404589-70-4

Upstream product

• 186581-53-3 diazomethane 
• 89421-95-4 l-(4-chloro-phenyl)-cyclobutanecarbonyl chloride 

Downstream Products

• 1009376-49-1 C₂₆H₂₉ClF₃NO₂ 
• 1067187-73-8 2-(1-(4-chlorophenyl)cyclobutyl)-2-oxoethyl acetate 
• 473705-85-0 N'-{4-[1-(4-chlorophenyl)cyclobutyl]thiazol-2-yl}-N,N-diethylpropane-1,3-diamine 
• 473705-93-0 1-{4-[1-(4-chlorophenyl)cyclobutyl]thiazol-2-yl}-4-methylpiperazine 

Relevant academic research and scientific papers

MULTIMEDIATOR TRANSPORTER INHIBITORS FOR USE IN TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS

The invention provides a class of inhibitors, packaged pharmaceuticals comprising such inhibitors, and uses of the inhibitors in treating, or the manufacturing medicaments for treating central nervous system disorders, including depression, anxiety, sleep

Discovery of 2-[1-(4-Chlorophenyl)cyclopropyl]-3-hydroxy-8- (trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury

Previously, we reported the discovery of PSI-697 (1a), a C-2 benzyl substituted quinoline salicylic acid-based P-selectin inhibitor. It is active in a variety of animal models of cardiovascular disease. Compound 1a has also been shown to be well tolerated and safe in healthy volunteers at doses of up to 1200 mg in a phase 1 single ascending dose study. However, its oral bioavailability was low. Our goal was to identify a back up compound with equal potency, increased solubility, and increased exposure. We expanded our structure-activity studies in this series by branching at the α position of the C-2 benzyl side chain and through modification of substituents on the carboxylic A-ring of the quinoline. This resulted in discovery of PSI-421 with marked improvement in aqueous solubility and pharmacokinetic properties. This compound has shown oral efficacy in animal models of arterial and venous injury and was selected as a preclinical development compound for potential treatment of such diseases as atherosclerosis and deep vein thrombosis.

Methods and Compositions for Selectin Inhibition

The present teachings relate to novel compounds of formula I: wherein the constituent variables are as defined herein. Compounds of the present teachings can act as antagonists of the mammalian adhesion proteins known as selecting. Methods for treating or preventing selectin-mediated disorders are provided, which include administration of these compounds in a therapeutically effective amount.

DOPAMINE TRANSPORTER INHIBITORS FOR USE IN TREATMENT OF MOVEMENT DISORDERS AND OTHER CNS INDICATIONS

The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors) , packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or the manufacturing medicaments for treating disease conditions, inlcudin

Thiazole and other heterocyclic ligands for mammalian dopamine, muscarinic and serotonin receptors and transporters, and methods of use thereof

One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various mammalian cellular receptors, including G-protein coupled receptors. A third aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors or transporters. Another aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, Tourette's syndrome, psychiatric disorders, stroke, senile dementia, peptic ulcers, pulmonary obstruction disorders, and asthma.