- COMPOUNDS AND THEIR USE AS BACE1 INHIBITORS
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The present invention relates to compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein X, Y, Z, Q, W, m, u, ring (A), R2, R3, R4, R5 and R6, are as defined in the specification and claims. The present invention provides a pharmaceutical composition containing the compounds of Formula (I) and a therapeutic method of treating and/or preventing Downs syndrome, β-amyloid angiopathy, disorders associated with cognitive impairment, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegenerative diseases, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, Alzheimer's disease and/or Down syndrome, age-related macular degeneration (AMD), glaucoma, olfactory function impairment, traumatic brain injury, progressive muscle diseases, Type II diabetes mellitus and cardiovascular diseases (stroke).
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Page/Page column 96; 97
(2016/11/17)
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- ISOTHIOUREA DERIVATIVES OR ISOUREA DERIVATIVES HAVING BACE1 INHIBITORY ACTIVITY
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The present invention provides, for example, a compound of the following formula (I): wherein R1 is substituted amino and the like, R2 is halogen and the like, R3 is substituted or unsubstituted lower alkyl and the like, RA and RB are each independently hydrogen, substituted or unsubstituted lower alkyl and the like, RC and RD are each independently hydrogen, substituted or unsubstituted lower alkyl, or RC and RD together with the carbon atom to which they are attached may form a substituted or unsubstituted carbocycle, and ring A is a carbocycle or a heterocycle, its pharmaceutically acceptable salt, or a solvate thereof as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-βproteins.
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Page/Page column 41
(2012/02/01)
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- 4-AMINO-1,3-THIAZINE OR OXAZINE DERIVATIVE
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The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-β proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3a
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Page/Page column 39
(2012/10/18)
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- 9-Arylpurines as a novel class of enterovirus inhibitors
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Here we report on a novel class of enterovirus inhibitors that can be structurally described as 9-arylpurines. These compounds elicit activity against a variety of enteroviruses in the low μM range including Coxsackie virus A16, A21, A24, Coxsackie virus B3, and echovirus 9. Structure-activity relationship (SAR) studies indicate that a chlorine or bromine atomis required at position 6 of the purine ring for antiviral activity. The most selective compounds in this series inhibited Coxsackie virus B3 replication in a dose-dependent manner with EC50 values around 5-8 μM. Notoxicity on different cell lineswas observed at concentrations up to 250 μM. Moreover, no cross-resistance to TBZE-029 and TTP-8307 CVB3 resistant strains was detected.
- Aguado, Leire,Thibaut, Hendrik Jan,Priego, Eva-María,Jimeno, María-Luisa,Camarasa, María-José,Neyts, Johan,Pérez-Pérez, María-Jesús
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experimental part
p. 316 - 324
(2010/05/02)
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- AMINODIHYDROTHIAZINE DERIVATIVES SUBSTITUTED WITH CYCLIC GROUPS
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This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alk
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Page/Page column 29
(2010/02/17)
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- Synthesis of fluorinated 1-(3-Morpholin-4-yl-phenyl)-ethylamines
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The synthesis of four (±)-fluorinated 1-(3-morpholin-4-yl-phenyl)-ethylamines and an enantioselective approach to these amines through reductive amination are described.
- Wu, Yong-Jin,He, Huan,Sun, Li-Qiang,Wu, Dedong,Gao, Qi,Li, Hui-Yin
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p. 1725 - 1728
(2007/10/03)
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- Benzenesulphonamide derivatives, preparation thereof and therapeutical uses thereof
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Benzenesulphonamide compounds of general formula (I), wherein R1is a hydrogen or halogen atom such as chlorine or fluorine, or a straight or branched C1-4alkyl or C1-4alkoxy group, each of R2, R3and R4, which are the same or different, is a hydrogen atom or a straight, branched or cyclic C1-4alkyl group, and R1is a hydrogen atom or a C1-2alkyl, C1-2fluoroalkyl or C1-2perfluoroalkyl group, in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures, as well as pharmaceutically acceptable acid addition salts thereof, are provided for therapeutical use.
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- Preparation of fluorinated anilines
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Fluorinated anilines, especially p-fluoroaniline and 2,4-difluoroaniline, are prepared by treating aromatic azides with anhydrous hydrogen fluoride. The aromatic azides, in turn, are prepared from the corresponding anilines by treatment with nitrous acid or salt thereof and an alkali metal azide in the presence of a mineral acid, and in an aqueous-nonaqueous, two-phase environment.
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