- THERAPEUTICALLY ACTIVE BICYCLIC-SULPHONAMIDES AND PHARMACEUTICAL COMPOSITIONS
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Pharmaceutical compounds have a bicyclic-sulphonamide structure and pharmaceutical compositions including the compounds may be used in therapy as brain-cell-death protectants and may be used, for example, in the treatment of chronic neurodegenerative diseases. The compounds are active as inhibitors of N-acylethanolamine-hydrolysing acid amidase (NAAA) and may be used for the therapeutic treatment and prevention of pain and inflammatory disorders and other disorders which benefit from the modulation of fatty acid ethanolamides, particularly palmitoylethanolamide (PEA).
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Paragraph 0086
(2019/05/18)
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- PYRIMIDINE DERIVATIVES AS GPCR MODTTLATORS FOR USE IN THE TREATMENT OF OBESITY AND DIABETES
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The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic di
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Page/Page column 46
(2010/07/09)
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- N-Bridged bicyclic sulfonamides as inhibitors of γ-secretase
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The structural modification of a series of [3.3.1] bicyclic sulfonamide based γ-secretase inhibitors is described. Appropriate substitution on the bicyclic scaffold provides a significant increase in the metabolic stability of the compounds resulting in an improved in vivo metabolic profile.
- Bowers, Simeon,Probst, Gary D.,Truong, Anh P.,Hom, Roy K.,Konradi, Andrei W.,Sham, Hing L.,Garofalo, Albert W.,Wong, Karina,Goldbach, Erich,Quinn, Kevin P.,Sauer, John-Michael,Wallace, William,Nguyen, Lan,Hemphill, Susanna S.,Bova, Michael P.,Basi, Guriqbal S.
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scheme or table
p. 6952 - 6956
(2010/06/16)
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- BRIDGED N-CYCLIC SULFONAMIDO INHIBITORS OF GAMMA SECRETASE
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The invention provides N-cyclic sulfonamido compounds and salts of Formula (I): wherein A is as described in the specification and R1 and R2combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula (I) are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula (I).
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Page/Page column 74-75
(2010/11/26)
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