- PROCESSES FOR THE SYNTHESIS OF SUBSTITUTED UREA COMPOUNDS
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The present invention concerns a process for preparing a compound having the Formula A; or a pharmaceutically acceptable salt or derivative thereof, or for preparing a substituted urea compound of Formula IIa, or a pharmaceutically acceptable salt or ester thereof, (Formula IIa) the process comprising the reaction of an imidazolyl intermediate of Formula IIa', with a carbamoyl halide of the formula: R1R2NC(=O)Hal, wherein Hal represents Cl, F, I or Br, wherein the intermediate of Formula IIa' is prepared by oxidation of the derivative of R5 and R6, R6-C(=O)CH2R5 to form a glyoxal intermediate R6-C(=O)(C=O)R5, which is subjected to treatment with ammonium hydroxide and an aldehyde R8CHO to provide the intermediate of Formula IIa', and wherein the compound substituents are as defined herein.
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Page/Page column 36; 37
(2015/10/05)
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- UREA COMPOUNDS AND THEIR USE AS FAAH ENZYME INHIBITORS
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A compound having Formula (I): wherein: R1 is selected from hydrogen, halogen, hydroxyl and C1-4 alkoxy; R2 is selected from hydrogen, halogen, hydroxyl and C1-4 alkoxy; R3 is C1-4 alkyl; R4 is aryl which is substituted with a group selected from OSO2NH2, NHCONH2, NHSO2NH2, NHSO2C1-4 alkyl and CONH2; and n is 0 or 1; or a pharmaceutically acceptable salt thereof; provided that the compound is not N-(1-benzylpiperidin-4-yl)-N-methyl-4-(4-(sulfamoylamino)phenyl)-1H-imidazole-1-carboxamide or N-(1-benzylpiperidin-4-yl)-N-methyl-4-(3-(methylsulfonamido)phenyl)-1H-imidazole-1-carboxamide. The compound may be used as an inhibitor of fatty acid amide hydrolase.
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Page/Page column 23; 24
(2015/02/25)
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- UREA COMPOUNDS AND THEIR USE AS ENZYME INHIBITORS
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A compound having the following structure: or a pharmaceutically acceptable salt or derivative thereof. The compound may be used in the treatment or prevention of a disorder selected from appetite regulation, obesity, metabolic disorders, cachexia, anorexia, pain, inflammation, neurotoxicity, neurotrauma, stroke, multiple sclerosis, spinal cord injury, Parkinson's disease, levodopa-induced dyskinesia, Huntington's disease, Gilles de la Tourette's syndrome, tardive dyskinesia, dystonia, amyotrophic lateral sclerosis, Alzheimer's disease, epilepsy, schizophrenia, anxiety, depression, insomnia, nausea, emesis, alcohol disorders, drug addictions such as opiates, nicotine, cocaine, alcohol and psychostimulants, hypertension, circulatory shock, myocardial reperfusion injury, atherosclerosis, asthma, glaucoma, retinopathy, cancer, inflammatory bowel disease, acute and chronic liver disease such as hepatitis and liver cirrhosis, arthritis and osteoporosis.
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Page/Page column 16
(2014/02/16)
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- Synthesis and histamine H3 and H4 receptor activity of conformationally restricted cyanoguanidines related to UR-PI376
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Recently, we identified highly potent agonists of the human histamine H4 receptor (hH4R) among a series of imidazolylbutylcyanoguanidines. Aiming at improved selectivity for the hH 4R relative to the H3 receptor
- Geyer, Roland,Buschauer, Armin
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p. 775 - 785
(2012/03/12)
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- Optimization of 1,3,4-benzotriazepine-based CCK2 antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion
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Starting from a novel, achiral 1,3,4-benzotriazepine-based CCK2 receptor antagonist, a process of optimization has afforded further compounds of this type that maintain the nanomolar affinity for recombinant, human CCK2 receptors and high selectivity over
- McDonald, Iain M.,Black, James W.,Buck, Ildiko M.,Dunstone, David J.,Griffin, Eric P.,Harper, Elaine A.,Hull, Robert A. D.,Kalindjian, S. Barret,Lilley, Elliot J.,Linney, Ian D.,Pether, Michael J.,Roberts, Sonia P.,Shaxted, Mark E.,Spencer, John,Steel, Katherine I. M.,Sykes, David A.,Walker, Martin K.,Watt, Gillian F.,Wright, Laurence,Wright, Paul T.,Xun, Wei
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p. 3101 - 3112
(2008/02/09)
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- Binding of Imidazole-Derived Nucleosides to a CG Base Pair
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Novel imidazole nucleosides with substituents of different flexibility were studied for their binding to a CG Watson-Crick base pair by 1H NMR spectroscopy in an aprotic solvent. Thermodynamic data as determined by titration experiments at diff
- Purwanto, Maria G. M.,Weisz, Klaus
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p. 195 - 197
(2007/10/03)
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- Recognition of all four base pairs of double-helical DNA by triple-helix formation: Design of nonnatural deoxyribonucleosides for pyrimidine-purine base pair binding
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The sequence-specific recognition of double-helical DNA by oligonuclcotide-directed triple-helix formation is limited mostly to purine tracts. Design leads that could expand the recognition code to all four Watson-Crick base pairs would provide one step t
- Griffin, Linda C.,Kiessling, Laura L.,Beal, Peter A.,Gillespie, Paul,Dervan, Peter B.
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p. 7976 - 7982
(2007/10/02)
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- CARBENIC REACTIONS OF 4-DIAZO-4H-IMIDAZOLE WITH BENZENE DERIVATIVES
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The electrophilic behavior of 4H-imidazolylidene is greatly modified by coordinating groups in benzene derivatives undergoing substitution.
- Amick, T. J.,Shechter, H.
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p. 901 - 904
(2007/10/02)
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