 4-fluorobenzylic alcohol 
• 18162-48-6 tert-butyldimethylsilyl chloride 

Downstream Products

• 113984-77-3 1-(tert-butyldimethylsiloxymethyl)-4-fluoro-3-hydroxybenzene 
• 128495-45-4 (4-fluoro-3-methoxy-phenyl)methanol 
• 141080-73-1 4-(bromomethyl)-1-fluoranyl-2-methoxybenzene 
• 113984-79-5 3-(tert-butyldimethylsilyloxy)-1-(tert-butyldimethylsilyloxymethyl)-4-fluoro-5-hydroxybenzene 
• 113984-82-0 3,5-bis(tert-butyldimethylsilyloxy)-1-hydroxymethyl-4-fluorobenzene 
• 113984-66-0 3,5-bis(tert-butyldimethylsilyloxy)-4-fluorobenzaldehyde 
• 113984-73-9 3,5-Bis-benzyloxy-4-fluoro-benzaldehyde 
• 113984-81-9 3,5-bis(tert-butyldimethylsilyloxy)-1-(tert-butyldimethylsilyloxymethyl)-4-fluorobenzene 
• 113984-80-8 3-(tert-Butyl-dimethyl-silanyloxy)-2-fluoro-5-hydroxymethyl-phenol 
• 113984-65-9 3-(tert-Butyl-dimethyl-silanyloxy)-4-fluoro-5-hydroxy-benzaldehyde 
• 132303-44-7 5,7-Bis-benzyloxy-6-fluoro-1H-indole 
• 132303-41-4 5,7-Bis-benzyloxy-6-fluoro-1H-indole-2-carbaldehyde 
• 132303-54-9 2-(5,7-Bis-benzyloxy-6-fluoro-1H-indol-3-yl)-ethylamine 
• 132303-47-0 (5,7-Bis-benzyloxy-6-fluoro-1H-indol-3-ylmethyl)-dimethyl-amine 

Relevant academic research and scientific papers

Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors

G protein-coupled receptor (GPCR) kinases (GRKs) regulate the desensitization and internalization of GPCRs. Two of these, GRK2 and GRK5, are upregulated in heart failure and are promising targets for heart failure treatment. Although there have been several reports of potent and selective inhibitors of GRK2 there are few for GRK5. Herein, we describe a ligand docking approach utilizing the crystal structures of the GRK2–Gβγ·GSK180736A and GRK5·CCG215022 complexes to search for amide substituents predicted to confer GRK2 and/or GRK5 potency and selectivity. From this campaign, we successfully generated two new potent GRK5 inhibitors, although neither exhibited selectivity over GRK2.

G PROTEIN-COUPLED RECEPTOR KINASE 2 INHIBITORS AND METHODS FOR USE OF THE SAME

Disclosed herein are novel GRK2 inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically

Therapeutic Aryl-Amido-Aryl Compounds and Their Use

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, a

THERAPEUTIC ARYL-AM I DO-ARYL COMPOUNDS AND THEIR USE

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as "AAA compounds"), which, inter alia, a

PYRIMIDINE AND QUINAZOLINE DERIVATIVES

This invention is concerned with compounds of the formula ( l ) wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

PYRIDINE, QUINOLINE AND PYRIMIDINE DERIVATIVES

This invention is concerned with compounds of the formula wherein A, R1 to R5 are as defined in the specification and G is a pyridine, quinoline or pyrimidine group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

BENZOIMIDAZOLE, TETRAHYDRO-QUINOXALINE, BENZOTRIAZOLE, DIHYDRO-IMIDAZO[4,5-c] PYRIDINONE AND DIHYDRO-ISOINDOLONE DERIVATIVES

This invention relates to compounds of the formula wherein A, R1 to R3 are as defined in the specification and G is benzoimidazole, quinoxaline, benzotriazole, dihydro-imidazo[4,5-c]pyridine and dihydro-isoindolone group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

4,4-DISUBSTITUTED PIPERIDINE DERIVATIVES

This invention relates to 4,4-disubstituted piperidine derivatives of the formula wherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceuti

ARYLOXAZOLE, ARYLOXADIAZOLE AND BENZIMIDAZOLE DERIVATIVES

This invention relates to compounds of the formula wherein X is O or NR8, Y is CR7 or N, and R1 to R8 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

PHENYL, PYRIDINE, QUINOLINE, ISOQUINOLINE, NAPHTHYRIDINE AND PYRAZINE DERIVATIVES

This invention is concerned with compounds of the formulaand pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.