- LXR MODULATORS
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The present invention provides compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as modulators of liver X receptors (LXR), compositions comprising any of such novel compounds, methods of using these compounds or compositions as medicaments for prevention or treatment of diseases or disorders related to liver X receptor (LXR), as well as methods of preparing these LXR modulators and using them in the manufacture of medicaments.
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Page/Page column 77
(2014/09/29)
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- Pyrimidine compounds and methods of making and using same
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Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.
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Page/Page column 53
(2013/02/27)
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- Lewis-acid-promoted arylation reaction: Synthesis of dihydrobenzofuran derivatives from aryltriazenes
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A Lewis-acid-promoted approach to the synthesis of highly functionalized dihydrobenzofuran derivatives was developed. A diverse range of functional groups are tolerated in this type of reaction. The reaction mechanism investigation indicates that the highly reactive phenyl cation intermediate is probably involved in this process. The chirality of substrate is retained under the reaction conditions.
- Zhao, Guoqing,Wang, Binjie,Yang, Weijun,Ren, Hongjun
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p. 6236 - 6247
(2013/01/15)
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- Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists
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We have developed a new class of diarylalkyl amides as novel TRPV1 antagonists. They exhibited potent 45Ca2+ uptake inhibitions in rat DRG neuron. In particular, the amide 59 was identified as a potent antagonist with IC50 of 57 nM. The synthesis and structure-activity relationship of the diarylalkyl amides are also described.
- Li, Fu-Nan,Kim, Nam-Jung,Paek, Seung-Mann,Kwon, Do-Yeon,Min, Kyung Hoon,Jeong, Yeon-Su,Kim, Sun-Young,Park, Young-Ho,Kim, Hee-Doo,Park, Hyeung-Geun,Suh, Young-Ger
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experimental part
p. 3557 - 3567
(2009/09/27)
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- N-phenpropylcuclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
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The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
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- Mo(CO)6 catalyzed one-pot conversion of allyl aryl ethers to dihydrobenzofurans
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Molybdenum hexacarbonyl effectively catalyses a tandem Claisen rearrangement-cyclization reaction of allyl aryl ethers to give good yields of dihydrobenzofurans.
- Bernard, Angela M.,Cocco, Maria T.,Onnis, Valentina,Piras, Pier P.
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- Benzoheterocyclyl ketone hydrazone insecticides
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Benzoheterocyclyl ketone hydrazones of the formula STR1 in which Y is methylene, difluoromethylene or oxygen and n is 0 or 1, compositions thereof and their use as insecticides are disclosed and exemplified.
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