917894-06-5

Upstream product

• 70502-87-3 3-amino-4-chlorobenzenethiol 
• 100-39-0 benzyl bromide 
• 97-08-5 3-nitro-4-chlorosulfonyl chloride 

Downstream Products

• 917894-07-6 2-chloro-5-S-benzyl-thioaniline hydrochloride 
• 917894-08-7 N-(5-benzylthio-2-chlorophenyl)-N'-(3-methylthiophenyl)-N'-methyl-guanidine hydrochloride 
• 917894-09-8 N-(2-chloro-5-mercaptophenyl)-N'-(3-methylthiophenyl)-N'-methyl-guanidine hydrochloride 
• 917894-11-2 N-(2-chloro-5-(S-2-fluoroethyl)thiophenyl)-N'-(3-methylthiophenyl)-N'-methyl guanidine 
• 917894-05-4 N-(2-chloro-5-fluoromethylthiophenyl)-N'-(3-methylthiophenyl)-N'-methyl-guanidine 
• 917894-23-6 N-(2-chloro-5-mercaptophenyl)-N'-methyl-N'-(3-thiomethylphenyl)guanidine 

Relevant academic research and scientific papers

N′-3-(Trifluoromethyl)phenyl Derivatives of N-Aryl-N′-methylguanidines as Prospective PET Radioligands for the Open Channel of the N-Methyl- d -aspartate (NMDA) Receptor: Synthesis and Structure-Affinity Relationships

N-Methyl-d-aspartate (NMDA) receptor dysfunction has been linked to several neuropsychiatric disorders, including Alzheimer's disease, epilepsy, drug addiction, and schizophrenia. A radioligand that could be used with PET to image and quantify human brain NMDA receptors in the activated "open channel" state would be useful for research on such disorders and for the development of novel therapies. To date, no radioligands have shown well-validated efficacy for imaging NMDA receptors in human subjects. In order to discover improved radioligands for PET imaging, we explored structure-affinity relationships in N′-3-(trifluoromethyl)phenyl derivatives of N-aryl-N′-methylguanidines, seeking high affinity and moderate lipophilicity, plus necessary amenability for labeling with a positron-emitter, either carbon-11 or fluorine-18. Among a diverse set of 80 prepared N′-3-(trifluoromethyl)phenyl derivatives, four of these compounds (13, 19, 20, and 36) displayed desirable low nanomolar affinity for inhibition of [3H](+)-MK801 at the PCP binding site and are of interest for candidate PET radioligand development.

Synthesis and in vitro evaluation of 18F-labelled S-fluoroalkyl diarylguanidines: Novel high-affinity NMDA receptor antagonists for imaging with PET

Two S-[18F]fluoroalkylated diarylguanidines were synthesized and evaluated in vitro as potential tracers for imaging of N-methyl-d-aspartate receptors (NMDARs) with positron emission tomography (PET). [18F]1 and [18F]10 we

NITROGENATED FUSED RING DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND USE OF THE SAME FOR MEDICAL PURPOSES

[Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, -OW1, -SW1, -COW2, -NW3W4, -SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, -CO-Y, -SO2-Y -S-(alkylene)-Y, -O-(alkylene)-Y, -SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.

IMAGING 18F OR 11C-LABELLED ALKYLTHIOPHENYL GUANIDINES

The invention provides a compound of formula (I); or a salt or solvate thereof, wherein: R1 is hydrogen or C1-4alkyl; R2 and R4 are each independently selected from C1-4 alkyl, [11C] C1 4alkyl, and [18F]-C1-4 fluoroalkyl provided that at least one of R2 and R4 is [11C] C1 4alkyl or [18F]-C1-4 fluoroalkyl; and R3 is halo. Such compounds having use for imaging central nervous system receptors.