29212-25-7Relevant academic research and scientific papers
INHIBITION OF P38 KINASE ACTIVITY USING SUBSTITUTED HETEROCYCLIC UREAS
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, (2012/03/10)
This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.
INHIBITION OF RAF KINASE USING SUBSTITUTED HETEROCYCLIC UREAS
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Page/Page column 29, (2010/11/28)
Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1- selective agonists: Synthesis and biological evaluation in vitro and in vivo
Michaelides, Michael R.,Hong, Yufeng,DiDomenico Jr., Stanley,Bayburt, Erol K.,Asin, Karen E.,Britton, Donald R.,Lin, Chun Wel,Shiosaki, Kazumi
, p. 1585 - 1599 (2007/10/03)
A series of substituted 9,10- dihydroxyhexahydrobenzo[f]thieno[c]quinolines (TB[f]Q), varying with respect to the position of the thiophene relative to the benzo[f]quinoline core and the nature and position of the substituent on the thiophene, were prepared and evaluated for their affinity and selectivity for the dopamine D1-like receptor. The thieno[3,2-c]B[f]Q regioisomers bearing a small alkyl (C1-C3) substituent at the 2 position were potent (K(i) 50) D1 agonists with close to full agonist activity (IA > 85%). The compounds were resolved and found to exhibit a high level of enantiospecificity in their interaction with the D1 receptor. Selected compounds were tested in vivo in the 6-OHDA rodent model of Parkinson's disease and for their liability to produce seizure-like activities in mice. (5aR)-trans-2-Propyl-4,5,5a,6,7,11b-hexahydro-3-thia-5-azacyclopent-1- ena[c]phenanthrene-9,10-diol (5) emerged as the compound with the best overall in vivo profile in terms of potency (ED50 = 0.04 μmol/kg) and safety.
TETRACYCLIC COMPOUNDS AS DOPAMINE AGONISTS
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, (2008/06/13)
A tetracyclic compound of the formula: STR1 wherein A and the atoms to which it is attached and the optional double bond represent a mono-or di-heterocyclic ring selected from: STR2 wherein R 1, R. sup.2, R 3, R 4 and X are specifically defined, which compounds are useful in the treatment of dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of substance abuse and other addictive behavior disorders, cognitive impairment and attention deficit disorder.
Synthesis of 5-functionalized 2-tert-butylthiophenes
Garrigues, B.,Oussaid, B.,Hubert, C.
, p. 58 - 63 (2007/10/02)
Functionalized 2-tert-butylthiophene derivatives containing the following groups : alcohol 2a-2c, 7, epoxide 3, cyano 4, 10a, 10b, amidoxime 11a, carboxylic acid 12, hydrazide 15a or amide 13, 15b at α-position of the sulfur atom are synthesized in good y
