5813-37-6Relevant academic research and scientific papers
THIAZOLE DERIVATIVES AS SGLT2 INHIBITORS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Page/Page column 53, (2012/01/06)
The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.
NAPHTHALENE CARBOXAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 32, (2011/12/14)
The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
NOVEL C-ARYL GLUCOSIDE SGLT2 INHIBITORS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Page/Page column 110, (2010/12/31)
A novel C-aryl glucoside compound, or a pharmaceutically acceptable salt or a prodrug thereof having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney; and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly, diabetes, are provided.
NEW CXCR2 INHIBITORS
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Page/Page column 156, (2008/06/13)
The invention relates to compounds of the formula (I), in which R1, R2, X, A, B, Z and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands
Huang,Luedtke,Freeman,Wu,Mach
, p. 1815 - 1826 (2007/10/03)
A series of naphthamides were synthesized, and the affinities of these compounds were determined for dopamine D2 and D3 receptors using radioligand binding techniques. The naphthamide compounds that were prepared include N-(1- alkylp
Structure-activity relationship studies of N-(9-benzyl)-9- azabicyclo[3.3.1]nonan-3-β-yl benzamide analogues for dopamine D2 and D3 receptors
Mach, Robert H.,Hammond, Philip S.,Huang, Yunsheng,Yang, Biao,Xu, Yueping,Cheney, Jason T.,Freeman, Rebekah,Luedtke, Robert R.
, p. 355 - 373 (2007/10/03)
A series of benzamide derivatives were prepared in order to determine the nature of the substituent effects in the benzamide aromatic ring on the affinity to dopamine D2 and D3 receptors. Both quantitative structure- activity relatio
Metal ion catalysis of the decomposition of transient 2-carboxy-2,5-cyclohexadienones in aqueous solution
Tee, Oswald S.,Iyengar, N. Rani
, p. 1194 - 1198 (2007/10/02)
Bromide ion induced debromination of the anion of 4-bromo-4-methyl-2,5-cyclohexadienone-2-carboxylic acid (1) is catalyzed by cupric ions and ferric ions.Similarly, the enolization of the anion of the benzocyclohexadienone 3, which is formed during the bromination of 1-naphthol-2-carboxylic acid, is catalyzed by some metal ions.The origin of the catalysis in these reactions is strong metal ion binding to the incipient dianion products that are of the salicylate type.Evidence for this is that the efficiency of the metal (and hydrogen) ion catalysis parallels the stability of the analogous complexes with the salicylate dianion.
Enolization of the benzocyclohexadienone formed during the bromination of 1-naphthol in aqueous solution
Tee, Oswald S.,Iyengar, N. Rani
, p. 1714 - 1718 (2007/10/02)
Benzo-4-bromo-2,5-cyclohexadienone (5) has been observed in the aqueous bromination of 1-naphthol and the kinetics of its enolization to 4-bromo-1-naphthol have been studied in the pH range 0-7.This process is catalyzed by the proton, hydroxide ion, water, buffer acids, and by buffer bases.For ctalysis by general bases the Broensted β = 0.59 whereas catalysis by general acids has a value of α ca. 0.These findings are very similar to those obtained previously for the 4-bromo-2,5-cyclohexadienone 2b, formed during the aqueous bromination of 2,6-dimethylphenol.The mechanistic implications of the results are discussed.The enolization of the related dienone 8, formed from bromine and 1-naphthol-2-carboxylic acid, was also studied.At acidic pHs the dienone 8 is much more reactive than 5, with the 2-COOH behaving as an internal catalyst having an "effective molarity" of about 110 M.The enolization of 8 is also catalyzed by buffer bases.
