1192189-66-4

Upstream product

• 1192189-65-3 1-tert-butyl 4-methyl 4-[(benzyloxycarbonylamino)methyl]piperidine-1,4-dicarboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 91419-52-2 1-tert-butoxycarbonyl-4-cyanopiperidine 
• 362703-35-3 1-tert-butyl 4-methyl 4-(aminomethyl)piperidine-1,4-dicarboxylate 
• 501-53-1 benzyl chloroformate 
• 1016258-66-4 1-(tert-butyl) 4-ethyl 4-cyanopiperidine-1,4-dicarboxylate 
• 247133-44-4 4-benzyloxycarbonylaminomethyl-4-ethoxycarbonylpiperidine-1-carboxylic acid tert-butyl ester 
• 1016258-69-7 1-tert-butyl 4-ethyl 4-(aminomethyl)piperidine-1,4-dicarboxylate 
• 4395-98-6 4-cyanopiperidine 

Downstream Products

• 1207178-51-5 C₁₂H₂₁N₃O₂ 
• 1338251-61-8 C₂₀H₂₉N₃O₅ 
• 1338251-62-9 C₂₀H₂₇N₃O₄ 
• 1338251-65-2 C₁₆H₂₁N₃O₃*ClH 
• 1338251-66-3 C₁₄H₁₅Cl₂N₃O*ClH 
• 1338251-70-9 C₂₄H₂₉N₃O₄ 
• 1338251-71-0 C₂₄H₂₉N₃O₄ 
• 1338251-72-1 C₂₄H₂₉N₃O₄ 
• 1338251-73-2 C₂₄H₂₆F₃N₃O₃ 
• 1338251-74-3 C₂₄H₂₆F₃N₃O₃ 
• 1338251-75-4 C₂₄H₂₆F₃N₃O₃ 
• 1338251-76-5 C₂₈H₃₃N₃O₄ 
• 1338251-77-6 C₂₄H₂₉N₃O₃ 
• 1338251-78-7 C₂₂H₂₃Cl₂N₃O₂ 

Relevant academic research and scientific papers

Discovery and development of LX7101, a dual LIM-kinase and ROCK inhibitor for the treatment of glaucoma

The structure of LX7101, a dual LIM-kinase and ROCK inhibitor for the treatment of ocular hypertension and associated glaucoma, is disclosed. Previously reported LIM kinase inhibitors suffered from poor aqueous stability due to solvolysis of the central urea. Replacement of the urea with a hindered amide resulted in aqueous stable compounds, and addition of solubilizing groups resulted in a set of compounds with good properties for topical dosing in the eye and good efficacy in a mouse model of ocular hypertension. LX7101 was selected as a clinical candidate from this group based on superior efficacy in lowering intraocular pressure and a good safety profile. LX7101 completed IND enabling studies and was tested in a Phase 1 clinical trial in glaucoma patients, where it showed efficacy in lowering intraocular pressure. (Figure Presented).

Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers

To obtain selective and potent inhibitor for T-type calcium channel by ligand based drug design, 4-piperidinecarboxylate and 4-piperidinecyanide derivatives were prepared and evaluated for in vitro and in vivo activity against α1G calcium channel. Among them, several compounds showed good T-type calcium channel inhibitory activity and minimal off-target activity over hERG channel (% inhibition at 10 μM = 61.85-71.99, hERG channel IC50 = 1.57 ± 0.14-4.98 ± 0.36 μM). Selected compound 31a was evaluated on SNL model of neuropathic pain and showed inhibitory effect on mechanical allodynia.

LIMK2 INHIBITORS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE

Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use. Particular compounds are of the formula: