- BENZOFURAN-2-SULFONAMIDES DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
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The present invention relates to novel benzofuran-2-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
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Paragraph 0329; 0330; 0331
(2013/09/12)
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- Identification of a sulfonamide series of CCR2 antagonists
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A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pKa, yielded highly potent CCR2 antagonists exh
- Peace, Simon,Philp, Joanne,Brooks, Carl,Piercy, Val,Moores, Kitty,Smethurst, Chris,Watson, Steve,Gaines, Simon,Zippoli, Mara,Mookherjee, Claudette,Ife, Robert
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scheme or table
p. 3961 - 3964
(2010/09/03)
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- IRON CATALYZED CROSS-COUPLING REACTIONS OF IMIDOYL DERIVATIVES
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Disclosed is a process for preparing a compound of formula A - N=C(D)(B), from a compound of formula A-N=C(E)(B) and a compound of formula D-M using an iron catalyst, where the process has is represented by Equation (I).
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Page/Page column 19; 48
(2010/11/27)
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- Iron-catalyzed cross-coupling of imidoyl chlorides with Grignard reagents
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A general, high yielding rapid iron-catalyzed cross-coupling reaction between Grignard reagents and imidoyl chlorides is described. These reactions are typically completed within 5 min, resulting in high yields of 71-96% using 5% iron catalyst in a THF-NM
- Ottesen, Lars K.,Ek, Fredrik,Olsson, Roger
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p. 1771 - 1773
(2007/10/03)
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- USE OF N-DESMETHYLCLOZAPINE AND RELATED COMPOUNDS AS DOPAMINE STABILIZING AGENTS
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Disclosed herein is the use of N-desmethylclozapine (NDMC) and related compounds to treat a variety of neuropsychiatric diseases including psychosis. It is shown that NDMC and related compounds are agonists or partial agonists at D2 and D3 dopamine receptors and thus may be effective as a dopamine stabilizing agent, allowing it to be used to treat or provide reduced incidence of Extrapyramidal symptoms (EPS) and/or tardive dyskinesias (TD). Also disclosed is administering NDMC and related compounds in combination with other anti-psychotic agents.
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Page/Page column 113
(2010/11/24)
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- AMINO SUBSTITUTED DIARYL[A,D]CYCLOHEPTENE ANALOGS AS MUSCARINIC AGONISTS AND METHODS OF TREATMENT OF NEUROPSYCHIATRIC DISORDERS
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Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.
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Page/Page column 94
(2008/06/13)
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