A compound of formula ##STR00001## 6-(methylcarbamoyl)-4-[(4-methylphenyl)amino]quinoline-3-carboxylic acid, and pharmaceutically acceptable salts thereof, is provided. The compound can be used to treat cancer, diabetic retinopathy, age-related macular degeneration, inflammation, stroke, ischemic myocardium, atherosclerosis, macular edema and psoriasis.

ClanoTech AB

Quinoline derivatives and their use as tyrosine kinase inhibitors

A new series of derivatives of 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid and their synthesis have been discovered. Surprisingly, by modifying the substituent of the 3-carboxylic acid group, new compounds were produced with high activity as PAF receptor antagonists. These compounds were shown to protect neurons from brain damage that normally occurs in response to stroke and other cerebrovascular diseases. These compounds are also protective against edema generation resulting from traumatic breakdown of the blood-brain barrier. Moreover, these compounds were found to be non-toxic and cytoprotective of cells undergoing oxidative stress that would normally trigger apoptotic cell death; and to have activity as (a) antagonists of an intracellular platelet activating factor ("PAF")-binding site, (b) inhibitors of PAF- and cytokine-mediated c-aminoterminal jun kinase (JNK) and extracellular regulated kinase (ERK), and (c) transcriptional inhibitors of COX-2 expression.

Board of Supervisors of Louisiana State University and Agricultural and Mechanical College

2,4,6-trimethyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid esters as neuroprotective drugs

It is intended to provide a drug which is efficacious in treating and preventing diseases wherein ischemia or an inflammatory substance associated with ischemia participates in the onset or worsening thereof. Because of containing as the active ingredient a substance selected from among farnesol, a farnesol derivative, a tocopherol derivative, a tocotrienol derivative, pharmacologically acceptable salts thereof and solvates thereof, the above-described inhibitor of ischemic disorders can exert therapeutic and preventive effects on diseases wherein ischemia or an inflammatory substance associated with ischemia participates in the onset or worsening thereof (for example, brain infarction, brain edema, cardiac infarction, etc.) not only by the administration in the acute ischemic stage but also by the therapeutic administration in subacute and/or chronic stages after ischemia-reperfusion. It is also intended to provide a farnesol carboxylic acid ester derivative and a method of producing the same.

Fukuoka University

Inhibitor of ischemic disorders

An improved skin cream composition according to the present invention provides protection against lumpiness, edema, and other effects of liposuction and cosmetic surgery, as well as increasing the smoothness of the skin. In general, a skin cream composition according to the present invention comprises: water, and emulsified and dispersed in the water: (1) a long-chain fatty acid ester of ascorbic acid; (2) a short-chain carboxylic acid ester of tocopherol; (3) a glyceryl ester complex comprising at least one glyceryl ester selected from the group consisting of glyceryl linoleate, glyceryl linolenate, and glyceryl arachidonate; (4) a first complex consisting essentially of water, propylene glycol, lecithin, caffeine benzoate, and palmitoyl carnitine; (5) a second complex consisting essentially of water, caffeine, carnitine, and hydrolyzed glycosaminoglycans; (6) a third complex consisting essentially of glycerol, butcher broom extract, passion flower extract, glycogen, hydrolyzed collagen, and PEG 6-32; (7) calendula extract; (8) a water-glycol extract of chamomile; (9) hydrophilic microcapsules; (10) lipophilic microcapsules; and (11) microcapsules comprising methylsilanol elastinate. Other, optional cosmetic ingredients and ancillary ingredients can also be used.

carboxylic acid/ödem

Quinoline derivatives and their use as tyrosine kinase inhibitors

2,4,6-trimethyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid esters as neuroprotective drugs

Inhibitor of ischemic disorders

Skin cream composition

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