873537-67-8

Upstream product

• 79-04-9 chloroacetyl chloride 
• 177906-48-8 trans-N-Boc-1,4-cyclohexanediamine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 2615-25-0 trans-1,4-cyclohexyldiamine 

Downstream Products

• 652138-87-9 trans-{4-[ 2-(dimethylamino)acetylamido]cyclohexyl}-carbamic acid tert-butyl ester 
• 873537-68-9 tert-butyl trans-4-({[(2-hydroxyethyl)(methyl)amino]acetyl}amino)-cyclohexylcarbamate 

Relevant academic research and scientific papers

Synthesis and biological evaluation of new dipicolylamine zinc chelators as metallo-β-lactamase inhibitors

Antibiotics are key drugs in modern healthcare, especially in hospitals, where multiresistant bacteria resides and is a potential threat to human health. In the present work, a new series of adjuvants working synergistically with the carbapenem meropenem, in which a selective zinc-chelating agent was covalently linked to the small bacterial peptide D-Ala-D-Ala, was synthesized and tested against VIM-2 and NDM-1 metallo-β-lactamases (MBLs). The nature of the linker was modified in a structure-activity relationship study. Compound 1i, having an ethyl piperidine linker, lowered the MIC of meropenem from 32 to 64 mg/L to 2 and 1–2 mg/L against VIM-2- and NDM-1-producing clinical isolates, respectively. The IC50 value of 1i against VIM-2 was 9.8 and 2.2 μM after 5 and 20 min, respectively. Compound 1i also showed intrinsic toxicity against three eukaryotic human tumoral cell lines between 50 and 120 μM.

Gadolinium Complex of DO3A-Tranexamates Conjugate

The present invention relates to an MRI contrast agent including a gadolinium complex. More specifically, The present invention relates to DO3A-tranexamic acid having a structure of Chemical formula 1, or a ester compound thereof, and a gardolinium complex of the same DO3A-tranexamic acid and the ester compound. According to the present invention, DO3A-tranexamic acid and the ester compound thereof can be produced; and the gardolinium complex can be produced by using the same compound. Gradolinium compounds, produced by a method of the present invention, have thermodynamic kinetic stability and a relaxation rate similar with that of a clinical contrast agent which is commercially used at present. Therefore, according to the present invention, the gardolinium complex can be widely used as a contrast agent for MRI.COPYRIGHT KIPO 2015

Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120)

Inhibition of tumor angiogenesis through blockade of the vascular endothelial growth factor (VEGF) signaling pathway is a newtreatment modality in oncology. Preclinical findings suggest that blockade of additional pro-angiogenic kinases, such as fibroblast and platelet-derived growth factor receptors (FGFR and PDGFR), may improve the efficacy of pharmacological cancer treatment. Indolinones substituted in position 6 were identified as selective inhibitors of VEGF-, PDGF-, and FGF-receptor kinases. In particular, 6-methoxycarbonyl-substituted indolinones showed a highly favorable selectivity profile. Optimization identified potent inhibitors of VEGF-related endothelial cell proliferation with additional efficacy on pericyctes and smooth muscle cells. In contrast, no direct inhibition of tumor cell proliferation was observed. Compounds 2 (BIBF 1000) and 3 (BIBF 1120) are orally available and display encouraging efficacy in in vivo tumor models while being well tolerated. The triple angiokinase inhibitor 3 is currently in phase III clinical trials for the treatment of nonsmall cell lung cancer.

THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY

To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R 1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R 2 is methyl; R 3 is a hydrogen atom; and R 4 is a group: -CONR 5 R 6 (in which any one of R 5 and R 6 is a hydrogen atom)].