- Quinolinone compound and application thereof in drugs
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The invention relates to a quinolinone compound and application thereof in drugs, particularly relates to a novel quinolinone compound, a pharmaceutical composition thereof and use of the compound or the pharmaceutical composition in preparing drugs. The drug is used for protecting, disposing, treating or alleviating HIF-related and/or EPO-related diseases of patients, wherein the HIF-related and/or EPO-related diseases comprise anemia, vascular diseases, regional myocardial ischaemia, metabolic disturbance, wound healing and the like.
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- HIGHLY PURE LAQUINIMOD OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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Provided herein is an impurity of laquinimod, N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxoquinoline-3-carboxamide (deschloro laquinimod impurity), and process for preparation and isolation thereof. Provided further herein is a highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity.
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- HIGHLY PURE LAQUINIMOD OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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Provided herein is an impurity of laquinimod, N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-1- methyl-2-oxoquinoline-3-carboxamide (deschloro laquinimod impurity), and process for preparation and isolation thereof. Provided further herein is a highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure laquinimod or a pharmaceutically acceptable salt thereof substantially free of deschloro laquinimod impurity.
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Page/Page column 27
(2010/08/05)
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- INHIBITORS OF UNDECAPRENYL PYROPHOSPHATE SYNTHASE
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The present invention relates to compounds that are selective and/or potent inhibitors of UPPS. In addition to compounds which inhibit UPPS, the invention also provides pharmaceutical compositions comprising these compounds and methods of using these comp
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Page/Page column 82
(2010/01/31)
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- A practical method for preparation of 4-hydroxyquinolinone esters
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(Chemical Equation Presented) 4-Hydroxyquinolinone esters are a common motif for many medicinal agents. Several methods exist for preparation of these compounds, generally involving the use of sodium hydride, which raises significant safety issues and limits their application to large-scale synthesis. In this note a practical, safe, and general method that employs a combination of diisopropylethylamine and sodium tert-butoxide is described. This allows for the synthesis of 4-hydroxyquinolinone esters and amides in good yields.
- Beutner, Gregory L.,Kuethe, Jeffrey T.,Yasuda, Nobuyoshi
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p. 7058 - 7061
(2008/02/11)
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- Design and synthesis of novel quinolinone-3-aminoamides and their α-lipoic acid adducts as antioxidant and anti-inflammatory agents
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A series of N-substituted-quinolinone-3-aminoamides and their hybrids containing the α-lipoic acid functionality were designed and synthesized as potential bifunctional agents combining antioxidant and anti-inflammatory activity. The new compounds were ev
- Detsi, Anastasia,Bouloumbasi, Dionysia,Prousis, Kyriakos C.,Koufaki, Maria,Athanasellis, Giorgos,Melagraki, Georgia,Afantitis, Antreas,Igglessi-Markopoulou, Olga,Kontogiorgis, Christos,Hadjipavlou-Litina, Dimitra J.
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p. 2450 - 2458
(2008/02/02)
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- Alkylidenephosphoranes in heterocyclic synthesis: Reactivity of benzoxazinones with resonance-stabilized phosphorus ylides
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2H-3,1-Benzoxazine-2,4(1H)-dione and its N-methyl analogue react with alkylidenephosphoranes to give substituted quinolines and benzazepines as well as indanone and furan derivatives. Reaction mechanisms to explain the formation of products obtained are outlined. Georg Thieme Verlag Stuttgart.
- Kamel, Azza A.,Abdou, Wafaa M.
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p. 1269 - 1273
(2007/12/27)
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- A novel short-step synthesis of functionalized 4-hydroxy-2-quinolones using a 1-hydroxybenzotriazole methodology
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A novel method for the synthesis of 3-substituted 4-hydroxy-1-methyl- and 1-phenyl-2-quinolones is presented. The compounds are produced in a one-step reaction in very good yields (51-76%). The major advantage of the methodology is the short time for the
- Zikou, Lamprini,Athanasellis, Giorgos,Detsi, Anastasia,Zografos, Alexandros,Mitsos, Christos,Igglessi-Markopoulou, Olga
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p. 1505 - 1508
(2007/10/03)
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- 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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p. 802 - 807
(2013/09/03)
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- Solution-phase combinatorial synthesis of 4-hydroxyquinolin-2(1H)-ones
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Ion-exchange resins catalyse an intramolecular Claisen-type condensation leading to the title compounds, and also serve to purify the products.
- Kulkarni, Bheemashankar A.,Ganesan
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p. 785 - 786
(2007/10/03)
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- Ring Closure and Rearrangement Reactions of 4-Azido-2-oxoquinoline-3-carboxylates and 4-Azidocoumarin-3-carboxylates [1]
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4-Azido-2-oxoquinoline-3-carboxylates and 4-azidocoumarin-3-carboxylates 6, which were obtained from the corresponding 4-hydroxy derivatives 1 via 4-tosylates 2 or 4-chloro compounds 4, cyclized upon thermolysis to 3-alkoxyisoxazolo[4,3-c]quinolin-4(5H)-ones or the corresponding coumarins 8, whereas at slightly higher temperatures a 3-O, 4-O-rearrangement took place to give the 4-alkoxy-isoxazolo[4,3-c]-quinolin-3-ones and the corresponding coumarins 9. The necessary reaction conditions could be obtained easily with the help of differential scanning calorimetry.
- Stadlbauer, Wolfgang,Prattes, Susanne,Fiala, Werner
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p. 627 - 636
(2007/10/03)
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