- COMPOUNDS FOR USING IN IMAGING AND PARTICULARLY FOR THE DIAGNOSIS OF NEURODEGENERATIVE DISEASES
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The invention relates to compounds of formula (II) for using in imaging and particularly for the diagnosis of neurodegenerative diseases
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- BICYCLIC DIAMINES AS JANUS KINASE INHIBITORS
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The instant invention provides compounds of formula I which are Jak inhibitors, and as such are useful for the treatment of Jak-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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- Synthesis and antiproliferative activity of substituted 3[2-(1h-indol-3-yl)- 1,3-thiazol-4-yl]-1h-pyrrolo[3,2-b]pyridines, marine alkaloid nortopsentin analogues
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A large number of indolyl-4-azaindolyl thiazoles, nortopsentin analogues, were conveniently synthesized. The antiproliferative activity of the new derivatives was examined against four human tumor cell lines with different histologic origin. Seven derivatives consistently reduced the growth of the experimental models independently of TP53 gene status and exhibited the highest activity against the malignant peritoneal mesothelioma (STO) cell line. The most active compound of this series acts as a CDK1 inhibitor, and was found to cause cell cycle arrest at G2/M phase, to induce apoptosis by preventing the phosphorylation of survivin in Thr34 and to increase the cytotoxic activity of paclitaxel in STO cells.
- Carbone,Pennati,Barraja,Montalbano,Parrino,Spanò,Lopergolo,Sbarra,Doldi,Zaffaroni,Cirrincione,Diana
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p. 1654 - 1666
(2014/05/20)
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- Novel 3-azaindolyl-4-arylmaleimides exhibiting potent antiangiogenic efficacy, protein kinase inhibition, and antiproliferative activity
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Tumor growth and metastasis are highly associated with the overexpression of protein kinases (PKs) regulating cell growth, apoptosis resistance, and prolonged cell survival. This study describes novel azaindolyl-maleimides with significant inhibition of PKs, such as VEGFR, FLT-3, and GSK-3β which are related to carcinogenesis. Furthermore, these compounds exhibit high kinase selectivity and potent inhibition of angiogenesis and cell proliferation, offering versatile options in cancer treatment strategies.
- Ganser, Christopher,Lauermann, Eva,Maderer, Annett,Stauder, Torsten,Kramb, Jan-Peter,Plutizki, Stanislav,Kindler, Thomas,Moehler, Markus,Dannhardt, Gerd
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p. 9531 - 9540
(2013/01/16)
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- 3-(INDOLYL)- OR 3-(AZAINDOLYL)-4-ARYLMALEIMIDE COMPOUNDS AND THEIR USE IN TUMOR TREATMENT
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The present invention relates to a compound of formula (I) wherein R, R and R are as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors
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- 4-AZAINDOLE BISPHOSPHONATES
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Novel 4-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
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Page/Page column 28
(2010/04/25)
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- Palladium-catalyzed reductive N-heterocyclization of alkenyl-substituted nitroarenes as a viable method for the preparation of bicyclic pyrrolo-fused heteroaromatic compounds
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Palladium-catalyzed, carbon monoxide-mediated reductive N-heterocyclization of nitro-heteroaromatic compounds having an alkene adjacent to the nitro-group affords bicyclic pyrrolo-fused heteroaromatic molecules. This type of reaction was used to prepare the fused bicyclo[3.3.0] ring-system: thieno[3,2-b]pyrrole, thieno[2,3-b]pyrrole, furo[2,3-b]pyrrole, pyrrolo[3,2-d]thiazole, and pyrrolo[2,3-d]imidazole and the bicyclo[4.3.0] ring-systems: pyrrolo[3,2-b]pyridine, pyrrolo[2,3-b]pyridine, pyrrolo[3,2-c]pyridine, pyrrolo[2,3-c]pyridine, pyrrolo[3,2-c]pyridazine, and pyrrolo[3,2-d]pyrimidine in 32-94% yield.
- Gorugantula, Sobha P.,Carrero-Martínez, Grissell M.,Dantale, Shubhada W.,S?derberg, Bj?rn C.G.
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experimental part
p. 1800 - 1805
(2010/04/06)
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- Site-selective azaindole arylation at the azine and azole rings via N-oxide activation
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Subjection of N-methyl 6-and 7-azaindole N-oxides to a Pd(OAc) 2/DavePhos catalyst system enables regioselective direct arylation of the azine ring. Following deoxygenation, 7-azaindole substrates undergo an additional regioselective azole direct arylation event in good yield.
