80100-20-5Relevant academic research and scientific papers
Fatty acid amide hydrolase inhibitors. 3: Tetra-substituted azetidine ureas with in vivo activity
Roughley, Stephen D.,Browne, Helen,MacIas, Alba T.,Benwell, Karen,Brooks, Teresa,D'Alessandro, Jalanie,Daniels, Zoe,Dugdale, Sarah,Francis, Geraint,Gibbons, Ben,Hart, Terance,Haymes, Timothy,Kennett, Guy,Lightowler, Sean,Matassova, Natalia,Mansell, Howard,Merrett, Angela,Misra, Anil,Padfield, Anthony,Parsons, Rachel,Pratt, Robert,Robertson, Alan,Simmonite, Heather,Tan, Kiri,Walls, Steven B.,Wong, Melanie
supporting information; experimental part, p. 901 - 906 (2012/03/11)
We describe here our attempts to optimise the human fatty acid amide hydrolase (FAAH) inhibition and physicochemical properties of our previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084. We describe the SAR of a series of analogues and conclude with the demonstration of in vivo dose-dependant FAAH inhibition in an anandamide-loading study in rats.
Benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives useful as D4 antagonists
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, (2008/06/13)
The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
2-halo-pyridines
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, (2008/06/13)
2-Halo-pyridines of the general formula I STR1 wherein X is Cl or Br; A is =0 or STR2 Ar is phenyl or substituted phenyl of the general formula STR3 in which n is 0, 1, 2 or 3; R is alkyl C1-4, alkoxy C1-4, phenoxy, alkylthio C1-4, halogen especially F and Cl, OH or C6 H5 ; and their salts, addition compounds and precursors (prodrugs). Furthermore the invention is directed to the production of these compounds and pharmaceuticals containing them.
