- 1-(HET)ARYLSULFONYL-(PYRROLIDINE OR PIPERIDINE)-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS TRPA1 ANTAGONISTS
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The invention is concerned with the compounds of formula I and salts thereof and other compounds of formulas II-IX as disclosed herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formulas I-IX as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain or asthma.
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Paragraph 01183; 01184; 01185
(2016/09/22)
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- OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS
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The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in pharmaceutically acceptable salt form, to their preparation, to their medical use and to medicaments comprising them.
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Page/Page column 78
(2012/07/28)
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- Bridged 5,6,7,8-tetrahydro-1,6-naphthyridines, analogues of huperzine A: Synthesis, modelling studies and evaluation as inhibitors of acetylcholinesterase
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Derivatives of 6,8-bridged 5,6,7,8-tetrahydro-1,6-naphthyrid-ines, designed as analogues of huperzine A, were synthe-sised and evaluated as inhibitors of acetylcholinesterase. In a first approach, C3-bridged naphthyridines were constructed by internal nucleophilic aromatic substitution of 2-chloro-3-(1-piperidinylmethyl)pyridine precursors containing a 3-CO 2Me group on the 1-piperidinyl ring moiety. Alternatively, ring-closing metathesis on 6,8-diallyl-substituted tetrahydro-1,6-naphthyridines was applied to construct an unsaturated C4 bridge. Some of the target compounds showed inhibition of acetylcholinesterase but lower than that of huperzine A. The relative order of inhibition activities could be rationalised by comparative docking simulation studies on the basis of the known crystal structure of the ace-tylcholinesterase-huperzine A complex.
- Vanlaer, Sofie,Voet, Arnout,Gielens, Constant,De Maeyer, Marc,Compernolle, Frans
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experimental part
p. 643 - 654
(2009/07/17)
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- BETA-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS
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Provided are novel compounds having an inhibitory activity against production or secretion of β-amyloid protein. They embrace compounds represented by the following formula (1): and capable of being replaced with a variety of substituents; and salts thereof, and solvates of any one of them.
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