203520-02-9

Upstream product

• 10314-98-4 1-benzyloxycarbonylpiperidine-4-carboxylic acid 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 501-53-1 benzyl chloroformate 
• 498-94-2 isonipecotic acid 

Downstream Products

• 203520-03-0 1-(tert-butoxycarbonyl)-4-(piperidin-4-ylcarbonyl)-piperazine 

Relevant academic research and scientific papers

N-(3-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PHENYL)BENZAMIDE DERIVATIVES

The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

Heterocyclic compounds useful as oxido-squalene cyclase inhibitors

This invention concerns heterocyclic derivatives of formula (I) which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocycl

A novel series of 4-piperidinopyridine and 4-piperidinopyrimidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase

A novel series of 4-piperidinopyridines and 4-piperidinopyrimidines showed potent and selective inhibition of rat 2,3-oxidosqualene cyclase-lanosterol synthase (OSC) (e.g. 26 IC50 rat = 398 ± 25 nM, human = 112 ± 25 nM) and gave selective oral inhibition of rat cholesterol biosynthesis (26 ED80 = 1.2 ± 0.3 mg/kg, n = 5; HMGCoA reductase inhibitor simvastatin ED80 = 1.2 ± 0.3 mg/kg, n = 5). The piperidinopyrimidine OSC inhibitors have a significantly lower pKa than the corresponding pyridine or the previously reported quinuclidine OSC inhibitor series. This indicates that other novel OSC inhibitors may be found in analogues of this series across a broader pKa range (6.0-9.0). These series may yield novel hypocholesterolemic agents for the treatment of cardiovascular disease.

Substituted pyrimidine derivatives and their pharmaceutical use

PCT No. PCT/GB97/02029 Sec. 371 Date Feb. 12, 1999 Sec. 102(e) Date Feb. 12, 1999 PCT Filed Jul. 25, 1997 PCT Pub. No. WO98/06705 PCT Pub. Date Feb. 19, 1998This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.