- Huestis, Malcolm P.,Fagnou, Keith
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supporting information; experimental part
p. 1357 - 1360
(2009/09/05)
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- 1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT6 receptor ligands
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1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines were prepared. Binding assays indicated they are 5-HT6 receptor ligands, among which 6f and 6g showed high affinity for 5-HT6 receptors with Ki = 3.9 and 1.7 nM, respectively.
- Bernotas, Ronald C.,Antane, Schuyler A.,Lenicek, Steven E.,Haydar, Simon N.,Robichaud, Albert J.,Harrison, Boyd L.,Zhang, Guo Ming,Smith, Deborah,Coupet, Joseph,Schechter, Lee E.
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scheme or table
p. 6935 - 6938
(2010/06/16)
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- 3' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein Q, R1, R4, m and Ar are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 136-138
(2009/04/25)
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- NOVEL ANTIMALARIA AGENT CONTAINING HETEROCYCLIC COMPOUND
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Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula -C(=O)-NH- or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.
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Page/Page column 64
(2008/06/13)
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- Facile synthesis of 2-substituted 4-azaindoles
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A novel and efficient strategy for the synthesis of 2-substituted 4-azaindoles from 2-chloro-3-nitropyridine through Pd-catalyzed Sonogashira cross-coupling, followed by reduction and heteroannulation on t-BuOK, is reported. Copyright Taylor & Francis Group, LLC.
- Sun, Li-Ping,Wang, Jin-Xin
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p. 2187 - 2193
(2008/02/05)
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- A novel series of parenteral cephalosporins exhibiting potent activities against Pseudomonas aeruginosa and other Gram-negative pathogens: Synthesis and structure-activity relationships
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A series of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(carboxymethoxyimino)acetamido]cephalosporins bearing a 1-(substituted)-1H-pyrrolo[3,2-b]pyridinium group at C-3′ position was synthesized and their in vitro antibacterial activities against Pseudomonas aeruginosa and other Gram-negative pathogens were evaluated. Among the cephalosporins prepared, 7β-[2-(2-amino-5-chlorothiazol-4yl)-2(Z)-((S)-1-carboxyethoxyimino)acetamido]cephalosporins (42d) showed potent antibacterial activities against P. aeruginosa and other Gram-negative pathogens including the strains which produce class C β-lactamase and extended spectrum β-lactamase (ESBL). These results imply that both the Cl atom on the C-7 aminothiazole moiety and the α-substituent at the iminoether moiety are essential for the stability against β-lactamase and the potent activity against Gram-negative bacteria including P. aeruginosa.
- Yamawaki, Kenji,Nomura, Takashi,Yasukata, Tatsuro,Uotani, Koichi,Miwa, Hideaki,Takeda, Kei,Nishitani, Yasuhiro
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p. 6716 - 6732
(2008/03/28)
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- Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists
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We herein report the optimization of cyclopentane- and cyclohexane-1,3-diamine derivatives as novel and potent MCH-R1 antagonists. Structural modifications of the 2-amino-quinoline and thiophene moieties found in the initial lead compound served to improve its metabolic stability profile and MCH-R1 affinity, and revealed unprecedented SAR when compared to other 2-amino-quinoline-containing MCH-R1 antagonists.
- Giordanetto, Fabrizio,Karlsson, Olle,Lindberg, Jan,Larsson, Lars-Olof,Linusson, Anna,Evertsson, Emma,Morgan, David G.A.,Inghardt, Tord
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p. 4232 - 4241
(2008/12/21)
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- NOVEL ANTIFUNGAL AGENT COMPRISING HETEROCYCLIC COMPOUND
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The present invention provides an antifungal agent represented by the formula: [wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula -NH-C(=O)-, a group represented by the formula -C(=O)-NH-, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents].
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Page/Page column 72
(2010/11/08)
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- Excited state tautomerization of azaindole
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Fluorescent tryptophan analogs, like azatryptophan, offer an advantage for exploring protein and peptide structure and dynamics. The chromophoric moieties, azaindole, of the azatryptophan analogs are investigated for their potential as fluorescent probes. The photophysical properties of 4-azaindole (4AI) and 5-azaindole (5AI) and their tautomers are characterized through computational and experimental methods. Both 4AI and 5AI undergo excited state tautomerization in the presence of 1 M NaOH. The protonated forms of 4AI and 5AI have a fluorescence emission of 415 and 410 nm, respectively, while the tautomers of 4AI and 5AI have a fluorescent emission of 480 and 450 nm, respectively. Gas phase computations (B3LYP/6-31+G**) show that the N1H azaindole tautomer is lower in energy in the ground state by as much as 12.5 kcal mol-1, while the N″H azaindole tautomer is lower in energy in the excited state by as much as 18.1 kcal mol-1. Solvent effects on the tautomer energy differences were computed using the isodensity polarized continuum model (IPCM). The polarity of the solvent helps to reduce the energy difference between the tautomers in the ground state by as much as 5.8 kcal mol-1, but not enough to reverse the ground state tautomer preference. The Royal Society of Chemistry 2005.
