1405128-38-2

Upstream product

• 1052715-29-3 (3R,5R)-benzyl 3-fluoro-5-hydroxypiperidine-1-carboxylate 
• 1318129-78-0 methyl (2R,4R)-1-(4-methoxybenzyl)-4-((methylsulfonyl)oxy)pyrrolidine-2-carboxylate 
• 1499-56-5 (R)-4-hydroxy-L-proline ethyl ester 
• 1611481-36-7 ((2S,4S)-4-amino-1-tritylpyrrolidin-2-yl)methanol 
• 1611480-94-4 tert-butyl ((3S,5R)-5-fluoro-1-(4-methoxybenzyl)piperidin-3-yl)carbamate 
• 1611480-91-1 tert-butyl (3S,5R)-5-fluoro-1-tritylpiperidin-3-ylcarbamate 
• 1611480-89-7 tert-butyl (3S,5S)-5-(hydroxymethyl)-1-(4-methoxybenzyl)pyrrolidin-3-ylcarbamate 
• 1611480-88-6 N-((3S,5S)-5-(hydroxymethyl)-1-tritylpyrrolidin-3-yl)benzamide 
• 1611480-85-3 (2S,4S)-methyl 4-azido-1-(4-methoxybenzyl)pyrrolidine-2-carboxylate 
• 1611480-84-2 (2S,4S)-methyl 4-azido-1-tritylpyrrolidine-2-carboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 40216-83-9 L-4-hydroxyproline methyl ester hydrochloride 
• 1611480-81-9 methyl (2S,4R)-4-hydroxy-1-[(4-methoxyphenyl)methyl]pyrrolidine-2-carboxylate 
• 51-35-4 4R-4-hydroxyproline 

Downstream Products

• 1611481-00-5 C₁₇H₂₃FN₂O₃ 
• 1611481-01-6 ((3S,5R)-3-amino-5-fluoropiperidin-1-yl)(phenyl)methanone 
• 1611481-07-2 tert-butyl (3S,5R)-5-fluoro-1-(4-methoxybenzoyl)piperidin-3-ylcarbamate 
• 1611481-08-3 ((3S,5R)-3-amino-5-fluoropiperidin-1-yl)(4-methoxyphenyl)methanone 
• 1611488-82-4 ((3S,5R)-3-amino-5-fluoropiperidin-1-yl)(3-methoxyphenyl)methanone 
• 1611488-81-3 ((3S,5R)-3-amino-5-fluoropiperidin-1-yl)(2-methoxyphenyl)methanone 
• 1611481-09-4 ((3S,5S)-3-amino-5-fluoropiperidin-1-yl)(4-nitrophenyl)methanone 
• 1611481-12-9 ((3S,5R)-3-amino-5-fluoropiperidin-1-yl)(4-nitrophenyl)methanone 
• 1611481-13-0 ((3S,5R)-3-amino-5-fluoropiperidin-1-yl)(3-nitrophenyl)methanone 
• 1611487-96-7 (3S,5R)-(9H-fluoren-9-yl)methyl 3-amino-5-fluoropiperidine-1-carboxylate hydrochloride 
• 1611488-00-6 N-((3S,5R)-5-fluoropiperidin-3-yl)-4-nitrobenzamide 
• 1611488-01-7 N-((3S,5R)-5-fluoropiperidin-3-yl)-3-nitrobenzamide 
• 1611488-02-8 N-((3S,5R)-5-fluoropiperidin-3-yl)-2-nitrobenzamide 
• 1052715-31-7 (3S,5R)-benzyl 3-((tert-butoxycarbonyl)amino)-5-fluoropiperidine-1-carboxylate 

Relevant academic research and scientific papers

PYRAZOLOPYRIMIDINE INHIBITORS OF IRAK4 ACTIVITY

The present invention relates to pyrazolopyrimidine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

Enantioselective synthesis and physicochemical properties of libraries of 3-amino- and 3-amidofluoropiperidines

The enantioselective syntheses of 3-amino-5-fluoropiperidines and 3-amino-5,5-difluoropiperidines were developed using the ring enlargement of prolinols to access libraries of 3-amino- and 3-amidofluoropiperidines. The study of the physicochemical properties revealed that fluorine atom(s) decrease(s) the pKa and modulate(s) the lipophilicity of 3-aminopiperidines. The relative stereochemistry of the fluorine atoms with the amino groups at C3 on the piperidine core has a small effect on the pK a due to conformationnal modifications induced by fluorine atom(s). In the protonated forms, the C-F bond is in an axial position due to a dipole-dipole interaction between the N-H+ and C-F bonds. Predictions of the physicochemical properties using common software appeared to be limited to determine correct values of pKa and/or differences of pK a between cis- and trans-3-amino-5-fluoropiperidines.

BICYCLIC PYRIDAZINE COMPOUNDS AS PIM INHIBITORS

The invention relates to bicyclic compounds of formulas I and I', and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

Pim kinase inhibitors and methods of their use

The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.

PIM KINASE INHIBITORS AND METHODS OF THEIR USE

The present invention relates to new compounds of Formulas (I) and (II), their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmac