- A method for preparing thiol compounds
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The invention provides a preparation method of a thiol compound. According to the preparation method, gas-liquid reaction is carried out on sulfuretted hydrogen and an organic compound containing carbon-carbon double bonds in a solid base catalyst and a reaction solvent through Michael addition under the conditions that the temperature is 20-80 DEG C and the pressure is 0.10-0.12MPa, so as to prepare the thiol compound. The preparation method is mild in reaction condition; the adopted solid base catalyst is strong in alkalinity; the alkaline catalysis position has relatively strong steric hindrance, and the applicability is wide; the solid base catalyst is easy to filter and recover, and can be repeatedly used after being activated; the reaction conversion rate and the selectivity are high; the side reaction is reduced; and the atomic economic utilization rate of the reaction is high.
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Paragraph 0040-0041
(2017/05/12)
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- Core refinement toward permeable β-secretase (BACE-1) inhibitors with low hERG activity
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By use of iterative design aided by predictive models for target affinity, brain permeability, and hERG activity, novel and diverse compounds based on cyclic amidine and guanidine cores were synthesized with the goal of finding BACE-1 inhibitors as a treatment for Alzheimer's disease. Since synthesis feasibility had low priority in the design of the cores, an extensive synthesis effort was needed to make the relevant compounds. Syntheses of these compounds are reported, together with physicochemical properties and structure-activity relationships based on in vitro data. Four crystal structures of diverse amidines binding in the active site are deposited and discussed. Inhibitors of BACE-1 with 3 μM to 32 nM potencies in cells are shown, together with data on in vivo brain exposure levels for four compounds. The results presented show the importance of the core structure for the profile of the final compounds.
- Ginman, Tobias,Viklund, Jenny,Malmstr?m, Jonas,Blid, Jan,Emond, Rikard,Forsblom, Rickard,Johansson, Anh,Kers, Annika,Lake, Fredrik,Sehgelmeble, Fernando,Sterky, Karin J.,Bergh, Margareta,Lindgren, Anders,Johansson, Patrik,Jeppsson, Fredrik,F?lting, Johanna,Gravenfors, Ylva,Rahm, Fredrik
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p. 4181 - 4205
(2013/07/19)
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- ESTER PRODRUGS
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This invention relates to ester prodrugs for alkanoic acid compounds useful as leukotriene antagonists, and pharmaceutical compositions containing such ester prodrug compounds. This invention also relates to methods of treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
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- THIOPHENYL ALKANOIC ACIDS USEFUL AS LEUKOTRIENE ANTAGONISTS
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This invention relates to alkanoic acid compounds having phenyl and thio substituents which are useful as leukotriene antagonists and pharmaceutical compositions containing such compounds. This invention also relates to treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
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- Leukotriene antagonists
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This invention relates to alkanoic acid compounds having phenyl and thio substituents which are useful as leukotriene antagonists and pharmaceutical compositions containing such compounds. This invention also relates to methods of treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
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- Oxiranes
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There are described compounds of formula STR1 in which n is 0, 1 or 2, R1 is a hydrocarbyl group optionally substituted with an optionally substituted phenyl group and containing from 5 to 30 carbon atoms, R2 is optionally substitute
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- Amides of leurosine, leuroformine, desacetylleurosine and desacetylleuroformine
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C-3 Carboxamides of leurosine, leuroformine, 4-desacetylleurosine and 4-desacetylleuroformine, useful as antitumor agents.
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