- Cash, Michael T.,Schreiner, Peter R.,Phillips, Robert S.
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p. 3701 - 3706
(2007/10/03)
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- 1,1,1-TRIFLUORO-4-PHENYL-4-METHYL-2-(1H-PYRROLO
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Compounds of Formula (IA), IB), IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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Page/Page column 191
(2010/02/11)
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- Azaindolylalkylamine derivatives as 5-hydroxytryptamine-6 ligands
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The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
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- CONDENSED HETEROAROMATIC RING SYSTEMS. XXII. SIMPLE AND GENERAL SYNTHESIS OF 1H-PYRROLOPYRIDINES
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Four kinds of 1H-pyrrolopyridines having no substituent were simply and easily synthesized by the palladium-catalyzed reaction of easily available nitropyridine derivatives with (Z)-1-ethoxy-2-tributylstannylethene as a key reaction.
- Sakamoto, Takao,Satoh, Chisato,Kondo, Yoshinori,Yamanaka, Hiroshi
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p. 2379 - 2384
(2007/10/02)
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- Synthesis of Pyrrolopyridines (Azaindoles)
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Improved, convenient, and reliable routes for synthesis of 4-,5-,6-, and 7-azaindole, 7-methyl-4-azaindole, 7-methyl-6-azaindole, and the hithero unreported 7-amino-4-azaindole are described.The syntheses have been accomplished either by significant modifications to established procedures or by new methods with afford the compounds in improved yields.
- Mahadevan,Indumathy,Rasmussen, Malcolm
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p. 359 - 367
(2007/10/02)
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- Condensed Heteroaromatic Ring Systems. XII. Synthesis of Indole Derivatives from Ethyl 2-Bromocarbanilates
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The palladium-catalyzed reaction of ethyl 2-bromocarbanilate with trimethylsilylacetylene yielded ethyl 2-(trimethylsilylethynyl)carbanilate, which was treated with sodium ethoxide to give indole.The carbanilates having a methyl or a bromo substituent were similarly transformed to corresponding indole derivatives.Furthermore, pyrrolo- and Pyrrolopyridines were synthesized by this method.Keywords---palladium-catalyzed reaction; trimethylsilylacetylene; ethyl 2-halocarbanilate; ethyl 2-halopyridinecarbamate; ethyl 2-(trimethylsilylethynyl)carbanylate; ethyl o-(trimethylsilylethynyl)pyridinecarbamate;indole;pyrrolopyridine
- Sakamoto, Takao,Kondo, Yoshinori,Iwashita, Shigeki,Yamanaka, Hiroshi
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p. 1823 - 1828
(2007/10/02)
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- Condensed Heteroaromatic Ring Systems. VI. Synthesis of Indoles and Pyrrolopyridines from o-Nitroarylacetylenes
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Catalytic hydrogenation of o-nitrophenylacetaldehyde diethyl acetal over palladium-carbon, followed by intramolecular cyclization of the resulting o-aminophenylacetaldehyde diethyl acetal with hydrochloric acid, gave indole.Similarly, 4-methylindole, ethyl 5-indolecarboxylate, and various pyrrolopyridines were synthesized from the corresponding o-nitroarylacetaldehyde derivatives.The preparation of the desired o-nitroarylacetaldehydes was accomplished by the condensation of o-halonitroaromatics with trimethylsilylacetylene in the presence of dichloro-bis(triphenylphosphine)palladium as a catalyst, followed by ethanolysis of the resulting o-(trimethylsilylethenyl)nitroaromatics.Keywords - o-halonitroaromatic; o-cyanohaloaromatic; trimethylsilylacetylene; palladium-catalyzed reaction; cyclization; indole; pyrrolopyridine
- Sakamoto, Takao,Kondo, Yoshinori,Yamanaka, Hiroshi
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p. 2362 - 2368
(2007/10/02)
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- SRN1 REACTION. SYNTHETIC APPLICATION TO 4-AZAINDOLES
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A new synthetic method for 4-azaindoles, based on nucleophilic heteroaromatic substitution via a radical intermediate (SRN1 reaction) is described.
- Fontan, Rafael,Galvez, Carmen,Viladoms, Pere
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p. 1473 - 1474
(2007/10/02)
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