- 5H-PYRROLO[3,4-£>]PYRAZIN-7-AMINE DERIVATIVES INHIBITORS OF BETA-SECRETASE
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The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β- amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
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Page/Page column 38-39
(2011/02/24)
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- NEW COMPOUNDS 574
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The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome,
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Page/Page column 21
(2010/06/13)
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- PHENOXY-PYRIDYL DERIVATIVES
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Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis
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Page/Page column 71-72
(2009/07/25)
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- Non-nucleoside reverse transcriptase inhibitors
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The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a, R5b, R6a, R6b and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
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Page/Page column 37
(2008/12/06)
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- BICYCLIC COMPOUNDS USEFUL AS CATHEPSIN S INBHIBITORS
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Compounds of formula (I), wherein R1, R2, R3, Ra and E are are defined within, and pharmaceutically acceptable salts, solvates, hydrates and N-oxides thereof having utility in the treatment of disorders mediated by cathepsin S.
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Page/Page column 40
(2010/11/29)
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- MONOAMINE RE-UPTAKE INHIBITORS AND METHODS RELATING THERETO
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Monoamine re-uptake inhibitors and more specifically serotonin and noradrenaline re-uptake inhibitors are disclosed that have utility in the treatment of disorders of the central or peripheral nervous system in both men and women. The compounds of this invention have the structure: wherein R1, R2, R3, R4, R5, R6, m, n, W, X, Y, and Z are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts, esters and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting monoamine re-uptake in a subject in need thereof.
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Page/Page column 29
(2010/11/25)
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- CATHEPSIN S INHIBITORS
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Compounds of the formula (I) where R1 is C1-C4 straight or branched alkyl, optionally substituted with up to three substituents selected from halo and hydroxy; R2 is halo, hydroxy, methyloxy, or C1-C2 alkyl, which alkyl is optionally substituted with up to three halogens or an hydroxy or a methyloxy; D is - C3-C7 alkylene-, thereby defining a cycloalkyl ring; E is -C(=O)-, -S(=O)m-, -NRdS(=O)m-, -NRaC(=O)-, -OC(=O)-, R3 is an optionally substituted carbocyclic or heterocyclic ring R10 is H, ORc, SRc or together with the gem H is =O or (ORc)2; Ra is independently selected from H, C1-C4 alkyl; have utility in the inhibition of cathepsin S and are thus useful pharmaceuticals against disorders such as autoimmune disorders and chronic pain.
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Page/Page column 95
(2010/11/08)
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- DIRECT FLUORINATION OF PHENOL AND CRESOLS
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A study has been made of the reaction of phenol with elemental fluorine using a variety of solvents and reaction temperatures.Yields of o- and p-fluorophenol were obtained as high as 85percent.The isomer ratio changed drastically between phenol conversions of 10percent and 56percent.The o-isomer changed to unidentified polymeric substances at higher conversion, but it might also be assumed that interconversion of some isomers is occuring.The three cresols have also been succesfully fluorinated with elemental fluorine. p-Cresol gave some expected 2-fluoroderivative but also formed a fluorocyclohexadienyl ketone.
- Misaki, Susumu
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p. 159 - 172
(2007/10/02)
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