- New chiral and achiral imines and bisimines derived from 2-phenyl-1h-imidazole-4-carbaldehyde. Synthesis, structural studies and complexation stability constants
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Synthesis and properties of new imines and bisimines derived from 2-phenyl-1H-imidazole-4-carbaldehyde and amines/diamines were studied. (2-Phenyl-1H-imidazole-4-yl)methanol was oxidized to 2-phenyl-1H-imidazole-4- carbaldehyde with better yield 55% by th
- Parik,Chlupaty
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- 13C CPMAS NMR as a tool for full structural description of 2-phenyl substituted imidazoles that overcomes the effects of fast tautomerization
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Tautomerization of 2-phenylimidazolecarbaldehydes has not been studied in detail so far, although this process is a well-known phenomenon for imidazole derivatives. That is why we focus our study on a series of 2-phenylimidazolecarbaldehydes and their par
- Burdzhiev, Nikola,Ahmedova, Anife,Borrisov, Boris,Graf, Robert
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- PYRROLOPYRIMIDINES AS CFTR POTENTIATORS
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The present invention relates to compounds of Formula I, wherein R1a, R1b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiator
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Paragraph 0497; 0498; 0503; 0504
(2018/06/04)
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- PIPERIDINE-CONTAINING COMPOUNDS AND USE THEREOF
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A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I) wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.
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Page/Page column 168
(2010/08/04)
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- 5-Substituted imidazole-4-acetic acid analogues: Synthesis, modeling, and pharmacological characterization of a series of novel γ-aminobutyric acidC receptor agonists
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A series of ring-substituted analogues of imidazole-4-acetic acid (IAA, 4), a partial agonist at both GABAA and GABAC receptors (GABA = γ-aminobutyric acid), have been synthesized. The synthesized compounds 8a-1 have been evaluated a
- Madsen, Christian,Jensen, Anders A.,Liljefors, Tommy,Kristiansen, Uffe,Nielsen, Birgitte,Hansen, Camilla P.,Larsen, Mogens,Ebert, Bjarke,Bang-Andersen, Benny,Krogsgaard-Larsen, Povl,Fr?lund, Bente
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p. 4147 - 4161
(2008/02/13)
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- Highly potent geminal bisphosphonates. From pamidronate disodium (Aredia) to zoledronic acid (Zometa)
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Bisphosphonates (BPs) are pyrophosphate analogues in which the oxygen in P-O-P has been replaced by a carbon, resulting in a metabolically stable P-C-P structure. Pamidronate (1b, Novartis), a second-generation BP, was the starting point for extensive SAR studies. Small changes of the structure of pamidronate lead to marked improvements of the inhibition of osteoclastic resorption potency. Alendronate (1c, MSD), with an extra methylene group in the N-alkyl chain, and olpadronate (1h, Gador), the N,N-dimethyl analogue, are about 10 times more potent than pamidronate. Extending one of the N-methyl groups of olpadronate to a pentyl substituent leads to ibandronate (1k, Roche, Boehringer-Mannheim), which is the most potent close analogue of pamidronate. Even slightly better antiresorptive potency is achieved with derivatives having a phenyl group linked via a short aliphatic tether of three to four atoms to nitrogen, the second substituent being preferentially a methyl group (e.g., 4g, 4j, 5d, or 5r). The most potent BPs are found in the series containing a heteroaromatic moiety (with at least one nitrogen atom), which is linked via a single methylene group to the geminal bisphosphonate unit. Zoledronic acid (6i), the most potent derivative, has an ED50 of 0.07 mg/kg in the TPTX in vivo assay after sc administration. It not only shows by far the highest therapeutic ratio when comparing resorption inhibition with undesired inhibition of bone mineralization but also exhibits superior renal tolerability. Zoledronic acid (6i) has thus been selected for clinical development under the registered trade name Zometa. The results of the clinical trials indicate that low doses are both efficacious and safe for the treatment of tumor-induced hypercalcemia, Paget's disease of bone, osteolytic metastases, and postmenopausal osteoporosis.
- Widler, Leo,Jaeggi, Knut A.,Glatt, Markus,Müller, Klaus,Bachmann, Rolf,Bisping, Michael,Born, Anne-Ruth,Cortesi, Reto,Guiglia, Gabriela,Jeker, Heidi,Klein, Rémy,Ramseier, Ueli,Schmid, Johann,Schreiber, Gerard,Seltenmeyer, Yves,Green, Jonathan R.
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p. 3721 - 3738
(2007/10/03)
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- 2-Phenyl-4-(aminomethyl)imidazoles as Potential Antipsychotic Agents. Synthesis and Dopamine D2 Receptor Binding
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A series of 2-phenyl-4-(aminomethyl)imidazoles were designed as conformationally restricted analogs of the dopamine D2 selective benzamide antipsychotics.The title compounds were synthesized and tested for blockade of YM-09151 binding in cloned African green monkey dopamine D2 receptor preparations.The binding affinity data thus obtained were compared against that of the benzamides and a previously described series of 2-phenyl-5-(aminomethyl)pyrroles.
- Thurkauf, Andrew,Hutchison, Alan,Peterson, John,Cornfield, Linda,Meade, Robin,et al.
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p. 2251 - 2255
(2007/10/02)
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- Process for the production of hydroxymethylimidazoles
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This invention discloses a process for the production of hydroxymethylimidazoles which comprises reacting imidazolecarboxylic acids, their esters or inorganic salts with a formaldehyde agent in the presence of an alkali in an aqueous medium.
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