- BIARYL DERIVATIVE AS GPR120 AGONIST
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The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
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Paragraph 0072
(2017/11/17)
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- BROMODOMAIN INHIBITORS
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The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
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- SULFAMATE AND SULFAMIDE DERIVATIVES FOR THE TREATMENT OF EPILEPSY AND RELATED DISORDERS
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The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical composlons containing them and their use in the treatment of epilepsy and related disorders.
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Page/Page column 44
(2010/02/15)
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- A highly efficient enantioselective synthesis of 2-methyl chromans via four sequential palladium-catalyzed reactions
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An enantioselective synthesis of substituted 2-methyl chromans was accomplished in four steps using four sequential Pd-catalyzed reactions. A study of the key palladium-catalyzed regioselective aryl ether ring formation of two different substrates was also carried out to better understand the factors which affect the selectivity of the reaction.
- Palucki, Michael,Yasuda, Nobuyoshi
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p. 987 - 990
(2007/10/03)
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- Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform
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This paper examines the relative effectiveness of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II (CA-II). Topiramate (1) and its sulfamide analogue 4, and 4,5-cyclic sulfate 6 and its sulfamide analogue 5, were compared for inhibition of human CA-II. A colorimetric assay, based on the pH shift that accompanies hydration of carbon dioxide, and an esterase assay were used. For these bioisosteric pairs, 1/4 and 6/5, the sulfamate compound was markedly more potent than its sulfamide counterpart. A similar, large difference in potency was also observed for the sulfamate/sulfamide pairs 14/15 and 16/17. These results indicate that the sulfamide moiety is not particularly suitable for obtaining potent carbonic anhydrase inhibition. A discussion of this structure-activity relationship with respect to the interactions of 1 and 6 with CA-II from published X-ray data is presented. A metabolic acidosis study was performed in rats with 1, 4, 6, and 2, and the results are discussed with respect to the degree of inhibition of CA-II in vivo.
- Maryanoff, Bruce E.,McComsey, David F.,Costanzo, Michael J.,Hochman, Coralie,Smith-Swintosky, Virginia,Shank, Richard P.
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p. 1941 - 1947
(2007/10/03)
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- Novel sulfamate and sulfamide derivatives useful for the treatment of epilepsy and related disorders
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The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders.
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Page/Page column 19
(2010/11/29)
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- A highly efficient, mild, and selective cleavage of beta-methoxyethoxymethyl (MEM) ethers by cerium(III) chloride in acetonitrile.
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[structure: see text]. A highly selective cleavage of MEM ethers has been achieved in high yields using CeCl3.7H2O in refluxing acetonitrile under mild and neutral reaction conditions. The method is very rapid and compatible with other hydroxyl protecting groups such as Bn, TBDPS, Ac, Me, Tr, PMB, benzylidene, THP, MOM, BOM, and NHAc present in the substrate.
- Sabitha,Babu,Rajkumar,Srividya,Yadav
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p. 1149 - 1151
(2007/10/03)
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- Benzopyran derivatives having leukotriene-antagonistic action
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The present invention relates to novel 4-oxo-4H-1-benzopyran compounds containing benzyloxymethyl, 3-phenylpropyl, or other araliphatic substituents in their 8-position. These compounds show a leukotriene-antagonistic activity. The compounds are characterized by good oral adsorption. The compounds of the present invention may be used as anti-inflammatory and antiallergic medicaments, and in the treatment of cardiovascular diseases.
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- PIPERIDYLMETHYL-SUBSTITUTED CHROMAN DERIVATIVES
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Piperidylmethyl-substituted chroman derivatives can be prepared by first reducing corresponding chromancarboxylic acid derivatives, if appropriate with prior activation, with the cyclic amines and then reducing the carbonyl group, or by reacting chromanme
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- Process and intermediates for 2R-benzyl-chroman-6-carbaldehyde
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Optically active (C1 -C3) alkyl 2R-chroman-2-carboxylates are prepared by partial hydrolysis of the corresponding racemic ester using a microbial lipase as catalyst. Said 2R-chromancarboxylate is converted via novel 2R-(hydroxymethyl) chroman, 2R-(trifluoromethylsulfonyloxymethyl) chroman and 2R-benzylchroman intermediates into 2R-benzylchroman-6-carbaldehyde, a compound of known utility in the manufacture of certain hypoglycemic agents.
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- Hydrogenated 1-benzooxacycloalkylpyridinecarboxylic acid compounds
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The invention relates to novel hydrogenated 1-benzooxacycloalkylpyridinecarboxylic acid compounds of formula STR1 in which the variable R1, R2, R3, R4, R5, alk, X, Z, m, n and p, the dotted line and t
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- Research of antiallergic agents: 2-hydroxymethylchromone and structural analogs
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The 2-hydroxymethylchromone as well as eight parent compounds, five of which are not previously described, were assayed in the passive cutaneous anaphylaxis test and in two tests for H1 antihistaminic activity. Their activity in the passive cutaneous anaphlyaxis test is similar to that of sodium cromoglycate used as reference in the same conditions, and is sometimes higher.
- Payard,Mouysset,Tronche,Bastide
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p. 117 - 120
(2007/10/02)
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