77992-46-2Relevant articles and documents
Synthesis of 2,3-Disubstituted 5-Iodo-1H-Pyrrolo[2,3-b]pyridines via Fischer Cyclization
Alekseyev, Roman S.,Amirova, Sabina S.,Terenin, Vladimir I.
, p. 2656 - 2663 (2017/09/26)
A simple and convenient procedure for the preparation of some unknown 2,3-disubstituted 5-iodo-1H-pyrrolo[2,3-b]pyridines from readily available starting materials by Fischer indole cyclization in polyphosphoric acid is described. The present methodology provides an alternative synthetic approach to the synthesis of 5-iodo-7-azaindole scaffold. All synthesized compounds were characterized by IR, MS, 1H and 13C NMR, and elemental analysis.
Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors
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Page/Page column 204; 205, (2016/09/13)
The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
A novel pyrazolopyridine with in vivo activity in Plasmodium berghei- and Plasmodium falciparum-infected mouse models from structure-activity relationship studies around the core of recently identified antimalarial imidazopyridazines
Le Manach, Claire,Paquet, Tanya,Brunschwig, Christel,Njoroge, Mathew,Han, Ze,Gonzàlez Cabrera, Diego,Bashyam, Sridevi,Dhinakaran, Rajkumar,Taylor, Dale,Reader, Janette,Botha, Mariette,Churchyard, Alisje,Lauterbach, Sonja,Coetzer, Theresa L.,Birkholtz, Lyn-Marie,Meister, Stephan,Winzeler, Elizabeth A.,Waterson, David,Witty, Michael J.,Wittlin, Sergio,Jiménez-Díaz, María-Belén,Santos Martínez, María,Ferrer, Santiago,Angulo-Barturen, I?igo,Street, Leslie J.,Chibale, Kelly
supporting information, p. 8713 - 8722 (2015/11/25)
Toward improving pharmacokinetics, in vivo efficacy, and selectivity over hERG, structure-activity relationship studies around the central core of antimalarial imidazopyridazines were conducted. This study led to the identification of potent pyrazolopyridines, which showed good in vivo efficacy and pharmacokinetics profiles. The lead compounds also proved to be very potent in the parasite liver and gametocyte stages, which makes them of high interest.
Synthesis and stability evaluation of new HYNIC derivatives as ligands for Technetium-99m
Joyard, Yoann,Bischoff, Laurent,Levacher, Vincent,Papamicael, Cyril,Vera, Pierre,Bohn, Pierre
, p. 208 - 214 (2014/05/20)
An efficient synthetic route to prepare two new HYNIC derivatives with a 2-nitroimidazole moiety designed for tumor hypoxia imaging is described. During the course of the synthesis, the optimization of N-alkylation reaction of 2- nitroimidazole with propargyl bromide is reported to favor the formation of the terminal alkyne versus allene. Thereafter, the two ligands were used with tricine/EDDA to complex 99mTc. However, decomposition of these ligands was observed and we suggest a reasonable explanation based on LC-MS analysis.
Nitrogen bicyclic compounds as inhibitors for Scyl1 and Grk5
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Paragraph 0148; 0149, (2015/01/18)
The present invention relates to compounds assumed to be capable of modulating the activity of the proteins ScyI1 and Grk5, thereby regulating the expression and/or release of insulin as well as to pharmaceutical compositions containing such compounds and the use thereof especially for the treatment of a metabolic disease such as diabetes, obesity and impaired adipogenesis.
HETEROCYCLIC PROTEIN KINASE INHIBITORS
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Paragraph 00561, (2013/03/26)
The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
Design and synthesis of a new class of membrane-permeable triazaborolopyridinium fluorescent probes
Hapuarachchige, Sudath,Montano, Gilbert,Ramesh, Chinnasamy,Rodriguez, Delany,Henson, Lauren H.,Williams, Casey C.,Kadavakkollu, Samuel,Johnson, Dennis L.,Shuster, Charles B.,Arterburn, Jeffrey B.
supporting information; experimental part, p. 6780 - 6790 (2011/06/22)
A new class of fluorescent triazaborolopyridinium compounds was synthesized from hydrazones of 2-hydrazinylpyridine (HPY) and evaluated as potential dyes for live-cell imaging applications. The HPY dyes are small, their absorption/emission properties are
4-(PYRIDIN-3-YL)-2-(PYRIDIN-2-YL)-1,2-DIHYDRO-3H-PYRAZOL-3-ONE DERIVATIVES AS SPECIFIC HIF-PROLYL-4-HYDROXYLASE INHIBITORS FOR TREATING CARDIOVASCULAR AND HAEMATOLOGICAL DISEASES
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Page/Page column 40, (2008/06/13)
The object of the invention is to provide new compounds which can be used for the treatment of diseases, in particular cardiovascular and haematological diseases. The present invention describes compounds which act as specific HIF-prolyl-4-hydroxylase inhibitors and which, because of this specific in vivo action mechanism, induce HIF target genes, such as erythropoietin, and the thus produced biological processes, such as erythropoiesis, after parenteral or oral administration. The present invention relates to compounds having the general formula (I), in which A stands for CH or N, R1 stands for a substituent selected from the group formed by (C1-C6)-alkyl, trifluoromethyl, halogen, cyano, nitro, hydroxy, (C1-C6)-alkoxy, amino, (C1-C6)-alkoxycarbonyl, hydroxycarbonyl and C(=O)-NH-R4; R2 stands for a substituent selected from the group formed by halogen, cyano, nitro, (C1-C6)-alkyl, trifluoromethyl, hydroxy, (C1-C6)-alkoxy, trifluoromethoxy, amino, hydroxycarbonyl and C(=O)-NH-R8; m equals 0, 1 or 2; n equals 0, 1, 2 or 3, it being possible for these meanings to be the same or different when R1 or R2 occurs multiple times; and R3 stands for hydrogen, (C1-C6)-alkyl or (C3-C7)-cycloalkyl. The invention also relates to the salts, solvates, and salt solvates of these compounds.
PHENYLALANINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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Page 63-64, (2010/02/07)
The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.