- Using DOE to achieve reliable drug administration: A case study
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Design of experiments (DOE), a statistical tool, and mathematical modeling techniques are established and proven methodologies for process and product improvements in the pharmaceutical industry. This contribution presents a case study where an unsatisfac
- Sjoevall, Sven,Hansen, Lars,Granquist, Bo
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- Modified synthesis and antiangiogenic activity of Linomide
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A modified procedure for the synthesis of Linomide is described. The synthesized drug was characterized and assessed for its in vivo antiangiogenic activity. In a murine angiogenesis assay Linomide treatment inhibited new blood vessel formation as documented by reduced microvessel area and blood volume.
- Khan, Saeed R.,Mhaka, Annastasiah,Pili, Roberto,Isaacs, John T.
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Read Online
- Preparation method of roquinimex
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A preparation method of roquinimex comprises the following steps: carrying out a reflux reaction on 1, 2-dihydro-4-hydroxy-1-methyl-2-oxoquinoline-3-methyl formate shown as a formula II, N-methylaniline shown as a formula III and a catalyst calcium chloride in a solvent, removing methanol generated by reaction and trace water in the system by adopting an A-type molecular sieve pervaporation inorganic membrane, ending the reaction, filtering a reaction solution at 60-70 DEG C after the reaction is finished, cooling and crystallizing a filtrate, and carrying out filtering and drying to obtain the N-methyl-N-phenyl-1, 2-dihydro-4-hydroxy-1-methyl-2-oxoquinoline-3-formamide (roquinimex) shown in a formula I. The yield reaches 98.5%, and the product content reaches 99.7% (liquid spectrum external standard). The preparation method has the advantages of simple process, no need of distillation, high product purity and yield and the like.
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Paragraph 0023-0028
(2020/10/14)
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- 1,2-DIHYDRO-4-HYDROXY-2-OXO-QUINOLINE-3-CARBOXANILIDES AS AHR ACTIVATORS.
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The present invention relates to compounds which are 1, 2-dihydro-4- hydroxy-2-oxo-quinoline-3-carboxanilides, their thieno-pyridone analogs, and prodrugs thereof. This invention specifically relates to such derivatives containing an N-hydrogen in the carboxanilide moiety and which exhibit modulating activity towards the aromatic hydrocarbon receptor (AhR), and, specifically, also to prodrugs thereof. The present invention also relates to use of said compounds as a medicament, and for the treatment of cancer, autoimmune disorders and other disorders with an immunological component, and a pharmaceutical composition comprising one or more of said compounds and a method of treatment.
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Page/Page column 30
(2012/05/04)
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- Synthesis and Biological Evaluation of New 1,2-Dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for Treatment of Autoimmune Disorders: Structure-Activity Relationship
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Roquinimex-related 3-quinolinecarboxamide derivatives were prepared and evaluated for treatment of autoimmune disorders. The compounds were tested in mice for their inhibitory effects on disease development in the acute experimental autoimmune encephalomyelitis model and selected compounds in the beagle dog for induction of proinflammatory reaction. Structure-activity relationships are discussed. Compound 8c, laquinimod, showed improved potency and superior toxicological profile compared to the lead compound roquinimex (1b, Linomide) and was selected for clinical studies (currently in phase II).
- J?nsson, Stig,Andersson, Gunnar,Fex, Tomas,Fristedt, Tomas,Hedlund, Gunnar,Jansson, Karl,Abramo, Lisbeth,Fritzson, Ingela,Pekarski, Olga,Runstr?m, Anna,Sandin, Helena,Thuvesson, Ingela,Bj?rk, Anders
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p. 2075 - 2088
(2007/10/03)
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- Structure-activity relationships studies of the anti-angiogenic activities of linomide
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The synthesis and anti-angiogenic activities of linomide and its analogues are reported. Three of the analogues are 3.3-69 times more potent than linomide at inhibiting blood vessel formation in the CAM angiogenesis assay. These compounds possessed consid
- Shi, Jiandong,Xiao, Zili,Ihnat, Michael A.,Kamat, Chandrashekhar,Pandit, Bulbul,Hu, Zhigen,Li, Pui-Kai
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p. 1187 - 1189
(2007/10/03)
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- DRUGS AUGMENTING NKT CELLS
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There is provided a NKT cell augmentation-mediated autoimmunosuppressant and/or potentiator on normal immune responses characterized by its comprising a compound of the following general formula or a pharmaceutically acceptable salt thereof as an active ingredient.[wherein R1 represents hydrogen or halogen,R2 represents hydroxy,R3 represents lower alkyl,R4 represents lower alkyl,R5 represents hydrogen or lower alkoxy, andZ represents O or S] Also provided is a novel process for synthesizing the above compound.
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