- Method of preparing rupatadine fumarate through microchannel reaction device
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The invention discloses a method of preparing rupatadine fumarate through a microchannel reaction device. A process is optimized on a known path of synthesis for rupatadine fumarate; the microchannelreaction device helps greatly shorten the reaction time and provide high throughput and good product quality stability; high continuity is good for continuous scaled production; operating is simple, safety is high, and separating is easy; the defects of the traditional synthetic path can be effectively overcome; the yield is significantly increased, up to 90%. Desloratadine prepared in the production process is subjected to continuous separation and continuous liquid separation; the solution is added directly to next reaction to obtain rupatadine; the yield is not reduced, and the operation issimplified.
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Paragraph 0025; 0034-0039
(2019/05/22)
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- BENZOCYCLOHEPTANETHIOPHENE DERIVATIVES FOR ANTI-ALLERGIC REACTIONS
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The present invention provides inhibitors of allergy, and allergic reactions specifically compounds of the present invention are described by the following chemical Formula I: A method for treating an allergic reaction, or allergy diseases or disorders includes administering a therapeutically effective composition comprising a compound of Formula I or a pharmaceutically acceptable salt, solvate or prodrug thereof and a pharmaceutically acceptable carrier, vehicle or excipient to a subject in need thereof.
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Paragraph 0217-0218
(2014/05/20)
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- PYRAZOLOPYRIMIDINE DERIVATIVES AND USES AS ANTICANCER AGENTS
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Novel compounds having a fused pyrazolopyrimidine derivatives and related fused ring systems are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Pharmaceutical compositions, and methods of using these compounds and compositions to treat cancer and other diseases related to the dysregulation of kinase (such as Aurora A, Aurora B, Aurora C, cMet, JAK2, ROS1, but not limited to) pathways are disclosed. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.
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Page/Page column 43
(2012/07/28)
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- NOVEL CRYSTALLINE FORM OF RUPATADINE FREE BASE
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The present invention relates to a novel crystalline form of rupatadine free base, process for its preparation and to a pharmaceutical composition containing it. In accordance with the present invention rupatadine is suspended in n-hexane, n-heptane, cyclohexane, diethyl ether or diisopropyl ether, stirred for at least 1 hour, filtered the solid and dried to give crystalline rupatadine form-B. The isolation of novel rupatadine free base as crystalline form-B may be useful as a purification of rupatadine or a salt thereof.
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Page/Page column 2
(2009/08/16)
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- A PROCESS FOR THE PREPARATION OF RUPATADINE
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Rupatadine is synthesized by phase transfer catalysed N-alkylation of Desloratadine in biphasic solvent system using aqueous alkali by reaction of a compound of formula (I), with Desloratadine at temperature up to 500C , wherein solvent selected is water immiscible organic solvent. Rupatadine is further converted to Rupatadine fumarate by reaction of Rupatadine in ketonic solvent with an alcoholic solution of fumaric acid.
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Page/Page column 6; 7
(2008/06/13)
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- [(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine
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A series of [(3-pyridylalkyl)piperidylidene]- and (nicotinoylpiperidylidene)benzocycloheptapyridine derivatives, Ia,b, were prepared and evaluated for PAF antagonist and H1 antihistamine activity. PAF antagonist activity was investigated by the in vitro PAF-induced platelet aggregation assay (PPA) and the in vivo PAF-induced hypotension test in rats (PH) and mortality test in mice (PM). For the evaluation of H1 antihistamine activity, the in vitro histamine-induced contraction of the guinea-pig ileum assay (HC) and the in vivo histamine-induced hypotension test (HH) in normotensive rats were used. The potential antiallergic activity of the compounds was evaluated using the active anaphylactic shock test in mice. These compounds are structurally related to loratadine (1) and were generated by replacement of the ethoxycarbonyl group of 1 with substituted 3- pyridylmethyl and nicotinoyl moieties. Both anti-PAF and H1 antihistamine activities have shown a high dependence on the exact nature and position of the substituent in the pyridine ring. Optimum structure 19 (UR-12592) incorporating a (5-methyl-3-pyridyl)methyl radical displayed an unique dual activity inhibiting both PAF-induced effects (PPA, IC50 = 3.7 μM; PH, ID50 = 0.44 mg/kg iv; PM, ID50 = 1.9 mg/kg po) and histamine-induced effects (HC, IC50 = 3.9 nM; HH, ID50 = 1.4 mg/kg iv). Furthermore, 19 was highly active in the passive cutaneous anaphylactic shock in rats (ID50 = 1.2 mg/kg po) and strongly protected mice and rats from mortality induced by endotoxin (ID50 = 1.2 and 0.5 mg/kg iv, respectively). Compound 19 showed itself to be devoid of CNS depressant effects, neither modifying spontaneous motor activity nor prolonging barbiturate-sleeping time in mice at a dose of 100 mg/kg po, and is now under development.
- Carceller,Merlos,Giral,Balsa,Almansa,Bartroli,Garcia- Rafanell,Forn
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p. 2697 - 2703
(2007/10/02)
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- Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity
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Since the hypothetical mechanisms of hydroperoxydation of arachidonic acid by, respectively, 5-lipoxygenase (5-LPO) and cyclooxygenase (CO) involve a redox cycle, a compound which reduces 5-LPO and CO to their inactive state would give a nonselective inhi
- Bruneau,Delvare,Edwards,McMillan
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p. 1028 - 1036
(2007/10/02)
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