- Rhodium-Catalyzed ipso-Borylation of Alkylthioarenes via C-S Bond Cleavage
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Rhodium-catalyzed transformation of alkyl aryl sulfides into arylboronic acid pinacol esters via C-S bond cleavage is reported. In combination with transition-metal-catalyzed sulfanyl group-guided regioselective C-H borylation reactions of alkylthioarenes, this method allows the synthesis of a diverse range of multisubstituted arenes.
- Uetake, Yuta,Niwa, Takashi,Hosoya, Takamitsu
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supporting information
p. 2758 - 2761
(2016/06/15)
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- FUSED THIOPHENE AND THIAZOLE DERIVATIVES AS ROR GAMMA MODULATORS
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The present invention provides fused thiophene and thiazole derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; in which R1, R2, R3, R4, R5, R6, R7, X1, X2, L, m, n and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in disease(s) or disorder(s) where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the fused thiophene and thiazole derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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- TRISUBSTITUTED HETEROCYCLIC DERIVATIVES AS ROR GAMMA MODULATORS
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The present invention provides trisubstituted heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; (I) in which R1, R2, R3, Ra, X, L, m and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the trisubstituted heterocyclic derivatives of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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Page/Page column 31; 34
(2014/09/03)
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- Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients
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Glucokinase (GK) activation as a potential strategy to treat type 2 diabetes (T2D) is well recognized. Compound 1, a glucokinase activator (GKA) lead that we have previously disclosed, caused reversible hepatic lipidosis in repeat-dose toxicology studies.
- Sarabu, Ramakanth,Bizzarro, Fred T.,Corbett, Wendy L.,Dvorozniak, Mark T.,Geng, Wanping,Grippo, Joseph F.,Haynes, Nancy-Ellen,Hutchings, Stanley,Garofalo, Lisa,Guertin, Kevin R.,Hilliard, Darryl W.,Kabat, Marek,Kester, Robert F.,Ka, Wang,Liang, Zhenmin,Mahaney, Paige E.,Marcus, Linda,Matschinsky, Franz M.,Moore, David,Racha, Jagdish,Radinov, Roumen,Ren, Yi,Qi, Lida,Pignatello, Michael,Spence, Cheryl L.,Steele, Thomas,Tengi, John,Grimsby, Joseph
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supporting information
p. 7021 - 7036
(2012/11/07)
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- 5-(4-methanesulfonyl-phenyl)-thiazole derivatives for the treatment of acute and chronic inflammatory diseases
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The invention relates to the use of a compound of formula (I): or a pharmaceutically acceptable salt, prodrug and/or solvate thereof, in the preparation of a medicament for the treatment of an acute or chronic inflammatory disease, by inhibiting the produ
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Page/Page column 15
(2009/12/28)
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- 5-(4-METHANESULFONYL-PHENYL)-THIAZOLE DERIVATIVES FOR THE TREATMENT OF ACUTE AND CHRONIC INFLAMMATORY DISEASES
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The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt, prodrug and/or solvate thereof, and to a method for the treatment an acute or chronic inflammatory disease by inhibiting the production of at least one pro-inflamma
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Page/Page column 9-10
(2009/12/27)
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- CYCLIC TERTIARY AMINE COMPOUND
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The present invention provides a cyclic tertiary amine compound which is capable of inhibiting the production of inflammatory cytokines. It is either a compound having a structure represented by the following general formula (I): (wherein A represents an optionally substituted trivalent group derived from pyrimidine, pyrrole, or the like; R1 represents an aryl or a heteroaryl group which may optionally be substituted; R2 represents a heteroaryl group which may optionally be substituted; and R3 represents a cyclic tertiary amino group) or a pharmacologically acceptable salt of the compound.
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Referential example 7
(2010/11/08)
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- Synthesis and selective cyclooxygenase-2 (COX-2) inhibitory activity of a series of novel bicyclic pyrazoles
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Novel series of pyrazolo[5,1-b]1,3-oxazolidines, pyrazolo[5,1-b]1,3- oxazines and imidazolidino[1,2-d]pyrazoles were synthesized. These compounds were evaluated in vitro for their ability to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) in human whole blood (HWB). Several of the compounds were found to be novel and selective COX-2 inhibitors, the most potent and selective being 1-(5-cyclohexyl (2H,3H-pyrazolo[5,1-b]-1,3- oxazolidin-6-yl)-4-(methylsulfonyl)benzene, 7a (IC5o for COX-1>100 μM; for COX-2=1.3 μM).
- Ranatunge, Ramani R.,Garvey, David S.,Janero, David R.,Letts, L. Gordon,Martino, Allison M.,Murty, Madhavi G.,Richardson, Stewart K.,Young, Delano V.,Zemetseva, Irina S.
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p. 1357 - 1366
(2007/10/03)
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- Substituted-cycloalkyl and oxygenated-cycloalkyl glucokinase activators
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2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
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- Fused heteroaromatic glucokinase activators
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Glucokinase activating amides are useful for increasing insulin secretion in the treatment of type II diabetes.
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- Heteroaromatic glucokinase activators
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2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
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