60017-02-9

Upstream product

• 1122-42-5 2-iodo-p-xylene 

Downstream Products

• 290354-18-6 C₂₈H₄₅IN₄O₂ 
• 346691-76-7 (E,E)-2,5-bis(4’-hydroxy-3’-carbomethoxystyryl)-1-iodobenzene 
• 1176244-38-4 tetraethyl 1,4-bis(phosphonomethyl)-2-iodobenzene 
• 687635-87-6 1,4-bis-[(N,N'-bis-tert-butyloxycarbonyl)guanidinomethyl]-2-iodobenzene 

Relevant academic research and scientific papers

IL4I1 INHIBITORS AND METHODS OF USE

Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as IL4I1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for IL4I1-related diseases.

Tritium-labeled (E,E)-2,5-bis(4′-hydroxy-3′-carboxystyryl)benzene as a probe for β-amyloid fibrils

Accumulation of Aβ in the brains of Alzheimer disease (AD) patients reflects an imbalance between Aβ production and clearance from their brains. Alternative cleavage of amyloid precursor protein (APP) by processing proteases generates soluble APP fragments including the neurotoxic amyloid Aβ40 and Aβ42 peptides that assemble into fibrils and form plaques. Plaque-buildup occurs over an extended time-frame, and the early detection and modulation of plaque formation are areas of active research. Radiolabeled probes for the detection of amyloid plaques and fibrils in living subjects are important for noninvasive evaluation of AD diagnosis, progression, and differentiation of AD from other neurodegenerative diseases and age-related cognitive decline. Tritium-labeled (E,E)-1-[3H]-2,5-bis(4′-hydroxy-3′-carbomethoxystyryl)benzene possesses an improved level of chemical stability relative to a previously reported radioiodinated analog for radiometric quantification of Aβ plaque and tau pathology in brain tissue and in vitro studies with synthetic Aβ and tau fibrils.

Meta-iodobenzylguanidine derivatives containing a second guanidine moiety

Radioiodinated meta-iodobenzylguanidine (MIBG) is used in the diagnosis and therapy of various neuroendocrine tumors. To investigate whether an additional guanidine function in the structure of MIBG will yield analogues that may potentially enhance tumor-to-target ratios, two derivatives - one with a guanidine moiety and another with a guanidinomethyl group at the 4-position of MIBG - were prepared. In the absence of any uptake-1 inhibiting conditions, the uptake of 4-guanidinomethyl-3-[131I]iodobenzylguanidine ([ 131I]GMIBG) by SK-N-SH cells in vitro was 1.7±0.1% of input counts, compared to a value of 40.3±1.4% for [125I[MIBG suggesting that guanidinomethyl group at the 4-position negated the biological properties of MIBG. On the other hand, 4-guanidino-3-[131I] iodobenzylguanidine ([131I]GIBG) had an uptake (5.6±0.3%) that was 12-13% that of [125I]MIBG (46.1±2.7%), and the ratio of uptake by control over DMI-treated (nonspecific) cultures was higher for [131I]GIBG (20.9±0.3) than [125I]MIBG itself (15.0±2.7). The exocytosis of [131I]GIBG and [ 125I]MIBG from SK-N-SH cells was similar. The uptake of [ 131I]GIBG in the mouse target tissues, heart and adrenals, as well as in a number of other tissues was about half that of [125I]MIBG. These results suggest that substitution of guanidine functions, especially a guanidinomethyl group, in MIBG structure may not be advantageous.

INHIBITORS OF BACE

The present invention relates to inhibitors of aspartic proteinases, particularly, BACE. The present invention also relates to compositions thereof and methods therewith for inhibiting BACE activity in a mammal, and for treating Alzheimer's Disease and other BACE-mediated diseases.

New carbamoylpiperidines as human platelet aggregation inhibitors

A series of 3-carbamoylpiperidines (nipecotamides) are designed, synthesized and tested for their inhibitory action against adenosine diphosphate (ADP)-induced aggregation of human platelets. A structure- activity analysis of the bis(nipecotamido)aralkane type showed that a substituent on the piperidine ring should preferably be an amide and that the electronegativity of the carbonyl oxygen and the orientation of the amide group affected activities. Based on the knowledge of factors influencing platelet activation and aggregation, a nitric ester moiety which could release nitric oxide (NO) in situ, is incorporated into the nipecotamide structure. These compounds exhibit increased activity compared to those having no -ONO2 function. They also show stereoselectivity, with the meso isomer being approximately twice as potent as the synthetic diastereomeric mixture. Replacement of the -ONO2 function with hydroxyl, ester or alkyl groups considerably diminishes aggregation-inhibitory potential. Nipecotamides are shown here to inhibit the basal and collagen-induced rise in platelet inositol trisphosphate (IP3) levels, as well as phosphoinositide turnover. A comprehensive mechanism of action is proposed taking earlier results into consideration. (C) 2000 Elsevier Science Ltd.

Potential organ- or tumor-imaging agents. 18. Radioiodinated diamines and bisquaternaries

The purpose of this research was to employ diamines and their quaternary derivatives as carrier molecules for γ-emitting radiation. The diamine putrescine is widespread in nature and has been reported to selectively concentrate in the rat ventral prostate