- SELECTIVE OCTAHYDRO-CYCLOPENTA[C] PYRROLE NEGATIVE MODULATORS OF NR2B
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Compounds that selectively negatively modulate NMDA receptors containing an NR1/NR2B subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed. Such diseases include, without limitation, neurological dysfunction such as Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, and seizure disorders; emotional disorders; depression; bipolar disorder; obsessive-compulsive disorder; and other anxiety disorders.
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- SYNTHESIS OF BACE1 INHIBITORS
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The present invention provides a one step carbonylation of a compound of formula II in the presence of water to afford a compound of formula (I), useful in processes to manufacture BACE inhibitors.
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Page/Page column 17
(2014/11/13)
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- FUSED AMINODIHYDROTHIAZINE DERIVATIVES
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The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; R is monofluoromethyl or difluoromethyl; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
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Page/Page column
(2014/07/08)
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- FUSED AMINODIHYDROTHIAZINE DERIVATIVES
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The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine;A is CH or N;Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C≡N; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
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Page/Page column 34
(2012/07/31)
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- FUSED AMINODIHYDROTHIAZINE DERIVATIVES USEFUL AS BACE INHIBITORS
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The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or -C≡N; and pharmaceutically acceptable salts thereof; which compound has an Αβ production inhibitory effect or a BACEl inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Αβ and typified by Alzheimer-type dementia.
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Page/Page column 67
(2012/08/07)
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- FUSED AMINODIHYDROTHIAZINE DERIVATIVES
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The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; R is monofluoromethyl or difluoromethyl; and pharmaceutically acceptable salts thereof; which compound has an Αβ production inhibit
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Page/Page column 86-87
(2012/08/07)
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- NEW COMPOUNDS 806
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The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.
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Page/Page column 157-158
(2008/12/08)
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