- AMINOPYRROLIDINES AS CHEMOKINE RECEPTOR ANTAGONISTS
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The present invention is directed to novel aminopyrrolidines of formula I, pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compou
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Page/Page column 118
(2008/12/05)
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- INDOLE DERIVATIVES AND DRUGS CONTAINING THE SAME
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An indole derivative represented by the following general formula (1) : wherein at least one of R1, R2, R3, and R4 represents an alkoxy group containing 1 to 20 carbon atoms, and other groups of the R1, R2, R3, and R4 represent hydrogen, an alkyl group containing 1 to 6 carbon atoms, acetyl group, or hydroxyl group; and either one of X and Y represents -(CH2)nOH wherein n is an integer of 0 to 30, and the other one of the X and Y represents hydrogen atom; or a salt thereof; and a drug and an agent for promoting differentiation of a stem cell containing such indole derivative or its salt as an effective component. The indole derivative (1) of the present invention has action of inducing differentiation of neural stem cell specifically into a neuron, and this indole derivative is useful as a prophylactic or therapeutic drug for brain dysfunction or neuropathy caused by loss or degeneration of the neuron.
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Page/Page column 8
(2010/02/11)
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- ACETYLENE DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE
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The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
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Page/Page column 46
(2010/02/11)
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- Effects of indole fatty alcohols on the differentiation of neural stem cell derived neurospheres
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In a search for inducers of neuronal differentiation to treat neurodegenerative diseases such as Alzheimer's disease, a series of indole fatty alcohols (IFAs) were prepared, 13c (n = 18) was able to promote the differentiation of neural stem cell derived neurospheres into neurons at a concentration of 10 nM. Analysis of the expression of the Notch pathway genes in neurospheres treated during the differentiation phase with 13c (n = 18) revealed a significant decrease in the transcription of the Notch 4 receptor.
- Coowar, Djalil,Bouissac, Julien,Hanbali, Mazen,Paschaki, Marie,Mohier, Eliane,Luu, Bang
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p. 6270 - 6282
(2007/10/03)
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- The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: Hydroxyindole derivatives
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As part of continuing effort to identify novel scaffolds that inhibit the pp60(c-src) protein tyrosine kinase, a series of hydroxyindole amides was rationally designed and synthesized. The most potent derivative was found to bind non-competitively with respect to ATP. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Milkiewicz, Karen L.,Marsilje, Thomas H.,Woodworth Jr., Richard P.,Bifulco Jr., Neil,Hangauer, Matthew J.,Hangauer, David G.
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p. 483 - 486
(2007/10/03)
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- 2-[N-acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists
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The synthesis of several novel indole melatonin analogues substituted at the 2-position with acylaminomethyl (8-11), acylaminoethyl (5a-k), or acylaminopropyl (13) side chains is reported. On the basis of a novel in vitro functional assay (specific bindin
- Spadoni, Gilberto,Balsamini, Cesarino,Bedini, Annalida,Diamantini, Giuseppe,Di Giacomo, Barbara,Tontini, Andrea,Tarzia, Giorgio,Mor, Marco,Plazzi, Pier Vincenzo,Rivara, Silvia,Nonno, Romolo,Pannacci, Marilou,Lucini, Valeria,Fraschini, Franco,Stankov, Bojidar Michaylov
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p. 3624 - 3634
(2007/10/03)
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- Anti-aids piperazines
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The present invention includes diaromatic substituted heterocyclic compounds (III) STR1 which are useful in treating individuals infected with the HIV virus. The invention includes certain previously generically disclosed anti-AIDS piperazinyl compounds (V) and a method of treating HIV infected individuals with the indoles of formula (V) and the anti-AIDS amines (X).
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- Indoline Analogues of Idazoxan: Potent α2-Antagonists and α1-Agonists
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The synthesis and α-adrenergic activity of a series of substituted 2-imidazolinylindolines are described.Substitution in the indoline ring generated compounds with a spectrum of adrenoceptor antagonist/agonist profiles that proved sensitive to both the nature and position of the substituent.Many of the derivatives possess greater presynaptic antagonist potency that the corresponding benzodioxan 1, dihydrobenzofuran 2, and indan 3 analogues; however, this α2-antagonism is often accompanied by α1-agonist activity.It was not possible to separate α2-antagonist from α1-agonist properties in this series.Compounds of most interest proved to be the N-ethyl 6, 5-chloro-N-methyl 18 and 5-chloro-N-ethyl 23 derivatives, all being potent α2-antagonists and α1-agonists.Substitution at the 4- and 7-position of the indoline ring generally gave compounds with nonselective agonist properties.
- Fagan, Gay P.,Chapleo, Christopher B.,Lane, Anthony C.,Myers, Malcolm,Roach, Alan G.,et al
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p. 944 - 948
(2007/10/02)
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