181701-30-4

Upstream product

• 40064-34-4 piperidine-4,4-diol hydrochloride 
• 80149-80-0 2-(Trimethylsilyl)ethyl 4-nitrophenyl carbonate 
• 41979-39-9 4-piperidone hydrochloride 
• 840493-49-4 2-trimethylsilylethyl 4-hydroxypiperidine-1-carboxylate 
• 2916-68-9 2-(Trimethylsilyl)ethanol 
• 3612-20-2 1-phenylmethyl-4-piperidone 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 

Downstream Products

• 375854-77-6 2-(trimethylsilyl)ethyl 1,2,3,6-tetrahydro-4-trifluoromethylsulfonyloxy-pyridine-1-carboxylate 
• 725228-49-9 tert-butyl 3-(piperidin-4-yl)benzylcarbamate 
• 375854-52-7 2-(trimethylsilanyl)ethyl 4-(3-cyanophenyl)-3,6-dihydro-2H-pyridine-1-carboxylate 

Relevant academic research and scientific papers

COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES

The present disclosure relates to compounds according to Formulae (I), (II) and (VIII), useful for treating diseases.

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.

On the preparation of azepinones

We report here a simple and efficient preparation of 1H-azepin-5(2H)-ones and their unexpectedly facile isomerization to 1H-azepin-5(4H)-ones under mildly basic reaction conditions.

Nanoscale molecular rods with a new building block for solubility enhancement

(Chemical Equation Presented) A new building block bearing a [1,3]dioxolo[4,5-f][1,3]benzodioxole core was developed to enhance the solubility of molecular rods by lateral alkyl chains. On incorporation in molecular rods with oligospiroketal structure, the straight geometry is retained, which was concluded from the X-ray crystal structure analysis of one of the rods. The determination of the solubility of a collection of rods bearing this building block revealed that already a butyl group efficiently hinders the aggregation of the rods and consequently causes a considerable enhancement of the solubility. Piperidine rings are located at the ends of the rods, which offer the opportunity for versatile functionalization. Thus, an N,N′-bis(azidoacetyl)-functionalized rod was prepared, which could serve as rigid linkage, initiated by a "Click" reaction.

SUBSTITUTED BIS ARYL AND HETEROARYL COMPOUNDS AS SELECTIVE 5HT2A ANTAGONISTS

The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R 1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.

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