- Sulfur-containing compound based on glutaryl imide skeleton and application of compound
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The present disclosure relates to compound shown in a formula (I) or salts, solvates, isotope-enriched analogs, tautomers, polymorphs, stereoisomers, or mixtures of stereoisomers of the compound, andthe application thereof in the treatment of tumours. The present disclosure also provides tumor treatment application of the compound showed in a formula (I') or pharmaceutically acceptable salts, solvates, isotope-enriched analogs, tautomers, polymorphic substances, stereoisomers, or mixtures of stereoisomers of the compound.
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Paragraph 0775-0776
(2020/09/12)
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- AMINOTRIAZOLE DERIVATIVES AS ALX AGONISTS
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The invention relates to aminotriazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds. The compounds are useful for the prevention or treatment of diseases, which respond to the modulation of the ALX receptor such as inflammatory diseases.
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Page/Page column 81
(2009/07/18)
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- Structure-Activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating mycobacterium tuberculosis
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Tuberculosis (TB) remains as a global pandemic that is aggravated by a lack of health care, the spread of HIV, and the emergence of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDRTB) strains. New anti-TB drugs are urgently required to shorten the long 6-12 month treatment regimen and to battle drug-resistant Mtb strains. We have identified several potent quinoline-based anti-TB compounds, bearing an isoxazole containing side-chain. The most potent compounds, 7g and 13, exhibited submicromolar activity against the replicating bacteria (R-TB), with minimum inhibitory concentrations (MICs) of 0.77 and 0.95 μM, respectively. In general, these compounds also had micromolar activity against the nonreplicating persistent bacteria (NRP-TB) and did not show toxicity on Vero cells up to 128 μM concentration. Compounds 7g and 13 were shown to retain their anti-TB activity against rifampin, isoniazid, and streptomycin resistant Mtb strains. The results suggest that quinoline-isoxazole-based anti-TB compounds are promising leads for new TB drug development.
- Lilienkampf, Annamaria,Jialin, Mao,Baojie, Wan,Yuehong, Wang,Franzblau, Scott G.,Kozikowski, Alan P.
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scheme or table
p. 2109 - 2118
(2009/12/31)
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- Synthesis of epothilones, intermediates thereto and analogues thereof
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The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
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- Biaryloxymethylarenecarboxylic acids as glycogen synthase activator
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The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.
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Page/Page column 19; 20
(2010/02/10)
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- Synthesis of epothilones, intermediates thereto and analogues thereof
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The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
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- Synthesis of epothilones, intermediates thereto and analogues thereof
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The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
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- Insights into long-range structural effects on the stereochemistry of aldol condensations: A practical total synthesis of desoxyepothilone F
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A processable total synthesis of a potent antitumor agent, desoxyepothilone F (dEpoF, 21-hydroxy-12,13-desoxyepothilone B, 21-hydroxyepothilone D), has been accomplished. The route is highly convergent. The new technology has also been applied to a total
- Chul Bom Lee,Wu,Zhang,Chappell,Stachel,Chou,Guan,Danishefsky
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p. 5249 - 5259
(2007/10/03)
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- Leukotriene B4 derivatives, in particular oximo-LTB4- antagonists
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PCT No. PCT/EP98/03139 Sec. 371 Date Mar. 27, 2000 Sec. 102(e) Date Mar. 27, 2000 PCT Filed May 22, 1998 PCT Pub. No. WO98/52915 PCT Pub. Date Nov. 26, 1998Leukotriene-B4 derivatives of general formula (I), in which R1 represents H, CF3, CH2OH, and R2 rep
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- Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists
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Studies conducted with the goal of discovering a second-generation platelet-activating factor (PAF) antagonist have identified a novel class of potent and orally active antagonists which have high aqueous solubility and long duration of action in animal m
- Curtin, Michael L.,Davidsen, Steven K.,Heyman, H. Robin,Garland, Robert B.,Sheppard, George S.,Florjancic, Alan S.,Xu, Lianhong,Carrera Jr., George M.,Steinman, Douglas H.,Trautmann, Jeff A.,Albert, Daniel H.,Magoc, Terrance J.,Tapang, Paul,Rhein, David A.,Conway, Richard G.,Luo, Gongjin,Denissen, Jon F.,Marsh, Kennan C.,Morgan, Douglas W.,Summers, James B.
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