- COMPOUNDS AS MODULATORS OF ROR GAMMA
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The present invention encompasses compounds of the formula (I)(I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
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Page/Page column 136
(2019/03/28)
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- COMPOUNDS AS MODULATORS OF ROR GAMMA
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The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
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Page/Page column 146-147
(2015/11/09)
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- INHIBITORS OF BETA-SECRETASE
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The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.
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Paragraph 0172-0173
(2014/03/24)
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- Total synthesis of hydroxy-α- and hydroxy-β-sanshool using Suzuki-Miyaura coupling
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Here, we describe the first total synthesis of hydroxyl-α- and hydroxyl-β-sanshool, which involves Suzuki-Miyaura coupling (SMC). Hydroxy-α-sanshool (1) was synthesized by SMC of bromoalkyne 4 with boronate 3 followed by (Z)-selective reduction of the triple bond in the coupling product. Hydroxy-β-sanshool (2) was synthesized by regio- and (E)-selective conversion of 4 to iodoalkene 11 followed by SMC with 3.
- Igarashi, Yasushi,Aoki, Katsuyuki,Nishimura, Hiroaki,Morishita, Isao,Usui, Kimitoshi
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experimental part
p. 1088 - 1091
(2012/10/07)
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