375854-52-7

Usage

Structure

2-(trimethylsilyl)ethyl 4-(3-cyanophenyl)-5,6-dihydropyridine-1(2H)-carboxylate

Type of compound

Dihydropyridine derivative

Functional groups

Trimethylsilyl group, cyanophenyl group, carboxylate

Usage

Precursor in organic synthesis, pharmaceutical industry (production of calcium channel blockers)

Medical application

Treatment of high blood pressure and angina

Potential applications

Medicinal chemistry, drug discovery

Upstream product

• 375854-77-6 2-(trimethylsilyl)ethyl 1,2,3,6-tetrahydro-4-trifluoromethylsulfonyloxy-pyridine-1-carboxylate 
• 150255-96-2 (3‐cyanophenyl)boronic acid 
• 181701-30-4 4-oxo-piperidine-1-carboxylic acid 2-(trimethylsilyl)ethyl ester 
• 6952-59-6 3-cyanobromobenzene 
• 80149-80-0 2-(Trimethylsilyl)ethyl 4-nitrophenyl carbonate 
• 37595-74-7 N,N-phenylbistrifluoromethane-sulfonimide 

Downstream Products

• 725228-49-9 tert-butyl 3-(piperidin-4-yl)benzylcarbamate 
• 725228-57-9 4-(3-cyanophenyl)pyridine-1-carboxylic acid 2-trimethylsilanyl-ethyl ester 

Relevant academic research and scientific papers

INDOLYL-PIPERIDINYL BENZYLAMINES AS BETA-TRYPTASE INHIBITORS

The present invention discloses and claims a series of substituted indolyl-piperidinyl benzylamines of formula (I), wherein R1, R2 and R3 are as described herein. More specifically, the compounds of this invention are inhibitors of β-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted indolyl-piperidinyl benzylamines. In one of the embodiments, there is provided the compounds of formula (I) wherein R3 is (II).

[4[4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL)-METHANONES AND SYNTHESIS THEREOF

The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase including but not limited to for example asthma and other inflammatory diseases including age-related macular degeneration.

Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: Novel, potent, selective, and orally bioavailable inhibitors of βII tryptase

Tryptase is a serine protease found almost exclusively in mast cells. It has trypsin-like specificity, favoring cleavage of substrates with an arginine (or lysine) at the P1 position, and has optimal catalytic activity at neutral pH. Current evidence suggests tryptase β is the most important form released during mast cell activation in allergic diseases. It is shown to have numerous pro-inflammatory cellular activities in vitro, and in animal models tryptase provokes broncho-constriction and induces a cellular inflammatory infiltrate characteristic of human asthma. Screening of in-house inhibitors of factor Xa (a closely related serine protease) identified β-amidoester benzamidines as potent inhibitors of recombinant human βII tryptase. X-ray structure driven template modification and exchange of the benzamidine to optimize potency and pharmacokinetic properties gave selective, potent and orally bioavailable 4-(3-aminomethyl phenyl)piperidinyl-1-amides.

[4-(3-AMINOMETHYLPHENYL) PIPERIDIN-1-YL]- [5-(2-FLUOROPHENYLETHYNYL)FURAN-2-YL]-METHANONE AS AN INHIBITOR OF MAST CELL TRYPTASE

The present invention extends to the compund of formula (I): (I) or a prodrug, pharmaceutically acceptable salt, or solvate of said compound; to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of forumula (I), a

Chemical compounds

Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a condition, disease, or disorder that can be ameliorated by the administration of an inhibitor of tryptase, e.g., asthma and inflammatory diseases, to name only a few.