- ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF
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The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.
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Page/Page column 28
(2008/12/06)
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- BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
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Page/Page column 100-101
(2010/11/27)
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- 2,9-DIAMINO- AND 2-AMINO-8-CARBAMOYL-4-HYDROXY-ALKANOIC ACID AMIDE DERIVATIVES
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Compounds of the formula I STR1 in which R 1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a carbonyl or methylene group, R 2 and R 3 independently of one another are hydrogen or lower alkyl or, together with the carbon atom with which they are bonded, are a cycloalkylidene radical, R 4 is hydrogen, lower alkyl, lower alkanoyl or lower alkoxycarbonyl, R 5 is hydroxyl, lower alkanoyloxy or lower alkoxycarbonyloxy, R 6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, aryl-lower alkyl or heteroaryl-lower alkyl having 5 to 7 ring atoms in the heteroaryl ring and R 7 is hydrogen or lower alkyl, or R 6 and R. sub.7, together with the carbon atom with which they are bonded, are a cydoalkylidene radical and R 8 denotes an aliphatic, cycloaliphatic-aliphatic or heteroarylaliphatic radical, and their salts can be used as active ingredients for medicaments for treatment of high blood pressure.
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- Reduction of Quinolinecarboxylic Acids by Raney Alloy
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The heterocyclic nucleus in quinolinecarboxylic acids is reduced by Raney alloy (nickel-aluminium) in alkaline media to give 1,2,3,4-tetrahydro-2-,3-,4-,5-,6-, and 8-quinolinecarboxylic acids and 8-methyl-5-quinolinecarboxylic acid and their ethyl esters.
- Gracheva, I. N.,Tochilkin, A. I.
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