- FATTY ACID CYSTEAMINE CONJUGATES OF CFTR MODULATORS AND THEIR USE IN TREATING MEDICAL DISORDERS
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The invention relates to fatty acid cysteamine conjugates of a CFTR modulator, compositions comprising a fatty acid cysteamine conjugate of a CFTR modulator, and methods for using such conjugates and compositions to treat disease, such as a disease caused
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Paragraph 00203
(2016/06/14)
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- Synthesis and characterization of an unsymmetrical cobalt(III) active site analogue of nitrile hydratase
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The design, synthesis, and characterization of an unsymmetrical diamidato-dithiol ligand (H4 1, where the hydrogen atoms represent deprotonatable amide and thiol protons) and its cobalt(III) complex, a synthetic analogue of the cobalt-containin
- Angelosante, Jennifer K.,Schopp, Lauren M.,Lewis, Breia J.,Vitalo, Amber D.,Titus, Dustin T.,Swanson, Rebecca A.,Stanley, April N.,Abolins, Brendan P.,Frome, Michelle J.,Cooper, Lisa E.,Tierney, David L.,Moore, Curtis,Rheingold, Arnold L.,Daley, Christopher J. A.
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experimental part
p. 937 - 947
(2012/05/04)
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- Unsaturated hydroxyalkylquinoline acids as leukotriene antagonists
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Compounds having the formula I: STR1 are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
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- Fluorinated hydroxyalkylquinoline acids as leukotriene antagonists
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Compounds having the formula I: STR1 are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
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- HYDROXYALKYLQUINOLINE ETHER ACIDS AS LEUKOTRIENE ANTAGONISTS
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Compounds having the formula I: STR1 are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina
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- Synthesis and pharmacological activities of novel cyclic disulfide and cyclic sulfide derivatives as hepatoprotective agents
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In order to search for anti-hepatitis drugs, we synthesized a series of eight- and nine-membered cyclic disulfides (1) and six- and seven-membered cyclic sulfides (2) and evaluated them for ability to reduce mortality in the model of acute hepatic failure
- Ito,Ota,Suhara,Tabashi,Kawashima
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p. 1066 - 1073
(2007/10/02)
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- Synthetic Approaches towards the Novel 1,3-Dioxo-1,2-dithiolane Moiety in the Antitumour Antibiotic Substance Leinamycin
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A number of complementary synthetic approaches to the β-thiolactone intermediate 9 for elaboration to the novel 1,3-dioxo-1,2-dithiolane moiety 6 found in the antitumour antibiotic substance leinamycin 1 are described.Thus, deprotection of the benzylthio ether produced from 3-methylbut-2-enoic acid and toluene-α-thiol, leads to the mercapto acid 12 which on cyclisation produces the thiolactone 13. α-Methylation of the thiolactone 13, followed by α-oxygenation then gives rise to the substituted β-thiolactone 9.The β-thiolactone 9 is also produced when: (i) thesodium glycidate 17 is stirred with sodium sulfide leading to 18, followed by thiolactonisation; (ii) thioacetone is treated with the ketene derived from 2-acetoxypropanoyl chloride; and (iii) by irradiation of 3-methyl-2-trimethylsilyloxybut-2-ene 22 with thiophosgene leading to 23, followed by hydrolysis.The β-thiolactone 9 is then converted in three steps into the 1,3-dioxo-1,2-dithiolane 6 by: (i) ring opening to the thioic acid 15, using hydrogen sulfide-triethylamine; (ii) ring closure of 15 to 8 in the presence of aqueous ferric chloride; and finally (iii) oxidation using dimethyldioxirane.Treatment of the ethyl glycidate 19 with disodium disulfide in hot ethanol for 3 days provides the 1,2-dithiolane 8 directly, but in low yields (11-15percent).When the aforementioned reaction sequences are translated to the glycidate 24, derived from 4-methylcyclohex-3-enone and α-chloropropanoic acid, the syntheses of the key intermediates 25, 27 and 26 en route to the spiro-fused 1,3-dioxo-1,2-dithiolane 7 and leinamycin 1 (see Scheme 1) were secured.
- Pattenden, Gerald,Shuker, Anthony J.
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p. 1215 - 1222
(2007/10/02)
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