39093-77-1Relevant academic research and scientific papers
Deacetylcolchicine deriv.
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Paragraph 0110, (2016/10/08)
Provided are 4-modified colchicine compounds and medicines using the same. Specifically provided are colchicine derivatives represented by general formula (1), salts thereof, and solvates of the same. In general formula (1), R1 is a halogen atom, a hydroxyl group, a nitro group, an amino group, or a mono-, di- or tri-fluoromethyl group; R2, R3 and R4 are each a methoxy group or a hydroxyl group, or alternatively R2 and R3, or R3 and R4 together represent a methylenedioxy group; R5 and R6 may be the same or different and are each a hydrogen atom, a C1-6 alkyl group, an arylalkyl group, a C2-6 alkenyl group, -COR7, -COOR8, -SO2R9, -CONR10R11, or -CSNR12R13, or alternatively R5 and R6 together with the nitrogen atom to which R5 and R6 are bonded may form a three- to seven-membered cyclic amino group; R7 is a C1-6 alkyl group or the like; R8 is a C1-6 alkyl group or the like; R9 is a C1-6 alkyl group or the like; R10 and R11 may be the same or different and are each a hydrogen atom, a C1-6 alkyl group, or the like; and R12 and R13 may be the same or different and are each a hydrogen atom, an alkyl group, or the like.
ISOQUINOLINE AND NAPHTHYRIDINE DERIVATIVES
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Page/Page column 92-93, (2013/08/15)
The invention provides novel compounds having the general formula(I) wherein A, R1 and R2 are as described herein, compositions including the compounds and use of the compounds for inhibiting angiogenesis by inhibition of MAP4K4.
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD)
Moffett, Kristofer,Konteatis, Zenon,Nguyen, Duyan,Shetty, Rupa,Ludington, Jennifer,Fujimoto, Ted,Lee, Kyoung-Jin,Chai, Xiaomei,Namboodiri, Haridasan,Karpusas, Michael,Dorsey, Bruce,Guarnieri, Frank,Bukhtiyarova, Marina,Springman, Eric,Michelotti, Enrique
supporting information; experimental part, p. 7155 - 7165 (2012/01/15)
Discovery of a new class of DFG-out p38α kinase inhibitors with no hinge interaction is described. A computationally assisted, virtual fragment-based drug design (vFBDD) platform was utilized to identify novel non-aromatic fragments which make productive hydrogen bond interactions with Arg 70 on the αC-helix. Molecules incorporating these fragments were found to be potent inhibitors of p38 kinase. X-ray co-crystal structures confirmed the predicted binding modes. A lead compound was identified as a potent (p38α IC50 = 22 nM) and highly selective (≥150-fold against 150 kinase panel) DFG-out p38 kinase inhibitor.
Compounds Which Modulate The CB2 Receptor
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Page/Page column 18, (2010/02/17)
Compounds of formula (I) are disclosed. Compounds according to the and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
PYRROLIDINE COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR
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Page/Page column 127, (2010/08/04)
Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
HETEROCYCLIC COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR
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Page/Page column 78-79, (2010/09/17)
Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
DIAZEPANE COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR
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Page/Page column 54, (2009/05/30)
Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
PHARMACEUTICAL USE OF SUBSTITUTED AMIDES
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Page/Page column 46, (2009/05/28)
The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Quinoline and quinazoline compounds useful in therapy
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, (2008/06/13)
Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents an aryl group or a heteroaryl group, optionally substituted by C1-4 alkyl or SO2
