362703-34-2Relevant articles and documents
LIM KINASE INHIBITORS
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, (2015/11/02)
The present invention relates to new kinase inhibitors, more specifically LIM Kinase inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and Prophylaxis of disease. In particular, the present invention relates to new LIMK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and Prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said Compounds in the manufacture of a medicament for the application to a number of therapeutic indications including Ophthalmic and intestinal diseases.
Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers
Woo, Hyun Min,Lee, Yun Suk,Roh, Eun Joo,Seo, Seon Hee,Song, Chi Man,Chung, Hye Jin,Pae, Ae Nim,Shin, Kye Jung
, p. 5910 - 5915 (2011/10/09)
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.
Synthesis and structure-activity relationship of a novel, achiral series of TNF-α converting enzyme inhibitors
Gilmore, John L.,King, Bryan W.,Harris, Cathy,Maduskuie, Thomas,Mercer, Stephen E.,Liu, Rui-Qin,Covington, Maryanne B.,Qian, Mingxin,Ribadeneria, Maria D.,Vaddi, Krishna,Trzaskos, James M.,Newton, Robert C.,Decicco, Carl P.,Duan, James J.-W.
, p. 2699 - 2704 (2007/10/03)
A novel series of achiral TNF-α converting enzyme (TACE) inhibitors has been discovered. These compounds exhibited activities from 0.35 to 11 nM in a porcine TACE assay and inhibited TNF-α production in an LPS-stimulated whole blood assay with an IC5
Beta-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-alpha
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Page/Page column 46, (2010/11/30)
The present application describes novel β-amino acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, Ua, Xa, Ya, Za, R1, R2, R3