- ROR MODULATORS AND THEIR USES
-
The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR. The invention is based in part on the discovery of ROR modulators which interact with RORa and/or RORy and thereby inhibit or induce RORa and/or RORy-activity, and RORa- and/or RORy-regulated target gene and protein expression.
- -
-
Paragraph 0100
(2013/11/05)
-
- Polyvinylpyrrolidone-bromine complex: An efficient polymeric reagent for selective preparation of benzyl bromides in the presence of hexamethyldisilane
-
Benzylic bromides were conveniently obtained in high yields via the reaction of the corresponding alcohols with crosslinked polyvinylpyrrolidone- bromine complex (PVPP-Br2)/hexamethyldisilane in chloroform at reflux condition. Selective conversion of benzyl alcohol to benzyl bromide in the presence of primary aliphatic alcohols, e.g. 2-phenylethanol was also achieved.
- Mokhtary, Masoud,Lakouraj, Moslem M.
-
p. 305 - 309
(2012/10/29)
-
- An efficient synthesis of benzyl bromides from aromatic aldehydes using polymethylhydrosiloxane and (bromodimethyl)sulfonium bromide or N-bromosuccinimide
-
Polymethylhydrosiloxane (PMHS) in combination with (bromodimethyl)sulfonium bromide or NBS has been utilized for the first time for reductive bromination of aromatic aldehydes at room temperature to afford the corresponding benzyl bromides in excellent yields.
- Das, Biswanath,Srinivas, Yallamalla,Holla, Harish,Laxminarayana, Keetha,Narender, Ravirala
-
p. 6681 - 6683
(2008/03/12)
-
- A mild, phosphine-free method for the conversion of alcohols into halides (Cl, Br, I) via the corresponding O-alkyl isoureas
-
A novel procedure for the conversion of primary and secondary alcohols into the corresponding alkyl chlorides, bromides and iodides is described. The transformation is high-yielding in the case of chlorides and bromides, tolerates a range of functional groups, and does not rely on the use of phosphines.
- Li, Zhengning,Crosignani, Stefano,Linclau, Bruno
-
p. 8143 - 8147
(2007/10/03)
-
- Method for treating glaucoma
-
Methods of using prostaglandin agonists for the reduction of intraocular pressure, and accordingly glaucoma.
- -
-
-
- Prevention of loss and restoration of bone mass by certain prostaglandin agonists
-
Prostaglandin agonists of formula (I), in which, for example, A is a sulphonyl or acyl group, B is N or CH, M contains a ring and K and Q are linking groups, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits useful for the treatment of bone disorders including osteoporosis. STR1
- -
-
-
- Bromomethylation of aromatics mediated by low frequency ultrasound
-
We report herein bromomethylation of aromatics mediated by low frequency ultrasound to yield bromomethylated aromatic rings which are useful synthetic intermediates.
- Khurana, Jitender M.,Maikap, Golak C.
-
p. 216 - 217
(2007/10/03)
-
- Use of conjugated dienones in cyclialkylations: The total syntheses of (±)-barbatusol, (±)-pisiferin, (±)-deoxofaveline, (±)-xochitlolone, and (±)-faveline
-
Concise syntheses of five tricyclic diterpenoids are reported. The key reaction in each synthesis is a cyclialkylation of a functionalized arene with a Lewis acid-activated conjugated dienone to generate a 6,7,6-fused tricycle.
- Majetich, George,Hicks, Rodgers,Zhang, Yong,Tian, Xinrong,Feltman, Terry Lee,Fang, Jing,Duncan Jr., Sam
-
p. 8169 - 8185
(2007/10/03)
-
- Substituent effects on benzylic radical hydrogen hyperfine coupling constants. Part 4. The effect of branching of the alkyl substituent
-
The effects of substituents in the meta and para positions of the benzyl radical on the α-hydrogen hyperfine coupling constants (hfc's) are discussed.The electron spin resonance (esr) spectra of the para-methyl, ethyl, isopropyl, and tert-butyl substituted benzyl and cumyl radicals are analysed.Hyperconjugation involving the C-C bond is 40-60percent as effective as C-H hyperconjugation for delocalizing spin density.This conclusion is supported by INDO molecular orbital calculations.Similar analysis of the 13Cmr spectra of the para-alkyl substituted cumyl carbocations provides evidence that C-C hyperconjugation is 75-90percent as effective as C-H hyperconjugation for delocalizing charge density.
- Wayner, Danial D. M.,Arnold, Donald R.
-
p. 2378 - 2383
(2007/10/02)
-
- Unidirectional Dieckmann Cyclizations on a Solid Phase and in Solution
-
Dieckmann cyclization of 2percent divinylbenzene-copolystyrene resin alkyl pimelates and analogous benzyl alkyl pimelates is reported.The use of uniquely single-labeled dioate esters has allowed analysis of the direction of closure via decarboxylation of the keto ester products.The influence of steric factors on the competition between enolate condensation and transesterification and upon the direction of closure of the cyclization has been evaluated, and the conditions for achieving >99percent regioselective closure are described.Modifications in the conditions of solid-phase peptide synthesis required for successful high-temperature enolate cyclization have been developed and the results are compared to solution reactions of benzyl alkyl esters under similar conditions.The resin attachment afforded a clear benefit over the benzyl models and greatly simplified isolation and purification of the resulting β-keto esters.
- Crowley, John I.,Rapoport, Henry
-
p. 3215 - 3227
(2007/10/02)
-