80258-61-3Relevant articles and documents
MACROCYCLES AS KINASE INHIBITORS
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Page/Page column 69; 70, (2014/12/09)
Compounds of the formula I in which X, Y, Q1, M, Q2 and B have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
A new type of ketolides bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether synthesis and structure-activity relationships
Nomura, Takashi,Iwaki, Tsutomu,Yasukata, Tatsuro,Nishi, Koichi,Narukawa, Yukitoshi,Uotani, Koichi,Hori, Toshihiko,Miwa, Hideaki
, p. 6615 - 6628 (2007/10/03)
A new type of ketolides, bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether and a cyclic carbonate at the C-11,12 position was prepared and the antibacterial activities of the compounds were evaluated. Some of the derivatives showed potent ant
Novel CD40 : CD154 binding interruptor compounds and use thereof to treat immunological complications
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Page/Page column 22-23, (2010/11/30)
The present invention relates to novel CD40:CD154 binding interrupter compounds and use of these compounds and pharmaceutical compositions comprising them, to treat conditions associated with inappropriate CD154 activation in a subject. Specifically, this
A novel series of 2-carboxytetrahydroquinolines provides new insights into the eastern region of glycine site NMDA antagonists
Dannhardt, Gerd,Gruchalla, Markus V.,Kohl, Beate K.,Parsons
, p. 267 - 274 (2007/10/03)
A series of potent 4-substituted tetrahydroquinolines has been synthesized and biologically tested in order to refine the eastern region of the pharmacophore model for glycine site NMDA antagonists concerning the assessment of lipophilicity, flexibility, and hydrogen bonding. Displacement studies on rat cortical membranes using [3H]-5,7-dichlorokynurenic acid as a radioligand indicated that binding affinities are markedly enhanced when additional hydrogen-accepting groups are introduced into the eastern region of the 2-carboxytetrahydroquinolines. Among the most potent ligands were some urea, sulfonylurea, and crown ether compounds as interesting leads for new diagnostics, especially for the evaluation of PET tracers, which allow biodistribution studies and NMDA receptor studies in the living organism.
Synthesis and pharmacological studies of N-substituted 6-[(2- aminoethyl)amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinediones, novel class III antiarrhythmic agents
Katakami,Yokoyama,Miyamoto,Mori,Kawauchi,Nobori,San-nohe,Kaiho,Kamiya
, p. 3325 - 3330 (2007/10/02)
A series of 6-[(2-aminoethyl)amino]-1,3-dimethyl-2,4(1H,3H)- pyrimidinedione derivatives were synthesized and studied for their class III electrophysiological activity and class II (β-blocking) effects in in vitro and in vivo models. Structure-activity re
Pyrimidinedione compounds, method of producing the same and antiarrythmic agents containing the same
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, (2008/06/13)
A pyrimidinedione derivative compound has a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a structure comprising an alkyl chain containing at least two nitrogen atoms. The pyrimidinedione derivative is useful for a medical treatment of cardiac arrhythmias.
Peripherally Acting Enkephalin Analogues. 2. Polar Tri- and Tetrapeptides
Hardy, George W.,Lowe, Lawrence A.,Mills, Gail,Sang, Pang Yih,Simpkin, Dean S. A.,et al.
, p. 1108 - 1118 (2007/10/02)
The design, synthesis, and biological activity of a series of -Arg2-enkephalin-derived tetrapeptide amides and tripeptide aralkylamides are reported.These polar analogues were designed to be excluded from the central nervous system with their action thus limited to peripheral opioid receptors.The effects of the nature of the aromatic ring, aryl ring substitution, and aralkylamine chain length on activity were investigated; in a number of cases the N-terminal amino group of Tyr1 was converted to a guanidino group to further increase hydrophilicity.The peptides were all synthesized by classical solution methodology.The opioid activit y of the peptides was assessed in vitro on the guinea pig ileum and their antinociceptive activity was determined in vivo in chemically induced writhing models (peripheral activity) and in the hot-plate test (central activity), in rodents.That the analgesic effects were predominantly mediated in the periphery was demonstrated by antagonism of antinociception by the peripheral opioid antagonist N-methylnalorphine and by comparison of the activities in the writhing and hot-plate tests.As a class, the tetrapeptides were more potent than the tripeptides; Nα-amidination generally increased activity.A number of compounds exhibited very potent opioid activity and had the desired pharmacological profile, indicating a high degree of peripheral selectivity.
Potential Antitumor Agents. 36. Quanitative Relationships between Experimental Antitumor Activity, Toxicity, and Structure for the General Class of 9-Anilinoacridine Antitumor Agents
Denny, William A.,Cain, Bruce F.,Atwell, Graham J.,Hansch, Corwin,Panthananickal, Augustine,Leo, A.
, p. 276 - 300 (2007/10/02)
Quantitative relationships (QSAR) have been derived between antileukemic (L1210) activity and agent physicochemical properties for 509 tumor-active members of the general class of 9-anilinoacridines.One member of this class is the clinical agent m-AMSA (NSC 249992).Agent hydrophobicity proved a significant but not a dominant influence on in vivo potency.The electronic properties of substituent groups proved important, but the most significant effects on drug potency were shown by the steric influence of groups placed at various positions on the 9-anilinoacridine skeleton.The results are entirely consistent with the physiologically important step in the action of these compounds being their binding to double-stranded DNA by intercalation of the acridine chromophore between the base pairs and positioning of the anilino group in the minor groove, as previously suggested.An equation was also derived for the acute toxicities of 643 derivatives of 9-anilinoacridine.This equation took a somewhat similar form to the one modeling antileukemia potency, emphasizing the usual fairly close relationship between potency and acute toxicity for antitumor agents in general.This study demonstrated the power of QSAR techniques to structure very large amounts of biological data and to allow the extraction of useful information from bearing on the possible site of action of the compounds concerned.
