18341-31-6Relevant academic research and scientific papers
4-(PYRAZOL-3-YLAMINO) PYRIMIDINE DERIVATIVES FOR USE IN THE TREATMENT OF CANCER
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Page/Page column 214-215, (2008/06/13)
A compound of Formula (I); wherein the substituents are as defined in the text for use in modulating insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.
FUNGAL CELL WALL SYNTHESIS GENE
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, (2008/06/13)
A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed.Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
Substituted bicyclic derivatives useful as anticancer agents
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, (2008/06/13)
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3and R4are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals with administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
Muscarinic Receptor Binding and Activation of Second Messengers by Substituted N-Methyl-N-acetamides
Bradbury, Barton J.,Baumgold, Jesse,Paek, Robert,Kammula, Udai,Zimmet, Jeff,Jacobson, Kenneth A.
, p. 1073 - 1079 (2007/10/02)
A series of substituted azacycloalkyl analogues of the muscarinic agonist UH 5 (N-methyl-N-acetamide, 1a) were synthesized and evaluated pharmacologically.These compounds were developed as intermediates for further derivatization leading to functionalized congeners of 1a.The compounds were synthesized by using a Mannich-type condensation of N-acetyl-N-methylpropargylamine to various substituted saturated azaheterocycles.The compounds were screened at a single concentration in competitive binding assays in rat cerebral cortical membranes against either N-methylscopolamine (at 100 μM) or oxotremorine-M (at 1 μM) labels.Candidates were then selected for further evaluation of their effect on phosphoinositide (PI) turnover in membranes from A9L cells transfected with cDNA of either m1-muscarinic cholinergic receptors (m1AChRs) or m3AChRs.The analogues were also tested for the inhibition of adenylate cyclase in NG108-15 cells expressing m4AChRs.The azetidine analogue of 1a had a Ki value of 12 nM for the inhibition of oxotremorine-M binding in rat brain and had an agonist potency at m1-, m3-, and m4AChRs comparable to 1a.The substituted 5- and 6-member ring analogues generally had lower binding affinities and were less potent than 1a in stimulating PI turnover.Several compounds were moderately effective in inhibiting cyclic AMP production in NG108-15 cells.
3- or 4-substituted oxotremorine derivatives
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, (2008/06/13)
This disclosure describes novel 3 or 4 substituted oxotremorine derivatives having polar substituted oxygen or sulfur groups. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and processes for the production of the compounds.
N-(4-Amino-2-butynyl)imides
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, (2008/06/13)
N-(4-Amino-2-butynyl)imides are prepared from N-propargylimides, paraformaldehyde and the appropriate secondary amine. The compounds are useful as stimulants or depressants of the central nervous system.
