Cycloalkyl-containing carboxylic acids and uses thereof
A technology of alkyl and cycloalkane, applied in the field of cycloalkyl-containing carboxylic acid and its application, can solve problems such as edema and weight gain
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[0286] The preparation of solvates is generally known. Thus, for example, M. Caira et al., J. Pharmaceutical Sci., 93(3), 601-611 (2004) describe the preparation of solvates of antifungal fluconazole in ethyl acetate and water. Similar preparations of solvates, hemisolvates, hydrates, etc. are by E.C. van Tonder et al., AAPS Pharm SciTech., 5(1), paper 12 (2004); and A.L. Bingham et al., Chem. Commun., 603– 604 (2001) description. A typical non-limiting procedure involves dissolving a compound disclosed herein in the desired amount of the desired solvent (organic or water or a mixture thereof) at a temperature above ambient, and cooling the solution at a rate sufficient to form crystals, The crystals are then isolated by standard methods. Analytical techniques such as infrared spectroscopy show the presence of the solvent (or water) in the crystals as a solvate (or hydrate).
[0287] pharmaceutical composition
[0288] In another aspect, the present disclosure provides a...
Embodiment 1
[0339] Example 1 : Synthesis of compounds
[0340] All HPLC chromatograms and mass spectra were recorded on an HP 1100 LC-MS Agilent instrument using an analytical C18 column (250 x 4.6 mm, 5 microns) with a gradient of 15-99% acetonitrile-water with 0.01% trifluoro over 5 min Acetic acid was used as eluent and the flow rate was 2 mL / min.
[0341] General Scheme for the Preparation of 2-Cyclopropyl Acetate Compounds
[0342]
[0343] R=F, Cl, Br or Me
[0344] Compound I: Synthesis of sodium salt of 2-(2,2-difluoro-3-hexylcyclopropyl)acetic acid
[0345]
[0346] step 1 : 3-Decenoic acid (10 g, 58.7 mmol) was dissolved in methanol (100 mL) at room temperature. Concentrated sulfuric acid (0.5 mL) was added and the reaction was stirred for 16 h. Saturated sodium bicarbonate solution (100 mL) was added, and the mixture was extracted three times with ethyl acetate. The organic layers were combined, washed with brine and dried over anhydrous sodium sulfate. The ...
Embodiment 2
[0643] Example 2 : Effects of representative compounds disclosed herein on the induction of hemoglobin production in vitro
[0644] The effect of representative compounds disclosed herein on the induction of hemoglobin production in human myeloid chronic myeloid leukemia cells (K562) was assessed using a 2,7-diaminofluorene (DAF) assay by pseudo-passage of free hemoglobin. Oxidase activity to measure DAF oxidation. K562 cells were incubated with various compounds (compounds I, II and III) at the stated concentrations for 5 days. On day 5, cells were centrifuged and washed in PBS. make 2x10 6 Cells were lysed in 140 μl NP-40 (0.01%, 5 min on ice). 2 mg of DAF (2,7-diaminofluorene, 97%, Aldrich, catalog #D17106-1G) was resuspended in 200 μl glacial acetic acid 90% and a working solution was prepared as follows: 100 μl DAF + 100 μl H 2 O 2 30% + 10ml Tris-HCl 0.1M / 6M Urea pH 7, Vortex. 50 μl of cell lysate was transferred to wells and 150 μl of DAF working solution was ad...
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