- SUBSTITUTED-3-CYANO-[1.7],[1.5], AND [1.8]-NAPHTHYRIDINE INHIBITORS OF TYROSINE KINASES
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This invention provides compounds of formula (I) having structure (a) wherein A'' is a diavalent moiety selected from the group (a, b, c) which are useful as inhibitors of protein tyrosine kinase.
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- ANTICANCER COMPOUNDS
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This invention features compounds having formula (I): wherein, R1, R 2,R3, R4, R6, R7, T, X, and Y are as defined herein. This invention also features a method for treating cancer. The method includes administrating to a subject in need thereof a compound of formula (I).
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- Synthesis and Purification of 6-Ethoxy-4-oxo-1,4-dihydro-[1,5] naphthyridine-3-carboxylic Acid Benzylamide
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The synthesis of 6-ethoxy-4-oxo-1,4-dihydro-[1,5]naphthyridine-3- carboxylic acid benzylamide (1) on multikilogram scale is described. The major challenge for the synthesis of this quinolone GABA partial agonist was in the isolation of product of acceptable purity for clinical studies due to the insolubility of this compound. Also described are efforts to circumvent a high-temperature cyclization required for the synthesis of the quinolone ring system.
- Beaudin, Justin,Meltz, Clifford N.,Meltz, Morgan,Phillips, James E.,Ragan, John A.,Brown Ripin, David H.,Singer, Robert A.,Tucker, John L.,Wei, Lulin,Bourassa, Dennis E.,Bowles, Paul,Castaldi, Michael J.,Clay, Ronald,Couturier, Michel A.,Karrick, Gregory,Makowski, Teresa W.,McDermott, Ruth E.
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p. 873 - 878
(2013/09/05)
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- Substituted 4-oxo-napthyridine-3-carboxamides: GABA brain receptor ligands
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The present invention encompasses structures of the Formula or the pharmaceutically acceptable non-toxic salts thereof wherein: x is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y is (un)substituted alkyl, aryl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.
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- Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure-activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamides
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A new series of 3-(3-pyridyl)acrylamides 16, 17, 19, and 26, and 5-(3-pyridyl)-2,4-pentadienamides 20-25 were prepared and evaluated for their antiallergic activity. Several of these compounds exhibited more potent inhibitory activities than the parent compounds 1a [(E)-N-[4 [4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamide] against the rat passive cutaneous anaphylaxis (PCA) reaction and the enzyme 5-lipoxygenase. Particularly, 4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3-pyridyl)acrylamide (17p) showed an ED50 value of 3.3 mg/kg po in the rat PCA test, which was one-fifth of ketotifen and oxatomide. As compared with ketotifen and oxatomide, compound 17p (AL-3264) possessed a better balance of antiallergic properties due to inhibition of chemical mediator release, inhibition of 5-lipoxygenase, and antagonism of histamine.
- Nishikawa,Shindo,Ishii,Nakamura,Kon,Uno
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p. 583 - 593
(2007/10/02)
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